Evolocumab

Names

[ Name ]:
Evolocumab

[Synonym ]:
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

Biological Activity

[Description]:

Evolocumab (AMG 145) is a human monoclonal antibody that inhibits PCSK9. Evolocumab binds to the circulating PCSK9 protein, inhibiting it from binding to the LDLR. Evolocumab can be used for the research of hypercholesterolemia and atherosclerotic cardiovascular diseases[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Ser/Thr Protease

Research Areas >> Metabolic Disease

[Target]

PCSK9[1]

[References]

[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.

Chemical & Physical Properties

[ Boiling Point ]:
1364.0±75.0 °C at 760 mmHg

[ Molecular Formula ]:
C₅₈H₉₇N₁₅O₁₆S₂Se

[ Molecular Weight ]:
1403.572

[ Flash Point ]:
778.7±37.1 °C

[ Exact Mass ]:
1403.584473

[ LogP ]:
3.66

[ Vapour Pressure ]:
0.0±0.6 mmHg at 25°C