Catalog No.
Product Name
Application
Product Information
Citations
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Amino-terminal Fragment of AGRP
Agouti-Related Protein (54-82) (human) is an amino-terminal fragment of the agouti-related protein (AGRP), specifically spanning residues 54 to 82. This peptide plays a critical role in the regulation of appetite and energy homeostasis by acting as an antagonist of the melanocortin receptors. It is widely utilized in research examining metabolic disorders, obesity, and neuroendocrine signaling pathways. -
MC4R Agonist
MK-0489 is a selective agonist targeting the melanocortin-4 receptor (MC4R). Demonstrating a strong binding affinity with an IC50 of 13 nM and functional activity characterized by an EC50 of 4.6 nM in human MC4R, it also exhibits an EC50 of 22 nM for mouse MC4R and 1.7 μM for mouse MC3R. This compound is valuable for research applications focused on obesity and related metabolic disorders. -
ACTH Analogue
ACTH (3-24) is a peptide fragment of adrenocorticotropic hormone (ACTH) consisting of residues 3-24. This ACTH analogue plays a critical role in modulating adrenal steroidogenesis and has been utilized in research focused on various diseases, including cancer, immune disorders, and cardiovascular diseases. Its ability to influence hormone release makes it valuable for studying endocrine function and related pathologies across different species, including human, bovine, and rodent models. -
MC4R Agonist
Bivamelagon hydrochloride is a potent agonist of the melanocortin 4 receptor (MC4R), demonstrating EC50 values of 0.562 nM in luciferase assays and 36.5 nM in cAMP assays, along with a Ki of 65 nM. This compound exhibits oral bioavailability and the ability to cross the blood-brain barrier, making it a valuable tool in research focused on metabolic disorders, particularly obesity and diabetes. Bivamelagon hydrochloride facilitates the exploration of MC4R signaling pathways and their implications in metabolic regulation. -
hMC5R Antagonist
Ac-c[Cys-Glu-His-d-Phe-Arg-Trp-d-Cys]-Pro-Pro-Lys-Asp-NH2 is a selective antagonist of the human melanocortin 5 receptor (hMC5R), exhibiting an IC50 value of 10 nM. This compound is crucial for studies focusing on hMC5R-related signaling pathways and their implications in various physiological processes. Its specificity makes it a valuable tool for investigating the role of hMC5R in metabolic regulation and other biological functions. -
Melanogenesis Inhibitor
Amphistin is a melanogenesis inhibitor derived from actinomycetes. It effectively suppresses melanin production in B16 melanoma cells while demonstrating no significant impact on cellular growth. This compound is of interest for research applications focused on hyperpigmentation disorders and skin-related studies. -
Melanogenesis Inhibitor
Albocycline K3 acts as a melanogenesis inhibitor and is derived from microbial sources. This compound effectively reduces melanin production, making it suitable for research in skin biology and pigmentation disorders. Its unique mechanism of action provides valuable insights into the modulation of melanin synthesis and may aid in the development of therapies for conditions such as hyperpigmentation. -
Melanin Biosynthesis Inhibitor
Melanocin A is a potent melanin biosynthesis inhibitor that specifically targets tyrosinase, demonstrating an IC50 of 9.0 nM and a MIC of 0.9 μM. This compound effectively reduces melanin production and exhibits antioxidant properties, making it valuable for research into skin pigmentation disorders and oxidative stress-related conditions. Melanocin A can be utilized in studies examining the regulation of melanogenesis and potential therapeutic approaches for hyperpigmentation. -
ACTH Inhibitor
Delmadinone acetate is an orally active ACTH inhibitor that exerts its effects by suppressing adrenal function through the inhibition of adrenocorticotropic hormone release from the pituitary gland. This compound is primarily used in veterinary medicine for the control of estrus and ovulation in both female and male pets. Its ability to modulate endocrine functions makes it valuable for research focused on reproductive biology and hormonal regulation. -
Melanin Biosynthesis Inhibitor
Melanoxazal is an inhibitor of melanin biosynthesis. It effectively reduces melanin formation in silkworm larva hemolymph, with an IC50 of 30.1 μg/mL, and demonstrates a potent inhibitory effect on mushroom tyrosinase, exhibiting an IC50 of 4.2 μg/mL. This compound is primarily utilized in research exploring pigmentation processes and the role of melanin in various biological systems. -
