Catalog No.
Product Name
Application
Product Information
Citations
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GLP-1 Receptor Positive Allosteric Modulator
GLP-1R agonist 39 is a potent positive allosteric modulator of the GLP-1 receptor. This compound enhances the activity of the GLP-1 receptor, making it valuable for studies related to obesity and type 2 diabetes. Its application in research enables the exploration of therapeutic strategies aimed at metabolic disorders. -
GLP-1R Agonist
GLP-1R agonist 38 is a selective agonist of the glucagon-like peptide-1 receptor (GLP-1R). This compound exhibits significant biological activity in enhancing insulin secretion, suppressing glucagon release, and promoting weight reduction, making it a valuable tool for studying metabolic disorders. It is applicable in research related to type II diabetes mellitus (T2DM), obesity, and non-alcoholic fatty liver disease (NASH). -
GLP-1 Receptor Agonist
GLP-1 Receptor Agonist 18 is a potent GLP-1 receptor agonist with an EC50 of 0.22 nM. This compound demonstrates significant biological activity by lowering blood glucose levels and promoting weight loss, making it valuable for diabetes research. Its efficacy in modulating GLP-1 receptor signaling positions it as a useful tool for investigating therapeutic strategies in metabolic disorders. -
GLP-1R Agonist
GLP-1R agonist 26 is a potent agonist of the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 of less than 10 nM. This compound plays a crucial role in enhancing insulin secretion, promoting weight loss, and exhibiting cardioprotective effects. It is primarily utilized in research focused on metabolic disorders, diabetes, and obesity treatment. -
GLP-1R Agonist
GLP-1R agonist 29 is a potent agonist of the GLP-1 receptor, effectively stimulating cAMP production with an EC50 value of 0.018 nM. This compound demonstrates favorable pharmacokinetic properties, evidenced by a robust body exposure reflected in an AUC0-∞,sc of 77688 ng·h/mL. It serves as a valuable tool for research applications related to metabolic disorders and diabetes, allowing for exploration of GLP-1R signaling pathways. -
GLP-1R Agonist
GLP-1R Agonist 25 is a selective agonist for the glucagon-like peptide-1 receptor (GLP-1R), exhibiting an EC50 value of 0.167 nM. This compound plays a crucial role in stimulating insulin secretion and regulating glucose metabolism, making it a valuable tool for research focused on type II diabetes and related metabolic disorders. Its potent biological activity supports the exploration of therapeutic strategies aimed at improving glycemic control. -
GPR120 Agonist
AZ13581837 is a potent GPR120 agonist, demonstrating human and mouse EC50 values of 5.2 nM and 4.3 nM, respectively. This compound activates Gαq, Gαs, and β-arrestin signaling pathways, effectively reducing cAMP levels, stimulating GLP-1 secretion, promoting glucose lowering, and enhancing insulin secretion. AZ13581837 is valuable for research related to type 2 diabetes, providing insights into potential therapeutic strategies targeting metabolic disorders. -
GPR119 Agonist
AS1269574 is a potent agonist of GPR119, exhibiting an EC50 of 2.5 μM in HEK293 cells expressing the human receptor. This compound activates TRPA1 cation channels, thereby facilitating the secretion of glucagon-like peptide-1 (GLP-1). Notably, AS1269574 induces glucose-dependent insulin secretion from pancreatic β-cells exclusively under high-glucose conditions, making it a valuable tool for research into type 2 diabetes. -
GPR119 Agonist
K-833 is a potent GPR119 agonist with EC50 values of 39.8 nM in humans, 100 nM in mice, 75.4 nM in rats, and 12.6 nM in dogs. This compound enhances GLP-1 secretion and exhibits a synergistic effect on GLP-1 levels when administered alongside AM-5262 in acute gut peptide secretion assays in mice. K-833 is suitable for research focusing on weight loss and metabolic regulation. -
H1R Antagonist
Fexofenadine Impurity F is a derivative of Fexofenadine, primarily acting as a histamine H1 receptor (H1R) antagonist. This compound exhibits biological activity associated with anti-allergic properties, making it relevant in the study of allergic reactions and potential therapeutic interventions for conditions such as seasonal allergic rhinitis and chronic idiopathic urticaria. It serves as a useful reagent for research in drug development and impurity profiling. -
Active Metabolite of Cannabinol
11-Hydroxy cannabinol is an active metabolite of Cannabinol, primarily targeting cannabinoid receptors in the endocannabinoid system. This compound exhibits biological activity that may influence numerous physiological processes, including pain modulation and anti-inflammatory effects. It is utilized in preclinical research to explore therapeutic applications related to cannabinoid signaling pathways and their potential impact on various health conditions. -
