- 抑制劑
- 化合物庫
- 抗體
- 生物試劑
- 新產(chǎn)品
- 聯(lián)系我們
Home
GPCR & G Protein
MT Receptor agonist
-
ATF/CREB & c-Fos/c-Jun inhibitor
-
COX inhibitor
-
Autophagy modulator
-
Apoptosis related modulator
-
Mitophagy activator
Melatonin
僅限科研使用
Melatonin
別名: NSC 56423, N-Acetyl-5-methoxytryptamine,NSC 113928,MT 中文名稱：褪黑素
Melatonin是一種 MT receptor 激動劑激素, 用作膳食補充品。Melatonin 是一種選擇性的 ATF-6 的抑制劑并可下調(diào) COX-2。Melatonin 可增強線粒體自噬并調(diào)節(jié)凋亡和自噬的穩(wěn)態(tài)。
Melatonin Chemical Structure
CAS: 73-31-4
產(chǎn)品質(zhì)控
批次：
純度：
99.95%
99.95
Melatonin相關(guān)產(chǎn)品
| 相關(guān)靶點 | MT1 receptor MT2 receptor | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Luzindole | 點擊展開 |
| 相關(guān)化合物庫 | FDA藥物庫 天然產(chǎn)物庫 已知活性藥物庫-I GPCR小分子化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| PC12 | Neuroprotective assay | 25 uM | 2 hrs | Neuroprotective activity against H2O2-induced oxidative damage in rat PC12 cells assessed as increase in cell viability at 25 uM preincubated for 2 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay | 28800459 |
| PC12 | Neuroprotective assay | 20 uM | 24 hrs | Neuroprotective activity against amyloid beta (1 to 42 residues) induced cell death in rat PC12 cells assessed as increase in cell viability at 20 uM preincubated for 24 hrs followed by amyloid beta (1 to 42 residues) addition measured after 24 hrs by MTT | 27484514 |
| PC12 | Neuroprotective assay | 10 uM | 2 hrs | Neuroprotective activity against H2O2-induced damage in rat PC12 cells assessed as cell viability at 10 uM preincubated for 2 hrs followed by H2O2 addition for 24 hrs by MTT assay | 27460699 |
| SH-SY5Y | Neuroprotective assay | 10 uM | 24 hrs | Neuroprotective activity against H2O2-induced oxidative stress-associated death in human SH-SY5Y cells assessed as increase in cell viability at 10 uM incubated for 24 hrs prior to H2O2 challenge measured after 24 hrs by MTT assay | 26363866 |
| Primary neural stem cells | Neurogenic assay | 10 uM | 48 hrs | Neurogenic activity in Wistar rat Primary neural stem cells assessed as cell maturation by measuring MAP-2 at 10 uM after 48 hrs by DAPI staining-based immunohistochemistry | 24738476 |
| Primary neural stem cells | Neurogenic assay | 10 uM | 48 hrs | Neurogenic activity in Wistar rat Primary neural stem cells assessed as cell maturation by measuring TuJ1 at 10 uM after 48 hrs by DAPI staining-based immunohistochemistry | 24738476 |
| NIH3T3 | Function assay | 1 nM | Activity at MT1 receptor expressed in NIH3T3 cells assessed as inhibition of forskolin-stimulated cAMP synthesis at 1 nM | 16759094 | |
| CHO | Function assay | 1 hr | Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in CHO cells incubated for 1 hr by gamma counting method, Ki=0.00095μM | 31727472 | |
| COS7 | Function assay | 1.5 hrs | Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method, Ki=0.00088μM | 31727472 | |
| CHO | Function assay | 1 hr | Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting method, Ki=0.00046μM | 31727472 | |
| NIH3T3 | Function assay | 90 mins | Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis, Ki=0.0002042μM | 31727472 | |
| NIH3T3 | Function assay | 90 mins | Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis, Ki=0.000302μM | 31727472 | |
| COS7 | Function assay | 1.5 hrs | Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method, Ki=0.00018μM | 31727472 | |
| MDA-MB-231 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=0.9μM | 29144746 | |
| CHO | Function assay | 60 mins | Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method, IC50=0.00011μM | 27876250 | |
| HEK293 | Function assay | 120 mins | Displacement of [125I]2-Iodomelatonin from human MT2 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay, Ki=0.00034μM | 26785296 | |
| HEK293 | Function assay | 120 mins | Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay, Ki=0.00025μM | 26785296 | |
| HEK293 | Function assay | 120 mins | Displacement of 2-[125I]iodomelatonin from human MT2 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting, Ki=0.00041μM | 25232966 | |
