203891

CRAC Channel Inhibitor III, Pyr6

• Synonym(e): CRAC Channel Inhibitor III, Pyr6, N-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-3-fluoroisonicotinamide
• Empirische Formel (Hill-System): C₁₇H₉F₇N₄O
• Molekulargewicht: 418.27
• UNSPSC-Code: 12352200

Eigenschaften

• Assay: ≥99% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Wirksamkeit: 490 nM IC₅₀
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: light beige
• Löslichkeit: DMSO: 100 mg/mL
• Versandbedingung: wet ice
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

A cell-permeable pyrazole derivative that acts as a selective blocker of Stim1 and Orai1-coupled CRAC (Ca²⁺ release-activated Ca²⁺) channel-mediated SOCE (store-operated Ca²⁺ entry) in RBL-2H3 cells (IC₅₀ = 490 nM by Fura-2), while exhibiting much reduced potency against the transient receptor potential cation channel TRPC3-medated ROCE (receptor-operated Ca²⁺ entry) upon carbachol (Cat. No. 212385) stimulation in TRPC3-expressing HEK293 cells (IC₅₀ = 18.46 µM; by Fura-2). A great complement to Pyr2 (Cat. No. 203890), Pyr3 (Cat. No. 648490), and Pyr10 (Cat. No. 648494) in Ca²⁺ signaling studies.

A cell-permeable pyrazole derivative that acts as a selective blocker of Stim1 and Orai1-coupled CRAC (Ca²⁺ release-activated Ca²⁺) channel-mediated SOCE (store-operated Ca²⁺ entry) in RBL-2H3 cells (IC₅₀ = 490 nM by Fura-2; peak current density pA/pF = -1.31 and -7.50, respectively, with or without 3 µM Pyr6 by whole cell clamp), while exhibiting much reduced potency against the transient receptor potential cation channel TRPC3-medated ROCE (receptor-operated Ca²⁺ entry) upon carbachol (Cat. No. 212385) stimulation in TRPC3-expressing HEK293 cells (IC₅₀ = 18.46 µM; by Fura-2; pA/pF = -9.50 and -18.50, respectively, with or without 3 µM Pyr6). A great complement to Pyr2 (Cat. No. 203890), Pyr3 (Cat. No. 648490), and Pyr10 (Cat. No. 648494) in Ca²⁺ signaling studies.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
Orai3

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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