Enlicitide Decanoate (MK-0616 Decanoate)

CAS No.: 2861205-06-1
Synonyms: MK-0616 decanoate
Target: PCSK9

Product Attributes

Attribute	Details
Molecular Formula	C82H110FN14O15.C10H19O2
Molecular Weight	1722.09
Exact Mass	1720.9644
Appearance	Solid powder
Purity	≥98% (HPLC)
Storage	Powder: -20°C (1 year) or -80°C (2 years), sealed, away from moisture; In solvent: -80°C (6 months) / -20°C (1 month)
Solubility	DMSO: ~14.29 mg/mL (8.30 mM, with ultrasonic assistance); Ethanol: up to 100 mg/mL

Note on Molecular Formula: KEGG and ChEBI list C82H110FN14O15.C10H19O2 as the consolidated formula, while ProbeChem and MCE present the free base and decanoate moieties separately as C82H110FN14O15.C10H19O2. Both representations are chemically equivalent; the separated format is preferred for clarity.

Biological Activity & Mechanism

Enlicitide decanoate is a highly potent, orally bioavailable macrocyclic peptide inhibitor of PCSK9.

Mechanism of Action: The compound binds with high affinity to the LDLR-binding domain of PCSK9, blocking the PCSK9–LDLR interaction. This prevents PCSK9-mediated lysosomal degradation of hepatic LDL receptors, thereby increasing LDLR availability on hepatocyte surfaces and enhancing hepatic clearance of circulating LDL-C.

Pharmacodynamic Effects: Reduces LDL-cholesterol, non-HDL-cholesterol, apolipoprotein B (ApoB), and lipoprotein(a) [Lp(a)]. As the first orally administered PCSK9-targeting therapy, it represents a significant advance over injectable PCSK9 inhibitors (monoclonal antibodies and siRNA).

Sequence Information (Research Reference)

Sequence: Ala-{Dpr}-Phe-Trp-Pro-Thr-Tyr-Pro
Covalent Bridges: Phe3–Pro5, Ala1–Trp4, Trp4–Pro8, Ala1–Pro8, D-Dpr2

Handling & Storage Precautions

• For research use only. Not for human or therapeutic use.

• Store powder sealed in a dry environment. Avoid repeated freeze-thaw cycles. After reconstitution, aliquot and store at -80°C for up to 6 months or -20°C for up to 1 month.

• For in vivo studies, prepare a clear DMSO stock solution first, then dilute sequentially using PEG300/Tween-80/saline or SBE-β-CD-based systems as appropriate.

Data Verification Summary

Verification Item	Sources	Conclusion
CAS–Name correspondence	ProbeChem / KEGG / ChEBI	Consistent
Molecular Weight	ProbeChem / KEGG / MCE	1722.09, consistent across sources
Ki / IC??	ProbeChem / MCE (citing Li H, JACS 2025)	5 pM / 2.5 nM, consistent
Mechanism	ProbeChem / Nature Cardiovasc Res / GlpBio	PCSK9–LDLR blockade, consistent
Storage Conditions	MCE / Selleck	Low-temperature, sealed, desiccated; MCE provides more detailed thresholds

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