1369773-39-6

• 常用中文名：AHU377钙盐
• 常用英文名：AHU-377 hemicalcium salt
• CAS号：1369773-39-6
• 分子式：C₄₈H₅₆CaN₂O₁₀
• 分子量：861.0
• 相关类别： 信号通路 代谢酶/蛋白酶 脑啡肽酶
• 发布时间：2018-09-16 20:26:30
• 更新时间：2026-06-30 13:31:22
• Sacubitril (AHU-377) hemicalcium salt 是有效的NEP抑制剂,IC50值为5 nM。AHU-377是治疗心力衰竭药物LCZ696的一个组分。

名称

• 中文名: AHU-377 钙盐
• 英文名: AHU-377 (heMicalciuM salt)
• 中文别名: LCZ696中间体,10 MM DMSO 溶液; 沙库必曲钙LCZ696中间体; 沙库必曲钙盐(LCZ696中间体); 沙库巴曲钙盐; (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; LCZ696杂质; 3-羧基-1-氧代丙基)氨基]-ALPHA-甲基联苯-4-戊酸乙酯钙盐; LCZ696杂质P; 沙库必曲(LCZ696)钙盐 CRS; (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(2:1); 4-(((2R,4S)-1-([1,1'-联苯]-4-基)-5-乙氧基-4-甲基-5-氧代戊烷-2-基)氨基)-4-氧代丁酸钙盐; SACUBITRIL钙盐; 沙库必曲钙盐 CRS; (ALPH,GAMMAS)-GAMMA-[(3-羧基-1-氧代丙基)氨基]-ALPHA-甲基联苯-4-戊酸乙酯钙盐(2:1); 沙库巴曲缬沙坦杂质1; (ALPH,GAMMAS)-GAMMA-[(3-羰基-1-氧代丙基)氨基]-ALPHA-甲基联苯-4-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); 沙库必曲/缬沙坦/LCZ696; 沙库必曲钙盐SACUBITRIL CALCIUM; AHU-377 (半钙盐); LCZ696中间体7 AHU-377 (HEMICALCIUM SALT); Sacubitril hemicalcium salt :沙库比曲钙盐; 沙库必曲钙盐; AHU 377钙盐(LCZ696中间体-); LCZ-696杂质29 钙盐; (ALPH,GAMMAS)-GAMMA-[(3-羧基-1-氧代丙基)氨基]-ALPHA; LCZ696中间体 8; HU377钙盐; 沙库必曲钙盐-AHU377钙盐/LCZ696中间体; 沙库巴曲钙; AHU-377 钙盐1369-6; AHU377钙盐(LCZ696中间体); 沙库比曲钙盐; LCZ696原研; 沙库必曲钙盐/AHU377钙盐; 沙库必曲钙盐(中间体/医药中间体); (alphaR,gammaS)-gamma-[(3-羧基-1-氧代丙基)氨基]-alpha-甲基联苯-4-戊酸乙酯钙盐; 沙库巴曲半钙; LCZ696中间体; LCZ696中间体(AHU-377钙盐); 沙库必曲(LCZ696)钙盐; SACUBITRIL-D5 钙盐; 原研; (ALPH,GAMMAS)-GAMMA-[(3-羧基-1-氧代丙基)氨基]-ALPHA-甲基联苯-4-戊酸乙酯钙盐; LCZ中间体; (ΑR,ΓS)-Γ-[(3-羧基-1-氧代丙基)氨基]-Α-甲基联苯-4-戊酸乙酯钙盐; (ALPH,GAMMAS)-GAMMA-[(3-羧基-1-氧代丙基)氨基]-ALPHA-甲基联苯-4-戊酸乙酯钙; 沙卡布曲钙盐; 4-((2S,4R)-1-(联苯-4-基)-5-乙氧基-4-甲基-5-氧代戊烷-2-基氨基)-4-氧代丁酸钙; (αR,γS)-γ-[(3-羧基-1-氧代丙基)氨基]-α-甲基联苯-4-戊酸乙酯钙盐; 沙库比曲; 沙库比曲半钙盐; 沙库必曲半钙盐; GAMMAS)-GAMMA-[(3-羧基-1-氧代丙基)氨基]-ALPHA-甲基联苯-4-戊酸乙酯钙; Sacubitril hemicalcium salt试剂; SACUBITRIL-13C4 钙
• 英文别名: Calcium bis(4-{[(2S,4R)-1-(4-biphenylyl)-5-ethoxy-4-methyl-5-oxo-2-pentanyl]amino}-4-oxobutanoate); LCZ696 Impurity; Sacubitrial Calcium; (αR,γS)-γ-[(3-Cboxy-1-oxopropyl)amino]-α-methyl-[1,1'-biphenyl]-4-pentanoicacid4-ethylestercalciumsal; (αR,γS)-γ-[(3-Carboxy-1-oxopropyl)amino]-α-methyl-[1,1'-biphenyl]-4-pentanoic acid 4-ethyl ester calcium salt; SACUBITRIL-13C4 CALCIUM; [1,1'-Biphenyl]-4-pentanoic acid, γ-[(3-cboxy-1-oxopropyl)amino]-α-methyl-, 4-ethyl ester, calcium salt (2:1), (αR,γS); LCZ696(valstan + sacubitril) impurity 1; Sacubitril ca; (alph, gammaS) -gamma-[(3- carbonyl, -1-, oxo propyl), amino]-alpha-, biphenyl, -4-, ethyl valerate, calcium salt; LCZ696 hemicalcium salt; Ethyl (αR,γS)-γ-[(3-cboxy-1-oxopropyl)amino]-α-methyl-[1,1'-biphenyl]-4-pentanoate hemicalcium salt; (alph,gammaS)-gamma-[(3-Cboxy-1-oxopropyl)amino]-alpha-methyl-[1,1'-biphenyl]-4-pentanoic