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Catalog No.
Product Name
Application
Product Information
Citations
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PAR1 Allosteric Inhibitor
ML161 analog 1 is a selective allosteric inhibitor targeting Proteinase-Activated Receptor 1 (PAR1) with an IC50 of 1.68 μM. This compound modulates PAR1 activity, making it a valuable tool for studying its role in various biological processes and disease mechanisms. Its application in research may provide insights into therapeutic strategies involving PAR1. -
Collagen/TRAP-6 Inhibitor
TRAP-6-IN-1 is a dual inhibitor targeting collagen and TRAP-6, with IC50 values of 17.12 µM and 11.88 µM, respectively. This compound effectively inhibits agonist-induced platelet aggregation in a non-competitive manner, making it a valuable tool for research into platelet function and coagulation disorders. Its dual action may provide insights into therapeutic strategies for cardiovascular diseases associated with platelet hyperactivity. -
PAR-2 Inhibitor
PAR-2-IN-2 is a selective inhibitor of protease-activated receptor 2 (PAR-2), exhibiting an IC50 of 10.79 μM against the PAR-2 peptide SLIGKV, while demonstrating a significantly higher IC50 of over 200 μM for Trypsin. This compound is valuable for studying PAR-2 signaling pathways and exploring its role in inflammatory responses and pain modulation. PAR-2-IN-2 serves as a critical tool for researchers investigating therapeutic targets in conditions associated with PAR-2 activation. -
Neurotensin Receptor Inhibitor
VGD071 is a neurotensin receptor inhibitor that specifically targets sortilin. This compound exhibits potential for modulating neurotensin signaling pathways, which may be relevant in the context of breast cancer research. VGD071 is suitable for preclinical studies and investigations into the role of neurotensin receptors in tumorigenesis and cancer progression. -
Neurotensin Inhibitor
L-156903 is a potent neurotensin inhibitor that selectively disrupts the binding of neurotensin to brain tissue. This compound is valuable for studying the neurotensinergic system and its role in various neurological conditions. Its inhibitory action can contribute to research aimed at understanding the mechanisms underlying neuropsychiatric disorders and potential therapeutic interventions. -
Enkephalinase Inhibitor
PL37 is a potent orally active enkephalinase inhibitor that targets both Neutral Endopeptidase and Aminopeptidase N, providing dual inhibition. This compound exhibits significant anti-hyperalgesic activity through the activation of μ-opioid receptors, demonstrating an ED50 of 13.4 mg/kg for analgesic effects in murine models. PL37 is valuable for research into the mechanisms underlying diabetic neuropathic pain and related pain management strategies. -
μ-opioid Receptor Activator, hERG (Kv11.1) Potassium Channel Inhibitor
ERG-IN-6 is a potent μ-opioid receptor activator, exhibiting an EC50 of 0.12 nM, which makes it an effective tool for studies related to pain modulation. Additionally, ERG-IN-6 functions as a hERG (Kv11.1) potassium channel inhibitor with an IC50 of 0.681 μM. This compound is valuable for research applications investigating the interplay between opioid signaling and ion channel regulation. -
ORL-1 Inhibitor
SB-612111 is a potent antagonist of the opiate receptor-like orphan receptor (ORL-1), exhibiting high affinity for human ORL-1 with a Ki of 0.33 nM. It demonstrates selectivity towards μ-, κ-, and δ-opioid receptors, with Ki values of 57.6 nM, 160.5 nM, and 2109 nM, respectively. SB-612111 effectively antagonizes the pronociceptive effects of nociceptin in acute pain models, making it a valuable tool for research into pain modulation and opioid receptor pathways. -
AVP Release Inhibitor/Kappa Opioid Receptor Agonist
Niravoline is an arginine vasopressin (AVP) release inhibitor and a selective kappa opioid receptor agonist. This compound is notable for inducing a pure water diuresis effect while minimizing electrolyte loss. Additionally, Niravoline has demonstrated efficacy in reducing brain edema following transient forebrain ischemia in rodent models, making it a valuable tool for research in neuroprotection and fluid balance mechanisms. -
Gβγ-subunit Inhibitor
M119 (NSC 119910) is a selective Gβγ-subunit inhibitor that modulates μ-opioid receptor signaling. This compound has been shown to enhance μ-opioid-dependent antinociception by inhibiting μ-receptor-dependent phospholipase (PLC) activation. M119 is useful in pain research, particularly in studies investigating opioid analgesia, as well as in the assessment of acute tolerance and dependence in animal models. -
Opioid Receptor Inhibitor
Neuropeptide AF (human) is an endogenous peptide that acts as an opioid receptor inhibitor. This neuropeptide plays a critical role in modulating pain and stress responses, making it a valuable tool for studies focused on opioid signaling pathways. Research applications include investigations into pain management, addiction, and the physiological effects of endogenous opioid peptides. -