| HEK293 | Function assay | 120 mins | Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting, Ki=0.00014μM | 25232966 | |
| CHO | Function assay | 1 hr | Intrinsic activity at human melatonin MT1 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr, EC50=0.0017μM | 24417958 | |
| CHO | Function assay | 1 hr | Intrinsic activity at human melatonin MT2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr, EC50=0.0004μM | 24417958 | |
| CHOK1 | Function assay | 3 hrs | Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs, IC50=0.00021μM | 23403082 | |
| CHOK1 | Function assay | 3 hrs | Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs, Ki=0.00011μM | 23403082 | |
| HEK293 | Function assay | 2 hrs | Displacement of [125I]2-iodomelatonin from human recombinant MT2 receptor expressed in HEK293 cells after 2 hrs by gamma counting, Ki=0.0005μM | 23265885 | |
| HEK293 | Function assay | 2 hrs | Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting, Ki=0.0002μM | 23265885 | |
| CHO | Function assay | 60 mins | Displacement of [3H]melatonin from human MT2 receptor expressed in CHO cells after 60 mins by microbeta scintillation method, Ki=0.000429μM | 23228808 | |
| CHO | Function assay | 60 mins | Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method, Ki=0.000296μM | 23228808 | |
| NIH3T3 | Function assay | 90 mins | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0003388μM | 22047556 | |
| NIH3T3 | Function assay | 90 mins | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.000263μM | 22047556 | |
| CHO | Function assay | 30 mins | Agonist activity at human MT2 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader, EC50=0.00082μM | 21568291 | |
| CHO | Function assay | 30 mins | Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader, EC50=0.000026μM | 21568291 | |
| CHO | Function assay | 30 mins | Agonist activity at human MT2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers, EC50=0.0008511μM | 21473625 | |
| CHO | Function assay | 30 mins | Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers, EC50=0.0000257μM | 21473625 | |
| CHO-Galpha16 | Function assay | 20 mins | Binding affinity to rat MT2 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=0.0011μM | 21237644 | |
| CHO-Galpha16 | Function assay | 20 mins | Binding affinity to rat MT1 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=0.00056μM | 21237644 | |
| NIH3T3 | Function assay | 90 mins | Displacement of [125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0006166μM | 20674373 | |
| NIH3T3 | Function assay | 90 mins | Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0003311μM | 20674373 | |
| CHO | Function assay | 60 mins | Displacement of [3H]melatonin from human melatonin MT2 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki=0.000429μM | 20227878 | |
| CHO | Function assay | 60 mins | Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki=0.000296μM | 20227878 | |
| CHO | Function assay | 1 hr | Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis, Ki=0.0004571μM | ChEMBL | |
| CHO | Function assay | 1 hr | Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT2 expressed in CHO cells after 1 hr by gamma counting analysis, Ki=0.000955μM | ChEMBL | |
| NIH3T3 | Function assay | Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assay, Ki=0.00066μM | 31727472 | ||
| NIH3T3 | Function assay | Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in NIH3T3 cells membranes by radioligand binding assay, Ki=0.00033μM | 31727472 | ||
| HEK293 | Function assay | Agonist activity at MT2 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay, EC50=0.025μM | 31204226 | ||
| HEK293 | Function assay | Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay, EC50=0.001μM | 31204226 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| CHO | Function assay | Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells, IC50=0.00011μM | 26988801 | ||
| HEK293 | Function assay | Displacement of [125L]iodomelatonin from human MT2 receptor expressed in HEK293 cells, Ki=0.00041μM | 24930835 | ||
