Catalog No.
Product Name
Application
Product Information
Citations
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GLP-1R/GIPR Agonist
Brenipatide is a dual agonist of the glucagon-like peptide-1 (GLP-1) receptor and the gastric inhibitory polypeptide (GIP) receptor. It is primarily utilized in researching metabolic disorders, obesity, and diabetes, demonstrating significant potential in enhancing insulin secretion and promoting weight loss. This compound is essential for studies investigating the pathways and mechanisms involved in glucose homeostasis and energy balance. -
GLP-1 Receptor Agonit
Utreglutide is a potent glucagon-like peptide-1 (GLP-1) receptor agonist that plays a significant role in the regulation of glucose metabolism. This compound not only aids in lowering blood pressure and blood lipid levels but also contributes to weight reduction and enhances cardiovascular health. Utreglutide is particularly valuable in research focusing on type 2 diabetes and obesity-related conditions, facilitating a deeper understanding of metabolic disorders. -
GLP-1R Agonist
CHU-128 is a selective GLP-1 receptor (GLP-1R) agonist that effectively activates the Gs/cAMP signaling pathway. This compound is characterized by its strong signal specificity, as it does not engage the Gq/calcium signaling pathway, ERK phosphorylation, or recruit β-inhibitory proteins. CHU-128 is suitable for research applications focused on type 2 diabetes and related metabolic disorders. -
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. -
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. -
Endogenous Metabolite
1-Methylhistamine dihydrochloride is a metabolite of histamine that primarily targets histamine receptors. This compound exhibits significant biological activity in the modulation of allergic responses and neurotransmission processes. It is widely utilized in research applications focusing on histamine signaling pathways and its role in various physiological and pathological conditions. -
Drug Metabolite
Desmethyl Bosentan is an active metabolite of the endothelin receptor antagonist bosentan. It functions primarily by activating the pregnane X receptor (PXR), as demonstrated in CV-1 monkey kidney cells expressing the human receptor in a reporter assay at a concentration of 25 μM. This compound is valuable for studying drug metabolism and the regulatory pathways involved in pharmacokinetics and toxicology research. -
DAGL-α/DAGL-β Inhibitor
LEI105 is a selective and reversible dual inhibitor of diacylglycerol lipase (DAGL)-α and DAGL-β. This compound effectively decreases levels of 2-arachidonoylglycerol in Neuro2A cells, demonstrating its potential to modulate endocannabinoid signaling. Research applications include investigations into the mechanisms underlying obesity, metabolic disorders, and neuroinflammation, as well as studies of cannabinoid receptor-mediated synaptic plasticity in mouse hippocampal slices. -
Drug Metabolite
Quetiapine sulfoxide dihydrochloride is a primary metabolite of the second-generation antipsychotic quetiapine. This compound functions as a 5-HT receptor agonist and a dopamine receptor antagonist, contributing to its pharmacological effects. It is commonly utilized in research related to neuropharmacology and metabolic profiling of antipsychotic drugs, offering insights into the drug's therapeutic activity and safety profile. -
Metabolite of Acebutolol
Diacetolol is an active metabolite of the beta-adrenoceptor antagonist Acebutolol. It exhibits pharmacological activity by selectively inhibiting β1-adrenergic receptors, which plays a significant role in cardiovascular research. Diacetolol is utilized to study beta-blocker pharmacodynamics and to explore its effects on heart rate and blood pressure regulation. -
Drug Metabolite
3-Hydroxy Medetomidine is a primary metabolite of the α2-adrenergic receptor agonist medetomidine. This compound exhibits important biological activity as it participates in modulating adrenergic signaling pathways. Research applications include studies on drug metabolism and the pharmacokinetics of sedatives in both veterinary and medical contexts. -
Lurasidone Metabolite
Lurasidone Metabolite 14283 hydrochloride is a significant active metabolite of the antipsychotic agent Lurasidone, which targets serotonin and dopamine receptors. This compound plays a crucial role in the pharmacological activity of Lurasidone, contributing to its efficacy in the treatment of schizophrenia. Research applications include studying the metabolic profile of Lurasidone and its pharmacodynamics in neural systems. -
5-HT2A Inverse Agonist
N-Desmethyl Pimavanserin is a potent inverse agonist of the 5-HT2A receptor, serving as an active metabolite of Pimavanserin. With high affinity demonstrated by a pIC50 of 8.73 and pKd of 9.3, this compound has significant implications in research focused on psychiatric disorders, such as schizophrenia and Parkinson's disease psychosis. Its role in modulating serotonergic signaling makes it an important reagent for studies investigating the therapeutic potential of 5-HT2A antagonism. -
Drug Metabolite
Quetiapine sulfoxide hydrochloride is a primary metabolite of Quetiapine, a second-generation antipsychotic. This compound acts primarily as a 5-HT receptor agonist and dopamine receptor antagonist, contributing to the pharmacological profile of Quetiapine. It is valuable in research focusing on the metabolism and pharmacokinetics of antipsychotic medications, providing insights into their therapeutic effects and potential side effects. -
Drug Metabolite
1-epi-Regadenoson is an α-isomer impurity of Regadenoson, a potent and selective agonist for the adenosine A2A receptor. This compound is primarily used in research to investigate the pharmacological effects of adenosine receptor activation and its implications in cardiovascular function. The study of 1-epi-Regadenoson can aid in understanding the metabolic pathways and potential therapeutic effects associated with adenosine receptor modulation. -
Active Metabolite of delta 9-Tetrahydrocannabinol
9α,10α-Epoxyhexahydrocannabinol is an active metabolite of delta 9-tetrahydrocannabinol, primarily targeting cannabinoid receptors. This compound exhibits notable anticonvulsant properties, effectively reducing body temperature and prolonging pentobarbital-induced sleep in animal models. Additionally, it has demonstrated protective effects against pentylenetetrazol-induced seizures, making it valuable for research in seizure disorders and cannabinoid pharmacology. -
Quetiapine Metabolite
7-Hydroxyquetiapine is the primary active metabolite of the antipsychotic agent Quetiapine. It functions by modulating various neurotransmitter systems, particularly serotonin and dopamine receptors, contributing to its therapeutic effects in managing psychiatric disorders. This compound is valuable for studying the pharmacological profile of Quetiapine and investigating its metabolic pathways in both in vitro and in vivo research settings. -
Drug Metabolite
Silodosin Glucuronide sodium is the sodium salt of Silodosin β-D-glucuronide, a metabolite of the selective α1A-adrenergic receptor antagonist Silodosin. It exhibits high affinity for the α1A-AR, facilitating a Ki value of 0.036 nM. This compound is crucial for studying the pharmacokinetics and metabolic pathways of Silodosin, contributing to research applications in urology and cardiovascular studies. -
Terbutaline Derivative
Terbutalone is a derivative of terbutaline, targeting the β2-adrenergic receptors. As an orally active agonist, it demonstrates significant bronchodilator activity, making it a valuable tool in asthma and respiratory research. Terbutalone may also have applications in studying other β2-adrenergic receptor-mediated physiological responses. -
Drug Metabolite
Carvedilol Glucuronide is a significant metabolite of the β/α-1 adrenergic receptor antagonist, Carvedilol. This compound demonstrates key biological activity by modulating β-adrenergic signaling and exhibits potential application in studying the metabolic pathway of Carvedilol. Research indicates that Carvedilol can inhibit lipid peroxidation and has properties as an antihypertensive agent, as well as an autophagy inducer that affects the NLRP3 inflammasome. Carvedilol Glucuronide serves as an important reagent for investigating drug metabolism and pharmacokinetics in cardiovascular research. -
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. -
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. -
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.
