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

239821
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₁H₃₄N₄S₂ • HCl 1258011-83-4

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      239821-10MG
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          10 mg
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          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®
          Synonyms1,3-Dicyclohexyl-2-(3-methyl-6,6-dimethyl-5,6-dihydroimidazo[1,2-b]thiazole)-2-thiopseudourea, HCl, Fusin Antagonist II, IT1t
          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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          239821

          References

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

          Revision06-April-2011 RFH
          Synonyms1,3-Dicyclohexyl-2-(3-methyl-6,6-dimethyl-5,6-dihydroimidazo[1,2-b]thiazole)-2-thiopseudourea, HCl, Fusin Antagonist II, IT1t
          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 -20°C
          Hygroscopic
          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.
          Toxicity Standard Handling
          ReferencesWu, B., et al. 2010. Science 330, 1066.
          Thoma, G., et al. 2008. J. Med. Chem. 51, 7915.