SB 452533 是TRPV1的选择性拮抗剂，pKb为 7.8。

SB 452533 is an antagonist of the vanilloid receptor 1(pKb: 7.8).

SB 452533 significantly reduced Capsaicin-induced phosphorylation of AMPK and CAMKK2[1].

Small dose Cap significantly reduced bleomycin-induced pulmonary fibrosis in mice and obviously reversed alveolar epithelial cells epithelial-mesenchymal transition (EMT) (the expression of E-cadherin and ZO-1 were increased(P＜0.05 or P＜0.01)and the expression of α-SMA and Vimentin were decreased (P＜0.05 or P＜0.01) after drugs treatment for 21 day, concomitantly with the increase the expressions of TRPV1 and CGRP (P＜0.05 or P＜0.01), and inhibiting ERK1/2 phosphorylation and eIF3a expression (P＜0.05 or P＜0.01). These effects of small dose Cap were abolished in the presence of TRPV1 receptor antagonist SB 452533[2].

459429-39-1

C18H22BrN3O

376.29

Ethanol:<1 mgml
DMSO:50 mg/ml(132.876 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years