沙库巴曲钙
| 中文名称 | 沙库巴曲钙 |
|---|---|
| 中文同义词 | AHU377钙盐;沙库必曲钙盐;AHU-377 钙盐1369773-39-6;HU377钙盐;LCZ696中间体(AHU-377钙盐);(2R,4S)-5-(联苯-4-基)-4-(氨基)-5-(3-羧基-丙酰基氨基)-2甲基-戊酸乙酯钙盐;(2S,4R)-5-(联苯基-4-基)-4-[(3-羧基丙酰基)氨基]-2-甲基戊酸乙酯 钙盐(2:1);原研534-06 |
| 英文名称 | AHU-377 (heMicalciuM salt) |
| 英文同义词 | AHU-377 (heMicalciuM salt);(alphaR,gammaS)-gamma-[(3-Carboxy-1-oxopropyl)amino]-alpha-methyl-[1,1'-biphenyl]-4-pentanoic acid 4-ethyl ester calcium salt (2:1);(2S,4R)-5-(Biphenyl-4-yl)-4-[(3-carboxypropionyl)amino]-2-methylpentanoic acid ethyl ester,calcium salt(2:1);AHU-377 hemicalcium salt (2:1);Calciumbis(4-{[(1S,3R)-1-([1,1'-biphenyl]-4-ylmethyl)-4-ethoxy-3-methyl-4-oxobutyl] amino} -4-oxobutanoate);Sacubitril Hemicalcium salt;(αR,γS)-γ-[(3-Carboxy-1-oxopropyl)amino]-α-methyl-[1,1'-biphenyl]-4-pentanoic acid 4-ethyl ester calcium salt;[1,1'-Biphenyl]-4-pentanoic acid, γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl-, 4-ethyl ester, calcium salt (2:1), (αR,γS)- |
| CAS号 | 1369773-39-6 |
| 分子式 | C48H56CaN2O10 |
| 分子量 | 861.04364 |
| EINECS号 | 935-847-3 |
| 相关类别 | LCZ696 中间体;医药中间体;杂质对照品;LCZ696中间体;对照品-杂质对照品;抗高血压;化工原料;原料药及中间体;医药原料;化学试剂;lcz696;LCZ 696;Pharmaceutical Intermediates;Intermediates |
| Mol文件 | 1369773-39-6.mol |
| 结构式 |  |
沙库巴曲钙 性质
| 熔点 | >140°C (dec.) |
|---|---|
| 密度 | 1.24g/cm3 at 20℃ |
| 蒸气压 | 0.001Pa at 20℃ |
| 储存条件 | -20°C |
| 溶解度 | DMSO（微溶，加热）、甲醇（微溶） |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| LogP | -0.66-2.9 at 20℃ and pH2-7 |
沙必利是一种与缬沙坦联合使用的降压药。这种名为缬沙坦/沙必利的联合药物在试验中被称为LCZ696，并以Entresto品牌销售，是一种治疗心力衰竭的药物。本品用作该药物中间体和杂质对照品，用于药品申报检测等。
Sacubitril (AHU-377) hemicalcium salt 是有效的NEP抑制剂，IC50值为5 nM。Sacubitril hemicalcium salt 是研究心力衰竭药物 LCZ696 的一个组分。IC50: 5 nM (NEP)
Sacubitril (AHU-377) is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and Sacubitril hemicalcium salt, a neprilysin inhibitor (1:1 ratio). Sacubitril (AHU-377) is converted by enzymatic cleavage of the ethyl ester into the active neprilysin inhibiting metabolite LBQ657. The inactive NEPi precursor, Sacubitril hemicalcium salt, does not inhibit collagen accumulation in fibroblasts nor cardiac myocyte hypertrophy. In cardiac fibroblasts, the active NEPi LBQ657 had no discernible effects. In contrast, LBQ657 modestly inhibits cardiac myocyte hypertrophy.
In humans, Sacubitril (AHU-377)(t max 0.5-1.1 h) are absorbed quickly. Sacubitril hemicalcium salt is converted rapidly into LBQ657 with its t max being reached in 1.9-3.5 h. Mean t 1/2 values for the biologically active LBQ657 is 9.9-11.1 h.In vehicle-treated dogs, ANF increases urinary sodium excretion from 17.3±3.6 to 199.5±18.4 pequivkglmin. This effect is potentiated significantly in animals which receive Sacubitril (AHU-377). Urinary volume is also potentiated in animals which receive an iv administration of Sacubitril (AHU-377).
安全信息
| 危险品运输编号 | UN2811 - class 6.1 - PG 3 - EHS - Toxic solids, organic, n.o.s., HI: all |
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| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/11/08 | HY-15407A | LCZ696中间体 Sacubitril hemicalcium salt | 1369773-39-6 | 2mg | 410元 |
| 2024/11/08 | HY-15407A | LCZ696中间体 Sacubitril hemicalcium salt | 1369773-39-6 | 5mg | 700元 |