| HEK293 | Function assay | Displacement of [125L]iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00014μM | 24930835 | ||
| HEK293 | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in human HEK293 cells by radioligand binding assay, Ki=0.00034μM | 21764185 | ||
| HEK293 | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay, Ki=0.00025μM | 21764185 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.00024μM | 21568291 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00021μM | 21568291 | ||
| CHO | Function assay | Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting, Ki=0.00024μM | 21473625 | ||
| CHO | Function assay | Displacement of [125I]-2-iodomelatonin from human MT2 receptor expressed on CHO cells microscintillation counting, Ki=0.00021μM | 21473625 | ||
| CHO | Function assay | Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.0015μM | 21420861 | ||
| CHO | Function assay | Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.00042μM | 21420861 | ||
| HEK293 | Function assay | Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in HEK293 cells, Ki=0.00034μM | 21420861 | ||
| HEK293 | Function assay | Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00025μM | 21420861 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00035μM | 21392858 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.00022μM | 21392858 | ||
| CHO-Galpha16 | Function assay | Displacement of [3H]melatonin from rat MT1 receptor expressed in CHO-Galpha16 cells, Ki=0.00099μM | 21237644 | ||
| CHO-Galpha16 | Function assay | Displacement of [3H]melatonin from rat MT2 receptor expressed in CHO-Galpha16 cells, Ki=0.00058μM | 21237644 | ||
| CHO | Function assay | Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.0022μM | 20444610 | ||
| CHO | Function assay | Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.00049μM | 20444610 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting, Ki=0.0004571μM | 19473848 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells by gamma counting, Ki=0.000955μM | 19473848 | ||
| CHO | Function assay | Agonist activity at human MT1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding, EC50=0.00224μM | 19329323 | ||
| CHO | Function assay | Agonist activity at human MT2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding, EC50=0.00049μM | 19329323 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.000955μM | 19193160 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.0004571μM | 19193160 | ||
| CHO | Function assay | Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay, EC50=0.00049μM | 18778943 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00041μM | 18778943 | ||
| HEK293 | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00014μM | 18778943 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human melatonin MT2 receptor expressed in CHO cells, Ki=0.000741μM | 18657980 | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells, Ki=0.000525μM | 18657980 | ||
| CHO | Function assay | Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells, IC50=0.06457μM | 18400335 | ||
| HEK293 | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in HEK293 cells, IC50=0.00053μM | 18372181 | ||
| HEK293 | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells, IC50=0.0002μM | 18372181 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells, Ki=0.0002399μM | 18052314 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells, Ki=0.0001413μM | 18052314 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells, Ki=0.0003μM | 17481904 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells, Ki=0.0002μM | 17481904 | ||
| NIH3T3 | Function assay | Displacement of 2[125I]iodomelatonin from human recombinant MT2 receptor expressed in NIH3T3 cells, Ki=0.0003388μM | 17459711 | ||
| NIH3T3 | Function assay | Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells, Ki=0.000263μM | 17459711 | ||
| NIH 3T3 | Function assay | Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells, Ki=0.000389μM | 17346859 | ||