acid 4-ethyl ester calcium salt (2:1); AHU-377 Hemicalcium; Sacubitril calcium salt; Calcium 4-((2S,4R)-1-(biphenyl-4-yl) -5-ethoxy-4-methyl-5-oxopentan-2-ylamino)-4-oxobutanoate (Intermediate of Sacubitril Valstan Sodium); AHU377 Calcium Salt; [1,1'-Biphenyl]-4-pentanoic acid, γ-[(3-carboxy-1-oxopropyl)amino]-α-methyl-, α-ethyl ester, calcium salt, (αR,γS)- (2:1); (alph,gammaS)-gamma-[(3-Cboxy-1-oxopropyl)amino]-alpha-methyl-[1,1'-biphenyl]-4-pentanoic acid 4-ethyl ester calcium salt; (2R, 4S) -5- (biphenyl-4-yl) -4- (amino) -5- (3-cboxy-propionylamino-2-methyl-ventrate ethyl ester calcium salt; 1'-biphenyl]-4-pentanoic acid 4-ethyl ester calcium salt (2:1); AHU-377 hemicalcium salt (2:1); Sacubitril-d5 Calcium Salt; Sacubitril Calcium; Sacubitril hemicalcium salt, 10 mM in DMSO; Calciumbis(4-{[(1S,3R)-1-([1,1'-biphenyl]-4-ylmethyl)-4-ethoxy-3-methyl-4-oxobutyl] amino} -4-oxobutanoate); Sacubitrol calcium salt; Sacubitril Calcium Salt CRS; gammas)-gamma-[(3-Cboxy-1-oxopropyl)amino]-alpha-methyl-[1; 1,1'-Biphenyl]-4-pentanoic acid, γ-[(3-cboxy-1-oxopropyl)amino]-α-methyl-, 4-ethyl ester, calcium salt (2:1), (αR,γS); (2S,4R)-5-(Biphenyl-4-yl)-4-[(3-cboxypropionyl)amino]-2-methylpentanoic acid ethyl ester,calcium salt(2:1); Sacubitril Valstan Sodium (LCZ696); Sacubitril hemicalciium salt; (alph,gammaS)-gamma-[(3-Cboxy-1-oxopropyl)amino]-alpha-methyl-[1,1'-biphenyl]-4-pentanoic acid 4-ethyl ester calcium salt (2:1) (AHU-377 hemicalcium salt); Sacubitril calcium salt（AHU-377 ）; Calcium 4-(((2S,4R)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoate; (αR,γS)-γ-[(3-Cboxy-1-oxopropyl)amino]-α-methyl-[1,1'-biphenyl]-4-pentanoic acid 4-ethyl ester calcium salt; Calcium(2R,4S)-ethyl5-(4-biphenylyl)-4-amino-2-methyl-5-(3-cboxypropanoylamino)pentanoate; Sacubitril hemicalcium; (alph,gammaS)-gamma-[(3-Cboxy-1-oxopropyl)amino]-alpha-m; Ethyl (2R,4S)-5-(Biphenyl-4-yl)-4-(amino)-5-(3-cboxypropionyl)amino]-2-methylpentanoate, calcium salt; Sacubitril hemicalcium salt/AHU-377; Sabatrol calcium; (alph; Calcium4-(((2R,4S)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoate; monocalciummono(4-(((2R,4S)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy- 4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoate); LCZ 696 hemicalcium salt; Sacubitril 13C4 CalciumQ: What is Sacubitril 13C4 Calcium Q: What is the CAS Number of Sacubitril 13C4 Calcium; LCZ-696 Impurity 29 calcium salt; Calcium 4-((2S,4R)-1-(biphenyl-4-yl) -5-ethoxy-4-methyl-5-oxopentan-2-ylamino)-4-oxobutanoate; Sacubitril Hemicalcium salt; LCZ696 intermediates，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)

