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Capsazepine
中文名称：辣椒平
Capsazepine是capsaicin的拮抗剂，是TRPV1的拮抗剂。细胞实验请选择01批次。
Capsazepine Chemical Structure
CAS: 138977-28-3
产品质控
批次：
纯度：
99.66%
99.66
Capsazepine相关产品
| 相关靶点 | TRPV TRPA TRPC TRPM TRPML | 点击展开 |
|---|---|---|
| 相关产品 | SKF96365 HC-030031 AMG-517 GSK2193874 2-APB (2-Aminoethyl Diphenylborinate) GSK1016790A SB705498 Caffeic Acid HC-067047 RN-1734 SB366791 (-)-Menthol Cardamonin ML204 | 点击展开 |
| 相关化合物库 | FDA药物库 天然产物库 离子通道配体库 外泌体分泌相关化合物库 钙通道阻滞剂库 | 点击展开 |
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Capsazepine是capsaicin的拮抗剂，是TRPV1的拮抗剂。细胞实验请选择01批次。 | ||||
|---|---|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 94.2 µg/ml的Capsazepine(CPZ)对破骨细胞的生长和增殖具有显著的抑制[2]。 Capsazepine将NKA转变为Na-ATPase。CPZ抑制K+依赖性活性，但不影响Na+转运相关的Na-ATPase。在没有K+的情况下，CPZ对Na-ATPase没有作用。CPZ还能抑制对硝基磷酸酶活性，尽管亲和力比较弱。CPZ显著地减少稳态EP水平。总之，CPZ阻滞NKA中Na+/K+循环，但保持Na+循环完整、减少泵的运输化学计量[3]。Capsazepine在骨髓-成骨细胞混合培养物及生成RNKL的破骨细胞中，剂量依赖性地抑制破骨细胞形成和骨吸收。Capsazepine还抑制RANKL诱导的IκB和ERK1/2的磷酸化，导致成熟破骨细胞的凋亡。在颅骨成骨细胞中还抑制碱性磷酸酶活性和骨结节形成[4]。 |
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|---|---|---|---|---|
| 细胞实验 | 细胞系 | 小鼠巨噬细胞细胞株RAW 264.7 | ||
| 浓度 | 94.2 µg/ml | |||
| 孵育时间 | 72 h | |||
| 方法 | 将细胞铺于细胞培养板中，并用不同浓度的化合物进行处理，使得增殖72小时。72小时后，用10% formalin saline (50μl/well)固定细胞30分钟。然后用crystal violet(0.05% w/v)对细胞进行染色，染色时间为30分钟。染色结束后，用蒸馏水冲洗几遍，将未结合上的染料洗去，用Sorenson’s buffer进行脱色。540 nm处测定其吸光值。 |
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| 体内研究(In Vivo) | ||
| 体内研究活性 | Capsazepine预处理可防止内毒素血症期间呼吸系统阻力的增加并减少组织阻尼的增加。 Capsazepine 还可通过减少脂多糖 (LPS) 引起的肺实质塌陷面积来减轻肺损伤。 |
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|---|---|---|
|
化学信息&溶解度
| 分子量 | 376.90 | 分子式 | C19H21ClN2O2S |
| CAS号 | 138977-28-3 | SDF | Download Capsazepine SDF |
| Smiles | C1CC2=CC(=C(C=C2CN(C1)C(=S)NCCC3=CC=C(C=C3)Cl)O)O | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : Insoluble ( ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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