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- 2x SYBR Green qPCR Master Mix
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- 蛋白酶抑制劑Cocktail
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Dapagliflozin
別名: BMS-512148 中文名稱：達(dá)格列凈
此產(chǎn)品容易吸水受潮，請(qǐng)密封保存。
Dapagliflozin是一種有效的，選擇性的hSGLT2抑制劑，EC50為1.1 nM，比作用于hSGLT1選擇性高1200倍。Phase 4。
Dapagliflozin Chemical Structure
CAS: 461432-26-8
產(chǎn)品質(zhì)控
批次：
純度：
99.99%
99.99
Dapagliflozin相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | SGLT1 SGLT2 | 點(diǎn)擊展開(kāi) |
|---|---|---|
| 相關(guān)產(chǎn)品 | Sotagliflozin Phlorizin Phloretin (RJC 02792) | 點(diǎn)擊展開(kāi) |
| 相關(guān)化合物庫(kù) | FDA藥物庫(kù) 天然產(chǎn)物庫(kù) 已知活性藥物庫(kù)-I GPCR小分子化合物庫(kù) | 點(diǎn)擊展開(kāi) |
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息 |
|---|---|---|---|---|---|
| HEK293.ETN cells | Function assay | 1.5 h | Inhibition of human SGLT2 transfected in HEK293.ETN cells assessed as AMG uptake after 1.5 hrs by scintillation counting, IC50=0.0067 μM | 19896374 | |
| CHOK1 cells | Function assay | 3 h | Inhibition of human SGLT2 expressed in CHOK1 cells assessed as inhibition of [14C]-AMG uptake after 3 hrs by microbeta scintillation counting analysis, IC50=0.001 μM | 24842618 | |
| CHO cells | Function assay | 2 h | Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50=0.00049 μM | 20434909 | |
| COS-7 cells | Function assay | 2 h | Inhibition of human SGLT1 transfected in COS-7 cells assessed as AMG uptake after 2 hrs by scintillation counting, IC50=0.89 μM | 19896374 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent methyl-alpha-D-[U-14C]glucopyranoside uptake after 2 hrs, IC50 = 0.0014 μM. | 20149653 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent methyl-alpha-D-[U-14C]glucopyranoside uptake after 2 hrs, IC50 = 1.2 μM. | 20149653 | |
| HEK293 | Function assay | 1.5 hrs | Inhibition of human SGLT2 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 1.5 hrs by liquid scintillation counting, IC50 = 0.0067 μM. | 20576578 | |
| COS7 | Function assay | 2 hrs | Inhibition of human SGLT1 expressed in african green monkey COS7 cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50 = 0.89 μM. | 20576578 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, EC50 = 0.003 μM. | 21128592 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT1 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, EC50 = 0.4285 μM. | 21128592 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50 = 0.00049 μM. | 21193308 | |
| CHO | Function assay | 60 mins | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting, IC50 = 0.004 μM. | 21398124 | |
| CHO | Function assay | 60 mins | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting in presence of 100% plasma, IC50 = 0.022 μM. | 21398124 | |
| CHO | Function assay | 60 mins | Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting, IC50 = 0.37 μM. | 21398124 | |
| CHO | Function assay | 60 mins | Inhibition of SGLT6 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting, IC50 = 0.38 μM. | 21398124 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counter, IC50 = 0.00049 μM. | 21514014 | |
| CHO | Function assay | 60 mins | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-Glucose uptake using [14C]-methyl glucopyranoside after 60 mins by microbeta plate counting, IC50 = 0.003 μM. | 21565497 | |
| COS7 | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in african green monkey COS7 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 2 hrs by scintillation counting in presence of 25 % human plasma, IC50 = 0.0032 μM. | 21737266 | |
| 293 | Function assay | 1.5 hrs | Inhibition of human SGLT1 expressed in human 293 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 1.5 hrs by scintillation counting in presence of 25 % human plasma, IC50 = 3.1 μM. | 21737266 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in CHO cells assessed as reduction of [14C]-labeled AMG after 2 hrs by liquid scintillation counting, IC50 = 0.00135 μM. | 21868239 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50 = 0.00049 μM. | 21906953 | |