MC4R Antagonist
MPCI is a selective antagonist of the melanocortin-4 receptor (MC4R), exhibiting pharmacological chaperone activity. With a Ki value of 0.218 μM determined in HEK293 cells expressing human MC4R, MPCI is valuable in researching the mechanisms underlying MC4R-deficient obesity. This compound can facilitate studies on metabolic regulation and potential therapeutic approaches for related disorders. -
Melanocortin Receptor Agonist
MC-4R Agonist 1 is a selective agonist of the human melanocortin-4 receptor (MC-4R), known for its role in regulating energy homeostasis and appetite. This compound has demonstrated significant biological activity in research focusing on obesity, diabetes, and sexual dysfunction, making it a valuable tool for studies exploring metabolic pathways and associated disorders. Its use in scientific investigations may provide insights into potential therapeutic approaches for these conditions. -
MT2 Receptor Antagonist
4-P-PDOT is a highly selective antagonist of the Melatonin MT2 receptor, exhibiting over 300-fold greater affinity for MT2 compared to the MT1 receptor. This compound effectively inhibits melatonin-induced antioxidant activities, as evidenced by its impact on the GSH/GSSG ratio, phospho-ERK levels, Nrf2 nuclear translocation, and Nrf2 DNA-binding activity. 4-P-PDOT is a valuable tool for research into melatonin signaling pathways and oxidative stress responses. -
MT1/MT2 Receptor Agonist
UCM 793 is a potent non-selective agonist of the MT1 and MT2 melatonin receptors, exhibiting pKis of 9.09 and 9.19, respectively. This compound is known to enhance the frequency of wakefulness episodes while reducing their duration, thereby influencing the quality of vigilance states. Importantly, UCM 793 facilitates a decrease in sleep onset without adversely affecting the maintenance of non-REM sleep, making it a valuable tool for research in sleep disorders and circadian rhythm studies. -
MT1 Antagonist
S26131 is a potent and selective antagonist of the MT1 melatonin receptor, exhibiting Ki values of 0.5 nM for MT1 and 112 nM for MT2. This compound's affinity and selectivity make it a valuable tool for studying melatonergic signaling pathways and their implications in various physiological and pathological processes. S26131 can be utilized in research exploring sleep regulation, circadian rhythms, and related neurobiological functions. -
MT1/MT2 Receptor Antagonist
S-22153 is a selective antagonist of the melatonin receptors MT1 and MT2, exhibiting high potency with EC50 values of 19 nM and 4.6 nM for hMT1 and hMT2, respectively. Its Ki values demonstrate strong binding affinity, measuring 8.6 nM for hMT1 in CHO cells and 16.3 nM in HEK cells, while exhibiting Ki values of 6.0 nM and 8.2 nM for hMT2 in the same cell lines. S-22153 is primarily utilized in research focusing on sleep regulation, circadian biology, and neuropharmacology. -
MT2 Receptor Agonist
8-M-PDOT is a selective agonist for the melatonin MT2 receptor, displaying a 5.2-fold preference for MT2 over MT1 receptors. It exhibits high binding affinity with human recombinant MT2 and MT1 receptors, demonstrating pKi values of 8.23 and 8.95, respectively. This compound exhibits anxiolytic-like properties, making it a valuable tool for research in sleep disorders and anxiety-related studies. -
MT1 Agonist
2-Iodomelatonin is a selective agonist of the melatonin receptor 1 (MT1), exhibiting a potent Ki value of 28 pM and a more than five-fold preference for MT1 over MT2. This compound is valuable for identifying, characterizing, and localizing melatonin binding sites in both brain and peripheral tissues. Its application in research facilitates the study of melatonin’s role in various physiological processes and may aid in the investigation of related disorders. -
Melatonin Agonist
UCM 608 is a high-affinity agonist of melatonin (MT) receptors, specifically targeting MT1 and MT2 with pKi values of 10.7 and 10.4, respectively. This compound exhibits significant biological activity in modulating melatonin signaling pathways, making it valuable for research applications related to sleep regulation, circadian rhythm studies, and potential therapeutic interventions for sleep disorders. -
Melatonin Receptor Agonist
N-Acetyltryptamine is a partial agonist for melatonin receptors, particularly in retinal tissues. It plays a crucial role in modulating circadian rhythms and has applications in studying melatonin signaling pathways. Additionally, N-Acetyltryptamine is utilized to assess serotonin N-acetyl transferase activity in biochemical research. -
