648494

TRPC3 Channel Inhibitor III, Pyr10

• Synonym(s): TRPC3 Channel Inhibitor III, Pyr10, N-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-4-methylbenzenesulfonamide
• Empirical Formula (Hill Notation): C₁₈H₁₃F₆N₃O₂S
• CAS Number: 1315323-00-2
• Molecular Weight: 449.37
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: semisolid; solid
• potency: 720 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: orange-brown; white to off-white
• solubility: DMSO: 100 mg/mL
• shipped in: wet ice
• storage temp.: 2-8°C

Description

General description

A cell-permeable pyrazole derivative that acts as a selective blocker of the transient receptor potential cation channel TRPC3-medated ROCE (receptor-operated Ca²⁺ entry) and inhibits Carbachol- (Cat. No. 212385) induced Ca²⁺ entry in TRPC3-expressing HEK293 cells (IC₅₀ = 0.72 µM; by Fura-2), while exhibiting much reduced potency against Stim1 and Orai1-coupled CRAC (Ca²⁺ release-activated Ca²⁺) channel-mediated SOCE (store-operated Ca²⁺ entry) in RBL-2H3 cells (IC₅₀ = 13.08 µM; by Fura-2). A great complement to Pyr2 (Cat. No. 203890), Pyr 3 (Cat. No. 648490), and Pyr6 (Cat. No. 203891) in Ca²⁺ signaling studies.

A cell-permeable pyrazole derivative that acts as a selective blocker of the transient receptor potential cation channel TRPC3-medated ROCE (receptor-operated Ca²⁺ entry) and inhibits Carbachol- (Cat. No. 212385) induced Ca²⁺ entry in TRPC3-expressing HEK293 cells (IC₅₀ = 0.72 µM; by Fura-2; peak current density pA/pF = -1.01 and -18.50, respectively, with or without 3 µM Pyr10 by whole cell clamp), while exhibiting much reduced potency against Stim1 and Orai1-coupled CRAC (Ca²⁺ release-activated Ca²⁺) channel-mediated SOCE (store-operated Ca²⁺ entry) in RBL-2H3 cells (IC₅₀ = 13.08 µM; by Fura-2; pA/pF = -4.39 and -7.50, respectively, with or without 3 µM Pyr10). A great complement to Pyr2 (Cat. No. 203890), Pyr 3 (Cat. No. 648490), and Pyr6 (Cat. No. 203891) in Ca²⁺ signaling studies.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
TRPC3

Reversible: yes

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

Schleifer, H. et al. 2012. Br. J. Pharmacol.167, 1712.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable