Pyr10 

Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca²⁺ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC₅₀ of 0.72 μM (IC₅₀ of 13.08 μM for store operated Ca²⁺ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels^[1].

Pyr10 has the ability to discriminate between the classical Orai-mediated, highly Ca²⁺ selective signalling pathway and the phospholipase C-dependent Ca²⁺ entry-mediated by TRPC channels, specifically by TRPC3. Pyr10 (3 μM) completely eliminates TRPC3 currents as well as Ca²⁺ entry while exerting modest effects on Orai-mediated responses. The selective block of TRPC3 channels by Pyr10 barely affected mast cell activation^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

449.37

Solid

C₁₈H₁₃F₆N₃O₂S

1315323-00-2

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

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]

  [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.  [Content Brief]