中文名卡比托辛英文名Carbetocin别名卡比托辛卡贝缩宫素醋酸卡贝缩宫素卡贝缩宫素三氟醋酸盐醋酸卡贝缩宫素,卡比托辛卡贝缩宫素-多肽原料委托生产卡贝缩宫素-多肽制剂一致性评价醋酸卡贝缩宫素 英文别名CarbetocinCARBETOCIN(BUTYRYL1,TYR(ME)2)-OXYTOCINCARBETOCIN TRIFLUOROACETATE SALT(2-O-METHYLTYROSINE)-DE-AMINO-1-CARBAOXYTOCIN(BUTYRYL1,TYR(ME)2)-OXYTOCIN TRIFLUOROACETATE SALT(Butyryl1,Tyr(me)2)-1-Carbaoxytocin trifluoroacetate salt(BUTYRYL1,TYR(ME)2)-1-CARBAOXYTOCIN TRIFLUOROACETATE SALTBUTYRYL-TYR(ME)-ILE-GLN-ASN-CYS-PRO-LEU-GLY-NH2 TRIFLUOROACETATE SALTBUTYRYL-TYR(ME)-ILE-GLN-ASN-CYS-PRO-LEU-GLY-NH2, (SULFIDE BOND BETWEEN BUTYRYL-4-YL AND CYS)1-{[(3R,6S,9S,12S,15S)-6-(2-Amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-(4-hydroxybenzyl)-16-methy-pentaoxo-1-thia-4,7,10,13,16-pentaazacycloicosan-3-yl]carbonyl}-L-prolyl-L-leucylglycinamideglycinamide, 1-[[(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-15-[(4-hydroxyphenyl)methyl]-16-methyl-12-[(1S)-1-methylpropyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentaazacycloeicos-3-yl]carbonyl]-L-prolyl-L-leucyl-CASEINECS化学式C45H69N11O12S分子量988.17InChIInChI=1/C45H69N11O12S/c1-6-25(4)38-44(67)50-28(15-16-34(46)58)40(63)51-30(21-35(47)59)41(64)53-31(23-69-(61)55(5)33(43(66)54-38)20-26-11-13-27(57)14-12-26)45(68)56-17-7-9-32(56)42(65)52-29(19-24(2)3)39(62)49-22-36(48)60/h-33,38,57H,6-10,15-23H2,1-5H3,(H2,46,58)(H2,47,59)(H2,48,60)(H,49,62)(H,50,67)(H,51,63)(H,52,65)(H,53,64)(H,54,66)/t25-,28-,29-,30-,3/m0/s1密度1.218±0.06 g/cm3(Predicted)熔点°C沸点1477.9±65.0 °C(Predicted)比旋光度D -69.0° (c = 0.25 in 1M acetic acid)闪点846.7°C蒸汽压0mmHg at 25°C溶解度DMSO (Slightly), Methanol (Slightly)折射率1.541酸度系数13.07±0.70(Predicted)存储条件-15°C稳定性Hygroscopic外观powder颜色white to beige体外研究Carbetocin is an agonist with about 10-fold lower affinity for the oxytocin receptor but with significantly higher stability and a longer duration of action. Carbetocin has higher affinity to the chimeric E1 receptor and especially to each of the combinations of E1 with the other extracellular domains, i.e. chimeric receptors E13 (K i =13 nM), E123 (K i =56 nM), and E1234 (K i =37 nM).