Pico145 是有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，抑制 (-)-englerin A 活化TRPC4/TRPC5 通道的IC50分别为 0.349 和 1.3 nM。

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

Pico145 is a remarkable small-molecule inhibitor of TRPC1/4/5 channels. Pico145 displays no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. Pico145 inhibits (?)-englerin A-activated TRPC4/TRPC5 channels (IC50s: 0.349 and 1.3 nM in cells). 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). Pico145 effectively inhibits RPC4-TRPC1 channels activated by sphingosine 1-phosphate (S1P) and suppresses S1P-evoked Ca2+ entry through TRPC4-TRPC1 channels (IC50: 0.011 nM). The potency of Pico145 can be reduced by increased (?)-englerin A concentration. 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].

1628287-16-0

C23H20ClF3N4O5

524.88

HC-608

DMSO:99 mg/mL (188.61 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years