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203891 CRAC Channel Inhibitor III, Pyr6 - Calbiochem

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203891
  
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Overview

Replacement Information
Description
Overview

This product has been discontinued.



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.

Catalogue Number203891
Brand Family Calbiochem®
SynonymsN-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-3-fluoroisonicotinamide
References
ReferencesSchleifer, H., et al. 2012. Br. J. Pharmacol. 167, 1712.
Product Information
FormLight beige solid
Hill FormulaC₁₇H₉F₇N₄O
Chemical formulaC₁₇H₉F₇N₄O
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetOrai3
Primary Target IC<sub>50</sub>490 nM
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
203891 0

Documentation

References

Reference overview
Schleifer, H., et al. 2012. Br. J. Pharmacol. 167, 1712.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision11-April-2013 JSW
SynonymsN-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-3-fluoroisonicotinamide
DescriptionA 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.
FormLight beige solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₇H₉F₇N₄O
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesSchleifer, H., et al. 2012. Br. J. Pharmacol. 167, 1712.