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LY2112688 trifluoroacetate

Chemical Structure : LY2112688 trifluoroacetate

CAS No.: 819048-44-7

LY2112688 trifluoroacetate (LY-2112688, LY2112688 TFA)

Catalog No.: PC-26945Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.).

Physicochemical Properties

M.Wt 1175.35 (free base)
Formula C51H70N18O11S2 · xC2HF3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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.

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