Pico145

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Pico145 是一种卓越的 TRPC1/4/5 通道抑制剂。 Pico145 抑制 (-)-englerin A 激活的 TRPC4/TRPC5 通道。

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 (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.

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HC-608

Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRPC4, cell assay|TRPC5, cell assay|TRPC4-TRPC1, cell assay|TRPC5-TRPC1, cell assay

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1628287-16-0

524.88

C23H20ClF3N4O5

>98% (HPLC)

DMSO : 99 mg/mL (188.61 mM)

CN(c1c(C(N2CCCO)=O)n(Cc(cc3)ccc3Cl)c(Oc3cc(OC(F)(F)F)ccc3)n1)C2=O

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(-20℃)

With Ice Pack

≥ 2 years