119152 Adenosine A₃ Receptor Antagonist, MRS 1523 - CAS 212329-37-8 - Calbiochem

119152
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Overview

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Key Spec Table

Empirical FormulaCAS #
C₂₃H₂₉NO₃S 212329-37-8

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119152-5MG
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      Description
      OverviewA pyridine derivative that acts as a highly selective antagonist of A3 receptor with excellent potency in both humans and rodents (Ki = 18.9 nM for human A3R, and 113 nM for rat A3R). Exhibits only a trivial antagonistic activity towards A1 and A2A receptors (Ki = 15.6 µM and 2.05 µM for rat A1R and A2AR, respectively). Abolishes the agonistic effects of Cl-IB-MECA (Cat. No. 119139) on A3R-mediated proliferation of primary human coronary smooth muscle cells. Also, reported to block NECA (Cat. No. 119140)-induced bronchoconstriction in an allergic murine model.
      Catalogue Number119152
      Brand Family Calbiochem®
      Synonyms3-propyl-6-ethyl-5[(ethylthio)carbonyl]-2-phenyl-4-propyl-3-pyridine-carboxylate, MRS 1523, MRS-1523
      References
      ReferencesChen, Z., 2012. FASEB J. 26, 1855.
      Chanyshev, B., et al. 2012. Pharmacol Res.65, 338.
      Choi, I., et al. 2011. Am J Pathol. 179, 2042.
      Fan, M., et al. 2003. Am J Physiol Lung Cell Mol Physiol. 284, L1012.
      Li, A. H., et al. 1998. J Med Chem. 41, 3186.
      Jacobson, K. A., et al. 1999. Drug Dev Res. 45, 113.
      Product Information
      CAS number 212329-37-8
      FormClear to light brown oil
      Hill FormulaC₂₃H₂₉NO₃S
      Chemical formulaC₂₃H₂₉NO₃S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetA₃ Receptor
      Primary Target K<sub>i</sub>18.9 nM
      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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      References

      Reference overview
      Chen, Z., 2012. FASEB J. 26, 1855.
      Chanyshev, B., et al. 2012. Pharmacol Res.65, 338.
      Choi, I., et al. 2011. Am J Pathol. 179, 2042.
      Fan, M., et al. 2003. Am J Physiol Lung Cell Mol Physiol. 284, L1012.
      Li, A. H., et al. 1998. J Med Chem. 41, 3186.
      Jacobson, K. A., et al. 1999. Drug Dev Res. 45, 113.
      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.

      Revision19-March-2018 JSW
      Synonyms3-propyl-6-ethyl-5[(ethylthio)carbonyl]-2-phenyl-4-propyl-3-pyridine-carboxylate, MRS 1523, MRS-1523
      DescriptionA pyridine derivative that acts as a highly selective antagonist of A3 receptor with excellent potency in both humans and rodents (Ki = 18.9 nM for human A3R, and 113 nM for rat A3R). Exhibits only a trivial antagonistic activity towards A1 and A2A receptors (Ki = 15.6 µM and 2.05 µM for rat A1R and A2AR, respectively). Abolishes the agonistic effects of Cl-IB-MECA (Cat. No. 119139) on A3R-mediated proliferation of primary human coronary smooth muscle cells. Also, reported to block NECA (Cat. No. 119140)-induced bronchoconstriction in an allergic murine model.
      FormClear to light brown oil
      Intert gas (Yes/No) Packaged under inert gas
      CAS number 212329-37-8
      Chemical formulaC₂₃H₂₉NO₃S
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 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
      ReferencesChen, Z., 2012. FASEB J. 26, 1855.
      Chanyshev, B., et al. 2012. Pharmacol Res.65, 338.
      Choi, I., et al. 2011. Am J Pathol. 179, 2042.
      Fan, M., et al. 2003. Am J Physiol Lung Cell Mol Physiol. 284, L1012.
      Li, A. H., et al. 1998. J Med Chem. 41, 3186.
      Jacobson, K. A., et al. 1999. Drug Dev Res. 45, 113.