SB 452533 is a potent and selective TRPV1 antagonist with the pKb of 7.8.
体外研究
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.
体内研究
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.
分子式
C18H22N3OBr
分子量
376.29
CAS号
459429-39-1
运输条件
Room temperature in continental US; may vary elsewhere.