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徐亚萍

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虫号: 233886
注册: 2006-03-30
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专业: 生物化学

[交流] 新药-比伐卢定大家讨论一下

比伐卢定:这种药除了上海子能制药还有别的生产厂家吗？它与蛇毒凝血酶是不是一种东西，

比伐卢定 [128270-60-0] Purity (HPLC)

≥98% D-Phe-Pro-Arg-Pro-Gly-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Glu-Glu-Ile-Pro-Glu-Glu-Tyr-Leu

合成工艺：Monograph Number:  1306
Title:  Bivalirudin
CAS Registry Number:  128270-60-0
Additional Names:  Hirulog-1;  hirulog-8
Manufacturers' Codes:  BG-8967
Trademarks:  Angiomax (Medicines Co.);  Hirulog (Biogen)
Molecular Formula:  C98H138N24O33
Molecular Weight:  2180.28.
Percent Composition:  C 53.99%, H 6.38%, N 15.42%, O 24.22%
Literature References:  Synthetic peptide of 20 amino acids; member of a novel class of bivalent thrombin inhibitors.  Characterized by an anion binding exosite (ABE) derived from hirudin, q.v., linked to a thrombin catalytic site inhibitor moiety by tetraglycine.  Prepn and structure activity study:  J. M. Maraganore et al., WO 91 02750; eidem, US 5196404 (1991, 1993 both to Biogen); eidem, Biochemistry 29, 7095 (1990).  Determn in plasma and whole blood:  T. J. Reid, B. M. Alving, Thromb. Haemostasis 70, 608 (1993).  Clinical pharmacology:  I. Fox et al., ibid. 69, 157 (1993).  Clinical study in myocardial infarction:  P. Théroux et al., Circulation 91, 2132 (1995); during coronary angioplasty:  J. A. Bittl et al., N. Engl. J. Med. 333, 764 (1995).  Review of antithrombotic activity and clinical evaluation:  J. M. Maraganore, Perspect. Drug Discovery Design 1, 461-478 (1993).
Therap-Cat:  Antithrombotic.
RCB_CT,74865Entry Name: Bivalirudin, BAN, INN, USAN
Synonym(s): Hirulog I. Angiomax. BG 8967
Chapman  Hall Number: NCZ48-N
CAS Registry Number: 128270-60-0
Type of Compound Code(s): XA2290 XA4500 XA1350
H-D-Phe-Pro-Arg-Pro-Gly-Gly-Gly-Gly-Asn-Gly-Asp-Phe-Glu-Glu-Ile-Pro-Glu-Glu-Tyr-Leu-OH
Molecular Formula: C98H138N24O33
Molecular Weight: 2180.309
Accurate Mass: 2178.985821
Percentage Composition: C 53.99%; H 6.38%; N 15.42%; O 24.22%
Biological Use/Importance: Anticoagulant. Haemostatic agent
Development Status: Approved by FDA
References:
Maraganore, J.M. et al., Biochemistry, 1990, 29, 7095, (synth, pharmacol)
Skrzypczak-Jankun, E. et al., J. Mol. Biol., 1991, 221, 1379, (struct)
Pat. Coop. Treaty (WIPO), 1991, 91 02 750 (Biogen); CA, 115, 150383j, (synth, pharmacol)
Maraganore, J.M., Adv. Exp. Med. Biol., 1993, 340, 227, (rev)
Roemisch, J. et al., Haemostasis, 1993, 23, 249, (pharmacol)
Fox, I. et al., Thromb. Haemostasis, 1993, 69, 157, (pharmacol)
Johnson, P.H., Annu. Rev. Med., 1994, 45, 165, (rev)
Scatena, R., Expert Opin. Invest. Drugs, 2000, 9, 1119-1127, (rev)
Carswell, C.I. et al., Drugs, 2002, 62, 841-870, (rev

新人，需鼓励

[ Last edited by 小小强 on 2006-5-18 at 22:37 ]

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