Pyr6

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）。

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
10mg

￥1912.00

1530.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajce51128
CAS: 245747-08-4
别名: N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide
分子式: C17H9F7N4O
分子量: 418.27
纯度: >98%
溶解度: DMSO : ≥ 100 mg/mL (239.08 mM)
储存: Store at -20°C
库存: 现货

Background

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.