Pyr10|1315323-00-2|-陌孚医药/Medlife

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Pyr10

目录号: PL12461 纯度: ≥98%

CAS No. :1315323-00-2

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中文名称	Pyr10
中文别名	Pyr10
英文名称	Pyr10
英文别名	Pyr10;Pyr-10;N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-benzenesulfonamide
Cas No.	1315323-00-2
分子式	C₁₈H₁₃F₆N₃O₂S
分子量	449.37
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	Pyr10 是一种吡唑衍生物和一种选择性 TRPC3 通道抑制剂。Pyr10 抑制卡巴可刺激的 TRPC3 转染的 HEK293 细胞中的 Ca²⁺ 流入，IC₅₀ 为 0.72 μM (对于 BRL-2H3 细胞中存储的 Ca²⁺ 进入，IC₅₀ 为 13.08 μM)。Pyr10 具有区分受体操纵的 TRPC3 和天然基质相互作用分子 1 (STIM1)/Orai1 通道的能力。
生物活性	Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC 50 of 0.72 μM (IC 50 of 13.08 μM for store operated Ca entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels.
性状	Solid
IC50 & Target[1][2]	TRPC3 0.72 μM (IC50)
体外研究(In Vitro)	Pyr10 has the ability to discriminate between the classical Orai-mediated, highly Ca selective signalling pathway and the phospholipase C-dependent Ca entry-mediated by TRPC channels, specifically by TRPC3. Pyr10 (3 μM) completely eliminates TRPC3 currents as well as Ca entry while exerting modest effects on Orai-mediated responses. The selective block of TRPC3 channels by Pyr10 barely affected mast cell activation. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Genetic deletion (TRPC3) and pharmacological channel blockade with Pyr10 blunts ventricular cardiac fibroblast activation and myocardial fibrosis in N(ω)-nitro-l-arginine methyl ester (l-NAME) hypertensive mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
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):1712-1722. [2]. Saliba Y, et al. Transient Receptor Potential Canonical 3 and Nuclear Factor of Activated T Cells C3 Signaling Pathway Critically Regulates Myocardial Fibrosis. Antioxid Redox Signal. 2019 Jun 1;30(16):1851-1879.

溶解度数据	In Vitro: DMSO : 100 mg/mL (222.53 mM; Need ultrasonic)配制储备液

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