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Capsazepine
中文名稱：辣椒平
Capsazepine是capsaicin的拮抗劑，是TRPV1的拮抗劑。細胞實驗請選擇01批次。
Capsazepine Chemical Structure
CAS: 138977-28-3
產(chǎn)品質(zhì)控
批次：
純度：
99.66%
99.66
Capsazepine相關(guān)產(chǎn)品
| 相關(guān)靶點 | TRPV TRPA TRPC TRPM TRPML | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | SKF96365 AMG-517 HC-030031 2-APB (2-Aminoethyl Diphenylborinate) GSK2193874 GSK1016790A SB705498 Caffeic Acid HC-067047 Cinnamaldehyde RN-1734 Cardamonin ML204 SB366791 (-)-Menthol | 點擊展開 |
| 相關(guān)化合物庫 | FDA藥物庫 天然產(chǎn)物庫 離子通道配體庫 外泌體分泌相關(guān)化合物庫 鈣通道阻滯劑庫 | 點擊展開 |
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 |
|---|---|---|---|---|---|
| HEK293T | Function assay | 100 uM | Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of proton-induced intracellular Ca2+ influx at 100 uM by fluorescence-based assay | 24484240 | |
| HEK T-REx cells | Function assay | >50 uM | Antagonist at TRPM8 isolated from mouse dorsal root ganglion cells expressed in HEK T-REx cells assessed as inhibition of icilin-induced intracellular Ca2+ influx at >50 uM by fluorescence-based assay | 24484240 | |
| HEK293T | Function assay | 10 uM | Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of proton-induced intracellular Ca2+ influx at 10 uM by fluorescence-based assay | 24484240 | |
| T-REx HEK cells | Function assay | 3 mins | Antagonist activity against human TRPV1 expressed in T-REx HEK cells assessed as inhibition of capsaicin-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to capsaicin stimulation by Fluo-4 AM dye based fluorescence assay, IC50=0.068μM | 25052206 | |
| T-REx HEK cells | Function assay | 3 mins | Antagonist activity against mouse TRPM8 expressed in T-REx HEK cells assessed as inhibition of cold-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to cold stimulation by Fluo-4 AM dye based fluorescence assay | 25052206 | |
| HeLa | Antiproliferative assay | 24 hrs | Antiproliferative activity against human HeLa cells after 24 hrs by cell titer 96 aqueous non-radioactive cell proliferation assay, IC50=30μM | 30528162 | |
| HEK293T | Function assay | Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-based assay, IC50=0.15μM | 24484240 | ||
| HEK293 | Function assay | Antagonist activity at human TRPV1 expressed in tetracycline-stimulated HEK293 cells assessed as inhibition of capsaicin-induced intracellular calcium levels by fluorimetric assay, EC50=2.51189μM | 20381363 | ||
| CHO | Function assay | Displacement of [3H]RTX from rat TRPV1 receptor expressed in CHO cells, Ki=1.3μM | 18072720 | ||
| CHO | Function assay | Antagonist activity at rat TRPV1 receptor expressed in CHO cells assessed as calcium 45 uptake, Ki=0.52μM | 18072720 | ||
| CHO | Function assay | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay, IC50=0.887μM | 17489570 | ||
| CHO | Function assay | Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by aequorin based assay, IC50=0.32μM | 17489570 | ||
| CHO | Function assay | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assay, IC50=0.22μM | 17489570 | ||
| CHO | Function assay | Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay, IC50=0.069μM | 17489570 | ||
