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Pico145(HC-608)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pico145(HC-608)图片
CAS NO:1628287-16-0
规格:98%
分子量:524.88
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
Pico145是一种高效的瞬时受体电位通道蛋白1/4/5(TRPC1/TRPC4/TRPC5)抑制剂,在细胞中,能够抑制(-)-englerinA活化的TRPC4/TRPC5通道,IC50值分别为0.349和1.3nM,对TRPC3,TRPC6,TRPV1,TRPV4,TRPA1,TRPM2和TRPM8无作用。
CAS:1628287-16-0
分子式:C23H20ClF3N4O5
分子量:524.88
纯度:98%
存储:Store at -20°C

Background:

Pico145 is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (-)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.


Pico145 (Compound 31, C31) is a remarkable small-molecule inhibitor of TRPC1/4/5 channels, inhibits (-)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells; Pico145 shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. Pico145 also inhibits human TRPC4-TRPC1 and TRPC5-TRPC1 concatemers expressed in HEK 293 Tet+ cells (IC50, 0.03 nM and 0.2 nM, respectively). The potency of Pico145 can be reduced by increased (-)-englerin A concentration. Furthermore, Pico145 potently inhibits RPC4-TRPC1 channels activated by sphingosine 1-phosphate (S1P), and suppresses S1P-evoked Ca2+ entry through TRPC4-TRPC1 channels with an IC50 of 0.011 nM. Pico145 also sensitizes EA-sensitive cancer cell line (Hs578T cells) (IC50, 0.11 nM). Pico145 (100 nM) lacks effect on store-operated Ca2+ entry and histamine-evoked Ca2+ entry into endothelial cells[1].



[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.