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

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Sinonimi: 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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534351
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CAS #Empirical Formula
1253186-56-9C₁₈H₁₂F₅N₃O₂

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5343510001
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      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
      Numero di catalogo GTIN
      5343510001 04054839324598

      Documentation

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

      Titolo

      Scheda di sicurezza (MSDS) 

      Riferimenti bibliografici

      Panoramica delle referenze
      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.
      Scheda tecnica

      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.