Catalog No.
Product Name
Application
Product Information
Citations
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Adenosine Analog
3',5'-TIPS-N-Ac-Adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant smooth muscle vasodilatory activity and has potential applications in inhibiting cancer progression. It is valuable for research related to vascular biology and oncology, facilitating the study of adenosine receptor signaling pathways and their therapeutic implications. -
Adenosine Analog
8-(Methylamino)adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant vasodilatory effects on smooth muscle and has been demonstrated to possess anti-cancer properties by inhibiting tumor progression. It is utilized in various research applications related to vascular biology and oncology. -
Adenosine Analog
N6-(3-Trifluoromethylbenzyl)-2’-C-methyl adenosine is an adenosine analog that primarily acts on adenosine receptors. This compound demonstrates smooth muscle vasodilatory properties and has potential applications in inhibiting cancer progression. Its structural modifications enhance its affinity and selectivity, making it a valuable reagent for research in vascular biology and oncology. -
Adenosine Analog
N6,N6-Dimethyl-xylo-adenosine is an adenosine analog with a primary mechanism of action involving modulation of adenosine receptors. This compound has demonstrated significant smooth muscle vasodilator activity and holds potential in inhibiting cancer progression. It is widely utilized in research applications focusing on vascular biology and oncology. -
Endogenous Metabolite
AZD-3199 is an ultra-long-acting beta2 adrenergic agonist primarily targeting the beta2 adrenergic receptor. It exhibits significant bronchodilator activity, making it a candidate for therapeutic use in asthma and chronic obstructive pulmonary disease (COPD) research. Its prolonged action facilitates investigations into novel treatment strategies for managing these respiratory conditions. -
Drug Derivative
Bmapn is a drug derivative with impactful interactions on dopamine signaling pathways. It exhibits rewarding and reinforcing properties by decreasing dopamine transporter levels and enhancing dopamine receptor D2 gene expression specifically in the striatum. This compound is valuable for research applications studying addiction, neuropharmacology, and the modulation of dopaminergic systems. -
Stable Isotope
Boc-Leu-OH·H2O-13C is a stable isotope-labeled derivative of N-Boc-L-leucine, featuring a carbon-13 (13C) label. This amino acid derivative, protected with a Boc group, serves as an essential building block for the synthesis of peptides, such as L-prolyl-L-leucyl-glycinamide, which exhibit modulatory activity on dopamine receptors. It is valuable for applications in peptide research, metabolic studies, and tracer experiments utilizing stable isotopes. -
Histamine N-methyltransferase
Histamine N-methyltransferase, rat is a biocatalyst that functions primarily by catalyzing the N-methylation of histamine. This enzyme plays a critical role in the metabolism of histamine, contributing to the regulation of physiological processes such as inflammatory responses and neurochemical signaling. Research applications include enzyme engineering aimed at optimizing reaction kinetics, enhancing substrate specificity, and improving enzyme stability under varying pH conditions, potentially facilitating dynamic control of enzymatic activity for various experimental needs. -
Activation Peptide
Enterostatin (rat) is an activation peptide of procolipase that plays a significant role in modulating fat intake. This peptide selectively reduces body fat consumption and lowers serum cholesterol levels through a cholecystokinin 1 (CCK1) receptor-dependent mechanism. It serves as a valuable tool for research on energy balance, appetite regulation, and metabolic disorders. -
N-acylserinol Compound
Myristoyl ethanolamide, an N-acylserinol compound, functions as a bioactive lipid signaling molecule. It is involved in modulating various biological processes, including inflammation and pain perception. Myristoyl ethanolamide serves as a valuable tool in research applications focused on lipid metabolism, neuromodulation, and the study of cannabinoid receptor interactions. This compound can enhance the understanding of endocannabinoid signaling pathways and their implications in physiological and pathological conditions. -
Blood Platelet Aggregation Inhibitor
Ent-8-Iso-15(S)-prostaglandin F2α is a potent inhibitor of blood platelet aggregation. This compound exhibits superior activity compared to its isomer, 8-Isoprostaglandin F2α, in whole blood assays, making it a valuable tool for studying platelet function and related cardiovascular research. Its mechanism of action can aid in the exploration of therapeutic strategies for conditions associated with abnormal platelet aggregation. -
