534351 Sigma-AldrichCRAC Channel Inhibitor IV, GSK-7975A - CAS 1253186-56-9 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

SDS
References
Data Sheet

Synonyms: 2,6-Difluoro-N-(1-(4-hydroxy-2-(trifluoromethyl)benzyl)-1H-pyrazol-3-yl)benzamide, CRAC Chanel Blocker, GSK-7975A, GSK7975A

Primary Target: CRAC

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Overview

Replacement Information

Key Specifications Table

CAS #	Empirical Formula
1253186-56-9	C₁₈H₁₂F₅N₃O₂

Pricing & Availability

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Description
Overview	A cell permeable pyrazol derivative that acts as a specific CRAC (Ca²⁺ release-activated Ca²⁺ entry) channel blocker (IC₅₀ = 800 nM in RBL cells) possibly downstream of STIM1 oligomerization and STIM1/Orail interaction. Shown to fully block Orail1 and at 10 µM in HeK293 cells (t_1/2 = 75-100 s), but with 2.5-fold slower than La3+ kinetically. Also inhibits Orail3 currents with similar potency but with faster kinetics (t_1/2 = ~20s). Exhibits good selectivity against a panel of more than 16 ion channels, only with reduced effects on L-type Ca²⁺ (CaV1.2) and TRPV6 channels. Inhibits store-operated Ca2+ entry (IC₅₀ = 3.4 µM) at 10 µM in normal pancreatic acinar cells, but not in pancreatic acinar cell line AR42J which has a neuronal phenotype and hepatocytes, and does not affect acetylcholine or cholecystokinin induced Ca²⁺ spiking. Shown to block palmitoleic acid ethyl ester-induced trysin and protease activitiest and abolish necrosis. Additionally, reduces Fc?RI-dependent Ca²⁺ influx, at 3 µM and reduces the release of histamine, leukotriene C4, and cytokines (IL-5/-8/-13 and TNFα) by up to 50% in human lung mast cells (HLMC) and from rat, mouse and guinea-pig preparations. Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Catalogue Number	534351
Brand Family	Calbiochem®
Synonyms	2,6-Difluoro-N-(1-(4-hydroxy-2-(trifluoromethyl)benzyl)-1H-pyrazol-3-yl)benzamide, CRAC Chanel Blocker, GSK-7975A, GSK7975A

References
References	Voronina, S., et al. 2015. Biochem. J. 465, 405. Derler, I., et al. 2013. Cell Calcium. 53, 139l. Gerasimenko, J.V., et al. 2013. PNAS. 110, 13186. Louise, V., et al. 2013. Eur. J. Pharmacol. 704, 49. Ashmole, I., et al. 2012. J. Aller. Clin. Immun. 129, 1628.

Product Information
CAS number	1253186-56-9
Form	Off-white solid
Hill Formula	C₁₈H₁₂F₅N₃O₂
Chemical formula	C₁₈H₁₂F₅N₃O₂
Reversible	Y
Quality Level	MQ100

Applications

Biological Information
Primary Target	CRAC
Purity	≥98% by HPLC

Physicochemical Information
Cell permeable	Y

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	-20°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following 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

Documentation

CRAC Channel Inhibitor IV, GSK-7975A - CAS 1253186-56-9 - Calbiochem SDS

Title
Safety Data Sheet (SDS)

References

Reference overview
Voronina, S., et al. 2015. Biochem. J. 465, 405. Derler, I., et al. 2013. Cell Calcium. 53, 139l. Gerasimenko, J.V., et al. 2013. PNAS. 110, 13186. Louise, V., et al. 2013. Eur. J. Pharmacol. 704, 49. Ashmole, I., et al. 2012. J. Aller. Clin. Immun. 129, 1628.

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.

Revision	24-October-2017
Synonyms	2,6-Difluoro-N-(1-(4-hydroxy-2-(trifluoromethyl)benzyl)-1H-pyrazol-3-yl)benzamide, CRAC Chanel Blocker, GSK-7975A, GSK7975A
Description	A cell permeable pyrazol derivative that acts as a specific CRAC (Ca²⁺ release-activated Ca²⁺ entry) channel blocker (IC₅₀ = 800 nM in RBL cells) possibly downstream of STIM1 oligomerization and STIM1/Orail interaction. Shown to fully block Orail1 and at 10 µM in HeK293 cells (t_1/2 = 75-100 s), but with 2.5-fold slower than La3+ kinetically. Also inhibits Orail3 currents with similar potency but with faster kinetics (t_1/2 = ~20s). Exhibits good selectivity against a panel of more than 16 ion channels, only with reduced effects on L-type Ca²⁺ (CaV1.2) and TRPV6 channels. Inhibits store-operated Ca2+ entry (IC₅₀ = 3.4 µM) at 10 µM in normal pancreatic acinar cells, but not in pancreatic acinar cell line AR42J which has a neuronal phenotype and hepatocytes, and does not affect acetylcholine or cholecystokinin induced Ca²⁺ spiking. Shown to block palmitoleic acid ethyl ester-induced trysin and protease activitiest and abolish necrosis. Additionally, reduces Fc?RI-dependent Ca²⁺ influx, at 3 µM and reduces the release of histamine, leukotriene C4, and cytokines (IL-5/-8/-13 and TNFα) by up to 50% in human lung mast cells (HLMC) and from rat, mouse and guinea-pig preparations.
Form	Off-white solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	1253186-56-9
Chemical formula	C₁₈H₁₂F₅N₃O₂
Purity	≥98% by HPLC
Solubility	DMSO (50 mg/ml)
Storage	-20°C Protect from light
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity	Standard Handling
References	Voronina, S., et al. 2015. Biochem. J. 465, 405. Derler, I., et al. 2013. Cell Calcium. 53, 139l. Gerasimenko, J.V., et al. 2013. PNAS. 110, 13186. Louise, V., et al. 2013. Eur. J. Pharmacol. 704, 49. Ashmole, I., et al. 2012. J. Aller. Clin. Immun. 129, 1628.