ORL-1 Inhibitor
rel-SB-612111 hydrochloride is a selective antagonist of the human opiate receptor-like orphan receptor (ORL-1), exhibiting a high binding affinity with a Ki value of 0.33 nM. This compound demonstrates notable selectivity against μ-, κ-, and δ-opioid receptors, with Ki values of 57.6 nM, 160.5 nM, and 2109 nM, respectively. rel-SB-612111 hydrochloride has been shown to effectively inhibit the pronociceptive effects of Nociceptin in acute pain models, making it a valuable tool for research into pain mechanisms and opioid receptor interactions. -
μ-Opioid Receptor Agoinst/AChE Inhibitor
Eseroline is a potent μ-opioid receptor agonist and a selective, competitive inhibitor of acetylcholinesterase (AChE), with Ki values of 0.1 μM for AChE and 200 μM for butyrylcholinesterase (BuChE). This compound also acts as a nicotinic acetylcholine receptor allosteric enhancing ligand, enhancing acetylcholine signal transduction without directly activating the receptor. Eseroline's neurotoxic effects include cell membrane damage and energy metabolism disruption, making it a valuable tool for investigating Alzheimer's disease pathology and cholinergic signaling. -
MOR Inhibitor
MOR agonist-1 is a selective μ-opioid receptor (MOR) agonist known for its pronounced analgesic activity. This compound is valuable for research focused on pain modulation and the exploration of pain-related disorders. Its mechanism of action makes it an essential tool for studies investigating opioid pharmacology and therapeutic interventions in pain management. -
OX1R Inhibitor
Tebideutorexant is a selective inhibitor of the orexin receptor 1 (OX1R), demonstrating significant oral bioavailability and the ability to cross the blood-brain barrier. With a human OX1R pKi of 8.17 and a rat OX1R pKi of 8.13, this compound specifically targets OX1R while exerting minimal effects on OX2R. Tebideutorexant is a valuable tool for investigating panic and anxiety disorders in preclinical research settings. -
Melanogenesis Inhibitor
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. -
MCHR1 Inhibitor
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. -
Melanogenesis Inhibitory Agent
Cadin-1(14)-ene-7a,11-diol is a sesquiterpene alcohol that functions as a melanogenesis inhibitory agent. It effectively suppresses melanin production in B16 melanoma cells stimulated by α-MSH, demonstrating potential application in skin-whitening treatments. This compound is valuable for research exploring mechanisms of pigmentation and therapies for hyperpigmentation disorders. -
Melanogenesis Inhibitor
(-)-Isodocarpin is a diterpenoid that acts as a potent melanogenesis inhibitor, exhibiting an IC50 of 0.19 μM in B16 4A5 cell lines. This compound effectively suppresses the expression of key melanogenic enzymes, including tyrosinase, tyrosine-related protein (TRP)-1, and TRP-2 mRNA. (-)-Isodocarpin is valuable for research applications focused on skin pigmentation, melanin synthesis, and related dermatological studies. -
α-MSH Inhibitor
Melanostatin, frog is a potent inhibitor of α-melanocyte-stimulating hormone (α-MSH) release, exhibiting an IC50 value of 60 nM. This peptide is primarily utilized in studies investigating melanogenesis and the regulation of pigment production. Its effects on α-MSH make it a valuable tool for research applications focusing on skin biology, obesity, and related metabolic pathways. -
Melanogenesis Inhibitor
IIIM-8 is a melanogenesis inhibitor that effectively suppresses pigment production in both in vitro and in vivo models. This compound shows no cytotoxicity in Human Adult Epidermal Melanocytes (HAEM), making it a suitable candidate for research in hyperpigmentation disorders. Its mechanism of action supports studies aimed at understanding melanin synthesis and skin pigmentation regulation. -
Melanocortin Receptor Inhibitor
Chlorophorin is an inhibitor of the Melanocortin Receptor, effectively reducing tyrosinase activity and melanogenesis. This compound demonstrates significant inhibition of α-melanocyte-stimulating hormone-induced melanin production in B16F10 melanoma cells, making it valuable for research on pigmentation disorders and melanoma. Its mechanism of action provides insights into the modulation of skin pigmentation and potential therapeutic strategies. -
Melanogenesis Inhibitor
(R)-Lirinidine is an aporphine-type alkaloid derived from Nelumbo nucifera, known for its role as a melanogenesis inhibitor. With an IC50 value of 19.3 μM, it effectively reduces melanin production, making it valuable for research in skin pigmentation disorders. Additionally, (R)-Lirinidine exhibits cytotoxic effects at concentrations of 100 μM, highlighting its potential in various biological studies. -
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. -
