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239821 CXCR4 Antagonist II - CAS 1258011-83-4 - Calbiochem

The CXCR4 Antagonist II, also referenced under CAS 1258011-83-4, controls the biological activity of CXCR4. This small molecule/inhibitor is primarily used for Cell Signaling applications.

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Synonyme: IT1t, 1,3-Dicyclohexyl-2-(3-methyl-6,6-dimethyl-5,6-dihydroimidazo[1,2-b]thiazole)-2-thiopseudourea, HCl, Fusin Antagonist II

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      Übersicht

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      1258011-83-4C₂₁H₃₄N₄S₂ • HCl
      Description
      OverviewA thiopseudourea compound that acts as a selective and highly potent CXCR4/Fusin antagonist (IC50 = 1.1 nM against SDF-1/CXCL12-induced Ca2+ mobilization in CEM cells) and effectively targets CXCR4-mediated binding of both CXCL12 (IC50 = 8 and 11 nM in competitive binding assays using human CEM and rat IR983F membrane, respectively) and HIV gp120 (IC50 = 7 nM in HIV attachment assays). Shown to be orally available in rat with good in vivo pharmacokinetics (32% availability, tmax = 0.5 h, Cmax= 18 ng/ml, t1/2 = 7.6 h, based on an oral dose of 1 mg/kg). Comparing to AMD3100 (Cat. No. 239820), CXCR4 Antagonist II is ~30-times more potent as a CXCR4-CXCL12 interaction blocker, while being ~2-fold less potent in blocking gp120-mediated HIV attachment.
      Catalogue Number239821
      Brand Family Calbiochem®
      SynonymsIT1t, 1,3-Dicyclohexyl-2-(3-methyl-6,6-dimethyl-5,6-dihydroimidazo[1,2-b]thiazole)-2-thiopseudourea, HCl, Fusin Antagonist II
      References
      ReferencesWu, B., et al. 2010. Science 330, 1066.
      Thoma, G., et al. 2008. J. Med. Chem. 51, 7915.
      Product Information
      CAS number1258011-83-4
      FormWhite solid
      Hill FormulaC₂₁H₃₄N₄S₂ • HCl
      Chemical formulaC₂₁H₃₄N₄S₂ • HCl
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      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 -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      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
      Bestellnummer GTIN
      239821 0

      Documentation

      CXCR4 Antagonist II - CAS 1258011-83-4 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      CXCR4 Antagonist II - CAS 1258011-83-4 - Calbiochem Analysenzertifikate

      TitelChargennummer
      239821

      Literatur

      Übersicht
      Wu, B., et al. 2010. Science 330, 1066.
      Thoma, G., et al. 2008. J. Med. Chem. 51, 7915.
      Datenblatt

      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.

      Revision06-April-2011 RFH
      SynonymsIT1t, 1,3-Dicyclohexyl-2-(3-methyl-6,6-dimethyl-5,6-dihydroimidazo[1,2-b]thiazole)-2-thiopseudourea, HCl, Fusin Antagonist II
      DescriptionA thiopseudourea compound that acts as a selective and highly potent CXCR4/Fusin antagonist (IC50 = 1.1 nM against SDF-1/CXCL12-induced Ca2+ mobilization in CEM cells) and effectively targets CXCR4-mediated binding of both CXCL12 (IC50 = 8 and 11 nM in competitive binding assays using human CEM and rat IR983F membrane, respectively) and HIV gp120 (IC50 = 7 nM in HIV attachment assays). Shown to be orally available in rat with good in vivo pharmacokinetics (32% availability, tmax = 0.5 h, Cmax= 18 ng/ml, t1/2 = 7.6 h, based on an oral dose of 1 mg/kg). Comparing to AMD3100 (Cat. No. 239820), CXCR4 Antagonist II is ~30-times more potent as a CXCR4-CXCL12 interaction blocker, while being ~2-fold less potent in blocking gp120-mediated HIV attachment.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1258011-83-4
      Chemical formulaC₂₁H₃₄N₄S₂ • HCl
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      -20°C
      Hygroscopic
      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
      ReferencesWu, B., et al. 2010. Science 330, 1066.
      Thoma, G., et al. 2008. J. Med. Chem. 51, 7915.