Name: Bivalirudin
Synonyms: bg8967; D09HVL; D03ZVY; D09FGS; D0F4HO; AN-7543; bg 8967; HS-2004; hirulog; DB00006; bg-8967; angiomax; EBD32115; gtpl6470; BC657176; Hirulog 1; LS-172701; hirulog-1; CHEBI:59173; BIVALIRUDIN; bivalirudine; SCHEMBL25739; bivalirudina; bivalirudinum; angiomax (tn); BITTERMELONP.E; Bivalirudin, TFA; c9h11no.c2h6.ch4; Human Bivalirudin; Bivalirudin Acetate; bivalirudin [usan:ban:inn]; BG 8967, Hirulog, Hirulog I; bivalirudin trifluoroacetate; BivalirudinBG 8967, Hirulog, Hirulog I; the medicines company brand of bivalirudin; 8-methoxy-naphtho[2,3-b]thiophen-4,9-quinone; (r,r)-2,6-bis(4-phenyl-2-oxazolinyl)pyridine; 126:PN: WO2004076484 PAGE: 31 claimed protein; phe-pro-arg-pro-(gly)4-desulfohirudin-(53-64); phe-pro-arg-pro-(gly)4 desulfato-tyr63'-hirugen; (+)-2,6-bis[(4r)-4-phenyl-2-oxazolin-2-yl]pyridine; (r,r)-2,6-bis(4,5-dihydro-4-phenyl-2-oxazolyl)pyridine; phe-pro-arg-pro-(gly)4-asn-gly-asp-phe-glu-glu-ile-pro-glu-glu-tyr-leu; DPHE-PRO-ARG-PRO-GLY-GLY-GLY-GLY-ASN-GLY-ASP-PHE-GLU-GLU-LLE-PRO-GLU-GLU-TYR-LEU; H-D-Phe-Pro-Arg-Pro-Gly-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Glu-Glu-Ile-Pro-Glu-Glu-Tyr-Leu-OH; H-D-Phe-Pro-Arg-Pro-Gly-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Glu-Glu-Ile-Pro-Glu-Glu-Tyr-Leu-OH trifluoroacetate salt
CAS Registry number: 128270-60-0
Molecular Formula: C98H138N24O33
Refractive index: 1.675
Density: 1.52
Appearance: white to off-white powder
Product Category: API;proteins;Peptide
Uses: Alternative medicine as ordinary heparin and platelet glycoprotein IIb/IIIa antagonists.
Description: Bivalirudin was launched in New Zealand as an anticoagulant for i.v. treatment of patients with unstable angina undergoing percutaneous transluminal coronary angioplasty. Bivalirubin is a synthetic 20 amino acid peptide rationally modeled on hirudin (residues 53- 64), the most potent and specific naturally-occuring known inhibitor of thrombin, the enzyme that plays a key role in hemostasis and blood clot formation. This peptide is a direct thrombin inhibitor that maintains the unique bivalent binding properties of hirudin to the catalytic site and to the fibrin-recognition exosite of the enzyme, so acting directly on thrombin with high affinity and specificity. In vitro studies demonstrated that alpha- and zeta-thrombins, both with the higher fibrinogen-procoagulant activities, were inhibited. In rats receiving high doses of bivalirudin, the platelet deposition in carotide was reduced by 63% compared to controls. The results of clinical studies, conducted only in patients receiving concomitant aspirin, suggested that the use of bivalirudin was more efficacious and more predictable than unfractionated heparin, with fewer bleeding complications. Despite some unresolved developmental issues, the attractive properties of this novel agent could make it a useful alternative to heparin in a variety of coagulation disorders.
Clinical Use: Bivalirudin, a 20-amino-acid peptide, has been approved for use in patients with unstable angina undergoing percutaneous coronary intervention.
关键字： 原料药与中间体;
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