Pico145 (HC-608) 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 (−)-englerin A 活化的 TRPC4/TRPC5 通道，IC₅₀ 值分别为 0.349 和 1.3 nM，对 TRPC3，TRPC6，TRPV1，TRPV4，TRPA1，TRPM2 和 TRPM8 无作用。

Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (?)-englerin A-activated TRPC4/TRPC5 channels, with IC 50 s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.

Solid

IC50: 0.349 nM (TRPC4, cell assay), 1.3 nM (TRPC5, cell assay), 0.03 nM (TRPC4-TRPC1, cell assay), 0.2 nM (TRPC5-TRPC1, cell assay)

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 Ca 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 Ca entry and histamine-evoked Ca

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : ≥ 100 mg/mL (190.52 mM)配制储备液