Setmelanotide Acetate(920014-72-8 free base) Bioactivity,Chemical Properties,Storage & Solubility Information Pathways-PeptideDB

Description	Setmelanotide Acetate(920014-72-8 free base) (RM-493 Acetate) is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively).
In vitro	黑色素皮质素受体激动剂在大脑中调节食物摄入和体重，并且与这些作用独立，影响胰岛素敏感性。Setmelanotide 对人类和大鼠MC4R（人类和大鼠MC4R的Kis分别为2.1和2.7 nM，EC50s分别为0.27和0.28 nM）表现出激动剂活性[1]。
In vivo	BIM-22493在夜间禁食后抑制再进食的效果依赖于功能性MC4R。BIM-22493能迅速改善葡萄糖稳态。在Lepob/Lepob小鼠中，BIM-22493显著增强葡萄糖清除效率，相较对照组。长期治疗BIM-22493与显著降低的血清胰岛素水平、血糖以及HOMA-IR值相关，这表明提高了胰岛素敏感性[1]。setmelanotide治疗能引起食物摄入短暂减少(35%)，并在8周治疗期间可持续减重(13.5%)，该数据来自一项饮食诱导的肥胖非人灵长类动物模型的研究[2]。
Target activity	MC4R (rat): 2.7 nM (ki), MC4R (rat):0.28 Nm (EC50), MC5R (human): 1600 nM (EC50), MC5R (human): 430 nM (ki), MC3R (human): 10 nM (ki), MC3R (human): 5.3nM (EC50), MC4R (human): 0.27 nM (EC50), MC4R (human): 2.1 nM (ki), MC1R (human):3.9 nM (ki), MC1R (human):5.8 nM (EC50)
Synonyms	RM-493 Acetate, IRC-022493 Acetate, BIM-22493 Acetate
molecular weight	1177.35
Molecular formula	C51H72N18O11S2
CAS	2759937-80-7
Storage	keep away from moisture　\|　Powder: -20°C for 3 years \| In solvent: -80°C for 1 year
Solubility	DMSO: 22.5 mg/mL (19.11 mM)
References	1. Kumar KG, et al. Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice. Peptides. 2009 Oct;30(10):1892-900. 2. Kievit P, et al. Chronic treatment with a melanocortin-4 receptor agonist causes weight loss, reduces insulin resistance, and improves cardiovascular function in diet-induced obese rhesus macaques. Diabetes. 2013 Feb;62(2):490-7.

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Setmelanotide Acetate(920014-72-8 free base)

CAS No.: 2759937-80-7