MCHR1 (GPR24)

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 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.

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

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

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.

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

SNAP 94847 hydrochloride is a selective antagonist targeting the melanin-concentrating hormone receptor 1 (MCHR1), exhibiting high affinity with a Ki value of 2.2 nM and Kd value of 530 pM. This compound demonstrates significant selectivity, showing over 80-fold and over 500-fold preference for MCHR1 over MCHα1A and MCHD2 receptors, respectively. SNAP 94847 hydrochloride binds effectively to MCHR1 in both mouse and rat models, displaying minimal cross-reactivity with other GPCRs, ion channels, enzymes, and transporters. Its properties make it a valuable tool for studying MCHR1-related biological processes and potential therapeutic applications.

Ethyl linolenate is a fatty acid ethyl ester that functions as a melanogenesis inhibitor. It effectively reduces melanin production in cells, exhibiting an IC50 of 70 μM. This compound is valuable in research applications focused on skin pigmentation and related disorders, as well as in the exploration of potential therapeutic agents for hyperpigmentation conditions.

BI 186908 is a selective and orally active antagonist of the melanin-concentrating hormone (MCH) receptor 1, demonstrating an IC50 of 22 nM and a Ki of 14 nM. This compound exhibits high affinity for recombinant MCH-R1 across several species, including human, cynomolgus monkey, dog, and rat, with IC50 values ranging from 18 nM to 23 nM. BI 186908 has been shown to significantly reduce body weight in diet-induced obese rat models, making it a valuable tool for research in obesity and related metabolic disorders.

RGH-706 is a selective MCH1 receptor antagonist with an IC50 of 6.2 nM against human MCHR1, demonstrating oral bioavailability and the ability to cross the blood-brain barrier. This compound is primarily utilized in research focused on obesity and Prader-Willi syndrome, as it effectively improves obesity-related outcomes without antagonizing hMCH2 receptors. RGH-706 serves as a valuable tool for studying mechanisms of appetite regulation and metabolic disorders.

BMS-830216 is a potent antagonist of the melanin-concentrating hormone receptor 1 (MCHR-1). As a phosphate ester prodrug, it exhibits effective conversion to its active form in biological systems. This compound is primarily utilized in obesity-related research, providing insights into the role of MCHR-1 in energy homeostasis and potential therapeutic strategies for weight management.

GW-803430 is a potent and selective antagonist of the melanin-concentrating hormone receptor 1 (MCH R1), exhibiting a pIC50 of 9.3. This compound demonstrates significant biological activity by inhibiting MCH R1, which plays a critical role in regulating energy balance and appetite. GW-803430 is primarily utilized in research applications focusing on obesity and metabolic disorders, providing insight into the therapeutic potential for weight management strategies.

ATC0175 is a potent and selective antagonist of the melanin-concentrating hormone 1 receptor (MCH1R) with an IC50 of 13.5 nM, exhibiting minimal effect on MCH2R (IC50 > 10,000 nM). This compound demonstrates significant antidepressant and anxiolytic activity in various animal models. ATC0175 serves as a valuable tool for investigating the mechanisms underlying depression and anxiety disorders in preclinical research.

(Phe13,Tyr19)-MCH (human, mouse, rat) is a selective agonist for the SLC-1 and S643b receptors. This compound exhibits robust biological activity that can be utilized to investigate the signaling pathways regulated by these receptors. It is suitable for research applications in neurobiology and pharmacology, providing valuable insights into receptor function and potential therapeutic targets.

Ac-hMCH(6-16)-NH2 is a non-selective agonist targeting the human melanin-concentrating hormone (MCH) receptors, specifically MCH-1R and MCH-2R, with IC50 values of 0.16 nM and 2.7 nM, respectively. This compound effectively activates both receptor subtypes in the brain, making it a valuable tool for studying the physiological roles of MCH signaling. Research applications include investigations into metabolic regulation, feeding behavior, and neuroendocrine function.

TC-MCH 7c is a selective antagonist of the melanin-concentrating hormone receptor 1 (MCH1R), featuring a phenylpyridone structure. This compound demonstrates high potency with an IC50 of 5.6 nM for human MCH1R, alongside Kis of 3.4 nM and 3.0 nM for human and mouse MCH1R, respectively. TC-MCH 7c is designed for oral administration and effectively penetrates the brain, making it a valuable tool for research in neurological disorders and metabolic regulation.