Endogenous Metabolite
9(R)-HODE is a monohydroxy fatty acid and an endogenous metabolite of linoleic acid, generated through the enzymatic actions of cyclooxygenase (COX) and lipoxygenase (LO). This compound is known to promote chemotaxis and elevate the expression of chemokine receptors CCR9 and CXCR4 in immune cells. Additionally, 9(R)-HODE effectively inhibits interleukin-6 (IL-6) release in primary human monocytes and suppresses CD3α- and CD28-induced proliferation in isolated human peripheral blood lymphocytes at a concentration of 25 μg/mL, making it a valuable tool for studying immune responses and inflammatory processes. -
2-arachidonoylglycerol derivative
1-Monoarachidin is a 2-arachidonoylglycerol derivative that primarily acts as a modulator of cannabinoid receptors. This fatty acid plays a crucial role in the endocannabinoid system, contributing to various biological processes such as inflammation and neuroprotection. It is utilized in research to investigate the physiological effects of endocannabinoids and their potential therapeutic applications in neurological and inflammatory disorders. -
O-Alkyl-N-acyloxy Homologues
Oxy-Arachidonoyl ethanolamide is an O-alkyl-N-acyl oxime derivative that acts on O-Alkyl-N-acyl homologues. This compound exhibits significant biological activity, particularly in the modulation of endocannabinoid systems. It is employed in research applications focusing on cannabinoid receptor signaling, lipid metabolism, and neuroprotective studies, illuminating potential therapeutic pathways for various neurological diseases. -
Endogenous Metabolite
N-Methylarachidonamide is an analog of the endogenous cannabinoid anandamide, primarily targeting the central cannabinoid receptor (CB1). This compound exhibits a binding affinity with a Ki value of 60 nM for CB1, influencing various physiological processes. Additionally, it effectively inhibits rat glial gap junction cell-cell communication by 100% at a concentration of 50 μM. As such, N-Methylarachidonamide is a valuable tool for research exploring cannabinoid receptor signaling and its implications in neurobiology and related fields. -
FAAH Inhibitor
3-Decyl-5,5'-diphenyl-2-thioxo-4-imidazolidinone is a potent inhibitor of fatty acid amide hydrolase (FAAH) with a pI50 of 5.89. This compound exhibits significant activity against endocannabinoids and lipid mediators, making it relevant for studies in pain management, inflammation, and cannabinoid signaling pathways. Its limited affinity for cannabinoid receptors CB(1) and CB(2) allows for targeted research into FAAH-related physiological processes without direct receptor modulation. -
NR4A1 Inhibitor
Glycerol kinase, microorganism functions as an NR4A1 inhibitor by directly binding to and inhibiting the transcription factor NR4A1, which plays a critical role in hepatic gluconeogenesis. This inhibition leads to reduced blood glucose levels and positively influences UCP1 expression through the β-adrenergic receptor-cAMP-CREB signaling pathway, promoting the browning of white adipose tissue and enhancing thermogenesis. Additionally, it modulates intracellular fatty acid composition and energy metabolism. Research using glycerol kinase in diabetic mouse models has demonstrated its ability to counteract NR4A1-induced hyperglycemia, indicating its potential applications in diabetes and obesity studies. -
Bile Acid Sequestrant
Colesevelam hydrochloride is a bile acid sequestrant that primarily acts by binding bile acids in the gastrointestinal tract, leading to the formation of nonabsorbable complexes. This action interrupts enterohepatic recirculation and enhances fecal bile acid elimination. In addition to lowering lipids, colesevelam modulates FXR, TGR5, and CYP7A1 activities, which in turn activates cAMP signaling and promotes GLP-1 release. Its applications in research include investigations into type 2 diabetes mellitus, hypercholesterolemia, and alcohol-related liver disease, while also influencing hepatic lipid and glucose metabolism. -
Platelet Aggregation Inhibitor
Myrianthic acid is a pentacyclic triterpenoid that functions as a platelet aggregation inhibitor. Isolated from the root wood of Myrianthus arboreus and the leaves of Campsis grandiflora, it effectively inhibits adrenaline-induced platelet aggregation, demonstrating an IC50 of 46.2 μM. This compound is valuable for research applications focused on thrombosis and related cardiovascular disorders. -
NR2B Antagonist
