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

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

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

Primary Target: CRAC
534351
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Aperçu

Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
1253186-56-9C₁₈H₁₂F₅N₃O₂

Products

RéférenceConditionnement Qté
5343510001 Flacon en verre 10 mg
Description
OverviewA 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 (t1/2 = 75-100 s), but with 2.5-fold slower than La3+ kinetically. Also inhibits Orail3 currents with similar potency but with faster kinetics (t1/2 = ~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 Number534351
Brand Family Calbiochem®
Synonyms2,6-Difluoro-N-(1-(4-hydroxy-2-(trifluoromethyl)benzyl)-1H-pyrazol-3-yl)benzamide, CRAC Chanel Blocker, GSK-7975A, GSK7975A
References
ReferencesVoronina, 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 number1253186-56-9
FormOff-white solid
Hill FormulaC₁₈H₁₂F₅N₃O₂
Chemical formulaC₁₈H₁₂F₅N₃O₂
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetCRAC
Purity≥98% 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 -20°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
Référence GTIN
5343510001 04054839324598

Documentation

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

Titre

Fiche de données de sécurité des matériaux (FDS) 

Références bibliographiques

Aperçu de la référence bibliographique
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.
Fiche technique

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.

Revision24-October-2017
Synonyms2,6-Difluoro-N-(1-(4-hydroxy-2-(trifluoromethyl)benzyl)-1H-pyrazol-3-yl)benzamide, CRAC Chanel Blocker, GSK-7975A, GSK7975A
DescriptionA 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 (t1/2 = 75-100 s), but with 2.5-fold slower than La3+ kinetically. Also inhibits Orail3 currents with similar potency but with faster kinetics (t1/2 = ~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.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1253186-56-9
Chemical formulaC₁₈H₁₂F₅N₃O₂
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
-20°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
ReferencesVoronina, 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.