Melatonin Receptor Antagonist
S-20928 is a selective antagonist of melatonin receptors, inhibiting melatonin’s binding to these receptors. This compound has been demonstrated to enhance the 2-Deoxy-D-glucose (2DG)-induced elevation of blood glucose and glucagon levels in rat brain studies. S-20928 is relevant for research on metabolic regulation and the physiological effects of melatonin modulation. -
MT2 Antagonist
N-Pentanoyl 2-benzyltryptamine is a selective antagonist of the MT2 melatonin receptor, exhibiting a pKi of 8.03 for human MT2. This compound demonstrates significant selectivity, with 89-fold and 229-fold preference for human MT2 over human MT1 and Xenopus mel1c receptor subtypes, respectively. N-Pentanoyl 2-benzyltryptamine effectively inhibits melatonin-induced enhancement of electrically-evoked responses, making it a valuable tool for research in circadian rhythms and melatonin signaling pathways. -
Melatonin Receptor Agonist
Melatonin Receptor Agonist 1 is a selective agonist for the melatonin receptors, specifically showing Ki values of 108 nM for MT2 and 1140 nM for MT1. This compound is useful for studying melatonin signaling pathways and their roles in various physiological processes, including sleep regulation and circadian rhythm modulation. Its potential applications in research extend to areas such as neurobiology, sleep disorders, and the effects of melatonin on metabolic processes. -
MT2 Inverse Agonist/MT1 Antagonist
UCM 549 is an inverse agonist of the melatonin MT2 receptor and an antagonist of the MT1 receptor. This compound modulates melatonin signaling pathways, making it a valuable tool for investigating sleep disorders and circadian rhythm regulation. Its application extends to studies focused on the role of melatonin receptors in neuroprotection and mood regulation. -
MT3 Receptor Agonist
5-MCA-NAT is an agonist of the melatonin MT3 receptor. It has been shown to induce contraction of the colonic band in a concentration-dependent manner and effectively reduce intraocular pressure (IOP) in glaucomatous primate models. This compound is valuable for research applications related to gastrointestinal motility and ocular health, particularly in studies addressing conditions such as glaucoma and colonic issues. -
MT2 Antagonist
DH97-7 is a potent antagonist of the melatonin receptor 2 (MT2), demonstrating a Ki value of 252 nM for MT2 and 1100 nM for MT1. It effectively blocks MT2 receptor activity, making it a valuable tool for research in circadian rhythm regulation and sleep disorders. This compound is suitable for studies aiming to elucidate the biological pathways influenced by melatonin signaling and its therapeutic implications. -
Melatonin Receptor Agonist
6-Chloromelatonin is a highly effective melatonin receptor agonist that exhibits enhanced metabolic stability compared to melatonin. It demonstrates strong binding affinity to the MT1 receptor, competing with both [3H]-melatonin and 2-[125I]-iodomelatonin (pKi = 8.9 and 9.1, respectively). Additionally, 6-Chloromelatonin shows significant competition for [3H]-melatonin binding at MT2 receptors with a pKi value of 9.77. This compound is valuable for research in sleep regulation, circadian rhythms, and neuropharmacology. -
Melatonin Receptor Agonist
GR 196429 is a melatonin receptor agonist primarily targeting the MT1 subtype. This compound has been shown to promote sleep and modify circadian rhythms, in addition to stimulating melatonin release in murine models. It serves as a valuable tool for investigating sleep disorders and the biological mechanisms underlying circadian regulation. -
Inactive Isomer of Melatonin Receptor
(R)-Ramelteon is an orally active compound that serves as an inactive isomer of melatonin receptors 1 and 2. It has been studied for its potential role in modulating sleep patterns and may provide insight into the mechanisms underlying sleep regulation. This compound is of particular interest in research applications related to sleep disorders and circadian rhythm studies. -
Melatonin Receptor Antagonist
GR 128107 is a competitive antagonist of melatonin receptors, exhibiting a high binding affinity with a pKi of 9.6. This compound is utilized in research to investigate the physiological roles of melatonin signaling pathways and its involvement in circadian rhythm regulation. GR 128107 can aid in the exploration of sleep disorders, neurodegenerative diseases, and the modulation of various neurochemical processes. -
Melatonin Receptor Agonist
