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Catalog No.
Product Name
Application
Product Information
Citations
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PDE3/PDE4/PDE5/HRH1 Inhibitor
Fenspiride hydrochloride is a non-steroidal anti-inflammatory agent and an antagonist of the H1-histamine receptor. It selectively inhibits phosphodiesterase activities, including PDE3, PDE4, and PDE5, with -log IC50 values of 3.44, 4.16, and approximately 3.8, respectively. This compound is valuable for research applications focused on respiratory diseases, highlighting its potential in therapeutic investigations and the modulation of inflammatory responses. -
Bacterial Inhibitor
Chlorprothixene hydrochloride functions as an antagonist of dopamine and histamine receptors, exhibiting Kis of 18 nM for hD1, 2.96 nM for hD2, 4.56 nM for hD3, 9 nM for hD5, and 3.75 nM for hH1 receptors. This compound demonstrates significant antipsychotic activity, making it a valuable tool for research into neuropharmacology and the mechanisms underlying psychotic disorders. Its receptor modulation also indicates potential applications in the study of bacterial inhibition mechanisms, providing insights into the interplay between neurotransmitter systems and microbial pathogenesis. -
VEGFR Inhibitor
Chloropyramine hydrochloride is an H1 histamine receptor antagonist that also serves as an inhibitor of vascular endothelial growth factor receptor 3 (VEGFR-3) and focal adhesion kinase (FAK). This compound exhibits key biological activities, contributing to research in angiogenesis and related pathways. It is valuable for studies aimed at understanding the role of VEGFR signaling in various physiological and pathological processes. -
Cannabinoid Receptor Inhibitor
Yangonin is a selective cannabinoid receptor inhibitor that demonstrates affinity for the human recombinant CB1 receptor, with an IC50 value of 1.79 μM and a Ki of 0.72 μM. This compound is of significant interest for research applications aimed at understanding cannabinoid signaling and its implications in various physiological processes. Its modulation of CB1 receptor activity may provide insights into therapeutic strategies targeting cannabinoid-related pathways. -
Adrenergic Receptor Inhibitor
Penbutolol sulfate is a potent adrenergic receptor inhibitor, primarily acting as a β-adrenoceptor and 5-HT receptor antagonist, with Ki values of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3 regions, respectively. This compound demonstrates significant biological activity through modulation of neurotransmitter signaling pathways, making it valuable for research applications involving cardiovascular studies and neuropharmacology. -
Histamine Receptor Inhibitor
Dexchlorpheniramine maleate is a potent histamine receptor inhibitor primarily utilized in the treatment of allergic conditions. This compound exhibits anti-inflammatory, anti-irritant, and anti-allergic properties, making it effective for managing symptoms of allergic rhinitis. Additionally, dexchlorpheniramine maleate has been shown to inhibit myocardial contraction in rat models, providing further insight into its biological effects. It serves as a valuable reagent for research applications exploring the mechanisms of allergic responses and their physiological effects. -
5-HT Receptor Inhibitor
BF-1 is a potent antagonist of the 5-HT2B receptor, exhibiting a pKi value of 10.05 and an IC50 of 2.6 nM. This compound demonstrates significant inhibitory activity, making it valuable for research applications in neurobiology and pharmacology. Its specificity for the 5-HT2B receptor allows for detailed investigation into serotonin signaling pathways and related physiological processes. -
5-HT Receptor Inhibitor
5-APDI hydrochloride is a selective inhibitor of the 5-HT receptor, exhibiting significant biological activity in modulating neurotransmitter uptake. It effectively inhibits the reuptake of serotonin, dopamine, and norepinephrine in crude synaptosomes, with IC50 values of 82 nM, 1,847 nM, and 849 nM, respectively. This compound is valuable in research applications related to neuropharmacology and the study of mood disorders. -
