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203890 CRAC Channel Inhibitor, BTP2 - CAS 223499-30-7 - Calbiochem

203890
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Empirical FormulaCAS #
C₁₅H₉F₆N₅OS223499-30-7

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      Description
      OverviewA cell-permeable pyrazole that acts as a more potent blocker of Stim1 and Orai1-coupled CRAC (Ca2+ release-activated Ca2+) channel-mediated SOCE (store-operated Ca2+ entry) in RBL-2H3 cells (IC50 = 590 nM by Fura-2; peak current density pA/pF = -1.13 and -7.50, respectively, with or without 3 µM BTP2/Pyr2 by whole cell clamp) than the transient receptor potential cation channel TRPC3-mediated ROCE (receptor-operated Ca2+ entry) inTRPC3-expressing HEK293 cells (IC50 = 4.21 µM by Fura-2; pA/pF = -1.54 and -18.50, respectively, with or without 3 µM BTP2/Pyr2). A great complement to Pyr 3 (Cat. No. 648490), Pyr6, and Pyr10 in Ca2+ signaling studies.
      Catalogue Number203890
      Brand Family Calbiochem®
      Synonyms[N-{4-[3,5-bis(Trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-4-methyl-1,2,3-thiadiazole-5-carboxamide], Pyr2, TPRC3 Channel Inhibitor II
      References
      ReferencesSchleifier, H., et al. 2012. Br J Pharmacol In Press
      Yonetoku, Y., et al. 2006. Bioorg. Med. Chem. 14, 5370.
      Yonetoku, Y., et al. 2006. Bioorg. Med. Chem. 14, 4750.
      Zitt, C., et al. 2004. J. Biol. Chem. 279, 12927.
      Trevillyan, J.M., et al. 2001. J. Biol. Chem. 276, 48118.
      Djuric, S.W., et al. 2000. J. Med. Chem. 43, 2975.
      Product Information
      CAS number223499-30-7
      ATP CompetitiveN
      FormSolid
      Hill FormulaC₁₅H₉F₆N₅OS
      Chemical formulaC₁₅H₉F₆N₅OS
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationCRAC Channel Inhibitor, BTP2, CAS 223499-30-7, is a cell-permeable, potent blocker of Stim1 and Orai1-coupled Ca2+ release-activated Ca2+ channel-mediated SOCE in RBL-2H3 cells (IC50 = 590 nM).
      Biological Information
      Primary TargetCRAC Channel
      Primary Target IC<sub>50</sub>590 nM by Fura-2
      Purity≥95% 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 Ambient Temperature Only
      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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      CRAC Channel Inhibitor, BTP2 - CAS 223499-30-7 - Calbiochem Certificates of Analysis

      TitleLot Number
      203890

      References

      Reference overview
      Schleifier, H., et al. 2012. Br J Pharmacol In Press
      Yonetoku, Y., et al. 2006. Bioorg. Med. Chem. 14, 5370.
      Yonetoku, Y., et al. 2006. Bioorg. Med. Chem. 14, 4750.
      Zitt, C., et al. 2004. J. Biol. Chem. 279, 12927.
      Trevillyan, J.M., et al. 2001. J. Biol. Chem. 276, 48118.
      Djuric, S.W., et al. 2000. J. Med. Chem. 43, 2975.
      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.

      Revision21-June-2013 JSW
      Synonyms[N-{4-[3,5-bis(Trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-4-methyl-1,2,3-thiadiazole-5-carboxamide], Pyr2, TPRC3 Channel Inhibitor II
      DescriptionA cell-permeable pyrazole that acts as a more potent blocker of Stim1 and Orai1-coupled CRAC (Ca2+ release-activated Ca2+) channel-mediated SOCE (store-operated Ca2+ entry) in RBL-2H3 cells (IC50 = 590 nM by Fura-2; peak current density pA/pF = -1.13 and -7.50, respectively, with or without 3 µM BTP2/Pyr2 by whole cell clamp) than the transient receptor potential cation channel TRPC3-mediated ROCE (receptor-operated Ca2+ entry) inTRPC3-expressing HEK293 cells (IC50 = 4.21 µM by Fura-2; pA/pF = -1.54 and -18.50, respectively, with or without 3 µM BTP2/Pyr2). A great complement to Pyr 3 (Cat. No. 648490), Pyr6, and Pyr10 in Ca2+ signaling studies.
      FormSolid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number223499-30-7
      Chemical formulaC₁₅H₉F₆N₅OS
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (5 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesSchleifier, H., et al. 2012. Br J Pharmacol In Press
      Yonetoku, Y., et al. 2006. Bioorg. Med. Chem. 14, 5370.
      Yonetoku, Y., et al. 2006. Bioorg. Med. Chem. 14, 4750.
      Zitt, C., et al. 2004. J. Biol. Chem. 279, 12927.
      Trevillyan, J.M., et al. 2001. J. Biol. Chem. 276, 48118.
      Djuric, S.W., et al. 2000. J. Med. Chem. 43, 2975.