BMS-819881 is a melaninconcentrating hormone receptor 1 (MCHR1) antagonist, which binds rat MCHR1 with a Ki of 7 nM. BMS-819881 also is selective and potent for CYP3A4 activity with an EC50 of 13 μM.
GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pIC50 of 9.3. GW-803430 is orally active in an animal model of obesity[1].
MCH (human, mouse, rat) is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively[1].
ALB-127158(a) is a potent and selective melanin concentrating hormone 1 (MCH1) receptor antagonist.
Ac-hMCH(6-16)-NH2 binds to and activates equally well both human MCH receptors present in the brain (non-selective agonist), with IC50 values of 0.16 nM and 2.7 nM for MCH-1R and MCH-2R[1].
A highly potent, subtype-selective melanin concentrating hormone receptor 1 (MCHR1) inhibitor with Ki of 17 nM, without inhibitory activity for MCHR2 at 10 uM; exhibits functional potency with Kb of 117 nM in FLIPR-based assay, with no activity for MCHR2 at 10 uM, dose-dependently reduces body weight in a chronic diet-induced obese model.
MCHr1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; MCHr1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells.
SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters[1][3].
[Ala17]-MCH, a MCH analogue (HY-P1525A), is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). [Eu3+ chelate-labeled [Ala17]-MCH shows high affnity for MCHR1 (Kd=0.37 nM) while has little demonstrable binding affnity for MCHR2[1].
Neuropeptide EI, rat displays functional melanin concentrating hormone (MCH)-antagonist and melanocyte-stimulating hormone (MSH) agonist activity in different behavioral paradigms[1].
MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM. MCH-1 antagonist 1 also inhibits CYP3A4 with an IC50 of 10 μM.
MCHr1 antagonist 1 is a selective antagonist of melanin concentrating hormone-1 (MCH1) receptor, with a Kb of 1 nM and a Ki of 4 nM at human MCH1, and may be used to reduce the body mass.
AMG-076 is an orally bioavailable and selective MCHR1 antagonist. AMG-076 results in significant reduction in body weight gain in nonobese mice fed a high-fat diet and in high-fat diet-induced obese (DIO) mice[1].
SB-568849 is a melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pKi of 7.7.
Ethyl linolenate is a fatty acid ethyl ester (FAEE). Ethyl linolenate plays an active role in inhibition of the cellular production on melanin with an IC50 of 70 μM. Anti-melanogenesis Effects[1].
TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R[1]. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively[2].
Melanin Concentrating Hormone, salmon is a 19-amino-acid neuropeptide initially identified in the pituitary gland of teleost fish, which regulates food intake, energy balance, sleep state, and the cardiovascular system. Melanin-concentrating hormone is a ligand for an orphan G protein-coupled receptor (SLC-1/GPR24) and MCHR2.
ATC0175 is a potent, selective and orally active melanin-concentrating hormone 1 recepter antagonist with IC50s of 13.5, >10000 nM for MCH1R, MCH2R, respectively. ATC0175 shows antidepressant effects and anxiolytic effects in animal models. ATC0175 has the potential for the research of depression and/or anxiety disorders[1].
AZD1979 is a Melanin-concentrating hormone receptor 1 (MCHr1) antagonist with an IC50 of ~12 nM.
NGD-4715 is a selective and orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist .
hMCH-1R antagonist 1 (Compound 30) is an effective and selective antagonist of human melanin-concentrating hormone receptor 1 (hMCHR1) with an KB value of 3.6 nM. HMCH-1R antagonist 1 can bind to hMCHR1 and hMCHR2 with IC50 values of 65 nM and 49 nM, respectively. HMCH-1R antagonistist 1 can be used for metabolic research[1].
SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCH1) antagonist with antidepressant-like activity, it differentiates from classic anxiolytic and antidepressant drugs.SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.SNAP 94847 is a high affinity antagonist (pA2 = 7.81) of MCH-evoked inositol phosphate formation[1].
MCHR1 antagonist 3 is a potent the melanin-concentrating hormone receptor-1 (MCHR1) antagonist. MCHR1 antagonist 3 is used to regulate energy metabolism[1].
(Phe13,Tyr19)-MCH (human, mouse, rat) is a potent SLC-1 and S643b receptor ligand. (Phe13,Tyr19)-MCH (human, mouse, rat) can be used as an agonist for SLC-1 and S643b receptor[1].