LY2112688 TFA is a potent and selective melanocortin receptor 4 (MC-4R, MC4R) agonist with Ki of 0.55/0.39 nM for human/rat MC4R, >30-fold selective over MC1/3/5 receptors.
LY2112688 TFA is a potent and selective melanocortin receptor 4 (MC-4R, MC4R) agonist with Ki of 0.55/0.39 nM for human/rat MC4R, >30-fold selective over MC1/3/5 receptors. LY2112688 selectively induces MC-4-mediated cAMP release (MC-4/3 EC50 = 0.25 nM/1.61 nM, MC-4/3 Emax = 94.5%/84.1% of NDP-α-MSH Emax using HEK293 expressing respective human receptors). LY2112688 exhibits in vivo efficacy in reducing daily food intake and promoting weight loss among diet-induced obese rats (75 & 299 nmol/kg/day s.c.).
物理化学性质&存储条件
分子量
1175.35 (free base)
分子式
C51H70N18O11S2 · xC2HF3O2
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-Cysteinamide, N2-acetyl-D-arginyl-L-cysteinyl-L-α-glutamyl-L-histidyl-D-phenylalanyl-L-arginyl-L-tryptophyl-, cyclic (2→8)-disulfide TFA salt
参考文献
1. Kievit P, et al. Diabetes. 2013 Feb;62(2):490-7.
2. Molden BM, et al. Mol Endocrinol. 2015 Nov;29(11):1619-33.
