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Catalog No.
Product Name
Application
Product Information
Citations
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5-HT Transporter Inhibitor
LY393558 is a potent, orally active inhibitor of the serotonin transporter (5-HT transporter) and an antagonist of the 5-HT1B and 5-HT1D receptors. This compound significantly increases extracellular serotonin levels in the frontal cortex of mouse models. LY393558 is valuable for research focused on depression and related serotonin modulation studies. -
MAO-A/5-HT2AR Inhibitor
MAO-A/5-HT2AR-IN-1 is a potent dual inhibitor of monoamine oxidase A (MAO-A) and serotonin receptor 2A (5-HT2AR), exhibiting IC50 values of 0.004 μM and 0.014 μM, respectively. This compound demonstrates significant potential in the field of antidepressant research, contributing to the modulation of serotonin levels and receptor activity. It is a valuable tool for investigating the pharmacological impact of MAO-A and 5-HT2AR inhibition in neuropsychiatric disorders. -
5-HT Receptor Inhibitor
Mirtazapine-d3 is a deuterated form of Mirtazapine, functioning primarily as a 5-HT receptor inhibitor. This compound exhibits potent noradrenergic and specific serotonergic antidepressant activity by selectively blocking 5-HT2 and 5-HT3 receptors. Mirtazapine-d3 is valuable for pharmacokinetic studies, metabolic profiling, and research into serotonergic modulation in neuropharmacology. -
5-HT Receptor Inhibitor
Strictosidinic acid is a glycoside indole monoterpene alkaloid that functions as a 5-HT receptor inhibitor. It acts by inhibiting precursor enzymes involved in the biosynthesis of serotonin (5-HT), subsequently reducing overall serotonin levels. This compound demonstrates significant peripheral analgesic and antipyretic effects in murine models, making it a valuable tool for researchers studying pain mechanisms and serotonin modulation. -
α2-adrenoceptor Antagonist/5-HT Receptor re-uptake Inhibitor
Napamezole (hydrochloride) functions as an α2-adrenoceptor antagonist and a serotonin (5-HT) reuptake inhibitor, exhibiting Ki values of 28 nM and 93 nM for rat α2 and α1 adrenergic receptors, respectively. This compound is particularly relevant for research into depression and related neuropsychiatric disorders, facilitating studies on serotonin modulation and adrenergic signaling pathways. Its dual action can provide insights into the mechanisms underlying mood regulation and therapeutic interventions. -
Dopamine D2/D3/5-HT7 Receptor Inhibitor
LB-102 is an orally bioavailable inhibitor of dopamine D2, D3, and 5-HT7 receptors. It exhibits significant antagonistic activity, making it a valuable tool for investigating the neurochemical pathways involved in schizophrenia and other psychiatric disorders. This compound is useful for studies aimed at understanding the role of these receptors in various neuropsychiatric conditions. -
PKC Inhibitor
NA 0345 is a potent protein kinase C (PKC) inhibitor, exhibiting IC50 values of 70 nM in the presence of 12-O-tetradecanoyl-13-acetate and 110 nM in its absence. This compound selectively inhibits PKC activity, effectively reducing the positive inotropic effects associated with α1-adrenergic receptors. NA 0345 is useful in research applications aimed at elucidating the role of PKC in cardiovascular function and signal transduction pathways. -
Protein Kinase C Inhibitor/LTD4 Antagonist
LY 170198 is a potent protein kinase C inhibitor and LTD4 antagonist. This compound exhibits significant biological activity relevant to studies on tumor promotion, oncogene activation, and protein phosphorylation. Additionally, it is valuable for investigating feedback mechanisms in signal transduction pathways and cellular responses to growth factors, making it a useful tool for cancer research and related fields. -
PAD4 Inhibitor
JBI-589 is a non-covalent inhibitor selectively targeting the PAD4 isoform. This compound effectively reduces CXCR2 expression and inhibits neutrophil chemotaxis, making it instrumental in the study of inflammatory processes. JBI-589 demonstrates potential in diminishing primary tumors and metastases while enhancing the efficacy of checkpoint inhibitors. It is suitable for various applications in cancer research. -
HK Inhibitor
Antibacterial agent 241 is a histidine kinase (HK) inhibitor with IC50 values of 14 μM for CckA and 238 μM for PhoQ. It demonstrates moderate antibacterial activity against various bacterial strains, including E. coli DC2, Bacillus cereus, and Bacillus subtilis, with minimum inhibitory concentration (MIC) values ranging from 12 to 74 μg/mL. This compound is suitable for research applications targeting bacterial signaling pathways and antibiotic resistance mechanisms. -
5-HT Reuptake Inhibitor
Mesembrine, also known as (+)-Mesembrine, is a potent inhibitor of the 5-HT transporter with a Ki value of 1.4 nM. This alkaloid, characterized by its aryloctahydroindole structure, also inhibits phosphodiesterase 4B (PDE4B) with an IC50 of 7.8 μM. Due to its selective targeting of serotonin reuptake, Mesembrine is valuable for studies related to mood regulation and various neuropsychiatric disorders, as well as investigations into PDE4B's role in inflammatory processes. -
β₂-adrenergic receptor Agonist/PDE4 Inhibitor
GS-5759 is a dual-action compound functioning as a β₂-adrenergic receptor agonist and a phosphodiesterase 4 (PDE4) inhibitor. By activating the β₂ receptor, GS-5759 elevates intracellular cAMP levels, resulting in bronchial dilation. Additionally, its inhibition of PDE4 activity decreases cAMP degradation, thereby enhancing anti-inflammatory responses. This compound is relevant for research into respiratory disorders, particularly chronic obstructive pulmonary disease (COPD), demonstrating significant bronchodilatory and anti-inflammatory effects in preclinical models. -
