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Volumn 20, Issue 22, 2010, Pages 6676-6679

Discovery of a vorapaxar analog with increased aqueous solubility

Author keywords

PAR 1 antagonist; SCH 530348 analog; SCH 602539; Solubility; Thrombin receptor antagonist; Vorapaxar analog

Indexed keywords

THROMBIN RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG; VORAPAXAR;

EID: 77958040965     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.09.009     Document Type: Article
Times cited : (19)

References (26)
  • 6
    • 85186492131 scopus 로고    scopus 로고
    • The TRA CER Executive and Steering Committees
    • The TRA CER Executive and Steering Committees. Am. Heart J. 2009, 158, 327.
    • (2009) Am. Heart J. , vol.158 , pp. 327
  • 13
    • 33748523149 scopus 로고    scopus 로고
    • For recent reviews on thrombin receptor (PAR-1) antagonists as antithrombotic agents, see: S. Chackalamannil J. Med. Chem. 49 2006 5389
    • (2006) J. Med. Chem. , vol.49 , pp. 5389
    • Chackalamannil, S.1
  • 22
    • 0034461768 scopus 로고    scopus 로고
    • Kinetic solubility test: The nephelometry (light scattering) method was used. The test compound (1.0 mg) was dissolved in DMSO to produce a 25 mM stock. A serial dilution into DMSO was performed on a robotic system and 3 μL of the compound in DMSO at various concentrations was added to the buffer (10 mM phosphate, pH 7.4). Following equilibration at room temperature for 30 min, the presence of precipitate was detected by nephelometry. Solubility was defined as the highest concentration of test compound that did not scatter light. Also, see: C.A. Lipinski J. Pharmacol. Toxicol. Methods 44 2001 235
    • (2001) J. Pharmacol. Toxicol. Methods , vol.44 , pp. 235
    • Lipinski, C.A.1
  • 24
    • 77958043225 scopus 로고    scopus 로고
    • For details of the ex vivo platelet aggregation assay in cynomolgus monkeys, see Ref. 12
    • For details of the ex vivo platelet aggregation assay in cynomolgus monkeys, see Ref. 12.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.