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Pico145

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Chemical Structure| 1628287-16-0 同义名 : HC-608
CAS号 : 1628287-16-0
货号 : A1165848
分子式 : C23H20ClF3N4O5
纯度 : 99%+
分子量 : 524.877
MDL号 : MFCD31657331
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(200.05 mM)，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 Pico145, also known as HC-608, is a notable inhibitor of TRPC1/4/5 channels, suppressing (−)-englerin A-activated TRPC4/TRPC5 channels with IC50 values of 0.349 nM and 1.3 nM in cells, respectively, without affecting the cells. Pico145 also inhibits human TRPC4-TRPC1 and TRPC5-TRPC1 heteromers expressed in HEK 293 Tet+ cells, with IC50 values of 0.03 nM and 0.2 nM, respectively. The potency of Pico145 can be diminished by increasing concentrations of (−)-englerin A. Moreover, Pico145 effectively inhibits 1-phosphatidylsphingosine (S1P) activated TRPC4-TRPC1 channels and suppresses S1P-induced Ca2+ entry through TRPC4-TRPC1 channels, with an IC50 of 0.011 nM. Pico145 also sensitizes EA-sensitive cancer cell lines (Hs578T cells) with an IC50 of 0.11 nM. At 100 nM, Pico145 does not affect store-operated Ca2+ entry into endothelial cells or histamine-induced Ca2+ entry into endothelial cells[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.53mL

1.91mL

0.95mL

19.05mL

3.81mL

1.91mL
参考文献

[1]Rubaiy HN, et al. Picomolar, selective, and subtype-specific small-molecule inhibition of TRPC1/4/5 channels. J Biol Chem. 2017 May 19;292(20):8158-8173.