5-HT Uptake Inhibitor
Litoxetine is a selective 5-HT uptake inhibitor that functions primarily through its action on serotonin transporters. It also acts as a 5-HT3 receptor antagonist, exhibiting a Ki value of 85 nM for cerebral 5-HT3 receptors. This compound is utilized in research related to depression and nausea, showcasing its potential as an antidepressant and antiemetic agent. -
5-HT6 Receptor Modulator/Lp-PLA2 Inhibitor
Goxalapladib is a selective modulator of the 5-HT6 receptor that also serves as an inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Its mechanism of action suggests potential applications in the investigation of atherosclerosis-related cardiovascular diseases. This compound facilitates research into the modulation of lipid metabolism and inflammation, making it a valuable tool for studies focused on cardiovascular health. -
5-HT2 Inhibitor
Cloroperone is a potent 5-HT2 receptor inhibitor with a Ki value of 4.5 nM. It demonstrates significant biological activity in modulating serotonin signaling pathways, making it useful in the study of psychiatric disorders. Cloroperone's inhibitory effects on the 5-HT2 receptor can aid in research focused on understanding the mechanisms underlying various neuropsychiatric conditions. -
5-HT Receptor Inhibitor
4-CAB hydrochloride is a potent 5-HT receptor inhibitor that acts as an analog of p-chloroamphetamine. It demonstrates significant inhibition of serotonin reuptake with an IC50 value of 330 nM, alongside dopamine reuptake inhibition with an IC50 of 2.3 μM. This compound is valuable for research focusing on serotonergic and dopaminergic neurotransmission, as well as investigations into the neuropharmacology of psychoactive substances. -
5-HT/NE Inhibitor
(R)-Indeloxazine benzenesulfonate is a potent inhibitor of serotonin (5-HT) and norepinephrine (NE) reuptake, exhibiting IC50 values of 0.35 μM and 3.3 μM, respectively. This compound demonstrates notable analgesic effects reminiscent of curative outcomes and may enhance nerve function by improving neurotrophic support. It is valuable for research applications focusing on pain management and the exploration of neurological disorders. -
5-HT Inhibitor
Femoxetine functions as a serotonin (5-HT) inhibitor, exhibiting potential antidepressant properties. By blocking the reabsorption of serotonin in nerve cells, it elevates serotonin concentrations in the synaptic cleft, thereby enhancing serotonin signaling. This compound is instrumental in researching the involvement of serotonin in depression and other affective disorders, as well as examining the effects of 5-HT reuptake inhibitors on mood regulation and behavioral responses. -
5-HT Receptor Inhibitor
5-IAI hydrochloride is a selective 5-HT receptor inhibitor that modulates serotonin signaling. This compound has been shown to significantly reduce serotonin uptake sites and decrease hippocampal serotonin levels in rat models. It serves as an important tool for research into serotonin-related pathways and their implications in neuropharmacology. -
5-HT Receptor Inhibitor
PF-05212377 is a selective inhibitor of the serotonin receptor 5-HT6. This compound serves as a substrate for the P-glycoprotein non-BCRP human transporter and demonstrates blood-brain barrier permeability in non-human primates. PF-05212377 holds potential for research applications related to Alzheimer's Disease, enabling exploration of its role in neurodegenerative mechanisms and therapeutic strategies. -
5-HT Receptor Inhibitor
DSP-6745 is a potent and orally active inhibitor of the 5-HT receptor. This compound exhibits significant biological activity in modulating serotonergic signaling, making it a valuable tool for research into depressive disorders. Its ability to selectively target 5-HT receptors enables the investigation of their role in mood regulation and related pathologies. -
5-HT/NA reuptake Inhibitor
