1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. MCHR1 (GPR24)

MCHR1 (GPR24)

Melanin concentrating hormone receptor 1

MCHR1 (GPR24), also known as Melanin concentrating hormone receptor 1, is a class A G-protein-coupled receptor (GPCR). MCHR1 has received considerable attention, as potent and selective antagonists acting at that receptor display anxiolytic, antidepressant and/or anorectic properties. MCHR1 is the sole receptor expressed in rodents and couples to Gi and Gq proteins.

MCH is a ubiquitous vertebrate neuropeptide predominantly synthesized by neurons of the diencephalon that can act through two G protein-coupled receptors, called MCHR1 and MCHR2. MCHR1 can inhibit cAMP accumulation and stimulate intracellular calcium flux, and is probably involved in the neuronal regulation of food consumption. Although structurally similar to somatostatin receptors, this protein does not seem to bind somatostatin.

MCHR1 (GPR24) Related Products (25):

Cat. No. Product Name Effect Purity
  • HY-P1205A
    MCH(human, mouse, rat) TFA
    Agonist 99.55%
    MCH (human, mouse, rat) TFA 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.
  • HY-P1525A
    Melanin Concentrating Hormone, salmon TFA
    Agonist 98.24%
    Melanin Concentrating Hormone, salmon TFA (MCH (salmon) TFA) 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.
  • HY-107625A
    SNAP 94847 hydrochloride
    Inhibitor 99.90%
    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.
  • HY-P1204
    [Ala17]-MCH
    Agonist 98.19%
    [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.
  • HY-111398
    ALB-127158(a)
    Antagonist 99.60%
    ALB-127158(a) is a potent and selective melanin concentrating hormone 1 (MCH1) receptor antagonist.
  • HY-120608
    BMS-814580
    Inhibitor
    BMS-814580 is an orally active, highly efficacious MCHR1 inhibitor with a Ki of 16.9 nM against hMCHR1. BMS-814580 shows antiobesity activities.
  • HY-107624
    ATC0175
    Antagonist
    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.
  • HY-107623
    TC-MCH 7c
    Antagonist ≥99.0%
    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. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively.
  • HY-100331
    MCH-1 antagonist 1
    Antagonist
    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.
  • HY-11083
    GW-803430
    Antagonist 98.06%
    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.
  • HY-100321
    MCHR1 antagonist 2
    Antagonist 98.27%
    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.
  • HY-U00257
    AZD1979
    Antagonist 98.09%
    AZD1979 is a Melanin-concentrating hormone receptor 1 (MCHr1) antagonist with an IC50 of ~12 nM.
  • HY-12433
    BMS-819881
    Antagonist
    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.
  • HY-P1869
    Neuropeptide EI, rat
    Antagonist
    Neuropeptide EI, rat displays functional melanin concentrating hormone (MCH)-antagonist and melanocyte-stimulating hormone (MSH) agonist activity in different behavioral paradigms.
  • HY-P3155
    Ac-hMCH(6-16)-NH2
    Agonist
    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.
  • HY-N2073S
    Ethyl linolenate-d5
    Inhibitor
    Ethyl linolenate-d5 is the deuterium labeled Ethyl linolenate. 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.
  • HY-136152
    MCHR1 antagonist 3
    Antagonist
    MCHR1 antagonist 3 is a potent the melanin-concentrating hormone receptor-1 (MCHR1) antagonist. MCHR1 antagonist 3 is used to regulate energy metabolism.
  • HY-P1204A
    [Ala17]-MCH TFA
    Agonist
    [Ala17]-MCH TFA, 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.
  • HY-100318
    NGD-4715
    Antagonist
    NGD-4715 is a selective and orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist .
  • HY-107625
    SNAP 94847
    Antagonist
    SNAP 94847 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 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.