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SB 452533

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Chemical Structure| 459429-39-1 同义名 : -
CAS号 : 459429-39-1
货号 : A1209512
分子式 : C18H22BrN3O
纯度 : 99%+
分子量 : 376.291
MDL号 : -
存储条件:

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(279.04 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 SB 452533 is a potent antagonist of the recombinant rat TRPV1 receptor cloned in HEK293 cells, with a pKb value of 7.7 and a pIC50 value of 7.0[1].SB 452533 reduces phosphorylation of CAMKK2 and AMPK[2].In skeletal muscle cells C2C12, SB 452533 at concentrations of 50, 100, 200 and 400 μM was applied for 30 min, followed by treatment of the cells with 200 μM capsaicin for 30 min. The results showed that SB 452533 significantly reduced capsaicin-induced phosphorylation of AMPK and CAMKK2.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.29mL

2.66mL

1.33mL

26.58mL

5.32mL

2.66mL

参考文献

[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.