648490

TRPC3 Channel Inhibitor, Pyr3

The TRPC3 Channel Inhibitor, Pyr3, also referenced under CAS 1160514-60-2, controls the biological activity of TRPC3 Channel. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

• Synonym(s): TRPC3 Channel Inhibitor, Pyr3, Ethyl-1-(4-(2,3,3-trichloroacrylamide)phenyl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate, SB-360475, CRAC Channel Inhibitor II
• Empirical Formula (Hill Notation): C₁₆H₁₁Cl₃F₃N₃O₃
• CAS Number: 1160514-60-2
• Molecular Weight: 456.63
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white to beige
• solubility: DMSO: 100 mg/mL; ethanol: 25 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C16H11Cl3F3N3O3/c1-2-28-15(27)10-7-23-25(12(10)16(20,21)22)9-5-3-8(4-6-9)24-14(26)11(17)13(18)19/h3-7H,2H2,1H3,(H,24,26)
• InChI key: RZHGONNSASQOAY-UHFFFAOYSA-N

Description

General description

A cell-permeable pyrazole that acts as an equally potent blocker of Stim1 and Orai1-coupled CRAC (Ca²⁺ release-activated Ca²⁺) channel-mediated SOCE (store-operated Ca²⁺ entry) in RBL-2H3 cells (IC₅₀ = 540 nM by Fura-2; peak current density pA/pF = -1.45 and -7.50, respectively, with or without 3 µM BTP2/Pyr3 by whole cell clamp) and the transient receptor potential cation channel TRPC3-mediated ROCE (receptor-operated Ca²⁺ entry) in TRPC3-expressing HEK293 cells (IC₅₀ = 540 nM; by Fura-2; pA/pF = -2.27 and -18.50, respectively, with or without 3 µM BTP2/Pyr3). Pyr3 is also demonstrated to alleviate pressure overload-induced cardiac hypertrophy following TAC (transverse aortic constriction) operation in mice (0.1 mg/kg/day via i.p. osmotic pump) in vivo. A great complement to Pyr 2 (Cat. No. 203890), Pyr6, and Pyr10 in Ca^{2+ signaling studies.}

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Schleifier, H., et al. 2012. Br J PharmacolIn Press
Kiyonaka, S., et al. 2009. Proc. Natl. Acad. Sci. USA106, 5400.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable