Bivalirudin

Bivalirudin is an inhibitor of alpha- and zeta-thrombin (Kis = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities. It is selective for alpha- and zeta-thrombin, lacking activity at trypsin and gamma-thrombin, which lacks clotting activity, at a >1,000-fold excess of bivalirudin. Bivalirudin inhibits alpha-thrombin-stimulated activation of the clotting factors Factor X, Factor V, and prothrombin in contact-activated plasma at a concentration of 0.1 µM. Administration of bivalirudin (0.5-1.5 mg/kg, i.v.) reduces platelet deposition in a rat carotid endarterectomy model in a dose-dependent manner. Formulations containing bivalirudin have been used to prevent ischemic events during angioplasty for thrombus-containing lesions.Formal Name: D-phenylalanyl-L-prolyl-L-arginyl-L-prolylglycylglycylglycylglycyl-L-asparaginylglycyl-L-alpha-aspartyl-L-phenylalanyl-L-alpha-glutamyl-L-alpha-glutamyl-L-isoleucyl-L-prolyl-L-alpha-glutamyl-L-alpha-glutamyl-L-tyrosyl-L-leucine. CAS Number: 128270-60-0. Molecular Formula: C98H138N24O33. Formula Weight: 2180.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 278 nm. SMILES: N[C@@H](C(N1[C@H](C(N[C@@H](CCCNC(N)=N)C(N2[C@H](C(NCC(NCC(NCC(NCC(N[C@@H](CC(N)=O)C(NCC(N[C@@H](CC(O)=O)C(N[C@@H](CC3=CC=CC=C3)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(O)=O)C(N[C@]([C@@H](C)CC)([H])C(N4CCC[C@H]4C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(O)=O)C(N[C@H](C(N[C@@H](CC(C)C)C(O)=O)=O)CC5=CC=C(O)C=C5)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCC2)=O)=O)CCC1)=O)CC6=CC=CC=C6. InChi Code: InChI=1S/C98H138N24O33/c1-5-52(4)82(96(153)122-39-15-23-70(122)92(149)114-60(30-34-79(134)135)85(142)111-59(29-33-78(132)133)86(143)116-64(43-55-24-26-56(123)27-25-55)89(146)118-67(97(154)155)40-51(2)3)119-87(144)61(31-35-80(136)137)112-84(141)58(28-32-77(130)131)113-88(145)63(42-54-18-10-7-11-19-54)117-90(147)66(45-81(138)139)110-76(129)50-107-83(140)65(44-71(100)124)109-75(128)49-106-73(126)47-104-72(125)46-105-74(127)48-108-91(148)68-21-13-38-121(68)95(152)62(20-12-36-103-98(101)102)115-93(15. InChi Key: OIRCOABEOLEUMC-GEJPAHFPSA-N.