5-HT/NA Reuptake Inhibitor-1 is a selective dual inhibitor of serotonin (5-HT) and norepinephrine (NA) reuptake, exhibiting IC50 values of 660 nM and 70 nM, respectively. This compound demonstrates favorable in vitro metabolic stability in humans, along with high hERG selectivity and passive membrane permeability. It is primarily utilized in research focused on mood disorders and neuropharmacology, providing valuable insights into the modulation of neurotransmitter systems. -
Serotonin/Norepinephrine/Dopamine Reuptake Inhibitor
Bicifadine is a serotonin/norepinephrine/dopamine reuptake inhibitor that demonstrates oral bioavailability. It exhibits significant antinociceptive properties across various models of acute, persistent, and chronic pain. Bicifadine is primarily utilized in research related to pain mechanisms and therapeutic interventions for pain management. -
5-HT6R/MAO-B Inhibitor
5-HT6R/MAO-B modulator 1 is a selective antagonist of the 5-HT6 receptor with Gs signaling activity and serves as an irreversible inhibitor of monoamine oxidase B (MAO-B). This compound demonstrates glioprotective effects and has the capability to reverse memory deficits induced by scopolamine. Additionally, it features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it a versatile tool for chemical biology applications. -
5-HT Inhibitor
Femoxetine hydrochloride is a selective serotonin (5-HT) inhibitor known for its antidepressant properties. By inhibiting the reuptake of serotonin, it elevates serotonin levels within the synaptic cleft, thereby enhancing serotonergic signaling. This compound is valuable in research focusing on the role of serotonin in mood regulation and its implications in depression and related emotional disorders. -
5-HT Receptor Inhibitor
Org 6582 is a competitive and selective inhibitor of the 5-HT receptor, demonstrating a Ki value of 89 nM. This compound exhibits a long-lasting inhibitory effect on serotonin uptake, persisting for over 48 hours. Org 6582 is primarily utilized in research focusing on depressive disorders, providing valuable insights into serotonergic modulation in various neuropsychological studies. -
5-HT Receptor Inhibitor
5-HT3-In-1 is a selective inhibitor of the 5-HT3 receptor, effectively blocking serotonin's action at this target. This compound demonstrates notable efficacy in inhibiting 5-HT3-mediated signaling pathways, making it valuable for research focused on neuropharmacology and gastrointestinal function. Its use extends to studying various conditions, including anxiety, depression, and nausea-related disorders. -
5-HT Reuptake Inhibitor
Ifoxetine hemisulfate is a selective inhibitor of the serotonin (5-HT) reuptake process in the central nervous system. By specifically targeting 5-HT transporters, it effectively blocks serotonin reuptake in the brain while sparing peripheral uptake in blood platelets. This compound shows promise for its antidepressant properties and is utilized in research focused on mood regulation and neuropharmacology. Additionally, Ifoxetine hemisulfate has been demonstrated to inhibit the uptake of radiolabeled 5-HT in rat brain synaptosomes, providing valuable insights into serotonin dynamics and receptor interactions. -
5-HT2C Inhibitor
SB 242084 monohydrochloride is a selective and high-affinity antagonist of the 5-HT2C receptor with a pKi value of 9.0. This compound effectively enhances the basal activity of dopaminergic neurons in the ventral tegmental area, stimulating dopamine release in the vomeronasal nucleus. Additionally, SB 242084 promotes mitochondrial gene expression and oxidative metabolism through 5-HT2A receptor interactions. Its potential applications in research include the investigation of negative symptoms associated with anxiety, depression, and schizophrenia, as well as the study of acute organ damage. -
Triple Reuptake Inhibitor
Tedatioxetine is a serotonin and norepinephrine-preferring triple reuptake inhibitor (TRI) that also functions as an antagonist of 5-HT2A, 5-HT2C, 5-HT3, and α1A-adrenergic receptors. This compound exhibits significant biological activity in modulating neurotransmitter levels, making it relevant for research in neuropharmacology. Its mechanism of action positions it as a valuable tool in studies related to mood disorders and anxiety. -
