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 (34):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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.
    SNAP 94847 hydrochloride
  • HY-P1205A
    MCH(human, mouse, rat) TFA
    Agonist 99.84%
    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.
    MCH(human, mouse, rat) TFA
  • HY-P1525A
    Melanin Concentrating Hormone, salmon TFA
    Agonist 99.94%
    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.
    Melanin Concentrating Hormone, salmon TFA
  • HY-U00257
    AZD1979
    Antagonist 98.09%
    AZD1979 is a Melanin-concentrating hormone receptor 1 (MCHr1) antagonist with an IC50 of ~12 nM.
    AZD1979
  • HY-111398
    ALB-127158(a)
    Antagonist 99.52%
    ALB-127158(a) is a potent and selective melanin concentrating hormone 1 (MCH1) receptor antagonist.
    ALB-127158(a)
  • HY-107626A
    ATC0065 free base
    Antagonist
    ATC0065 free base is a potent, selective and orally active melanin-concentrating hormone (MCH) receptor 1 (MCHR1) antagonist with an IC50 of 15.7 nM for human MCHR1. ATC0065 free base does not exhibits significant activity for MCHR2. ATC0065 free base has anxiolytic and antidepressant activities.
    ATC0065 free base
  • HY-116031
    ATC0175 free base
    Antagonist
    ATC0175 (free base) is a potent and selective antagonist of melanin-concentrating hormone receptor 1 (MCH-R1) with an IC50 value of 3.4 nM, as well as good selectivity over the Y5 and the α2A receptors. ATC0175 (free base) is promising for research of obesity.
    ATC0175 free base
  • HY-161899
    MCHR1 antagonist 4
    Antagonist
    MCHR1 antagonist 4 (Compound 2m) is a blood-brain barrier permeable MCHR1 antagonist with Ki values of 0.74 nM and 0.76 nM for hMCHR1 and rMCHR1, respectively. MCHR1 antagonist 4 is also an effective anti-obesity agent.
    MCHR1 antagonist 4
  • HY-11083
    GW-803430
    Antagonist 99.10%
    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.
    GW-803430
  • HY-107623
    TC-MCH 7c
    Antagonist 99.79%
    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.
    TC-MCH 7c
  • HY-P1525
    Melanin Concentrating Hormone, salmon
    Agonist 98.40%
    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.
    Melanin Concentrating Hormone, salmon
  • HY-107624
    ATC0175
    Antagonist 99.84%
    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.
    ATC0175
  • HY-P4680
    (Phe13,Tyr19)-MCH (human, mouse, rat)
    Agonist 98.30%
    (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.
    (Phe13,Tyr19)-MCH (human, mouse, rat)
  • HY-P3155
    Ac-hMCH(6-16)-NH2
    Agonist 99.94%
    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.
    Ac-hMCH(6-16)-NH2
  • 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.
    MCH-1 antagonist 1
  • HY-N2073
    Ethyl linolenate
    Inhibitor ≥98.0%
    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.
    Ethyl linolenate
  • 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.
    MCHR1 antagonist 2
  • HY-P1204
    [Ala17]-MCH
    Agonist 98.28%
    [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.
    [Ala17]-MCH
  • 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.
    BMS-819881
  • 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.
    BMS-814580