Pyr6

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

Pyr6 是一种选择性 TRPC3 抑制剂，IC50 为 0.49 uM（在毒胡萝卜素耗尽的天然 RBL-2H3 细胞中抑制 Ca2+ 流入）。Pyr6 是一种 Ca2+ 内流抑制剂，与 TRPC3 相比，它对 CRAC 通道介导的 Ca2+ 内流抑制效果更高。Pyr3是 TRPC3 的选择性抑制剂，以相似的效力抑制 Orai1 和 TRPC3 介导的 Ca(2+) 进入和电流以及肥大细胞激活。

Pyr6 is a selective TRPC3 inhibitor with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).Pyr6 is an inhibitor of Ca2+ entry, which displays higher potency to inhibit Ca2+ entry mediated by CRAC channel than by TRPC3.Pyr3 is selective inhibitor of TRPC3, inhibited Orai1- and TRPC3-mediated Ca(2+) entry and currents as well as mast cell activation with similar potency.?By contrast, Pyr6 exhibited a 37-fold higher potency to inhibit Orai1-mediated Ca(2+) entry as compared with TRPC3-mediated Ca(2+) entry and potently suppressed mast cell activation.

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N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide

Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRPC3

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245747-08-4

418.27

C17H9F7N4O

>98% (HPLC)

DMSO:95 mg/mL (227.12 mM)

O=C(C1=C(F)C=NC=C1)NC2=CC=C(N3N=C(C(F)(F)F)C=C3C(F)(F)F)C=C2

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(-20℃)

With Ice Pack

≥ 2 years