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Pyr6
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。
Pyr6图片
CAS NO:245747-08-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议

产品介绍
Pyr6 是 TRPC3 的选择性抑制剂,IC50 为 0.49 uM(在 thapsigargin 耗尽的天然 RBL-2H3 细胞中,Ca2+ 流入抑制)。
Cas No.245747-08-4
别名N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide
Canonical SMILESO=C(C1=C(F)C=NC=C1)NC2=CC=C(N3N=C(C(F)(F)F)C=C3C(F)(F)F)C=C2
分子式C17H9F7N4O
分子量418.27
溶解度DMSO : ≥ 100 mg/mL (239.08 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).IC50 value: 0.49 uM [1]Target: TRPC3 inhibitorPyr6 is a selective SOCE inhibitor (Yonetoku et al., 2008; Sweeney et al., 2009), Pyr6 displayed 37-fold (1.58 OM) higher potency for RBL SOCE than for TRPC3 ROCE, with an IC50 comparable to that of Pyr2 and Pyr3. Pyr6 at 3 uM diminished TRPC3 currents to only 52%. Consistent with inhibition of Orai channel activity Pyr2, Pyr3 or Pyr6 substantially inhibited typical Orai downstream signalling events in RBL mast cells (NFAT activation and degranulation) activated by passive store depletion.

[1]. Schleifer H, et al. Novel pyrazole compounds for pharmacological discrimination between receptor-operated and store-operated Ca(2+) entry pathways. Br J Pharmacol. 2012 Dec;167(8):1712-22.