物化性质

• 分子式: C₄₈H₅₆CaN₂O₁₀
• 分子量: 861.0
• 精确质量: 860.3560868
• PSA: 191.06000
• LogP: 5.78240
• 外观性状: 白色至米白色粉末
• 储存条件: -20℃

生物活性

• 描述: Sacubitril (AHU-377) hemicalcium salt 是有效的NEP抑制剂,IC50值为5 nM。AHU-377是治疗心力衰竭药物LCZ696的一个组分。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 脑啡肽酶
  研究领域 >> 心血管疾病
• 靶点:

  IC50: 5 nM (NEP)[1]

• 体外研究: Sacubitril(AHU-377)是一种单分子,由缬沙坦,ARB和Sacubitril hemicalcium盐(一种中性溶酶抑制剂(1：1比例))的分子部分组成。 Sacubitril(AHU-377)通过酶促裂解乙酯转化为活性脑啡肽酶抑制代谢物LBQ657 [2]。无活性的NEPi前体Sacubitril hemicalcium盐不抑制成纤维细胞中的胶原蛋白积聚,也不抑制心肌细胞肥大。在心脏成纤维细胞中,活性NEPi LBQ657没有可辨别的作用。相反,LBQ657适度抑制心肌细胞肥大[3]。
• 体内研究: 在人类中,Sacubitril(AHU-377)(tmax 0.5-1.1小时)被迅速吸收。将Sacubitril半钙盐快速转化为LBQ657,其tmax达到1.9-3.5小时。生物活性LBQ657的平均t1/2值为9.9-11.1小时[2]。在载体处理的狗中,ANF使尿钠排泄从17.3±3.6增加到199.5±18.4 pequivkglmin。在接受Sacubitril(AHU-377)的动物中,这种作用显着增强。接受静脉注射Sacubitril(AHU-377)的动物的尿量也增强[1]。
• 参考文献:

  [1]. Ksander GM, et al. Dicarboxylic acid dipeptide neutral endopeptidase inhibitors. J Med Chem. 1995 May 12;38(10):1689-700.

  [2]. Voors AA, et al. The potential role of valsartan + AHU377 ( LCZ696 ) in the treatment of heart failure. Expert Opin Investig Drugs. 2013 Aug;22(8):1041-7.

  [3]. von Lueder TG, et al. Angiotensin receptor neprilysin inhibitor LCZ696 attenuates cardiac remodeling and dysfunction after myocardial infarction by reducing cardiac fibrosis and hypertrophy. Circ Heart Fail. 2015 Jan;8(1):71-8.

安全

• 符号: GHS06, GHS09
• 信号词: Danger
• 危害声明: H301-H400
• 警示性声明: Missing Phrase - N15.00950417
• 危害码 (欧洲): Xi
• 危险品运输编码: UN2811 - class 6.1 - PG 3 - EHS - Toxic solids, organic, n.o.s., HI: all