mGluR2 Inhibitor
MK-8768 is a potent and selective negative allosteric modulator of the metabotropic glutamate receptor 2 (mGluR2), exhibiting an IC50 value of 9.6 nM. This compound demonstrates excellent bioavailability and brain permeability, making it suitable for investigations into neurological disorders associated with glutamate signaling. It serves as a valuable tool for research applications aimed at understanding the modulation of mGluR2 in various physiological and pathological contexts. -
mGluR Inhibitor
PF470 is a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5). It has demonstrated significant efficacy in preclinical models of Parkinson's disease, making it a valuable tool for investigating the role of mGluR5 in neurological disorders. Despite its potential, further clinical development was halted due to concerns identified in toxicology assessments. -
mGluR Inhibitor
Ro4491533 is a selective negative allosteric modulator of the mGluR2 and mGluR3 receptors. It effectively inhibits glutamate-induced calcium mobilization and decreases [35S]GTPγS binding, demonstrating its capacity to modulate glutamatergic signaling. This compound exhibits favorable pharmacokinetic properties, including high oral bioavailability and the ability to penetrate the blood-brain barrier. Additionally, Ro4491533 has shown potential in reversing motor inhibition caused by LY379268 and displays antidepressant effects in various behavioral tests such as the forced swim test and tail suspension test. -
Npr1 Inhibitor
JS11 is a selective inhibitor of natriuretic polypeptide receptor 1 (Npr1), exhibiting an IC50 of 1.9 μM for human Npr1. This compound has demonstrated the ability to alleviate pruritus in mouse models, making it a valuable tool for investigating the role of Npr1 in pruritic conditions. Its pharmacological activity positions JS11 as a significant reagent for research in dermatology and other fields related to itch sensation and regulation. -
Tachykinin/Substance P Receptor Inhibitor
CP-96,345 is a potent, non-peptide inhibitor targeting tachykinin and substance P receptors. This compound effectively inhibits the hypotensive effects induced by substance P and neurokinin A, making it a valuable tool for studying neurogenic inflammation. Its oral bioactivity allows for convenient application in research settings focused on pain modulation and inflammatory responses. -
Neurokinin Receptor Inhibitor
NK3R-IN-1 is a potent inhibitor of the Neurokinin Receptor NK3R, characterized as an imidazolepiperazine derivative with oral bioavailability. This compound effectively lowers blood luteinizing hormone levels in ovariectomized models, demonstrating significant influence on neuroendocrine regulation. It serves as a valuable tool for research in reproductive biology and neurobiology, particularly in studies involving hormone modulation and neurological signaling pathways. -
Substance P Inhibitor
[D-Pro2,D-Phe7,D-Trp9] Substance P is a synthetic analogue of Substance P that functions as a potent inhibitor of the neuropeptide. It exhibits a significant ability to modulate neurogenic inflammation and pain response by blocking Substance P-mediated signaling pathways. This compound is useful in studying the role of Substance P in pain and gastrointestinal motility research applications, particularly in models involving guinea-pig ileum contraction. -
NK1 Inhibitor
SR140333B is a selective inhibitor of the neurokinin-1 (NK1) receptor, primarily involved in modulating pain and inflammatory responses. This compound demonstrates significant efficacy in reducing LPS-induced fever and attenuating LPS-induced alterations in brain tissue in rat models. SR140333B is valuable for research focusing on neuroinflammation, pain pathways, and the therapeutic potential of NK1 receptor modulation. -
Neurokinin Receptor Inhibitor
SCH 60057 is a potent neurokinin receptor inhibitor, selectively targeting NK1 and NK2 receptors with IC50 values of 6 μM and 12 μM, respectively. This compound is derived from Acremonium sp. and is useful in research applications related to pain modulation, inflammation, and neurogenic disorders. Its ability to inhibit neurokinin signaling pathways makes it a valuable tool for investigating the roles of these receptors in various biological processes. -
Substance P Release Inhibitor
Dilopetine citrate is a potent inhibitor of substance P release, demonstrating significant activity in attenuating the vocalizations of isolated guinea pig pups in a dose-dependent manner. Its mechanisms suggest potential applications in the field of psychiatry, particularly as an antidepressant agent. This compound may facilitate research on the modulation of neuropeptide systems involved in mood regulation and pain perception. -
NK Inhibitor