Nedemelteon is a melatonin receptor agonist that selectively binds to MT1 and MT2 receptors, playing a crucial role in regulating circadian rhythms and sleep-wake cycles. Its primary biological activity includes promoting sleep onset and improving sleep quality, making it valuable for research on sleep disorders and related conditions. This compound is utilized in studies investigating the therapeutic potential of melatonin modulation in various neurological and psychological contexts. -
Melatonin Receptor
Pareptide monohydrochloride is a stable analogue of melanotropin-inhibiting factor (MIF) that primarily targets melatonin receptors. This compound exhibits significant biological activity in modulating melatonin signaling pathways, making it a valuable tool for research in circadian rhythms and sleep disorders. Its application spans various studies focused on neurobiology, pharmacology, and the mechanisms of sleep regulation. -
mGluR5 Negative Allosteric Modulator
VU0477573, a partial negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGluR5), demonstrates brain penetrance and engages in neuroprotective and anxiolytic activities. This compound is of significant interest in the research of neurological disorders, including Parkinson's disease, providing insights into potential therapeutic strategies targeting mGluR5. -
mGlu7 Modulator
VU6010608 is a negative allosteric modulator of the metabotropic glutamate receptor 7 (mGlu7), with an IC50 value of 0.76 μM, and effectively crosses the blood-brain barrier. This compound has been shown to inhibit long-term potentiation (LTP) of Schaffer-collateral CA1 synapses in mouse brain slices induced by high-frequency stimulation. VU6010608 is suitable for research applications investigating neurological disorders and the modulation of synaptic plasticity. -
mGluR1/5 Agonist
DHPG is a potent agonist for metabotropic glutamate receptors mGluR1 and mGluR5, with an EC50 of 60 nM for mGluR1. Its activation triggers the phospholipase C (PLC) signaling pathway, subsequently activating protein kinase C (PKC). DHPG is widely utilized in research to explore synaptic transmission, neuroplasticity, and the therapeutic potential of targeting mGluR signaling in neurological disorders. -
mGluRs Positive Allosteric Modulator
VU0422288 is a positive allosteric modulator of group III metabotropic glutamate receptors (mGluRs). It demonstrates inhibitory activity with EC50 values of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively, as established in calcium mobilization assays. This compound has potential applications in addressing deficits in contextual fear memory, social recognition, and apneas in models of Rett syndrome. -
mGluR1a Antagonist
LY367385 hydrochloride is a selective antagonist of the metabotropic glutamate receptor 1a (mGluR1a). It exhibits a potent inhibitory effect on quisqualate-induced phosphoinositide hydrolysis, with an IC50 value of 8.8 μM. This compound has demonstrated neuroprotective properties and exhibits anticonvulsant and antiepileptic effects, making it valuable for research in neurological disorders and related pharmacological studies. -
mGluR7 Antagonist
MMPIP hydrochloride is a selective allosteric antagonist of the metabotropic glutamate receptor 7 (mGluR7) with KB values ranging from 24 to 30 nM. It serves as a valuable pharmacological tool for investigating the role of mGluR7 in central nervous system functions. Research indicates that MMPIP hydrochloride can alleviate pain and restore normative affective and cognitive behaviors in models of neuropathic pain. -
mGluR Activator
Quisqualic acid is a potent mGluR (metabotropic glutamate receptor) activator derived from the natural source Quisqualis indica. As an excitatory amino acid agonist, it exhibits significant potency with an EC50 of 45 nM and a Ki of 10 nM for mGluR1R. This compound is valuable for research applications involving neurological studies, receptor signaling pathways, and the exploration of excitatory neurotransmission mechanisms. -
Group II/III mGluR Antagonist
CPPG ((RS)-CPPG) is a potent antagonist of group II and III metabotropic glutamate receptors (mGluRs). It demonstrates selective inhibition of group III mGluRs, with an IC50 of 2.2 nM, compared to an IC50 of 46.2 nM for group II mGluRs in rat cerebral cortex. Additionally, CPPG shows minimal activity at group I mGluRs. This compound is valuable for research into neuropharmacology and the modulation of glutamatergic signaling pathways. -
mGluR7 Agonist