NMDA-IN-1 dihydrochloride is a selective antagonist of the NMDA NR2B receptor, exhibiting a Ki of 0.85 nM and an IC50 of 9.7 nM for NR2B-mediated Ca2+ influx. This compound effectively inhibits Glu/Gly-stimulated Ca2+ flux in Ltk- cells expressing hNR1a/NR2B, demonstrating specificity as it does not interact with NR2A, NR2C, NR2D, hERG channels, or α1-adrenergic receptors. NMDA-IN-1 dihydrochloride displays significant efficacy in mechanical hyperalgesia models in rats and is relevant for investigations into stroke, Parkinson's disease, and neuropathic pain. -
σ Receptor Agonist
threo-Ifenprodil hemitartrate is a sigma (σ) receptor agonist, exhibiting Kis of 59.1 nM and 2 nM for σ1 and σ2 receptors, respectively. This compound also acts as a NR2B subunit-selective NMDA receptor antagonist, with an IC50 of 0.22 μM, and demonstrates inhibition of the hERG potassium channel with an IC50 of 88 nM, indicating potential antiarrhythmic activity. threo-Ifenprodil hemitartrate serves as a valuable tool in neuropharmacology and cardiovascular research. -
IBAT Inhibitor
Elobixibat hydrate is an orally active inhibitor of the intestinal bile acid transporter (IBAT), demonstrating potent activity with IC50 values of 0.53 nM for human IBAT, 0.13 nM for mouse IBAT, and 5.8 nM for canine IBAT. This compound has been shown to effectively lower LDL cholesterol levels, enhance serum GLP-1 concentrations, and promote colonic motility. Elobixibat hydrate is valuable for research applications related to chronic idiopathic constipation (CIC), dyslipidemia, non-alcoholic fatty liver disease, and the study of liver tumors, particularly in elderly populations. -
P/Q Type Ca2+ Channel Blocker
ω-Agatoxin IVA is a highly selective blocker of P/Q type calcium channels (Cav2.1), with IC50 values of 2 nM and 90 nM. This compound effectively inhibits glutamate exocytosis and calcium influx triggered by elevated potassium levels. Additionally, ω-Agatoxin IVA suppresses capsaicin-induced CGRP release and associated vasodilation. It is valuable for investigations into neurological and cardiovascular diseases, contributing to the understanding of calcium channel modulation in these contexts. -
Racemate of NNC 55-0396
(Rac)-NNC 55-0396 is a racemic mixture that targets the dopamine D2 receptor. This compound is of significant interest in neurological research due to its potential role in modulating dopaminergic signaling pathways. It is commonly utilized in studies investigating the pharmacological effects of dopamine receptor antagonists in various neurological disorders. -
Cholecystokinin
Cholecystokinin-J is a cholecystokinin peptide that primarily targets the cholecystokinin receptor. It is known to stimulate Ca2+ release, playing a significant role in various physiological processes such as digestion and satiety. This reagent is valuable for research applications in gastrointestinal physiology and neurobiology, facilitating studies on CCK-related pathways and functions. -
TRPA1 Channel Antagonist
ADM 12 is a selective antagonist of the transient receptor potential ankyrin 1 (TRPA1) channel. It effectively inhibits nitroglycerin-induced trigeminal hyperalgesia in animal models, leading to decreased expression of pain-related genes such as c-Fos and TRPA1, as well as neuropeptides including CGRP and substance P. This compound holds potential for research applications in the fields of migraine and neuropathic pain. -
TRP Channel Inhibitor
Cannabidiorcol (CBDO) is an inhibitor of transient receptor potential (TRP) channels. This compound, structurally related to cannabidiol with a shortened pentyl side chain, exhibits anti-inflammatory properties while displaying low affinity for cannabinoid receptors. Research applications include investigations into its potential role in modulating inflammation and exploring its effects on tumorigenesis at elevated concentrations. -
ACU Inhibitor/VR1 Agonist
OMDM-5 is a selective anandamide cellular uptake (ACU) inhibitor, exhibiting a Ki of 4.8 μM. In addition, OMDM-5 demonstrates potent activity as a vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM. This compound also shows weak activity as a cannabinoid receptor type 1 (CB1) ligand, with a Ki of 4.9 μM. Its properties make OMDM-5 useful for studies involving pain modulation and endocannabinoid signaling pathways. -
Stable Isotope
O-Desmethyl carvedilol-d5 is a deuterium-labeled derivative of O-Desmethylcarvedilol, a potent active metabolite of the non-selective β-adrenergic receptor antagonist Carvedilol. This compound exhibits inhibitory effects on store-overload-induced calcium release in HEK293 cells expressing the RyR2 R4496C mutation, with an IC50 of 7.62 μM. Additionally, O-Desmethyl carvedilol-d5 contributes to cardiovascular research by attenuating heart rate increases and stabilizing diastolic blood pressure in response to Isoproterenol in conscious rabbit models, demonstrating ED50 values of 32 and 5 μg/kg, respectively. -
