[Ala17]-MCH acetate is a selective ligand for MCHR1 with a Ki of 0.16 nM and Kd of 0.37 nM(Eu3+ chelate-labeled). [Ala17]-MCH acetate shows selectivity over MCHR2 with Ki of 34 nM.
TC-MCH 7c is an oral, selectable and blood-brain barrier penetrating MCH1R antagonist with IC50 performance of 5.6 nM against hMCH1R, and TC-MCH 7c is a phenylpyridone derivative with MCH1R Ki of 3.4 nM against human. In mice, MCH1R Ki was 3.0 nM.
AZD1979 is a highly potent MCHR1 (Melanin-concentrating hormone receptor 1) antagonist with an IC50 of 12 nM, exhibiting improved central nervous system (CNS) exposure and enhanced insulin sensitivity in steady-state model assessments, making it suitable for the treatment of obesity.
ATC 0175 hydrochloride is an orally active melanocyte concentrating hormone 1 receptor antagonist that is potent and selective. ATC 0175 hydrochloride has affinity for MCH1R, MCH2R, MCH1, 5-HT2B receptors and 5-HT1A receptors with IC50s of 13.5 nM, >10,000 nM, 13 nM, 9.66 nM and 16.9 nM, respectively. ATC 0175 hydrochloride exhibits antidepressant and anxiolytic effects in animal models. aTC 0175 can be used to study depression and or anxiety disorders.
MCH(human, mouse, rat) is a potent endogenous agonist at melanin-concentration hormone (MCH) receptors (IC50 values are 0.3 and 1.5 nM and EC50 values are 3.9 and 0.1 nM at MCH1 and MCH2 receptors respectively). Increases food intake in vivo.
SNAP 94847 (SNAP-94847) is a selective and competitive MCH1 receptor (MCH1-R) antagonist (Ki: 2.2 nM). It has anxiolytic and antidepressant activity and reduces food intake in mice.
[Ala17]-MCH TFA, a selective ligand for MCHR 1 (K i =0.16 nM) over MCHR 2 (K i =34 nM), is an analogue of MCH. When labeled with a [Eu 3+ chelate], [Ala17]-MCH exhibits high affinity for MCHR 1 (K d =0.37 nM) and negligible binding affinity for MCHR 2.
BMS-814580 is a potent and selective functional antagonist (Kb = 117 nM) of human MCHR1. BMS-814580 exhibits potent binding affinity (Ki = 17 nM) for human MCHR1. BMS-814580 also exhibits potent binding affinities for cynomolgus monkey and rat MCHR1 (Ki o
BMS-819881, a melanin-concentrating hormone receptor 1 (MCHR1) antagonist, binds rat MCHR1 with a Ki of 7 nM, and is selective and potent for CYP3A4 activity with an EC50 of 13 μM.
MCH (human, mouse, rat) TFA is a potent peptide agonist for MCH receptors, exhibiting binding IC50 values of 0.3 nM for MCH1R and 1.5 nM for MCH2R. It is particularly effective against MCH-2R in a CHO cell line, with functional activation EC50 values of 3.9 nM for MCH-1R and 0.1 nM for MCH-2R, as evidenced by intracellular calcium mobilization measured with FLIPR [1].
Potent melanin-concentrating hormone (MCH) receptor agonist (EC50 values are 17 and 54 nM at MCH1 and MCH2 receptors respectively). Displays some selectivity towards MCH1 over MCH2 (Ki values are 0.16 and 34 nM respectively).
Melanin Concentrating Hormone, salmon TFA (MCH (salmon) TFA), is a 19-amino-acid neuropeptide discovered in the pituitary gland of teleost fish; it regulates food intake, energy balance, sleep states, and cardiovascular functions, and acts as a ligand for the orphan G protein-coupled receptors SLC-1 GPR24 and MCHR2.