AMN082 is a selective mGluR7 agonist that operates through allosteric activation of the receptor signaling pathway. It effectively inhibits cAMP accumulation and promotes GTPγS binding in transfected mammalian cells, with EC50 values ranging from 64 to 290 nM. AMN082 demonstrates notable selectivity for mGluR7 over other mGluR subtypes and ionotropic glutamate receptors, making it a valuable tool for research into neuropharmacology and potential antidepressant effects. -
mGluR7 Allosteric Agonist
CVN636 is a selective allosteric agonist of the metabotropic glutamate receptor 7 (mGluR7) with an EC50 value of 7 nM for human mGluR7. This compound exhibits significant central nervous system (CNS) permeability, making it a valuable tool for exploring mGluR7 modulation. Its potent activity supports research applications in the investigation of neurological disorders and the pharmacological profiling of mGluR7-related pathways. -
mGlu3 Negative Allosteric Modulator
VU6010572 is a potent and selective negative allosteric modulator of the metabotropic glutamate receptor 3 (mGlu3), demonstrating an IC50 of 245 nM. Its high blood-brain barrier penetration makes it suitable for central nervous system studies. This compound is valuable in investigating the role of mGlu3 in neuropsychiatric disorders and evaluating potential therapeutic strategies in related research contexts. -
mGluR Agonist
L-Cysteinesulfinic acid monohydrate is a potent agonist that selectively targets rat metabotropic glutamate receptors (mGluRs), displaying pEC50 values of 3.92 for mGluR1, 4.6 for mGluR5, 3.9 for mGluR2, 2.7 for mGluR4, 4.0 for mGluR6, and 3.94 for mGluR8. This compound is valuable for studies investigating mGluR-mediated signaling pathways and provides insights into neuropharmacological responses. It can be utilized in research applications focused on neurological disorders and synaptic transmission mechanisms. -
mGlu1 Modulator
VU0483605 is a selective positive allosteric modulator of the metabotropic glutamate receptor 1 (mGlu1). It demonstrates strong PAM activity with EC50 values of 390 nM in human and 356 nM in rat, indicating effective modulation across species. This compound is valuable for investigating the role of mGlu1 in neurological disorders and in studying synaptic plasticity and cognitive functions. -
mGluR5 SAM
BMS-984923 is a potent silent allosteric modulator (SAM) of the metabotropic glutamate receptor 5 (mGluR5), characterized by a high binding affinity (Ki = 0.6 nM). This compound effectively inhibits the interaction between PrPC and mGluR5, thereby preventing pathological signaling associated with amyloid-beta oligomers while preserving normal glutamate signaling. BMS-984923 is suitable for research applications related to neurodegenerative diseases and offers favorable pharmacokinetic properties, including enhanced oral bioavailability and the ability to cross the blood-brain barrier. -
mGlu2 Negative Allosteric Modulator
VU6001966 is a potent negative allosteric modulator of the metabotropic glutamate receptor 2 (mGlu2), exhibiting an IC50 of 78 nM, while demonstrating selectivity for mGlu2 over mGlu3 with an IC50 of >30 µM. This compound effectively crosses the blood-brain barrier, making it a valuable tool for neurological research. VU6001966 can also be utilized as a positron emission tomography (PET) tracer for studying mGlu2 dynamics, contributing to the understanding of glutamatergic signaling in various cognitive processes and neuropsychiatric disorders. -
mGlu5 NAM
HTL14242 is an advanced, orally active negative allosteric modulator (NAM) of the metabotropic glutamate receptor 5 (mGlu5). With a pKi of 9.3 and a pIC50 of 9.2, HTL14242 demonstrates significant binding affinity, making it a valuable tool for exploring the role of mGlu5 modulation in neurological disorders. This compound is particularly relevant for research investigating the therapeutic potential in Parkinson's disease. -
Group II mGluRs Agonist
DCG-IV is a potent agonist of group II metabotropic glutamate receptors (mGluRs), displaying EC50 values of 0.35 μM for mGlu2R and 0.09 μM for mGlu3R. Additionally, it acts as a competitive antagonist at group I and group III mGluRs, with respective IC50 values of 389 μM and 22.5-630 μM. DCG-IV has demonstrated anticonvulsive and neuroprotective properties, making it valuable for research in neurobiology and pharmacology. -
mGlu7 Antagonist
ADX71743 is a highly selective, noncompetitive antagonist of the metabotropic glutamate receptor 7 (mGlu7). This compound demonstrates significant brain penetration, facilitating its efficacy in neurological research. ADX71743 exhibits anxiolytic properties and is utilized in studies exploring treatments for anxiety disorders and related neuropsychiatric conditions.
