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CAS No.: 138977-28-3

Capsazepine/辣椒平 Catalog No. CSN10542

Synonyms: 辣椒平;卡西平

Capsazepine is an antagonist of TRPV1 receptor with IC50 of 562 nM. It is synthetic analogue of sensory neurone excitotoxin.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 TRP Channel V1

IC50:562nM
描述TRPV1 is a non-selective cation channel, predominantly expressed by peripheral sensory neurons. It plays a key role in the detection of noxious painful stimuli, such as capsaicin, acid and heat. Capsazepine is a competitive TRPV1 antagonist and also works as ENaCδβγ activator. Intradermal injection of 1.5mg Capsazepine 5min prior to carrageenan injection significantly reduced Capsaicin-induced (but not formalin-induced) the number of cells with Fos-expression. Meanwhile, it blocked the carrageenan-induced hyperalgesia but not inflammation of rats at dose of 0.6mg and 1.5mg. Capsazepine markedly increased the inward currents at a holding potential of -60mV in hENaCδβγ-expressing Xenopus oocytes at concentration>1μM.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
CHO cells	-	Function assay	-	Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assay, IC50=0.039 μM	17489570
HEK293 cells	-	Function assay	-	Inhibition of 100 nM capsaicin effect on intracellular [Ca2+] concentration in HEK293 cells expressing human TRPV1, IC50=0.0562 μM	16000002
T-REx HEK cells	-	Function assay	-	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

动物研究
剂量
Mice: 1.5 mg/kg - 5 mg/kg^[3] (i.p.) Rat: 10 mg/kg^[4] (i.p.); guinea pig: 3 mg/kg - 30 mg/kg^[5] (s.c.)

给药途径
i.p., s.c.
参考文献

动物研究
剂量	Mice: 1.5 mg/kg - 5 mg/kg^[3] (i.p.) Rat: 10 mg/kg^[4] (i.p.); guinea pig: 3 mg/kg - 30 mg/kg^[5] (s.c.)
给药途径	i.p., s.c.

[1] Wang J, Tian W, et al. Anti-inflammatory and retinal protective effects of capsaicin on ischaemia-induced injuries through the release of endogenous somatostatin. Clin Exp Pharmacol Physiol. 2017 Jul;44(7):803-814.
[2] Sung B, Prasad S, et al. Capsazepine, a TRPV1 antagonist, sensitizes colorectal cancer cells to apoptosis by TRAIL through ROS-JNK-CHOP-mediated upregulation of death receptors. Free Radic Biol Med. 2012 Nov 15;53(10):1977-87.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6532 mL
- 13.2661 mL
- 26.5322 mL
- 5 mM
- 0.5306 mL
- 2.6532 mL
- 5.3064 mL
- 10 mM
- 0.2653 mL
- 1.3266 mL
- 2.6532 mL

技术信息

CAS号

138977-28-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H21ClN2O2S

运输

蓝冰

分子量

376.90

别名

辣椒平;卡西平

溶解度

DMSO	73.0 mg/mL (193.7 mM)
Water	Insoluble
Ethanol	73.0 mg/mL (193.7 mM)

动物实验配方

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Capsazepine/辣椒平 Catalog No. CSN10542

靶点选择性

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