Dopamine/5-HT Receptor Inhibitor
Loxapine hydrochloride is an orally active inhibitor of dopamine receptors and an antagonist of 5-HT receptors. This dibenzoxazepine compound exhibits significant antipsychotic properties, making it valuable for research into psychotropic effects and therapeutic interventions for schizophrenia and other psychiatric disorders. Its dual receptor activity contributes to its efficacy in modulating dopaminergic and serotonergic pathways. -
α2-adrenoceptor Antagonist/5-HT Receptor re-uptake Inhibitor
Napamezole is a potent α2-adrenoceptor antagonist and 5-HT receptor reuptake inhibitor, exhibiting Ki values of 28 nM and 93 nM for rat α2 and α1 adrenergic receptors, respectively. This compound is primarily utilized in research related to depression, facilitating studies on the modulation of serotonergic and adrenergic signaling pathways. Its unique pharmacological profile makes it a valuable tool for investigating potential therapeutic approaches in mood disorders. -
5-HT1A Receptor Inhibitor
LY 178210 is a selective partial agonist of the 5-HT1A receptor, exhibiting Ki values of 0.67 nM for 5-HT1A and 380 nM for 5-HT1D receptors, thereby demonstrating its specificity. Its minimal activity against α₂-adrenergic receptors, 5-HT₂, and other neurotransmitter receptors makes it a valuable tool in neuropharmacology. Additionally, LY 178210 effectively inhibits forskolin-stimulated cyclase activity, though with lower potency compared to full agonists like 8-OH-DPAT. This compound is significant for studies on serotonergic modulation, as it markedly reduces 5-hydroxyindoleacetic acid (5-HIAA) levels in the hypothalamus while increasing serum corticosterone concentrations. -
5-HT2A Receptor Inhibitor
Belaperidone is a selective 5-HT2A receptor inhibitor, demonstrating significant antidopaminergic and antiserotonergic properties. This compound is primarily employed in research related to neuropsychiatric disorders and may provide insight into therapeutic strategies for conditions such as schizophrenia and depression. Its mechanism of action makes Belaperidone a valuable tool in studying serotonin and dopamine receptor interactions within the central nervous system. -
5-HT2AR Inhibitor
5-HT2AR-IN-1 is a potent inhibitor of the 5-hydroxytryptamine 2A receptor (5-HT2AR) with demonstrated antidepressant activity. It effectively reduces both 5-HT2AR expression and serotonin transporter (SERT) protein levels. This compound is suitable for research into central nervous system disorders, including depression and addiction-related conditions, highlighting its potential in investigating therapeutic strategies for these ailments. -
5-HT Receptor Inhibitor
Citalopram hydrochloride is an orally active inhibitor of the 5-HT receptor, primarily functioning as a selective serotonin reuptake inhibitor (SSRI). This compound exhibits significant antidepressant activity and is widely utilized in research focused on depression and related mood disorders. Its mechanism aids in increasing serotonin levels in the synaptic cleft, making it a valuable tool for studying serotonin-related pathways and therapeutic interventions in psychiatric conditions. -
5-HT Reuptake Inhibitor
Ifoxetine is a selective inhibitor of the serotonin (5-HT) reuptake process, primarily targeting the central nervous system while sparing peripheral uptake in blood platelets. This compound effectively inhibits the uptake of radiolabeled 5-HT in rat brain synaptosomes, both in vitro and ex vivo. Due to its mechanism of action, Ifoxetine demonstrates potential antidepressant properties and can be utilized in research related to mood disorders and serotonin signaling. -
SERT Inhibitor/5-HT₂A receptor Antagonist
