648494

TRPC3 Channel Inhibitor III, Pyr10

• Synonim(y): TRPC3 Channel Inhibitor III, Pyr10, N-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-4-methylbenzenesulfonamide
• Wzór empiryczny (zapis Hilla): C₁₈H₁₃F₆N₃O₂S
• Numer CAS: 1315323-00-2
• Masa cząsteczkowa: 449.37
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Próba: ≥98% (HPLC)
• Poziom jakości: 100
• Postać: semisolid; solid
• siła działania: 720 nM IC₅₀
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: orange-brown; white to off-white
• rozpuszczalność: DMSO: 100 mg/mL
• Warunki transportu: wet ice
• temp. przechowywania: 2-8°C

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
TRPC3

Reversible: yes

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable