Catalog No.
Product Name
Application
Product Information
Citations
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CXCR Antagonist
GSK812397 is a potent CXCR4 antagonist that functions by inhibiting the CXC chemokine receptor 4, a critical co-receptor for HIV-1 entry into host cells. This compound has demonstrated significant biological activity, making it a promising candidate for HIV treatment research. Its ability to suppress the replication of various late cytopathic viruses marks GSK812397 as a valuable reagent in the development of innovative anti-HIV therapies. Additionally, scalable synthetic routes enable efficient production, ensuring sufficient quantities for comprehensive investigation. -
CXCR Antagonist
CXCR4 antagonist 1 is a selective antagonist of the chemokine receptor CXCR4. It exhibits significant anti-HIV activity by inhibiting the interaction of CXCR4 with its ligands, thereby blocking viral entry into host cells. This compound is valuable in research focused on HIV pathogenesis and the development of therapeutic strategies targeting CXCR4. -
CXCR4 Antagonist
HF50731 is a potent antagonist of CXCR4, demonstrating a binding affinity with an IC50 value of 19.8 nM. This compound effectively inhibits key biological processes such as calcium mobilization and cell migration, with IC50 values of 119.2 nM and 621.4 nM, respectively. Additionally, HF50731 demonstrates the ability to inhibit HIV-1 infection through CXCR4 coreceptor blockade, achieving an IC50 of 1.5 μM. HF50731 is valuable for research in immunology, virology, and cancer biology focused on CXCR4 signaling pathways. -
CXCR Inhibitor
AMD-3329 is a selective CXCR4 inhibitor that targets the chemokine receptor involved in HIV-1 and HIV-2 entry into host cells. By obstructing CXCR4, AMD-3329 effectively inhibits viral replication, making it a valuable tool in HIV research. This compound is suitable for studies focused on developing therapeutic strategies against X4-tropic HIV strains and understanding the mechanisms of viral entry and infection. -
Platelet-Activating Factor Antagonist
Acopafant is a potent platelet-activating factor antagonist that plays a critical role in modulating inflammatory responses. Its ability to inhibit human immunodeficiency virus (HIV) expression in chronically infected cells highlights its potential utility in HIV research. Acopafant is valuable for studies investigating the mechanisms of HIV infection and the development of therapeutics targeting viral latency and reactivation. -
HIV Inhibitor
KRH-3955 is a potent CXCR4 antagonist that demonstrates significant anti-HIV-1 activity, particularly against X4 strains. It effectively inhibits the replication of various X4 HIV-1 clinical isolates and is active against recombinant strains with resistance mutations in reverse transcriptase, protease, and tyrosinase. KRH-3955 disrupts the binding of SDF-1alpha to CXCR4, thereby interfering with calcium signaling through this receptor, along with inhibiting antibody binding to CXCR4. With an oral bioavailability of 25.6% in rats, KRH-3955 has shown efficacy in vivo, making it a valuable tool for HIV research. -
PAFR Antagonist
(Rac)-Modipafant is a selective, long-acting irreversible antagonist of the platelet activating factor receptor (PAFR). This compound demonstrates significant biological activity by effectively inhibiting PAFR-mediated pathways, which plays a critical role in regulating inflammatory responses. Research applications include the investigation of dengue virus infection mechanisms and the potential therapeutic effects of PAFR blockade in various inflammatory diseases. -
Adenosine Receptor Antagonist
Swertisin is an adenosine A1 receptor antagonist with additional SGLT2 inhibitory activity. This compound exhibits various biological functions, including anti-diabetic and antioxidant properties, as well as the ability to inhibit hepatitis B virus (HBV). Research has demonstrated that Swertisin can enhance cognitive function and alleviate memory impairments in murine models, making it a valuable tool for studies in diabetes, neuroprotection, and viral infections. -
Stable Isotope
Rimonabant-d10 hydrochloride is a deuterium-labeled derivative of Rimonabant hydrochloride, a selective antagonist of the central cannabinoid receptor (CB1) with a Ki of 1.8 nM. This compound is utilized in studies investigating the role of CB1 receptors in various physiological processes and the development of obesity therapies. Additionally, Rimonabant hydrochloride is known to inhibit Mycobacterial membrane protein Large 3 (MMPL3), making it relevant for research in tuberculosis and related infectious diseases. -
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. -
H1-Receptor Antagonist
Cetirizine Impurity B dihydrochloride is an impurity of the H1-receptor antagonist, cetirizine dihydrochloride. While cetirizine demonstrates significant antiallergic properties and effectively inhibits eosinophil chemotaxis during allergic responses, this specific impurity is valuable for analytical purposes and quality control in research applications. It aids researchers in understanding the pharmacological profile and potential effects associated with cetirizine and its metabolites. -
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. -
Adenosine Analog
3'-β-C-Methyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits biological activity as a smooth muscle vasodilator and has demonstrated potential in inhibiting cancer progression. It is useful in research applications focused on cardiovascular function and cancer biology. -
Adenosine Analog
9-(2-Deoxy-β-D-threo-pentofuranosyl)-9H-purin-6-amine is an adenosine analog that primarily acts on adenosine receptors. This compound exhibits smooth muscle vasodilatory activity and has demonstrated potential in inhibiting the progression of various cancers. It serves as a valuable tool in biochemical research focusing on vascular biology and oncology. -
Adenosine Analog
2-Amino-2′-O-(2-methoxy-2-oxoethyl)adenosine is an adenosine analogue targeting adenosine receptors. It exhibits smooth muscle vasodilatory effects and has demonstrated potential in inhibiting cancer progression. This compound is valuable for research applications focusing on vascular biology and cancer therapeutics. -
Adenosine Analog
2′-β-C-Methyl-2-methoxyadenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits vasodilatory effects on smooth muscle and has demonstrated potential in inhibiting cancer progression. Its applications extend to research involving cardiovascular function and cancer biology, making it a valuable tool for exploring therapeutic strategies in these areas. -
Adenosine Analog
N6-Benzoyl-2'-fluoro-2'-deoxyarabinoadenosine is an adenosine analog that primarily targets adenosine receptors. It exhibits significant vasodilatory effects on smooth muscle and has demonstrated potential in inhibiting cancer progression. This compound is valuable in research focused on vascular biology and cancer therapeutics, offering insights into adenosine receptor signaling pathways and their clinical implications. -
Adenosine Analog
2-Amino-6-chloro-9-[(2,3,5-tri-O-benzoyl-2-C-Methyl-beta-D-ribofuranosyl)]-9H-purine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits biological activities such as promoting smooth muscle vasodilation and potentially inhibiting cancer progression. It is a valuable reagent for researchers investigating vascular biology, cancer therapeutics, and adenosine signaling pathways. -
Adenosine Analog
2-Amino-N-(3-methyl-2-buten-1-yl)adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant smooth muscle vasodilatory activity and has been implicated in the inhibition of cancer progression. It serves as a valuable tool for research in vascular biology and cancer therapeutics, facilitating the exploration of adenosine receptor signaling pathways and their implications in various disease states. -
Adenosine Analog
5’-O-(4,4’-Dimethoxytrityl)-3’-O-t-butyldimethylsilyl adenosine is an adenosine analog that serves as a key modulator of adenosine receptors. This compound exhibits vasodilatory effects on smooth muscle and has potential applications in cancer research due to its ability to inhibit tumor progression. It is particularly useful for studies investigating the roles of adenosine in vascular biology and oncology. -
Adenosine Analog
2-Amino-N6,N6-dimethyl-2’-O-methyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits smooth muscle vasodilatory effects and has potential applications in inhibiting cancer progression. It is valuable for research in cardiovascular studies and oncology, providing insights into the therapeutic potential of adenosine-related pathways. -
Adenosine Analog
3’-beta-C-Methyl-N6-methyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant smooth muscle vasodilatory effects and has demonstrated potential in inhibiting cancer progression. Its unique structure allows for various research applications, particularly in studies focusing on cardiovascular function and tumor biology. -
Adenosine Analog
8-Allyloxyadenosine is an adenosine analog primarily targeting adenosine receptors. This compound exhibits significant biological activity as a smooth muscle vasodilator and has demonstrated potential in inhibiting cancer progression. It serves as a valuable tool in research applications focused on cardiovascular health and cancer therapy. -
Adenosine Analog
2-(4-Cyanobenzyl)thioadenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits potent vasodilatory effects on smooth muscle, making it of interest in cardiovascular research. Additionally, it has demonstrated potential in inhibiting cancer progression, making it a valuable tool for cancer biology studies. -
Adenosine Analog
4’-C-Methyl-N6-methyladenosine is an adenosine analogue that primarily targets adenosine receptors. This compound exhibits significant biological activity as a vasodilator, promoting smooth muscle relaxation, and has shown potential in inhibiting cancer cell progression. It serves as a valuable tool in research applications focused on vascular biology and cancer therapeutics. -
Adenosine Analog
N6-Isopentenyl-2’-C-methyladenosine is an adenosine analog that primarily acts as a vasodilator by influencing adenosine receptors. This compound has demonstrated potential in inhibiting cancer progression, making it valuable for research in oncology and cardiovascular studies. Its unique structure allows for diverse applications in studying nucleotide metabolism and therapeutic interventions targeting adenosine signaling pathways. -
Adenosine Analog
2-(4-Methylbenzyl)thioadenosine is an adenosine analog that primarily targets adenosine receptors. It is recognized for its vasodilatory effects on smooth muscle and demonstrates potential in inhibiting cancer progression. This compound serves as a valuable tool in researching adenosine receptor signaling, cardiovascular function, and cancer biology. -
Adenosine Analog
N-Propargyladenosine is an adenosine analogue that primarily acts as a vasodilator by targeting adenosine receptors. This compound exhibits significant biological activity, demonstrating potential in inhibiting cancer progression. Additionally, N-Propargyladenosine functions as a click chemistry reagent, containing an alkyne group that allows it to undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it valuable for various chemical biology applications. -
Adenosine Analog
3′-O-Methyladenosine is an adenosine analogue that primarily targets adenosine receptors. This compound exhibits significant biological activity as a smooth muscle vasodilator and has also demonstrated potential in inhibiting cancer progression. Its applications extend to various research fields, including cardiovascular studies and oncology, making it a valuable tool for investigating adenosine-related pathways and therapeutic targets. -
Adenosine Analog
2’,3’,5’-Tri-O-acetyl adenosine is an adenosine analog that primarily targets adenosine receptors, serving as a potent smooth muscle vasodilator. This compound has been shown to exert inhibitory effects on cancer progression, making it a valuable tool in oncology research. It is useful for studying adenosine signaling pathways and their implications in various biological processes. -
Adenosine Analog
2,8-Dimethyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant vasodilatory effects on smooth muscle and has demonstrated potential in inhibiting cancer progression. It serves as a valuable tool for research in cardiovascular studies and cancer biology. -
Adenosine Analog
2-Chloro-2′-β-C-methyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits vasodilatory effects on smooth muscle and demonstrates the potential to inhibit cancer progression. It serves as a valuable tool for research applications focused on vascular biology and cancer therapeutics. -
platelet aggregation inhibitor
Trifenagrel is an orally active platelet aggregation inhibitor that targets the pathways induced by arachidonic acid and collagen. It demonstrates significant biological activity, with ED50 values of 1.4 mg/kg and 9.4 mg/kg for the inhibition of AA- and collagen-induced platelet aggregation in guinea pigs, respectively. This compound serves as a valuable tool in cardiovascular research and the study of thrombotic disorders. -
Platelet-activating Factor Receptor (PAFR) Inhibitor
TSI-01 is a selective inhibitor of the Platelet-activating Factor Receptor (PAFR), targeting lysophosphatidylcholine acyltransferase (LPCAT)2. This compound exhibits a potent inhibitory effect with an IC50 of 0.47 μM for human LPCAT2, significantly more effective than its activity on LPCAT1 (IC50 = 3.02 μM). TSI-01 effectively suppresses PAF biosynthesis in mouse peritoneal macrophages when stimulated with a calcium ionophore at a concentration of 60 μM. This makes TSI-01 a valuable tool for investigating inflammatory processes and related conditions in research applications. -
PAFR Antagonist
MK 287 is a potent and selective antagonist of the platelet-activating factor receptor (PAFR). It effectively inhibits [3H]C18-PAF binding to human platelets, polymorphonuclear leukocytes (PMNs), and lung membranes, with K1 values of 6.1, 3.2, and 5.49 nM, respectively. MK 287 also demonstrates the ability to inhibit PAF-induced platelet aggregation and elastase release from PMNs, with ED50 values of 56, 1.5, and 4.4 nM. This compound is valuable for research focused on cardiovascular diseases, including thrombosis. -
PAF Antagonist
CV-6209 is a potent antagonist of platelet activating factor (PAF) that effectively inhibits PAF-induced aggregation in both rabbit and human platelets, demonstrating IC50 values of 75 nM and 170 nM, respectively. Additionally, CV-6209 has been shown to inhibit PAF-induced hypotension in rat models. This compound is valuable for research focused on platelet function, cardiovascular responses, and PAF-related pathways. -
PAF Agonist
Carbamyl-PAF is an analog and agonist of platelet-activating factor (PAF). It exhibits potent biological activity by stimulating PAF receptors, which play a crucial role in mediating inflammatory responses. Due to its stability and resistance to metabolism in Raji lymphoblasts at 37°C, Carbamyl-PAF is an effective reagent for studying PAF-related signaling pathways and inflammation mechanisms.
