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Pyr6

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Chemical Structure| 245747-08-4 同义名 : N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide
CAS号 : 245747-08-4
货号 : A510332
分子式 : C17H9F7N4O
纯度 : 99%+
分子量 : 418.268
MDL号 : MFCD28385867
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(251.03 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Pyr6 acts as a selective TRPC3 inhibitor, exhibiting an IC50 of 0.49 μM for inhibiting Ca2+ influx in thapsigargin-depleted native RBL-2H3 cells. The IC50 value is 0.49 μM[1]. The TRPC3 inhibitor Pyr6 is a specific suppressor of SOCE (Yonetoku et al., 2008; Sweeney et al., 2009). It demonstrates a 37-fold (1.58 OM) increase in efficacy for RBL SOCE compared to TRPC3 ROCE, with an IC50 similar to that of Pyr2 and Pyr3. At 3 uM concentration, Pyr6 reduces TRPC3 currents to only 52%. Moreover, consistent with the inhibition of Orai channel function, Pyr2, Pyr3, or Pyr6 significantly impede typical Orai downstream signaling pathways in RBL mast cells (NFAT activation and degranulation) triggered by passive store depletion.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.39mL

0.48mL

0.24mL

11.95mL

2.39mL

1.20mL

23.91mL

4.78mL

2.39mL
参考文献

[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.