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Setmelanotide (trifluoroacetate salt)

产品介绍
产品介绍
产品信息
简单描述
Setmelanotide is a cyclic peptide agonist of melanocortin receptor 4 (MC4R).1 It increases cAMP production in CHO-K1 cells expressing MC4R, MC1R, MC3R, and MC5R (EC50s = 0.27, 5.8, 5.3, and 1,600 nM, respectively, for the human receptors) but not in cells expressing MC2R (EC50 = >10 µM). Setmelanotide (6.4 µmol/animal) inhibits food intake in MC3R, but not MC4R, knockout mice. It also reduces food intake and hepatosteatosis, induces weight loss, and decreases serum insulin, glucose, and leptin levels in a mouse model of diet-induced obesity when administered at a dose of 300 nmol/kg per day. Formulations containing setmelanotide have been used in chronic weight management due to proopiomelanocortin (POMC), proprotein convertase subtilisin/kexin type 1 (PCSK1), or leptin receptor deficiency.WARNING This product is not for human or veterinary use.

商品描述
A peptide agonist of MC4R

分子量
1117.3

纯度
≥98%

产品类型
Biochemicals/Peptides/Receptor Pharmacology/Agonists

背景
别名
Formal_Name:cyclic (2→8)-disulfide N2-acetyl-L-arginyl-L-cysteinyl-D-alanyl-L-histidyl-D-phenylalanyl-L-arginyl-L-tryptophyl-L-cysteinamide, trifluoroacetate salt;Synonyms:BIM-22493 N-acetyl-RCAHFRWC-NH2 RM-493

研究领域
Endocrinology & Metabolism/Metabolic Diseases/Diabetes/Obesity/Steatotic Liver Diseases,Neuroscience/Behavioral Neuroscience/Food Intake
结构式
O=C([C@@H](NC([C@H](NC([C@@H](NC([C@H](NC([C@H](CSSC[C@H](NC1=O)C(N)=O)NC([C@@H](NC(C)=O)CCCNC(N)=N)

分子式
C49H68N18O9S2 • XCF3COOH

制备和贮存
保存
≥ 4 years

溶解方法
Water: soluble

保存方式
-20°C
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