Enlicitide chloride  (Synonyms: MK-0616 chloride)

Enlicitide chloride is an orally active inhibitor for PCSK9 that blocks the interaction between LPL receptor and PSCK9, with an IC₅₀ of 2.5 nM. Enlicitide chloride can be used in the study of cardiovascular diseases such as atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome or related cardiovascular and cardiometabolic disorders^[1][2][3].

Enlicitide chloride inhibits the protein-protein interaction between LPL receptor and PCSK9, increases the level of LPL receptor, and thus decreases the level of low-density lipoprotein cholesterol (LDL-C)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1586.29

C₈₂H₁₁₀ClFN₁₄O₁₅

2407527-16-4

Solid

White to off-white

Ala-{Dpr}-Phe-Trp-Pro-Thr-Tyr-Pro(Covalent bridge:Phe3-Pro5,Ala1-Trp4,Trp4-Pro8,Ala1-Pro8,D-Dpr2)

A-{Dpr}-FWPTYP(Covalent bridge:Phe3-Pro5,Ala1-Trp4,Trp4-Pro8,Ala1-Pro8,D-Dpr2)

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Ding FX, et al. Preparation of cyclic peptides as PCSK9 antagonist compounds: World Intellectual Property Organization, WO2019246349. 2019-12-26.

  [2]. WHO Drug Information-World Health Organization (WHO).

  [3]. Ahamad S, et al., Recent Update on the Development of PCSK9 Inhibitors for Hypercholesterolemia Treatment. J Med Chem. 2022 Dec 8;65(23):15513-15539.  [Content Brief]