203891

CRAC Channel Inhibitor III, Pyr6

• 別名: CRAC Channel Inhibitor III, Pyr6, N-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-3-fluoroisonicotinamide
• 実験式（ヒル表記法）: C₁₇H₉F₇N₄O
• 分子量: 418.27
• UNSPSCコード: 12352200

特性

• アッセイ: ≥99% (HPLC)
• 品質水準: 100
• 形状: solid
• 有効性: 490 nM IC₅₀
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: light beige
• 溶解性: DMSO: 100 mg/mL
• 輸送温度: wet ice
• 保管温度: 2-8°C

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
Orai3

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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