504187 | P2Y Antagonist II, BPTU - Calbiochem

504187
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₃H₂₂F₃N₃O₃

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.04187.0001
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          Glass bottle 10 mg
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          Description
          OverviewA phenoxypyridinyl-phenylurea that acts as a highly selective P2Y1 antagonist (Ki = 6 nM against 0.5 nM 2-MeS-ADP for human P2Y1 binding), while displaying much reduced or no affinity toward other P2Y family GPCRs (Ki = ≥2.5 µM toward hP2Y14; Ki >15 µM toward human P2Y2, P2Y6, P2Y11, and P2Y12). Effectively inhibits 2.5 µM ADP-induced platelet aggregation in vitro (IC50 = 2.1 µM) and reduces FeCl2-induced carotid artery blood clot formation in anesthetized rats in vivo (10 mg/kg/h i.v. infusion) with much less effect toward prolonging cuticle and mesenteric bleeding time when compared to another P2Y12 antagonist Clopidogrel. Pharmackinetic studies reveal only moderate oral bioavailability in rat.
          Catalogue Number504187
          Brand Family Calbiochem®
          SynonymsPurinergic Receptor P2Y Antagonist II, 1-(2-(2-tert-Butylphenoxy)pyridin-3-yl)-3-(4-(trifluoromethoxy)phenyl)urea
          References
          ReferencesZhang, D., et al. 2015. Nature In press.
          Chao, H., et al. 2013. J. Med. Chem. 56, 1704.
          Product Information
          FormWhite powder
          Hill FormulaC₂₃H₂₂F₃N₃O₃
          Chemical formulaC₂₃H₂₂F₃N₃O₃
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetP2Y₁
          Purity≥99% 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 +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
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Zhang, D., et al. 2015. Nature In press.
          Chao, H., et al. 2013. J. Med. Chem. 56, 1704.
          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.

          Revision09-August-2013 JSW
          SynonymsPurinergic Receptor P2Y Antagonist II, 1-(2-(2-tert-Butylphenoxy)pyridin-3-yl)-3-(4-(trifluoromethoxy)phenyl)urea
          DescriptionA phenoxypyridinyl-phenylurea that acts as a highly selective P2Y1 antagonist (Ki = 6 nM against 0.5 nM [β-33P]-2-MeS-ADP in competitive binding assays toward human P2Y1), while displaying much reduced or no affinity toward other P2Y family G-protein-coupled purinergic receptors (Ki = ≥2.5 µM against 0.5 nM [β-33P]-2-MeS-ADP binding toward hP2Y14; Ki >15 µM toward human P2Y2, P2Y6, P2Y11, and P2Y12). Effectively inhibits 2.5 µM ADP-induced platelet aggregation in vitro (IC50 = 2.1 µM using human platelet rich plasma) and reduces FeCl2-induced (via 10 min localized artery surface exposure to 50% FeCl2) carotid artery internal thrombus (blood clot) formation in anesthetized rats in vivo (by 68% 50 min post 10 min FeCl2 exposure; single 10 mg/kg i.v. 15 min prior to FeCl2 exposure, followed by continuous i.v. infusion at 10 mg/kg/h) with only 3.3- and 3.1-fold enhanced cuticle and mesenteric bleeding time, respectively. The same antithrombosis efficacy when achieved with the P2Y12 antagonist Clopidogrel (20 mg/kg p.o.) is reported to result in much prolonged cuticle and mesenteric bleeding time (4.1- and 8.2-fold of control level, respectively). Pharmacokinetic studies in rats indicate a moderate oral bioavailability (F = 10%; Cmax = 5.83 µM; Tmax = 2 h; T1/2 = 1.43 h; 30 mg/kg delivered with 10% cremophor:10% EtOH:80% H2O).
          FormWhite powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₃H₂₂F₃N₃O₃
          Structure formulaStructure formula
          Purity≥99% by HPLC
          SolubilityDMSO (100 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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesZhang, D., et al. 2015. Nature In press.
          Chao, H., et al. 2013. J. Med. Chem. 56, 1704.