LY 367265 is a potent inhibitor of the serotonin transporter (SERT) with an IC₅₀ value of 3.1 nM and also serves as a selective antagonist for the 5-HT₂A receptor (Kᵢ = 0.81 nM). It displays minimal activity on the norepinephrine transporter (NET) and low affinity for other serotonin receptor subtypes, reinforcing its selectivity. LY 367265 enhances the efflux of [³H]5-HT in a concentration-dependent manner (EC₅₀ = 250 nM) and can counteract the contraction induced by Sumatriptan, indicating its antagonistic effects on 5-HT₁D-like receptors. This compound is valuable for research into neurological disorders, including anxiety and post-traumatic stress disorder. -
5-HT Deamination Inhibitor
RS 2232 is a competitive inhibitor of 5-hydroxytryptamine (5-HT) deamination, demonstrating a Ki of 0.054 μM. This compound selectively and reversibly inhibits type A monoamine oxidase, making it a valuable tool in neurological research. RS 2232 is utilized to gain insights into the role of serotonin metabolism in various brain functions and disorders. -
Platelet Aggregation Inhibitor
Epoprostenol sodium, a synthetic derivative of prostaglandin I2, primarily acts as a potent inhibitor of platelet aggregation. This compound is widely recognized for its role in the management of pulmonary arterial hypertension (PAH) and is utilized in clinical settings such as pulmonary hypertension and organ transplantation. Its ability to modulate vasodilation and inhibit platelet activation makes it a valuable tool in related biomedical research applications. -
Histamine Release Inhibitor
Alginic acid is a natural polysaccharide recognized for its ability to inhibit histamine release, making it a valuable compound for research into allergic reactions and inflammation. Its remarkable water solubility, film-forming properties, and biodegradability enhance its applicability in various biological studies. Alginic acid has been demonstrated to induce oxidative stress-mediated effects, resulting in hormone secretion disorders, apoptosis, and autophagy in mouse granulosa cells and ovaries. This compound is of particular interest in anti-anaphylactic and anti-inflammatory research applications. -
CBR1 Inhibitor
Hydroxy-PP-Me is a selective inhibitor of the cannabinoid receptor type 1 (CBR1) with an IC50 of 759 nM. It effectively inhibits serum starvation-induced apoptosis and enhances the cytotoxic effects of chemotherapeutic agents such as Daunorubicin and Arsenic Trioxide (As2O3) on tumor cells. Hydroxy-PP-Me is a valuable tool for cancer research, particularly in the study of leukemia and related malignancies. -
NF-κB Expression Reducer, ERK 1/2 Activator, Beta-Adrenergic Receptor Modulator, Calcium Channel Inhibitor
Eupatorin is a flavonoid that functions primarily as an NF-κB expression reducer and an ERK 1/2 activator, while also modulating beta-adrenergic receptors and inhibiting calcium channels. It demonstrates significant antiproliferative and vasodilatory effects, inducing apoptosis and causing G2/M phase cell cycle arrest, alongside reactive oxygen species (ROS) production. Eupatorin has been shown to impact inflammatory mediators and calcium signaling pathways, making it relevant for research in breast cancer, hypertension, and leukemia. Metabolized by CYP1A1 and other CYP1 enzymes, Eupatorin yields bioactive metabolites that maintain antiproliferative properties. -
ICMT Inhibitor
UCM-1336 is a potent inhibitor of Isoprenylcysteine Carboxyl Methyltransferase (ICMT), exhibiting an IC50 of 2 μM. This compound effectively induces mislocalization of endogenous Ras, resulting in decreased Ras activation. UCM-1336 has shown the ability to trigger cell death through autophagy and apoptosis, making it a valuable tool for research in cancer biology and signal transduction pathways. -
Histamine Inhibitor
Spinacetin is a natural compound derived from Inula japonica that acts as a histamine inhibitor. It effectively inhibits histamine release, demonstrating notable anti-inflammatory properties. This reagent is valuable for research applications focused on allergic responses, inflammation studies, and the elucidation of histamine-related pathways. -
Histamine Receptor Inhibitor
