肝素
肝素(Heparin)
CAS: 9005-49-6;91449-79-5
化学式: C26H41NO34S4
| 中文名 | 肝素 |
| 英文名 | Heparin |
| 别名 | 肝素 瑞肝素钠 瑞维肝素钠 |
| 英文别名 | LMWH OP 386 FR 860 Vetren CY 216 Cy 222 KB 101 Fluxum OP 622 Arteven Pabyrin Heparin Pularin Eparina Clexane Liquemin Clivarin Heparine Heparina Vitrum AB Fragmin A HSDB 3094 Fragmin B Octaparin Bemiparin Reviparin Hepathrom Heparinum Clivarine Subeparin Ardeparin Liquaemin Triofiban Fraxiparin Sublingula Heparinate Parvoparin Sandoparin Lipo-hepin Tinzaparin Nadroparin Parnaparin Certoparin Multiparin Dalteparin Nadroparine Hed-heparin Novoheparin depo-Heparin alpha-Heparin SODIUM HEPARIN Thromboliquine Heparinic acid Heparin CY 216 Eparina [DCIT] UNII-E47C0NF7LV UNII-T2410KM04A Heparin sulfate HEPARIN SODIUM LMW HEPARIN SODIUM SALT Heparinum [INN-Latin] Heparine [INN-French] Heparina [INN-Spanish] PORCINE HEPARIN SODIUM HEPARIN SODIUM (BOVINE) HEPARIN SODIUM, PORCINE HEPARIN PORCINE SODIUM SALT LOW MOLECULAR WEIGHT HEPARIN SODIUM N-ethyl-3-hydroxy-N,N-dimethylanilinium 1,1-diphenyl-4-(piperidin-1-yl)butan-1-ol N-(2-bromobenzyl)-N,N-dimethylethanaminium 2-(carbamoyloxy)-N,N,N-trimethylethanaminium 2-{2-[(5-carboxypentyl)amino]-2-oxo-1-[(phenylacetyl)amino]ethyl}-5,5-dimethyl-1,3-thiazolidine-4-carboxylic acid (6R,7R)-7-{[(2E)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino}-3-{[(1-methyl-1H-tetrazol-5-yl)sulfanyl]methyl}-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (2S,3S,4R,5R,6R)-3-({(2R,3R,4R,5S,6R)-3-(acetylamino)-4,5-dihydroxy-6-[(sulfooxy)methyl]tetrahydro-2H-pyran-2-yl}oxy)-6-{[(2S,3S,4S,5R,6S)-6-{[(2R,3S,4S,5R)-2-carboxy-4,6-dihydroxy-5-(sulfooxy)tetrahydro-2H-pyran-3-yl]oxy}-2-hydroxy-4-(sulfomethyl)-5-(sulfooxy)tetrahydro-2H-pyran-3-yl]oxy}-4,5-dihydroxytetrahydro-2H-pyran-2-carboxylic acid (non-preferred name) |
| CAS | 9005-49-6 91449-79-5 |
| EINECS | 232-681-7 |
| 化学式 | C26H41NO34S4 |
| 分子量 | 1134.93 |
| InChI | InChI=1/C26H41NO34S4/c1-4(28)27-7-9(30)8(29)6(2-52-63(43,44)45)53-24(7)56-15-10(31)11(32)25(58-19(15)21(36)37)55-13-5(3-62(40,41)42)14(60-64(46,47)48)26(59-22(13)38)57-16-12(33)17(61-65(49,50)51)23(39)54-18(16)20(34)35/h5-19,22-26,29-33,38-39H,2-3H2,1H3,(H,27,28)(H,34,35)(H,36,37)(H,40,41,42)(H,43,44,45)(H,46,47,48)(H,49,50,51)/t5-,6+,7+,8+,9+,10+,11+,12-,13-,14+,15-,16-,17+,18+,19-,22-,23?,24+,25+,26-/m0/s1 |
| 密度 | 2.13g/cm3 |
| 熔点 | 250 °C (decomp) |
| 比旋光度 | D20 +55° |
| 溶解度 | H2O: 50毫克/毫升，透明，淡黄 |
| 折射率 | 1.711 |
| 外观 | 结晶 (细) |
| 颜色 | white |
| 物化性质 | 肝素钠系自猪或牛的肠黏膜中提取的硫酸氨基葡聚糖的钠盐，为白色或类白色的粉末，无臭无味，有引湿性。在水中易溶，不溶于乙醇、丙酮等有机溶剂。肝素注射液是肝素的灭菌水溶液，为无色或淡黄色的澄明液体；肝素冻疮软膏为含肝素钠的白色软膏。本品因最早在狗的肝脏中被发现，故名肝素。在自然界中，肝素广泛分布在哺乳动物的肝、肺、心、脾、肾、胸腺、肠黏膜、肌肉和血液里，多与蛋白质结合成复合体存在。这种复合体无抗凝血活性，随着蛋白质除去而活性增加。在体内被肝脏产生的肝素酶灭活而随尿排泄出去。肝素是含有硫酸酯的黏多糖，分子结构用一个四糖重复单元表示，组分是氨基葡萄糖、艾杜糖醛酸和葡萄糖醛酸。由于肝素分子中含有约占分子量的40%的硫酸根阴离子，因而带有许多负电荷，这种高度带负电的物理化学特性，干扰了血凝过程的许多环节。肝素的抗血栓形成作用，除了与各凝血因子活性被抑制外，尚有血管壁相互作用以及其他作用因素。此外，肝素还具有降血脂、抗动脉粥样硬化、抗炎、抗过敏的作用，还具有防止血栓形成、脑血管疾病、清除肾病形成等作用。 |
| 体外研究 | Heparin is a potent anticoagulant drug based on its ability to accelerate the rate at which antithrombin inhibits serine proteases in the blood coagulation cascade. Heparin and the structurally related heparan sulfate are complex linear polymers comprised of a mixture of chains of different length, having variable sequences. Heparin interactes most tightly with peptides containing a complementary binding site of high positive charge density. Heparin and heparan sulfate predominantly exhibit linear helical secondary structures with sulfo and carboxyl groups displayed at defined intervals and in defined orientations along the polysaccharide backbone. Heparin resembles DNA as both are highly charged linear polymers that behave as polyelectrolytes. Heparin is believed to function as an anticoagulant primarily through its interaction with AT III by enhancing AT-III-mediated inhibition of blood coagulation factors, including thrombin and factor Xa. Heparin binds to AT III and thrombin in a ternary complex, increasing the bimolecular rate constant for the inhibition of thrombin by a factor of 2000. Heparin is principally located in the granules of tissue mast cells that are closely associated with the immune response. Heparin makes numerous contacts with both FGF-2 and FGFR-1 stabilizing FGF–FGFR binding. Heparin also makes contacts with the FGFR-1 of the adjacent FGF–FGFR complex, thus seeming to promote FGFR dimerization. |
| 安全术语 | 24/25 - 避免与皮肤和眼睛接触。 |
| WGK Germany | 2 |
| RTECS | MI0850000 |
| FLUKA BRAND F CODES | 3-10 |
| 上游原料 | 乙醇 过氧化氢 滤纸 强碱性阴离子交换树脂 阴离子树脂 水 三氯甲烷 |
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