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196876 | BAY 41-2272 - CAS 256376-24-6 - Calbiochem

196876
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₀H₁₇FN₆ 256376-24-6

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      196876-5MG
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable pyrazolopyridinylpyrimidine compound that acts as a selective and potent stimulator of soluble guanylate cyclase (effective dose ~ 0.1 nM to 100 µM using recombinant soluble guanylate cyclase). The mode of activation is NO-independent and appears to be mediated through direct binding to the α1 and α2 subunits. Shown to be effective in treating numerous cardiovascular conditions in animal models. Inhibits phenylephrine-induced constriction of rabbit aortic rings (IC50 = 304 nM) and blocks collagen-induced aggregation of human platelets (IC50 = 36 nM). Does not inhibit phosphodiesterases.
          Catalogue Number196876
          Brand Family Calbiochem®
          Synonyms5-Cyclopropyl-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-4-ylamine
          References
          ReferencesBoerrigter, G., et al. 2003. Circulation 107, 686.
          Kalsi, J.S., et al. 2003. J Urol. 169, 761.
          Koglin, M., et al. 2002. Biochem. Biophys. Res. Commun. 292, 1057.
          Becker, E.M., et al. 2001. BMC Pharmacol. 1, 13.
          Stasch, J.P., et al. 2001. Nature 410, 212.
          Product Information
          CAS number256376-24-6
          ATP CompetitiveN
          FormWhite solid
          Hill FormulaC₂₀H₁₇FN₆
          Chemical formulaC₂₀H₁₇FN₆
          ReversibleN
          Structure formula Image
          Applications
          Biological Information
          Primary TargetSoluble guanylate cyclase
          Primary Target IC<sub>50</sub>304 nM inhibiting phenylephrine-induced constriction of rabbit aortic rings; 36 nM in blocking collagen-induced aggregation of human platelets
          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 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 3 months at -20°C.
          Packaging Information
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          196876

          References

          Reference overview
          Boerrigter, G., et al. 2003. Circulation 107, 686.
          Kalsi, J.S., et al. 2003. J Urol. 169, 761.
          Koglin, M., et al. 2002. Biochem. Biophys. Res. Commun. 292, 1057.
          Becker, E.M., et al. 2001. BMC Pharmacol. 1, 13.
          Stasch, J.P., et al. 2001. Nature 410, 212.
          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.

          Revision05-April-2011 RFH
          Synonyms5-Cyclopropyl-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-4-ylamine
          DescriptionA cell-permeable pyrazolopyridinylpyrimidine compound that acts as a selective and potent stimulator of soluble guanylate cyclase (effective dose ~0.1 nM to 100 µM using recombinant soluble guanylate cyclase). The mode of activation is NO-independent and appears to be mediated through direct binding to the α1 and α2 subunits. Shown to be effective in treating numerous cardiovascular conditions in animal models. Inhibits phenylephrine-induced constriction of rabbit aortic rings (IC50 = 304 nM) and blocks collagen-induced aggregation of human platelets (IC50 = 36 nM). Does not inhibit phosphodiesterases.
          FormWhite solid
          CAS number256376-24-6
          Chemical formulaC₂₀H₁₇FN₆
          Structure formula
          Purity≥98% by HPLC
          SolubilityDMSO (10 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesBoerrigter, G., et al. 2003. Circulation 107, 686.
          Kalsi, J.S., et al. 2003. J Urol. 169, 761.
          Koglin, M., et al. 2002. Biochem. Biophys. Res. Commun. 292, 1057.
          Becker, E.M., et al. 2001. BMC Pharmacol. 1, 13.
          Stasch, J.P., et al. 2001. Nature 410, 212.