| NIH 3T3 | Function assay | Displacement of 2[125I]iodomelatonin from recombinant human MT2 receptor expressed in NIH 3T3 cells, Ki=0.0003548μM | 17346859 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in NIH3T3 cells, Ki=0.000257μM | 17149869 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells, Ki=0.0003236μM | 17149869 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells, Ki=0.00039μM | 16759094 | ||
| NIH3T3 | Function assay | Displacement of 2-[125I]iodomelatonin from human recombinant MT2 receptor expressed in NIH3T3 cells, Ki=0.00035μM | 16759094 | ||
| NIH3T3 | Function assay | Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1B (MT2) expressed in NIH3T3 rat fibroblast cells , Ki=0.0002818μM | 15943478 | ||
| NIH3T3 | Function assay | Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells, Ki=0.0002884μM | 15943478 | ||
| NIH3T3 | Function assay | Binding affinity against Melatonin receptor type 1B stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin, Ki=0.0007μM | 15713384 | ||
| NIH3T3 | Function assay | Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin, Ki=0.0003μM | 15713384 | ||
| NIH3T3 | Function assay | Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1B, Ki=0.0007μM | 15380218 | ||
| NIH3T3 | Function assay | Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells, Ki=0.0002884μM | 15293992 | ||
| NIH3T3 | Function assay | Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A, Ki=0.0003μM | 15380218 | ||
| NIH3T3 | Function assay | Binding affinity for human recombinant Melatonin receptor type 2 expressed in NIH3T3 cells, Ki=0.0002818μM | 15293992 | ||
| NIH3T3 | Function assay | Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A, Ki=0.0004μM | 14980664 | ||
| NIH3T3 | Function assay | Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1B, Ki=0.0003μM | 14980664 | ||
| NIH3T3 | Function assay | Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells., Ki=0.0004μM | 14643330 | ||
| NIH3T3 | Function assay | Binding affinity against human MT2 melatonin receptor expressed in NIH3T3 cells, Ki=0.0003μM | 14643330 | ||
| HEK293 | Function assay | Binding affinity for human Melatonin receptor type 1B stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand, Ki=0.00041μM | 12646022 | ||
| HEK293 | Function assay | Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand, Ki=0.00014μM | 12646022 | ||
| CHO | Function assay | Binding affinity against human Melatonin receptor type 1A (MT1) in CHO cells, Ki=0.0000823μM | 12213063 | ||
| CHO | Function assay | Ability to inhibit 2-[125I]iodomelatonin specific binding to human melatonin receptor type 1A (MT1) expressed in CHO cells., Ki=0.0000823μM | 12213062 | ||
| CHO | Function assay | Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A, EC50=0.00192μM | 12061881 | ||
| CHO | Function assay | Intrinsic activity at human Melatonin receptor type 1B evaluated on [35S]GTP-gamma-S, binding in Chinese hamster ovarian (CHO) cells, EC50=0.00047μM | 12061881 | ||
| HEK293 | Function assay | Binding affinity on human melatonin receptor type 1B stably transfected in human embryonic kidney (HEK 293) cells using 2-[125I]iodomelatonin as radioligand., Ki=0.00031μM | 12061881 | ||
| HEK293 | Function assay | Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in HEK293 cells, Ki=0.00031μM | 11960497 | ||
| HEK293 | Function assay | Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells, Ki=0.00012μM | 11960497 | ||
| NIH 3T3 | Function assay | Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand, Ki=0.0002884μM | 11520198 | ||
| NIH 3T3 | Function assay | Binding affinity towards melatonin receptor type 1B stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin, Ki=0.0002818μM | 11520198 | ||
| HEK293 | Function assay | Binding affinity for melatonin receptor type 1B, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand), Ki=0.00053μM | 11063602 | ||
| HEK293 | Function assay | Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand), Ki=0.0002μM | 11063602 | ||
| NIH 3T3 | Function assay | Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay, Ki=0.00066μM | 10737738 | ||
