504187 P2Y Antagonist II, BPTU - Calbiochem

504187
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₃H₂₂F₃N₃O₃

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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®
      Synonyms1-(2-(2-tert-Butylphenoxy)pyridin-3-yl)-3-(4-(trifluoromethoxy)phenyl)urea, Purinergic Receptor P2Y Antagonist II
      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
      Quality LevelMQ100
      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

      P2Y Antagonist II, BPTU - Calbiochem 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
      Synonyms1-(2-(2-tert-Butylphenoxy)pyridin-3-yl)-3-(4-(trifluoromethoxy)phenyl)urea, Purinergic Receptor P2Y Antagonist II
      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.