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504187 P2Y Antagonist II, BPTU - Calbiochem

P2Y Antagonist II, BPTU - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 1-(2-(2-tert-Butylphenoxy)pyridin-3-yl)-3-(4-(trifluoromethoxy)phenyl)urea, Purinergic Receptor P2Y Antagonist II

Primary Target: P2Y₁
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504187
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₃H₂₂F₃N₃O₃

Products

Catalog NumberPackaging Qty/Pack
5.04187.0001 Glass bottle 10 mg
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 Protect from light
+2°C to +8°C
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.