| NIH 3T3 | Function assay | Binding affinity towards recombinant human melatonin receptor type 1B expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay, Ki=0.00033μM | 10737738 | ||
| NIH3T3 | Function assay | Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells, Ki=0.0002951μM | 9733487 | ||
| CHO | Function assay | Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells, Ki=0.00008μM | 9435890 | ||
| CHO | Function assay | Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1B expressed in CHO cells, Ki=0.00012μM | 9435890 | ||
| CHO | Function assay | Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells, Ki=0.00013μM | ChEMBL | ||
| CHO | Function assay | Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells, Ki=0.0002μM | ChEMBL | ||
| CHO | Function assay | Binding affinity against human Melatonin receptor type 1B by displacement of [125I]iodomelatonin stably expressed in CHO cells, Ki=0.00023μM | ChEMBL | ||
| CHO | Function assay | Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in CHO cells, Ki=0.00029μM | ChEMBL | ||
| CHO | Function assay | Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.0004571μM | ChEMBL | ||
| CHO | Function assay | Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells by Gamma counting, Ki=0.0004571μM | ChEMBL | ||
| CHO | Function assay | Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.000955μM | ChEMBL | ||
| CHO | Function assay | Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in CHO cells by Gamma counting, Ki=0.000955μM | ChEMBL | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Melatonin是一種 MT receptor 激動劑激素, 用作膳食補充品。Melatonin 是一種選擇性的 ATF-6 的抑制劑并可下調(diào) COX-2。Melatonin 可增強線粒體自噬并調(diào)節(jié)凋亡和自噬的穩(wěn)態(tài)。 | |
|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | Melatonin與高毒性羥基自由基相互作用，數(shù)率常數(shù)等于其他高效羥基自由基清除劑。Melatonin被報到能夠中和過氧化氫，單線態(tài)氧，過氧亞硝基陰離子，一氧化氮和次氯酸。[1] Melatonin被認為能夠清除高毒性羥基自由基，過氧亞硝酸鹽陰離子，可能也作用于氫過氧自由基。據(jù)報道，Melatonin清除超氧陰離子自由基，并且能夠淬滅單線態(tài)氧。Melatonin刺激超氧化物歧化酶的mRNA水平，并活化谷胱甘肽過氧化物酶，谷胱甘肽還原酶和葡萄糖-6-磷酸脫氫酶(都為抗氧化酶)，從而增加其抗氧化能力。[2] 在體外，Melatonin在無細胞體系中被證實能夠直接清除H2O2，單線態(tài)氧(1O2)和一氧化氮(NO*)，幾乎或完全沒有清除超氧陰離子自由基(O2*-)的能力。Melatonin也能夠直接作用于過氧亞硝基陰離子(ONOO-)和/或過氧亞硝酸(ONOOH)，或該分子的活化形式，ONOOH*，使它們失去毒性。Melatonin作為一種直接自由基清除劑，具有清除活性氧和活性氮自由基毒性的能力。[3] Melatonin抑制大部分檢測細胞中的cAMP積累，但至今為止，對其它信使吲哚基的作用僅在一種類型的細胞或組織中經(jīng)常觀察到。Melatonin也能夠調(diào)節(jié)轉(zhuǎn)錄因子，即cAMP響應(yīng)元件結(jié)合蛋白的磷酸化和c-Fos的表達。[4] |
|||
|---|---|---|---|---|
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | MT1 / MT2 / p-CREB / CREB / BDNF p-Raf / p-ERK / p-p90RSK / PKAα / p-AKT / p-JNK / p-CaMKII |
|
29570621 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04521972 | Not yet recruiting | Pregnancy Related|Labor; Poor|Uterine Contractions Weak |
Michigan State University|McLaren Health Care |
October 1 2024 | Not Applicable |
| NCT06390267 | Not yet recruiting | Acute Stress Reaction|Cognitive Performance |
Spark Biomedical Inc.|Battelle Memorial Institute |
August 2024 | Not Applicable |
| NCT06343805 | Not yet recruiting | Primary Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|PMF|PPV-MF|PET-MF |
Ajax Therapeutics Inc. |
July 15 2024 | Phase 1 |
化學(xué)信息&溶解度
| 分子量 | 232.28 | 分子式 | C13H16N2O2 |
| CAS號 | 73-31-4 | SDF | Download Melatonin SDF |
| Smiles | CC(=O)NCCC1=CNC2=C1C=C(C=C2)OC | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 47 mg/mL ( (202.34 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 47 mg/mL (202.34 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
技術(shù)支持
在訂購、運輸、儲存和使用我們的產(chǎn)品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術(shù)支持郵箱tech@selleck.cn，直接聯(lián)系到我們。我們會在24小時內(nèi)盡快聯(lián)系您。
如果有其他問題，請給我們留言。
* 必填項
Tags: buy Melatonin | Melatonin ic50 | Melatonin price | Melatonin cost | Melatonin solubility dmso | Melatonin purchase | Melatonin manufacturer | Melatonin research buy | Melatonin order | Melatonin mouse | Melatonin chemical structure | Melatonin mw | Melatonin molecular weight | Melatonin datasheet | Melatonin supplier | Melatonin in vitro | Melatonin cell line | Melatonin concentration | Melatonin nmr
