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

Overview

Key Specifications Table

CAS #Empirical Formula
223499-30-7C₁₅H₉F₆N₅OS

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203890-5MG
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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
      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
      Global Trade Item Number
      Catalog Number GTIN
      203890-5MG 04055977204070