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首页-小分子抑制剂&激动剂-GPCR-Glucagon Receptor-Retatrutide
Retatrutide

Chemical Structure : Retatrutide

CAS No.: 2381089-83-2

Retatrutide (LY3437943, LY-3437943)

货号: PC-21069Not For Human Use, Lab Use Only.

Retatrutide (LY3437943) is a potent, triple agonist peptide of glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R) with EC50 of 5.79 nM, 0.064 nM and 0.775 nM in cAMP assays.

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

生物&药学活性

Retatrutide (LY3437943) is a potent, triple agonist peptide of glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R) with EC50 of 5.79 nM, 0.064 nM and 0.775 nM in cAMP assays.
Retatrutide (LY3437943) is a full agonist at the GCGR, GIPR, and GLP-1R in the functional assays.
Retatrutide (LY3437943) also is a potent agonist at the mouse GCGR, GIPR, and GLP-1R in receptor binding affinity and functional potency assays in vitro.
Retatrutide (LY3437943) promotes body weight loss in C57/Bl6 diet-induced obese (DIO) mice with ED50 of 4.73 nmol/kg.
Retatrutide (LY3437943) increases energy expenditure through glucagon receptor engagement in obese mice.
Retatrutide (LY3437943) causes greater body weight loss in obese mice than tirzepatide (Cat# PC-72629), increases energy expenditure through glucagon receptor activation.

物理化学性质&存储条件

分子量 4731.33
分子式 C221H342N46O68
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

L-Serinamide, L-tyrosyl-2-methylalanyl-L-glutaminylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-alpha-aspartyl-L-tyrosyl-L-seryl-L-isoleucyl-2-methyl-L-leucyl-L-leucyl-L-alpha-aspartyl-L-lysyl-N6-[N-(19-carboxy-1-oxononadecyl)-L-gamma-glutamyl-2-[2-(2-aminoethoxy)ethoxy]acetyl]-L-lysyl-L-alanyl-L-glutaminyl-2-methylalanyl-L-alanyl-L-phenylalanyl-L-isoleucyl-L-alpha-glutamyl-L-tyrosyl-L-leucyl-L-leucyl-L-alpha-glutamylglycylglycyl-L-prolyl-L-seryl-L-serylglycyl-L-alanyl-L-prolyl-L-prolyl

参考文献

1. Coskun T, et al. Cell Metab. 2022 Sep 6;34(9):1234-1247.e9.

2. Rosenstock J, et al. Lancet. 2023 Aug 12;402(10401):529-544.

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