648494

TRPC3 Channel Inhibitor III, Pyr10

• Sinônimo(s): TRPC3 Channel Inhibitor III, Pyr10, N-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-4-methylbenzenesulfonamide
• Fórmula empírica (Notação de Hill): C₁₈H₁₃F₆N₃O₂S
• Número CAS: 1315323-00-2
• Peso molecular: 449.37
• Número MDL: MFCD28411625
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥98% (HPLC)
• Nível de qualidade: 100
• Formulário: semisolid; solid
• potência: 720 nM IC₅₀
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: orange-brown; white to off-white
• solubilidade: DMSO: 100 mg/mL
• Condições de expedição: wet ice
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres SMILES: FC(F)(F)c1[n](nc(c1)C(F)(F)F)c2ccc(cc2)N[S](=O)(=O)c3ccc(cc3)C
• InChI: 1S/C18H13F6N3O2S/c1-11-2-8-14(9-3-11)30(28,29)26-12-4-6-13(7-5-12)27-16(18(22,23)24)10-15(25-27)17(19,20)21/h2-10,26H,1H3

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
TRPC3

Reversible: yes

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable