Capsazepine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Capsazepine 是 TRPV1 受体的拮抗剂 ( IC50 : 562 nM)。 Capsazepine 可阻断由辣椒素（辣椒的活性成分）激活 TRPV1 离子通道引起的热痛感。

Capsazepine is an antagonist of TRPV1 receptor ( IC50 : 562 nM).?Capsazepine blocks the painful sensation of heat caused by capsaicin (the active ingredient of chilli pepper) which activates the TRPV1 ion channel.?It is therefore considered to be a capsaicin antagonist.

Capsazepine (50 μM) optimally enhances the upregulation of (death receptors) DRs without affecting cell viability HCT116 cells. Capsazepine (30-50 μM) induces ROS generation and ROS mediate Capsazepine-induced DR5 upregulation in HCT116 cells. Capsazepine (1-100 μM, 45 min preincubation) inhibits the evoked CGRP-LI release. Capsazepine (3-100 μM) prevents low pH- and capsaicin-induced CGRP-LI release from rat soleus muscle at concentrations which do not affect the release evoked by KCl. Capsazepine (3-100 μM, without 10 μM) produces a nonspecific inhibitory effect on CGRP-LI release from peripheral endings of the capsaicin-sensitive primary afferent neurone.

Capsazepine (15 mg/kg, s.c.) prevents the increase in respiratory system resistance and decreases the increase in tissue damping during endotoxemia. Capsazepine attenuates lung injury evidenced by reduction on collapsed area of the lung parenchyma induced by LPS.

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Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRPA1

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138977-28-3

376.9

C19H21ClN2O2S

>98% (HPLC)

DMSO:50 mg/mL (132.66 mM)

Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1

N-[2-(4-Chlorophenyl)ethyl]-1345-tetrahydro-78-dihydroxy-2H-2-benzazepine-2-carbothioamide

(-20℃)

With Ice Pack

≥ 2 years