Dazodeunetant is a selective inhibitor of neurokinin receptors (NK), exhibiting an IC50 of 75.99 nM against NK3R in HEK293-NK3 cells. This nitrogen-containing fused ring derivative demonstrates potential in the study of menopausal hot flashes and related therapeutic strategies. Its ability to modulate neurokinin signaling positions it as a valuable tool in neurobiology and women's health research. -
sGC Inhibitor
LY83583 is a selective inhibitor of soluble guanylate cyclase (sGC), effectively modulating the cGMP signaling pathway. This compound demonstrates significant biological activity by inhibiting kinase activity associated with tumor cell proliferation, particularly through the induction of the Cdk inhibitor p21. LY83583 is applicable for research in various cancer types, including colorectal cancer, breast cancer, and melanoma, as well as in studies related to cardiovascular disease. -
Guanylate Cyclase Inhibitor
Guanylate cyclase-IN-1 is a potent inhibitor of guanylate cyclase, a crucial enzyme involved in the regulation of intracellular signaling pathways. This compound exhibits significant biological activity by modulating nitric oxide signaling, making it a valuable tool for the study of cardiovascular diseases. Its applications extend to investigating the physiological and pathological roles of guanylate cyclase in various biological processes. -
Diguanylate Cyclases Inhibitor
Ebselen oxide is a selenone analogue that serves as a potent inhibitor of diguanylate cyclases (DGCs). By covalently modifying DGCs, it disrupts c-di-GMP-receptor interactions and subsequently decreases DGC activity. Additionally, Ebselen oxide demonstrates antibacterial properties by inhibiting alginate production in Pseudomonas aeruginosa, with an IC50 of 14 μM. It also exhibits inhibitory activity against various histone deacetylases (HDAC1 to HDAC9), with IC50 values ranging from 0.2 to 4.7 μM, making it useful for research involving epigenetic regulation. -
Guanylate Cyclase Inhibitor
2-Chloro-ATP functions as a soluble guanylate cyclase inhibitor, impacting intracellular signaling pathways. This compound elevates intracellular calcium concentrations at low concentrations, utilizing a mechanism that does not rely on inositol phosphate production. It is valuable for studies investigating the role of guanylate cyclase in various physiological and pathological conditions. Researchers can utilize 2-Chloro-ATP to understand the modulation of calcium signaling in cellular processes. -
ICMT Inhibitor
ICMT-IN-1 is a selective inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT) with an IC50 of 0.0013 μM. This compound has been shown to effectively induce the accumulation of ICMT in the cytoplasm of HCT-116 cells. Additionally, ICMT-IN-1 exhibits significant antiproliferative activity against various cancer cell lines that express K-Ras and N-Ras, making it a valuable tool for research in cancer biology and therapeutic development. -
ICMT Inhibitor
ICMT-IN-30 is a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), with an IC50 value of 0.27 μM. This compound is essential for studying the role of ICMT in various biological processes, including protein modification and signaling pathways. Its inhibition can be utilized in research focused on cancer, neurodegeneration, and other diseases associated with abnormal protein prenylation. -
ICMT Inhibitor
ICMT-IN-28 is a potent inhibitor of Isoprenylcysteine Carboxyl Methyltransferase (ICMT), exhibiting an IC50 value of 0.008 μM. This compound effectively disrupts the ICMT-mediated methylation of isoprenylated proteins, playing a critical role in cellular signaling pathways. ICMT-IN-28 is utilized in studies investigating the regulation of protein function and has potential applications in cancer research and other areas of cell biology. -
ICMT Inhibitor
ICMT-IN-52 is a specific inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 value of 0.052 μM. This compound plays a crucial role in research on post-translational modifications and protein maturation related to oncogenesis and cellular signaling. Its ability to effectively inhibit ICMT makes it a valuable tool for studying the biological implications of ICMT activity in various disease models. -
ICMT Inhibitor
ICMT-IN-5 is a potent inhibitor of Isoprenylcysteine carboxyl methyltransferase (ICMT) with an IC50 of 0.3 μM. This compound modulates protein localization and activity through the inhibition of ICMT, making it valuable for studying signal transduction pathways and post-translational modifications. ICMT-IN-5 is suitable for research applications focused on cancer biology, neurobiology, and other fields where ICMT plays a critical role in regulating protein function. -
ICMT Inhibitor
ICMT-IN-34 is a potent inhibitor of Isoprenylcysteine carboxyl methyltransferase (ICMT) with an IC50 of 0.17 μM. This compound exhibits significant biological activity in the modulation of protein methylation, influencing various cellular processes. It is valuable for research applications aimed at elucidating the roles of ICMT in signal transduction and cancer biology.