Lipid
DMG-PEG is a lipid compound that enhances the hydrophilicity and electrical neutrality of lPEI/DNA nanoparticles, facilitating improved transport and diffusivity in the gastrointestinal mucus layer. This pegylated lipid is pivotal in formulating liposomes for siRNA delivery, significantly increasing transfection efficiency. In vivo studies demonstrate that nucleic acid nanoparticles coated with DMG-PEG effectively maintain elevated levels of glucagon-like peptide-1 (GLP-1) expression in liver, lung, and intestinal tissues of type II diabetic mouse models, while also regulating blood glucose levels. Additionally, DMG-PEG serves as an effective component in the preparation of lipid nanoparticles for mRNA therapeutics. -
MAGL Inhibitor
OMDM169 is a selective inhibitor of monoacylglycerol lipase (MAGL), effectively increasing the levels of 2-arachidonoylglycerol (2-AG) in biological systems. This compound demonstrates significant analgesic properties through the indirect activation of cannabinoid receptors. OMDM169 exhibits an effective concentration of 0.13 μM, making it a valuable tool for research focused on pain modulation and cannabinoid receptor signaling pathways. -
HIF Inhibitor
Arylsulfonamide 64B is a potent inhibitor of hypoxia-inducible factor (HIF). This compound effectively suppresses hypoxia/HIF-mediated expression of key oncogenes such as c-Met and CXCR4, thereby demonstrating significant anti-tumor activity. Arylsulfonamide 64B is particularly relevant for research focused on uveal melanoma, as it has been shown to reduce primary tumor growth and metastasis in mouse models. -
P2X1 Receptor Antagonist
NF449 octasodium is a potent antagonist of the P2X1 receptor, exhibiting IC50 values of 0.28 nM, 0.69 nM, and 120 nM for recombinant P2X1, recombinant P2X1 with 5, and P2X2+3 receptors, respectively. It selectively targets the Gsα subunit of G proteins, effectively inhibiting GTP[γS] binding to Gsα-s and reducing adenylyl cyclase activity. NF449 octasodium is useful in research focused on the regulation of P2X1 receptor-mediated signaling pathways and β-adrenergic receptor interactions. -
Somatostatin
Tyr-Somatostatin-28 is a potent somatostatin analog featuring a tyrosine residue at the N-terminus. This modification enhances its stability and bioactivity, making it an important tool for studying somatostatin receptor interactions and signaling pathways. Tyr-Somatostatin-28 has applications in neurobiology and endocrinology research, particularly in the investigation of hormone regulation and therapeutic targets for diseases such as acromegaly and neuroendocrine tumors. -
Potassium Channel Blocker
Besipirdine hydrochloride is a potassium channel blocker that exerts both cholinergic and adrenergic effects. Its cholinergic activity is characterized by stimulation of phosphatidylinositol turnover and a reduction in potassium currents, while its adrenergic activity promotes norepinephrine release through the inhibition of presynaptic α2-adrenergic receptors and the blocking of norepinephrine reuptake. This compound is applicable in research related to Alzheimer's disease, providing insights into potential therapeutic pathways. -
RFamide Neuropeptide
Neuropeptide AF (cattle) is an amidated octadecapeptide that targets RFamide neuropeptide receptors. It serves as a ligand for Mas-related gene receptor A4 (MrgprA4) with an EC50 of approximately 60 nM and MrgprC11 with an EC50 around 300 nM. Additionally, it activates the G protein-coupled receptors NPFF1 and NPFF2, exhibiting EC50 values ranging from 25-325 nM and 1-5 nM, respectively. Neuropeptide AF (cattle) demonstrates anti-opiate properties and plays a significant role in pain modulation research applications. -
MCHR1 Antagonist
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. -
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. -
MCH Receptor 1 Antagonist
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. -
MCH1 receptor Antagonist
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. -
MCHR-1 Antagonist
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. -
MCH R1 Antagonist
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. -
MCH1R Antagonist
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. -
SLC-1/S643b Agonist
(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. -
MCH Receptor Agonist
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. -
Selective MCH1R Antagonist
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. -
MCHR1 Antagonist
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. -
MCHR1 Ligand
[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. -
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. -
MCHR1 Antagonist
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.