Quinotolast sodium is a histamine receptor inhibitor that effectively blocks the release of histamine, LTC4, and PGD2 in a concentration-dependent manner within the range of 1-100 μg/mL. This compound is valuable for research applications focused on allergic responses and inflammatory processes, as it helps elucidate the mechanisms of histamine signaling and associated pathophysiologies. -
CXCR-4 Inhibitor
SSB-2548 is a selective inhibitor of the chemokine receptor CXCR-4. It has demonstrated significant efficacy in inhibiting the proliferation and migration of acute myeloid leukemia cells, while also promoting apoptosis. Its favorable gastrointestinal absorption profile makes SSB-2548 a valuable tool for investigating the underlying mechanisms of leukemia and exploring potential therapeutic interventions. -
Platelet Aggregation Inhibitor
2'-Hydroxyflavanone is a flavanone that functions as a platelet aggregation inhibitor. It demonstrates significant bioactivity by inhibiting platelet aggregation induced by arachidonic acid and adenosine diphosphate, with IC50 values of 47.8 μM and 147.2 μM, respectively. Additionally, 2'-hydroxyflavanone has been implicated in inhibiting cancer cell proliferation and inducing apoptosis, making it valuable for research in cancer and inflammatory pathways. -
Noradrenergic Reuptake Inhibitor
Maprotiline is a selective noradrenergic reuptake inhibitor that exhibits significant antidepressant activity and also shows promise in antitumor and neuropathic pain relief. It facilitates cancer cell apoptosis through modulation of the ERK signaling pathway and interaction with cellular retinoic acid-binding protein 1 (CRABP1). This compound is valuable for research in mental health disorders, oncology, and pain management. -
LPAAT-β Inhibitor
CT 32228 is an inhibitor of lysophosphatidic acid acyltransferase-β (LPAAT-β), showing significant inhibition of tumor cell growth. It exhibits IC50 values in the range of 0.1-0.8 μM across various leukemia cell lines and effectively induces caspase activation in DHL-4 and Ramos cells. In combination with Rituximab, CT 32228 promotes apoptosis and demonstrates a 50% growth delay in xenograft models. This reagent is suitable for research applications targeting acute leukemia. -
Platelet Aggregation Inhibitor
Ergosta-7,22-dien-3-one functions as a platelet aggregation inhibitor, derived from the fruiting bodies of Ganoderma lucidum. This compound is known to enhance nitric oxide production and promote the expression of specific genes alongside the synthesis of Toll-like receptors (TLRs), cytokines, chemokines, and cellular adhesion molecules in vitro. Ergosta-7,22-dien-3-one is valuable for research in hematology, inflammation, and cellular signaling pathways. -
Platelet Aggregation Inhibitor
5(S),15(S)-DiHETE is a platelet aggregation inhibitor that functions as an activated intermediate in the biosynthesis of specialized pro-resolving mediators. With an IC50 of 1.3 μM, it effectively reduces platelet aggregation. Additionally, 5(S),15(S)-DiHETE enhances the rate of biosynthesis for lipoxins A4 (LXA4) and B4 (LXB4), making it valuable for research applications in inflammation and resolution processes. -
βH Inhibitor AND H1 Receptor Antagonist
Desmethylastemizole is a β-hematin (βH) inhibitor and a Histamine H1 receptor antagonist. It exhibits potent antiplasmodium activity against Plasmodium falciparum, with IC50 values of 0.12, 0.11, and 0.06 μM for the Pf3D7, PfDd2, and PfItG strains, respectively. Additionally, Desmethylastemizole effectively blocks hERG K+ channels and inhibits histone-lysine N-methyltransferase EZH2 activity. This compound is relevant for research in long QT syndrome and malaria. -
Histamine H1 Receptor Antagonist/5-Lipoxygenase Inhibitor
UCB-35440 is an orally active antagonist of the histamine H1 receptor and a selective inhibitor of 5-lipoxygenase. It demonstrates significant inhibition of leukotriene B4 (LTB4) formation in human whole blood, as well as a reduction in polymorphonuclear cell infiltration in mouse models. UCB-35440 also effectively inhibits histamine-induced bronchoconstriction and alleviates skin inflammation in guinea pig studies. This compound is suitable for research applications related to asthma and inflammatory skin conditions.