| CHO-K1 | Function assay | 120 mins | Inhibition of human SGLT2 expressed in CHO-K1 cells incubated for 120 mins at 37 degC by [14C]-AMG uptake assay, EC50 = 0.0024 μM. | 22818040 | |
| CHO-K1 | Function assay | 120 mins | Inhibition of human SGLT1 expressed in CHO-K1 cells incubated for 120 mins at 37 degC by [14C]-AMG uptake assay, EC50 = 0.593 μM. | 22818040 | |
| CHO | Function assay | 45 mins | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins, IC50 = 0.0013 μM. | 22889351 | |
| CHO | Function assay | 45 mins | Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins, IC50 = 0.8 μM. | 22889351 | |
| CHOK1 | Function assay | 3 hrs | Inhibition of human SGLT1 expressed in CHOK1 cells assessed as inhibition of [14C]-AMG uptake after 3 hrs by microbeta scintillation counting analysis, IC50 = 0.891 μM. | 24842618 | |
| CHO | Function assay | 2 hrs | Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting, IC50 = 0.00049 μM. | 24900297 | |
| CHO | Function assay | 2 hrs | Competitive inhibition of full-length human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by scintillation counting, IC50 = 0.005 μM. | 25650254 | |
| CHO | Function assay | 120 mins | Inhibition of human SGLT2 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method, IC50 = 0.0015 μM. | 28447791 | |
| CHO | Function assay | 120 mins | Inhibition of human SGLT1 expressed in CHO cells assessed as decrease in uptake of [14C]AMG after 120 mins by TopCount method, IC50 = 0.629 μM. | 28447791 | |
| CHO | Function assay | 1 hr | Inhibition of human SGLT2 expressed in CHO cells assessed as reduction in [14C]AMG uptake after 1 hr by microbeta counting method, EC50 = 0.002 μM. | 29216560 | |
| CHO | Function assay | 1 hr | Inhibition of human SGLT1 expressed in CHO cells assessed as reduction in [14C]AMG uptake after 1 hr by microbeta counting method, EC50 = 0.86 μM. | 29216560 | |
| CHO | Function assay | 1 hr | Inhibition of full-length human SGLT2 expressed in CHO cells assessed as decrease in [14C]-methyl alpha-D-glucopyranoside uptake after 1 hr by liquid scintillation counting method, IC50 = 0.00105 μM. | 29764742 | |
| HEK293 | Function assay | 10 mins | Inhibition of human SGLT2 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake preincubated for 10 mins followed by [14C]-AMG addition and measured after 2 hrs by liquid scintillation counting method, IC50 = 0.0014 μM. | 29954682 | |
| HEK293 | Function assay | 10 mins | Inhibition of human SGLT1 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake preincubated for 10 mins followed by [14C]-AMG addition and measured after 2 hrs by liquid scintillation counting method, IC50 = 1.83 μM. | 29954682 | |
| CHO | Function assay | Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation, EC50 = 0.0011 μM. | 18260618 | ||
| CHO | Function assay | Inhibition of rat SGLT2 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation, EC50 = 0.003 μM. | 18260618 | ||
| CHO | Function assay | Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation, EC50 = 1.39 μM. | 18260618 | ||
| HEK293.ETN | Function assay | Inhibition of human SGLT2 expressed in HEK293.ETN cells assessed as methyl-alpha-D-[U-14C]glucopyranoside uptake by scintillation counting, IC50 = 0.0067 μM. | 19700318 | ||
| COS7 | Function assay | Inhibition of human SGLT1 expressed in african green monkey COS7 cells assessed as methyl-alpha-D-[U-14C]glucopyranoside uptake by scintillation counting, IC50 = 0.885 μM. | 19700318 | ||
| HEK293 | Function assay | Inhibition of human SGLT1 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methylglucopyranoside uptake, IC50 = 0.81 μM. | 19785435 | ||
| CHO | Function assay | Inhibition of human recombinant SGLT2 expressed in CHO cells by liquid scintillation counting, IC50 = 0.00049 μM. | 20181486 | ||