Xylazine Metabolite
2,6-Dimethylphenylthiourea is a metabolite of xylazine, an established α2-adrenergic agonist. This compound serves as a valuable tool in pharmacological research, specifically in studies examining the metabolic pathways of xylazine and its effects on α2-adrenergic receptors. It provides insights into its pharmacokinetics and potential physiological implications. -
Adenosine A2A Receptor Inhibitor
4-Desmethyl Istradefylline is a selective adenosine A2A receptor antagonist, serving as a significant metabolite of Istradefylline. With a Ki of 2.2 nM, it demonstrates potent inhibition of the A2A receptor, making it relevant for exploring therapeutic strategies in Parkinson's disease and related neurological disorders. Its oral bioactivity allows for convenience in in vivo research applications targeting adenosine signaling pathways. -
Stable Isotope
Quetiapine Sulfoxide-d8 is a deuterated analog of Quetiapine sulfoxide, a primary metabolite of the second-generation antipsychotic Quetiapine. This compound acts as a 5-HT receptor agonist and dopamine receptor antagonist, playing a critical role in the pharmacokinetic studies of Quetiapine metabolism. Quetiapine Sulfoxide-d8 is commonly utilized in research applications involving drug metabolism, pharmacology, and analytical chemistry, particularly in the development and validation of quantitation methods in biological samples. -
Pergolide Metabolite
Pergolide sulfone is a metabolite of Pergolide, primarily acting as a dopamine receptor agonist. This compound exhibits significant dopaminergic activity, making it relevant for research into Parkinson's disease and other neurological disorders. Pergolide sulfone can be utilized in studies investigating the pharmacological profiles of dopamine receptor interactions and their implications in neurodegenerative conditions. -
Drug Derivative
(±)-p-Fluoro pseudoephedrine hydrochloride is a drug derivative associated with the pharmacological activity of pseudoephedrine. This compound exhibits decongestant properties, primarily functioning as a sympathomimetic agent that influences adrenergic receptors. Its biological activity is employed in studies related to respiratory distress, providing valuable insights into drug metabolism and therapeutic efficacy in treatments for nasal congestion. -
MMB-CHMICA Metabolite
MMB-ICA is a metabolite of MMB-CHMICA, primarily targeting the cannabinoid receptor system. This compound demonstrates significant biological activity in modulating receptor signaling pathways, making it valuable for research in cannabinoid pharmacology. MMB-ICA is utilized in studies investigating the therapeutic potential of cannabinoids and their metabolic pathways. -
PB-22 Metabolite
PB-22 N-(5-Hydroxypentyl)-3-carboxyindole metabolite is a primary metabolite of the cannabinoid PB-22. This compound exhibits biological activity through its interaction with the endocannabinoid system, influencing cannabinoid receptor signaling pathways. It is utilized in research to explore the metabolic pathways of synthetic cannabinoids and their pharmacological effects in various biological systems. -
Drug Metabolite
Reduced Haloperidol, a primary metabolite of Haloperidol, functions as a dopamine receptor antagonist. It exhibits significant antipsychotic activity, primarily utilized in research related to schizophrenia and other psychotic disorders. This compound is instrumental in studies investigating the modulation of neurotransmitter systems, aiding in the reduction of hallucinations and delusions associated with these conditions. -
Clonidine Metabolite
4-Hydroxyclonidine is a metabolite of Clonidine, primarily functioning as an alpha-2 adrenergic agonist. It exhibits comparable potency to Clonidine in displacing labeled Clonidine from specific antibodies. This compound is of significant interest in pharmacological research, particularly in studies examining adrenergic receptor interactions and the metabolic pathways of antihypertensive agents. -
Propranolol Active Metabolite
Norpropranolol hydrochloride is the active metabolite of Propranolol, primarily targeting beta-adrenergic receptors. It exhibits significant cardiovascular effects, including the reduction of heart rate and blood pressure. This compound is used in research applications focused on studying cardiovascular pharmacology and the modulation of stress response pathways. -
Bufuralol Metabolite
