MCHR1 (GPR24), also known as Melanin concentrating hormone receptor 1, belongs to a member of the G protein-coupled receptor family 1, is an integral plasma membrane protein which binds melanin-concentrating hormone, and is one of the melanin-concentrating hormone receptors found in all mammals. 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 is thought to regulate appetite, and also functions in stress, anxiety and depression.


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BMS-819881

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.

  • CAS Number: 1197420-05-5
  • MF: C24H21ClN2O4S
  • MW: 468.953
  • Catalog: MCHR1 (GPR24)
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 697.7±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 375.8±34.3 °C

ALB-127158(a)

ALB-127158(a) is a potent and selective melanin concentrating hormone 1 (MCH1) receptor antagonist.

  • CAS Number: 1173154-32-9
  • MF: C23H21FN4O2
  • MW: 404.44
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SNAP 94847 hydrochloride

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].

  • CAS Number: 1781934-47-1
  • MF: C29H33ClF2N2O2
  • MW: 515.03
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Neuropeptide EI (human, mouse, rat) trifluoroacetate salt

Neuropeptide EI, rat displays functional melanin concentrating hormone (MCH)-antagonist and melanocyte-stimulating hormone (MSH) agonist activity in different behavioral paradigms[1].

  • CAS Number: 125934-45-4
  • MF: C63H98N16O23
  • MW: 1447.55000
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MCH-1 antagonist 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.

  • CAS Number: 1039825-68-7
  • MF: C25H26N4O2
  • MW: 414.50000
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MCHr1 antagonist 1

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.

  • CAS Number: 391610-37-0
  • MF: C28H33F2N5O5
  • MW: 557.59
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SB-568849

SB-568849 is a melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pKi of 7.7.

  • CAS Number: 395679-53-5
  • MF: C28H31F3N2O3
  • MW: 500.55
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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[1].

  • CAS Number: 1191-41-9
  • MF: C20H34O2
  • MW: 306.483
  • Catalog: MCHR1 (GPR24)
  • Density: 0.9±0.1 g/cm3
  • Boiling Point: 374.4±0.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 100.7±20.4 °C

MCH (salmon)

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.

  • CAS Number: 87218-84-6
  • MF: C89H139N27O24S4
  • MW: 2099.48000
  • Catalog: Peptides
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ATC 0175 hydrochloride

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].

  • CAS Number: 510733-97-8
  • MF: C23H26ClF2N5O
  • MW: 461.93500
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SNAP-94847 hydrochloride

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].

  • CAS Number: 487051-12-7
  • MF: C29H33ClF2N2O2
  • MW: 515.03400
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GW 803430

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].

  • CAS Number: 515141-51-2
  • MF: C25H24ClN3O3S
  • MW: 481.99400
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MCHr1 antagonist 2

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.

  • CAS Number: 863115-70-2
  • MF: C23H21FN2O5
  • MW: 424.42
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

[Ala17]-MCH

[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].

  • CAS Number: 359784-84-2
  • MF: C97H155N29O26S4
  • MW: 2271.707
  • Catalog: MCHR1 (GPR24)
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TC-MCH 7c

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].

  • CAS Number: 864756-35-4
  • MF: C24H25FN2O3
  • MW: 408.46500
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NGD-4715

NGD-4715 is a selective and orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist .

  • CAS Number: 476322-70-0
  • MF: C19H24BrN3O3
  • MW: 422.31600
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ac-Arg-Cys-Met-5-aminopentanoyl-Arg-Val-Tyr-5-aminopentanoyl-Cys-NH2 trifluoroacetate salt (Disulfide bond)

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].

  • CAS Number: 353487-64-6
  • MF: C49H82N16O11S3
  • MW: 1167.471
  • Catalog: MCHR1 (GPR24)
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(Phe13,Tyr19)-MCH (human, mouse, rat)

(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].

  • CAS Number: 160201-86-5
  • MF: C109H160N30O26S4
  • MW: 2434.88000
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MCH(human, mouse, rat)

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].

  • CAS Number: 128315-56-0
  • MF: C105H160N30O26S4
  • MW: 2386.84000
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ac-hMCH(6–16)-NH2

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].

  • CAS Number: 1053601-50-5
  • MF: C58H99N21O13S3
  • MW: 1394.73
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AMG-076

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].

  • CAS Number: 1001438-96-5
  • MF: C32H39F3N2O5S
  • MW: 620.72300
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AZD1979

AZD1979 is a Melanin-concentrating hormone receptor 1 (MCHr1) antagonist with an IC50 of ~12 nM.

  • CAS Number: 1254035-84-1
  • MF: C25H26N4O5
  • MW: 462.498
  • Catalog: MCHR1 (GPR24)
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 636.6±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 338.8±34.3 °C

BMS 814580

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.

  • CAS Number: 1197420-11-3
  • MF: C24H19ClF2N2O4S
  • MW: 504.934
  • Catalog: MCHR1 (GPR24)
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 691.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 372.3±34.3 °C

MCHR1 antagonist 3

MCHR1 antagonist 3 is a potent the melanin-concentrating hormone receptor-1 (MCHR1) antagonist. MCHR1 antagonist 3 is used to regulate energy metabolism[1].

  • CAS Number: 1069622-60-1
  • MF: C29H36N4O2
  • MW: 472.62
  • Catalog: MCHR1 (GPR24)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A