| CHO | Function assay | Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay, IC50=0.053μM | 17489570 | ||
| CHO | Function assay | Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assay, IC50=0.039μM | 17489570 | ||
| CHO | Function assay | Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of calcium uptake, Ki=0.52μM | 17035013 | ||
| CHO | Function assay | Displacement of [3H]RTX from rat TRPV1 expressed in CHO cells, Ki=1.3μM | 17035013 | ||
| human TRPV1 expressing cells | Function assay | Inhibition of calcium influx evoked by capsaicin in human TRPV1 expressing cells by fluorescence assay, IC50=0.334μM | 16420034 | ||
| CHO | Function assay | In vitro binding affinity for rat TRPV1 expressed in CHO cells using [3H]-RTX, Ki=1.3μM | 16005215 | ||
| CHO | Function assay | Antagonist activity for rat TRPV1 expressed in CHO cells, Ki=0.52μM | 16005215 | ||
| CHO | Function assay | In vitro inhibition of [3H]RTX binding to rat TRPV1 expressed in CHO cells, Ki=1.3μM | 15993063 | ||
| HEK293 | Function assay | Inhibition of 100 nM capsaicin effect on intracellular [Ca2+] concentration in HEK293 cells expressing human TRPV1, IC50=0.0562μM | 16000002 | ||
| CHO | Function assay | Antagonist activity towards rat TRPV1 expressed in CHO cells, Ki=0.52μM | 15993063 | ||
| CHO | Function assay | Inhibition of capsaicin-induced [Ca2+] uptake by Rat Vanilloid receptor 1 (VR1) expressing CHO cells, Ki=0.52μM | 12825950 | ||
| CHO | Function assay | Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells, IC50=0.42μM | 15634002 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Capsazepine是capsaicin的拮抗劑，是TRPV1的拮抗劑。細胞實驗請選擇01批次。 | ||||
|---|---|---|---|---|---|
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | 94.2 µg/ml的Capsazepine(CPZ)對破骨細胞的生長和增殖具有顯著的抑制[2]。 Capsazepine將NKA轉(zhuǎn)變?yōu)镹a-ATPase。CPZ抑制K+依賴性活性，但不影響Na+轉(zhuǎn)運相關(guān)的Na-ATPase。在沒有K+的情況下，CPZ對Na-ATPase沒有作用。CPZ還能抑制對硝基磷酸酶活性，盡管親和力比較弱。CPZ顯著地減少穩(wěn)態(tài)EP水平?？傊珻PZ阻滯NKA中Na+/K+循環(huán)，但保持Na+循環(huán)完整、減少泵的運輸化學計量[3]。Capsazepine在骨髓-成骨細胞混合培養(yǎng)物及生成RNKL的破骨細胞中，劑量依賴性地抑制破骨細胞形成和骨吸收。Capsazepine還抑制RANKL誘導的IκB和ERK1/2的磷酸化，導致成熟破骨細胞的凋亡。在顱骨成骨細胞中還抑制堿性磷酸酶活性和骨結(jié)節(jié)形成[4]。 |
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|---|---|---|---|---|
| 細胞實驗 | 細胞系 | 小鼠巨噬細胞細胞株RAW 264.7 | ||
| 濃度 | 94.2 μg/ml | |||
| 孵育時間 | 72 h | |||
| 方法 | 將細胞鋪于細胞培養(yǎng)板中，并用不同濃度的化合物進行處理，使得增殖72小時。72小時后，用10% formalin saline (50μl/well)固定細胞30分鐘。然后用crystal violet(0.05% w/v)對細胞進行染色，染色時間為30分鐘。染色結(jié)束后，用蒸餾水沖洗幾遍，將未結(jié)合上的染料洗去，用Sorenson’s buffer進行脫色。540 nm處測定其吸光值。 |
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| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | Capsazepine預處理可防止內(nèi)毒素血癥期間呼吸系統(tǒng)阻力的增加并減少組織阻尼的增加。 Capsazepine 還可通過減少脂多糖 (LPS) 引起的肺實質(zhì)塌陷面積來減輕肺損傷。 |
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|---|---|---|
化學信息&溶解度
| 分子量 | 376.90 | 分子式 | C19H21ClN2O2S |
| CAS號 | 138977-28-3 | SDF | Download Capsazepine SDF |
| Smiles | C1CC2=CC(=C(C=C2CN(C1)C(=S)NCCC3=CC=C(C=C3)Cl)O)O | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : Insoluble ( ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : 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。
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