4-Hydroxybufuralol is a primary metabolite of Bufuralol, known for its significant role in pharmacokinetics. It exhibits interactions with beta-adrenergic receptors, contributing to cardiovascular research applications. This compound is essential for studies focused on drug metabolism and the pharmacological effects of beta-blockers. -
PB-22 Metabolite
PB-22 N-(4-Hydroxypentyl)-3-carboxyindole metabolite is a significant metabolite of the synthetic cannabinoid PB-22. This compound interacts primarily with cannabinoid receptors, influencing cannabinoid signaling pathways. It is valuable for research applications focused on studying the metabolism and pharmacological effects of cannabinoids, as well as providing insights into potential therapeutic uses and regulatory impacts associated with cannabinoid exposure. -
Alprenolol Metabolite
4-Hydroxyalprenolol is a metabolite of the β-receptor blocker Alprenolol, known for its role in modulating adrenergic signaling. This compound exhibits biological activity related to cardiovascular function and may be utilized in research focused on the pharmacokinetics and pharmacodynamics of β-blockers. Its analysis can provide insights into the metabolism of therapeutic agents and their effects on β-adrenergic receptors. -
MMB-CHMICA Metabolite
AB-INACA is a metabolite of the synthetic cannabinoid AB-CHMINACA, acting primarily on the cannabinoid receptors. This compound has been utilized in research to investigate synthetic cannabinoid metabolism and receptor interaction dynamics. Its biological activity provides valuable insights into the pharmacological pathways of synthetic cannabinoids, making it a useful tool for toxicological studies and drug metabolism research. -
5-HT Metabolite
5-Hydroxy NMT oxalate is a metabolite of serotonin (5-HT) that functions as a neuromodulator. This compound has been implicated in various neurophysiological processes and is associated with cocaine addiction, as elevated plasma levels have been observed in affected individuals. Its utility in research extends to the study of serotonergic signaling pathways and addiction-related behaviors. -
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. -
Neurokinin-1 Receptor Antagonist
TAK-637 is an orally active antagonist of the neurokinin-1 receptor, known for its role in modulating neuronal signaling pathways. This compound has been shown to enhance bladder storage capacity and may provide insights into the treatment of functional bowel diseases, including irritable bowel syndrome. TAK-637 serves as a valuable tool for researchers investigating the therapeutic potential of neurokinin-1 receptor modulation in urological and gastrointestinal disorders. -
NK1 Receptor Antagonist
TKA-731 is an NK1 receptor antagonist that effectively modulates nociceptive signaling. It has demonstrated the ability to reverse mechanical hyperalgesia and exhibit analgesic properties in neuropathic pain models, particularly in guinea pigs. This compound is valuable for research applications focused on understanding and targeting neuropathic pain mechanisms. -
NK3 Receptor Antagonist
SSR 146977 is a selective antagonist of the tachykinin NK3 receptor. It demonstrates potent inhibition of neurokinin B binding to NK3 receptors in Chinese hamster ovary cells, with a Ki value of 0.26 nM. This compound is valuable in research focused on neurokinin signaling pathways and their implications in physiological and pathological conditions. -
NK1 Receptor Antagonist
Rolapitant hydrochloride is a potent and selective neurokinin 1 (NK1) receptor antagonist, demonstrating a Ki value of 0.66 nM. This compound is distinguished by its long-acting and orally active properties. In pharmacological studies, rolapitant hydrochloride exhibits significant anti-emetic activity, as evidenced by its effectiveness in a ferret emesis model. Its unique mechanism makes it a valuable tool for research on emesis and nausea pathways. -
NK1R Fragment
Neurokinin Receptor (393-407), rat, is a fragment of the rat neurokinin 1 receptor (NK1R), which is known for its role in mediating cellular responses to substance P through rapid internalization and subsequent recycling to the plasma membrane. This reagent is essential for investigating neurogenic inflammation and offers insights into the pathways associated with NK1R signaling. It serves as a valuable tool for researchers studying receptor dynamics and neuroinflammatory mechanisms. -
NK1 Receptor Antagonist
L-703606 oxalate is a selective antagonist of the NK1 receptor, effectively inhibiting its activity. This compound plays a significant role in the study of gastric acid secretion, providing insights into neurokinin signaling pathways. Its potent inhibitory effects make it a valuable tool for research in gastrointestinal physiology and related disorders.
