For research use only. Not for therapeutic Use.
SB 452533 is a potent and selective TRPV1 antagonist with the pKb of 7.8[1].
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[1].
SB-452533 reduces phosphorylation of CAMKK2 and AMPK[2].
Capsaicin (Cap; small dose 2 mg/kg) significantly reduces Bleomycin-induced pulmonary fibrosis in mice. SB-452533 abolishes the effects of small dose Cap[3].
| Catalog Number | I009342 |
| CAS Number | 459429-39-1 |
| Synonyms | 1-(2-bromophenyl)-3-[2-(N-ethyl-3-methylanilino)ethyl]urea |
| Molecular Formula | C18H22BrN3O |
| Purity | ≥95% |
| InChI | InChI=1S/C18H22BrN3O/c1-3-22(15-8-6-7-14(2)13-15)12-11-20-18(23)21-17-10-5-4-9-16(17)19/h4-10,13H,3,11-12H2,1-2H3,(H2,20,21,23) |
| InChIKey | IFJYEGJUQIBBQV-UHFFFAOYSA-N |
| SMILES | CCN(CCNC(=O)NC1=CC=CC=C1Br)C2=CC=CC(=C2)C |
| Reference | [1]. Harshad K Rami, et al. Discovery of small molecule antagonists of TRPV1. Bioorg Med Chem Lett. 2004 Jul 16;14(14):3631-4. [2]. Parisa Vahidi Ferdowsi, et al. TRPV1 Activation by Capsaicin Mediates Glucose Oxidation and ATP Production Independent of Insulin Signalling in Mouse Skeletal Muscle Cells. Cells. 2021 Jun 21;10(6):1560. [3]. Lin Ming Lu, et al. Effect of small dose capsaicin for treatment of pulmonary fibrosis in mice and its mechanism. Zhongguo Ying Yong Sheng Li Xue Za Zhi. 2020 May;36(3):216-222. |
