Evolocumab

• 常用名: Evolocumab
• 英文名: Evolocumab
• CAS号: 1256937-27-5
• 分子量: 1403.572
• 密度: N/A
• 沸点: 1364.0±75.0 °C at 760 mmHg
• 分子式: C₅₈H₉₇N₁₅O₁₆S₂Se
• 熔点: N/A
• 闪点: 778.7±37.1 °C

Evolocumab用途

Evolocumab(AMG 145)是一种抑制PCSK9的人类单克隆抗体。Evolocumab与循环中的PCSK9蛋白结合,抑制其与LDLR结合。Evolocumab可用于研究高胆固醇血症和动脉粥样硬化性心血管疾病[1]。

Evolocumab名称

• 英文名: (2S,5S,8S,11R,14R,17S,20S,23S,26S,29S)-29-Amino-6,19,22,25,28-pentahydroxy-2-(2-hydroxy-2-iminoethyl)-17,23-bis[4-({hydroxy[(2R,3R)-3-methyl-3,4-dihydro-2H-pyrrol-2-yl]methylene}amino)butyl]-20-isobutyl-26-isopropyl-5-methyl-8-[2-(methylsulfanyl)ethyl]-9,10,15,16-tetraoxo-11-(selanylmethyl)-14-(sulfanylmethyl)-3,4,7,12,13,18,21,24,27-nonaazadotriaconta-6,18,21,24,27-pentaene-1,32-dioic acid

Evolocumab生物活性

• 描述: Evolocumab(AMG 145)是一种抑制PCSK9的人类单克隆抗体。Evolocumab与循环中的PCSK9蛋白结合,抑制其与LDLR结合。Evolocumab可用于研究高胆固醇血症和动脉粥样硬化性心血管疾病[1]。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> Ser/Thr蛋白酶
  研究领域 >> 代谢疾病
• 靶点:

  PCSK9[1]

• 参考文献:

  [1]. Fala L, et, al. Repatha (Evolocumab): Second PCSK9 Inhibitor Approved by the FDA for Patients with Familial Hypercholesterolemia. Am Health Drug Benefits. 2016 Mar;9(Spec Feature):136-9.

Evolocumab物理化学性质

• 沸点: 1364.0±75.0 °C at 760 mmHg
• 分子式: C₅₈H₉₇N₁₅O₁₆S₂Se
• 分子量: 1403.572
• 闪点: 778.7±37.1 °C
• 精确质量: 1403.584473
• LogP: 3.66
• InChIKey: PUHBRGRYFZDQIV-UHFFFAOYSA-N
• SMILES: CCCCN=C1NC(=Cc2ccc(-n3cnc(C)c3)c(OC)c2)C(=O)N1C(C)c1ccc(F)cc1.CCN=C1NC(=Cc2ccc(-n3cnc(C)c3)c(OC)c2)C(=O)N1C(C)c1ccc(F)cc1.COC1=NC(=Cc2ccc(-n3cnc(C)c3)c(OC)c2)C(=O)N1C(C)c1ccc(F)cc1.COc1cc(C=C2NC(=NCC3CC3)N(C(C)c3ccc(F)cc3)C2=O)ccc1-n1cnc(C)c1.COc1cc(C=C2NC(=NCCCO)N(C(C)c3ccc(F)cc3)C2=O)ccc1-n1cnc(C)c1
• 蒸汽压: 0.0±0.6 mmHg at 25°C
• 储存条件: -20℃，避光

Evolocumab英文别名

• 3,4,7,12,13,18,21,24,27-Nonaazadotriaconta-6,18,21,24,27-pentaene-1,32-dioic acid, 29-amino-17,23-bis[4-[[[(2R,3R)-3,4-dihydro-3-methyl-2H-pyrrol-2-yl]hydroxymethylene]amino]butyl]-6,19,22,25,28-pentahydroxy-2-(2-hydroxy-2-iminoethyl)-14-(mercaptomethyl)-5-methyl-26-(1-methylethyl)-20-(2-methylpropyl)-8-[2-(methylthio)ethyl]-9,10,15,16-tetraoxo-11-(selenylmethyl)-, (2S,5S,8S,11R,14R,17S,20S,23S,26S,29S)-
• (2S,5S,8S,11R,14R,17S,20S,23S,26S,29S)-29-Amino-6,19,22,25,28-pentahydroxy-2-(2-hydroxy-2-iminoethyl)-17,23-bis[4-({hydroxy[(2R,3R)-3-methyl-3,4-dihydro-2H-pyrrol-2-yl]methylene}amino)butyl]-20-isobutyl-26-isopropyl-5-methyl-8-[2-(methylsulfanyl)ethyl]-9,10,15,16-tetraoxo-11-(selanylmethyl)-14-(sulfanylmethyl)-3,4,7,12,13,18,21,24,27-nonaazadotriaconta-6,18,21,24,27-pentaene-1,32-dioic acid