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首页-小分子抑制剂&激动剂-Others-PCSK9-Enlicitide decanoate
Enlicitide decanoate

Chemical Structure : Enlicitide decanoate

CAS No.: 2861205-06-1

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Enlicitide decanoate (MK-0616 decanoate)

货号: PC-26305Not For Human Use, Lab Use Only.

Enlicitide decanoate (MK-0616) is a highly potent, orally bioavailable macrocyclic peptide inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) with Ki of 5 pM, binds to the LDLR binding domain of PCSK9.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Enlicitide decanoate (MK-0616) is a highly potent, orally bioavailable macrocyclic peptide inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) with Ki of 5 pM, binds to the LDLR binding domain of PCSK9.
Enlicitide (MK-0616) inhibitsPCSK9 with an IC50 2.5 nM in human plasma.
Enlicitide (MK-0616) has no observed off-target activity at 10 µM in 122 receptor, ion channel, enzyme radioligand binding, and cellular assays in the Eurofins Cerep Panlabs screening panel.
Enlicitide (MK-0616) is not only able to reduce LDL-cholesterol, non-HDL-cholesterol, and apoB, but can also lower Lp(a).

物理化学性质&存储条件

分子量 1722.09
分子式 C82H110FN14O15.C10H19O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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

参考文献

1. Li H, et al. J Am Chem Soc. 2025 Apr 2;147(13):11036-11048.

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