Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
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.
