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首页-小分子抑制剂&激动剂-GPCR-Ghrelin Receptor (GHSR)-LEAP2
LEAP2

Chemical Structure : LEAP2

CAS No.: 1683582-94-6

LEAP2 (LEAP-2, Human liver expressed antimicrobial peptide-2)

货号: PC-26750Not For Human Use, Lab Use Only.

LEAP2 (Liver expressed antimicrobial peptide-2, LEAP-2) is an endogenous peptide antagonist of ghrelin receptor (GHSR) with IC50 of 6 nM on GHSR activation in the presence of ghrelin.

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

生物&药学活性

LEAP2 (Liver expressed antimicrobial peptide-2, LEAP-2) is an endogenous peptide antagonist of ghrelin receptor (GHSR) with IC50 of 6 nM on GHSR activation in the presence of ghrelin.
LEAP2 inhibits the receptor with potency similar to that with which ghrelin activates the receptor.
LEAP2 is a noncompetitive antagonist of GHSR, likely modulating the receptor through binding to an allosteric site.
LEAP2 is highly and specifically expressed in enterocytes along the luminal surface of the villi, but not in lamina propria or crypts.
LEAP2 antagonizes ghrelin-induced growth hormone secretion and food intake in mice.

物理化学性质&存储条件

分子量 4581.27
分子式 C191H316N64O57S5
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

Met-Thr-Pro-Phe-Trp-Arg-Gly-Val-Ser-Leu-Arg-Pro-Ile-Gly-Ala-Ser-Cys-Arg-Asp-Asp-Ser-Glu-Cys-Ile-Thr-Arg-Leu-Cys-Arg-Lys-Arg-Arg-Cys-Ser-Leu-Ser-Val-Ala-Gln-Glu (Disulfide bridge:Cys17-Cys28;Cys23-Cys33)

参考文献

1. Ge X, et al. LEAP2 Is an Endogenous Antagonist of the Ghrelin Receptor. Cell Metab. 2018 Feb 6;27(2):461-469.e6.

2. Krause A, et al. Protein Sci. 2003 Jan;12(1):143-52.

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