| CHO | Function assay | Inhibition of human SGLT2 expressed in CHO cells using methyl-alpha-D-glucopyranoside by liquid scintillation counting, IC50 = 0.00135 μM. | 21592794 | ||
| CHO-K1 | Function assay | Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay, IC50 = 0.0013 μM. | 22652255 | ||
| CHO-K1 | Function assay | Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay, IC50 = 0.8 μM. | 22652255 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Dapagliflozin是一種有效的，選擇性的hSGLT2抑制劑，EC50為1.1 nM，比作用于hSGLT1選擇性高1200倍。Phase 4。 | ||
|---|---|---|---|
| 特性 | Dapagliflozin是第一類刺激血糖的藥物，作用于正常大鼠比其他SGLT2抑制劑更有效。 | ||
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | Dapagliflozin對(duì)hSGLT1不敏感，IC50是hSGLT2的1200倍。[1] Dapagliflozin作用于hSGLT2比Phlorizin效果高32倍。作用于hSGLT1比Phlorizin效果低4倍。Dapagliflozin高度選擇性抗GLUT轉(zhuǎn)運(yùn)蛋白，20 μM Dapagliflozin在無(wú)蛋白buffer中抑制達(dá)8-9%，在4%牛血清蛋白存在時(shí)沒(méi)有抑制效果。[2] Dapagliflozin可滲透Caco-2 細(xì)胞膜，可作為P-糖蛋白（P-gp）底物，但不是P-gp抑制劑。10 μM Dapagliflozin穩(wěn)定作用于大鼠，犬，猴，人類血清。Dapagliflozin作用于人類P450酶，沒(méi)有抑制反應(yīng)，也沒(méi)有誘導(dǎo)。Dapagliflozin在體外代謝通路中可參與糖脂化，羥乙基化，脫乙基作用。[3] |
|||
|---|---|---|---|---|
| 實(shí)驗(yàn)圖片 | 檢測(cè)方法 | 檢測(cè)指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot | HIF-1α / p-AMPK / AMPK / p-ERK / ERK / β-actin DDR1 HIF-1α / PHD2 / tubulin p-elf2α / t-elf2α / tubulin-α Bax / Bcl2 / PARP / β-actin |
|
27391020 | |
| Growth inhibition assay | Tumor volume |
|
28763435 | |
| IHC | TUNEL-positive cells HIF1 TUNEL-positive cells mice kidney sections HE staining / SGLT2 |
|
27391020 | |
| Immunofluorescence | Metabolic switch in diabetic kidneys F-actin EdU PECAM-1 / α-SMA podocytes |
|
32444604 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | Dapagliflozin按 0.1 mg/kg劑量口服給藥高血糖 鏈脲佐菌素(STZ)大鼠，降低血糖水平，降低達(dá)55%，歸因于與糖鏈相關(guān)的代謝穩(wěn)定。 Dapagliflozin具有很好的吸收，分布，代謝，排泄 (ADME) 譜，且具有口服生物有效性。[1] Dapagliflozin 按1 mg/kg 劑量作用于正常大鼠，處理24小時(shí)，造成明顯糖尿，這種作用存在劑量依賴性，且提高尿量。Dapagliflozin 作用于Zucker 糖尿病肥胖(ZDF)大鼠，處理6小時(shí)后，誘導(dǎo) 尿糖和尿量分泌升高。Dapagliflozin 處理ZDF大鼠，2周后，快速降低葡萄糖水平, 且不會(huì)對(duì)腎臟和肝臟造成毒性。[2] Dapagliflozin 明顯緩解多糖癥病情發(fā)展, 使血糖水平降低。Dapagliflozin 可提高胰島素敏感性,降低β細(xì)胞質(zhì)量和修復(fù)的胰腺功能。[4] |
|
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | 正常Sprague Dawley大鼠或鏈脲佐菌素誘導(dǎo)的雄性Sprague Dawley大鼠 |
| Dosages | 0.01-10 mg/kg (1 mL/kg) | |
| Administration | 口服處理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06012266 | Not yet recruiting | Heart Failure |
Centre Hospitalier Universitaire Vaudois|Great Ormond Street Hospital for Children NHS Foundation Trust|University College London |
August 2024 | Phase 2 |
| NCT06336330 | Recruiting | Heart Diseases|Cardiovascular Diseases|Heart Failure |
AstraZeneca |
April 25 2024 | -- |
| NCT04887935 | Not yet recruiting | Prostate Cancer|Cancer of Prostate |
Washington University School of Medicine|The Foundation for Barnes-Jewish Hospital |
April 30 2024 | Phase 1 |
| NCT06398977 | Recruiting | Peritoneal Dialysis Complication|Renal Function Aggravated|Sodium-glucose Co-transporter-2 Inhibitors |
Sichuan Academy of Medical Sciences |
March 11 2024 | Not Applicable |
化學(xué)信息&溶解度
| 分子量 | 408.87 | 分子式 | C21H25ClO6 |
| CAS號(hào) | 461432-26-8 | SDF | Download Dapagliflozin SDF |
| Smiles | CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)C3C(C(C(C(O3)CO)O)O)O)Cl | ||
| 儲(chǔ)存條件(自收到貨起) | 3年 -20°C 粉末（密封） | ||
|
體外溶解度 |
DMSO : 100 mg/mL ( (244.57 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO) Ethanol : 100 mg/mL (244.57 mM) Water : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | ||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)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(guò)該批次藥物DMSO溶解度，請(qǐng)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(jìn)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。
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