| Bioactivity | SB 452533 is a potent and selective TRPV1 antagonist with the pKb of 7.8[1]. |
| Invitro | 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]. Western Blot Analysis[2] Cell Line: |
| In Vivo | 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]. Animal Model: |
| Name | SB 452533 |
| CAS | 459429-39-1 |
| Formula | C18H22BrN3O |
| Molar Mass | 376.29 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 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. |