SB 452533

Research use only, not for human use.

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

SB 452533 is an antagonist of the vanilloid receptor 1(pKb: 7.8).(In Vitro):SB 452533 significantly reduced Capsaicin-induced phosphorylation of AMPK and CAMKK2.(In Vivo):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.

SB 452533 is potent as an antagonist at the cloned recombinant rat TRPV1 receptor in HEK293 cells with a pKb of 7.7 and a pIC50 of 7.0. SB-452533 reduces phosphorylation of CAMKK2 and AMPK. Western Blot Analysis Cell Line:Skeletal muscle (C2C12) cells Concentration:0, 50, 100, 200, and 400 μM Incubation Time:30 minutes; followed by 200 μM Capsaicin treatment for another 30 min. Result:Significantly reduced Capsaicin-induced phosphorylation of AMPK and CAMKK2.

Capsaicin (Cap; small dose 2 mg/kg) significantly reduces Bleomycin-induced pulmonary fibrosis in mice. SB-452533 abolishes the effects of small dose Cap. Animal Model:BALB/c mice bearing pulmonary fibrosis model Dosage:2.5 mg/kg Administration:Treatment received daily drug via subcutaneous injection for 21 days Result:The effect (reduced Bleomycin-induced pulmonary fibrosis) of Cap were abolished in the presence of SB-452533.

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Membrane Transporter/Ion Channel

TRP/TRPV Channel

NF-κB|p65

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459429-39-1

376.298

C18H22BrN3O

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (265.75 mM)

CCN(CCNC(=O)Nc1ccccc1Br)c1cccc(C)c1

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(-20℃)

With Ice Pack

≥ 2 years