GW856464 is a selective antagonist of the melanin-concentrating hormone receptor 1 (MCHR1). This compound exhibits potential biological activity in the modulation of appetite and energy homeostasis, making it useful for the investigation of mechanisms underlying obesity and related metabolic disorders. Additionally, GW856464 may aid in research related to cardiovascular diseases by elucidating the role of MCHR1 in cardiovascular function.

[Ala17]-MCH is a selective ligand for the melanin-concentrating hormone receptor 1 (MCHR1), exhibiting a Ki value of 0.16 nM, indicating strong affinity compared to MCHR2, which has a Ki of 34 nM. The Eu3+ chelate-labeled form demonstrates high binding affinity for MCHR1 with a Kd of 0.37 nM, while showing negligible interaction with MCHR2. This compound is valuable for research applications involving MCHR1-mediated pathways, particularly in the study of neuropeptide signaling and metabolic regulation.

BMS-814580 is a selective melanocortin receptor 1 (MCHR1) inhibitor with a Ki of 16.9 nM against human MCHR1. This compound demonstrates significant antiobesity effects, making it a valuable tool for research into metabolic disorders and weight management. BMS-814580 can be utilized in studies exploring the role of MCHR1 in energy homeostasis and therapeutic approaches to obesity.

MCHR1 antagonist 3 is a potent antagonist of the melanin-concentrating hormone receptor-1 (MCHR1). By inhibiting MCHR1 activity, this compound plays a pivotal role in the regulation of energy metabolism. It is valuable in research applications exploring metabolic disorders and the mechanisms underlying energy homeostasis.

hMCH-1R antagonist 1 is a selective antagonist of the human melanin-concentrating hormone receptor 1 (hMCHR1) with a binding affinity characterized by a KB value of 3.6 nM. This compound demonstrates effective inhibition of hMCHR1 and hMCHR2, with IC50 values of 65 nM and 49 nM, respectively. hMCH-1R antagonist 1 is suitable for investigations into metabolic pathways and the role of melanin-concentrating hormone in various physiological processes.

ATC0175 free base is a potent and selective antagonist of the melanin-concentrating hormone receptor 1 (MCH-R1), exhibiting an IC50 value of 3.4 nM. This compound demonstrates strong selectivity over Y5 and α2A receptors, making it an important tool for investigations in obesity research. Its mechanism of action provides valuable insights into metabolic regulation and potential therapeutic strategies for related conditions.

MCH (human, mouse, rat) is a cyclic neuropeptide that functions as an endogenous ligand for the melanin-concentrating hormone receptor (MCH-R). It exhibits high binding affinity with IC50 values of 0.3 nM and 1.5 nM for human MCH-1R and MCH-2R, respectively, and operational EC50 values of 3.9 nM and 88.7 nM. MCH plays a crucial role in regulating appetite as an orexigenic signal and is instrumental in maintaining energy homeostasis and sleep-wake cycles. This reagent is essential for research into obesity, sleep-related disorders, and related metabolic conditions.

MCHR1 Antagonist 4 is a potent antagonist targeting the Melanin-Concentrating Hormone Receptor 1 (MCHR1), demonstrating Ki values of 0.74 nM for human MCHR1 and 0.76 nM for rat MCHR1. This compound effectively penetrates the blood-brain barrier, making it a valuable tool in research related to obesity and metabolic disorders. Its role as an anti-obesity agent positions it as a significant candidate for studies focused on weight management and appetite regulation.

AMG-076 free base is a selective antagonist of the Melanin-Concentrating Hormone Receptor 1 (MCHR1). It has been shown to significantly reduce body weight gain in non-obese mice subjected to a high-fat diet, as well as in diet-induced obese (DIO) mice. This compound is valuable for research into obesity and metabolic disorders, providing insights into the therapeutic potential of targeting MCHR1 in weight management.

AMG-076 is a selective antagonist of the melanin-concentrating hormone receptor-1 (MCHR1). This compound has demonstrated significant reductions in body weight gain in both nonobese mice on a high-fat diet and in diet-induced obese (DIO) mice. AMG-076 serves as a valuable tool for studying obesity and metabolic disorders in preclinical research.

T-226296 is a selective antagonist of the melanin-concentrating hormone receptor, exhibiting IC50 values of 5.5 nM and 8.6 nM for human and rat SLC-1, respectively. This compound demonstrates potential in modulating weight and metabolic processes, making it useful in research on obesity and insulin resistance. Its oral bioavailability facilitates in vivo studies, providing insights into the role of melanin-concentrating hormone signaling in metabolic disorders.