LPA Antagonist/ATX Inhibitor
BrP-LPA is a potent lysophosphatidic acid (LPA) antagonist and autotoxin (ATX) inhibitor. It exhibits broad-spectrum antagonism against LPA receptors LPA1-4, resulting in decreased blood vessel density and reduced anxiety-like behaviors. Additionally, BrP-LPA demonstrates significant anticancer activity, effectively inhibiting cell proliferation in breast, colon, and lung cancer models. This compound is valuable for research focused on cancer biology and vasculature modulation. -
hA2A AR/hCA XII Inhibitor
hA2A/hCA XII modulator 1 is a potent inhibitor of the human A2A adenosine receptor (hA2AAR) and human carbonic anhydrase XII (hCA XII). It demonstrates high affinity with IC50 values of 6.4 nM for hA2AAR and 6.2 nM for hCA XII, while exhibiting selectivity against other adenosine receptor subtypes and carbonic anhydrases. This compound is valuable for cancer research, particularly in studies related to tumor microenvironment modulation and metabolic pathways involving adenosine signaling and carbonic anhydrase activity. -
DPP-IV Inhibitor
AGFAGDDAPR is a competitive and orally active inhibitor of dipeptidyl peptidase-IV (DPP-IV). By inhibiting DPP-IV, AGFAGDDAPR increases levels of glucagon-like peptide-1 (GLP-1), which stimulates insulin secretion, enhances β-cell function, and suppresses excessive α-cell proliferation, resulting in beneficial anti-diabetic effects. This peptide is suitable for investigating mechanisms and therapeutic approaches related to type 2 diabetes. -
DPPIV Inhibitor
K579 is a potent dipeptidyl peptidase IV (DPPIV) inhibitor that exhibits oral bioactivity. This compound effectively mitigates blood glucose elevation by increasing plasma insulin levels and enhancing the active forms of glucagon-like peptide-1 (GLP-1). K579 is suitable for research applications focused on diabetes and glucose metabolism regulation. -
DPP-4 Inhibitor
(2S,4R)-Teneligliptin is a selective inhibitor of dipeptidyl peptidase IV (DPP-4). By enhancing the plasma concentration of active glucagon-like peptide-1 (GLP-1), it promotes insulin secretion in response to elevated blood glucose levels, demonstrating significant hypoglycemic activity. This compound holds promise for research applications focused on type 2 diabetes management and related metabolic disorders. -
Dipeptidyl Peptidase Inhibitor
Retagliptin hydrochloride is an effective inhibitor of dipeptidyl peptidase-4 (DPP-4), a key enzyme in glucose metabolism. This compound enhances glycemic control in type 2 diabetes by prolonging the action of incretin hormones, including glucagon-like peptide-1 (GLP-1). It is utilized in research applications focused on metabolic disorders and the regulation of insulin secretion. -
DPP4 Inhibitor
Cetagliptin is an orally active dipeptidyl peptidase 4 (DPP-4) inhibitor that also engages CYP2D6 with an IC50 value of 6 µM. By inhibiting DPP-4, cetagliptin effectively reduces the degradation of glucagon-like peptide-1 (GLP-1), contributing to the regulation of postprandial blood glucose levels. This compound is primarily utilized in type 2 diabetes mellitus research, making it a valuable tool for studying glucose homeostasis and metabolic responses. -
DPP-4 Inhibitor
DPP-4-IN-18 is a potent and selective Dipeptidyl Peptidase-4 (DPP-4) inhibitor with an IC50 of 27 nM. By inhibiting DPP-4, this compound prevents the degradation of glucagon-like peptide 1 (GLP-1), leading to increased levels of active GLP-1. DPP-4-IN-18 is primarily utilized in research focused on type 2 diabetes and related metabolic disorders. -
DPP-IV Inhibitor
Gosogliptin hydrochloride is a selective, competitive inhibitor of DPP-IV, an enzyme crucial for the degradation of incretin peptides such as GLP-1 and glucose-dependent insulinotropic polypeptide. This compound exhibits rapid and reversible inhibition of plasma DPP-4 activity, leading to enhanced insulin secretion and improved glucose tolerance. Gosogliptin hydrochloride is primarily utilized in research focused on diabetes and metabolic disorders, providing valuable insights into glucose regulation and insulin dynamics. -
DPP-4 Inhibitor
DPP-4-IN-10 is a potent DPP-4 inhibitor that acts to prevent the degradation of glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP). By inhibiting DPP-4, this compound may enhance glycemic control in individuals with type 2 diabetes mellitus (T2DM). Its oral bioavailability makes it suitable for pharmacological studies focused on glucose metabolism and diabetes management. -
DPP-IV Inhibitor
ASP8497 is a competitive inhibitor of dipeptidyl peptidase IV (DPP-IV), which plays a critical role in glucose metabolism. This compound effectively reduces blood glucose levels and elevates plasma active GLP-1 and insulin concentrations without inducing hypoglycemia in fasted normal mice. ASP8497 is suitable for research applications focused on antihyperglycemic mechanisms and glucose regulation. -
DPP-IV Inhibitor
Carmegliptin is a potent and orally active DPP-IV inhibitor, demonstrating an IC50 value of 6.8 nM for human DPP-IV. By binding to the S1 pocket of DPP-IV, it effectively inhibits the degradation of GLP-1, leading to increased plasma insulin levels, improved glucose tolerance, and alleviation of hyperglycemia. Carmegliptin serves as a substrate for human P-glycoprotein without inhibiting the transporter, exhibiting low in vitro cell permeability. This compound is valuable for research focused on type 2 diabetes and non-insulin-dependent diabetes mellitus. -
DPP-4 Inhibitor
16-Hydroxycleroda-3,13-dien-15,16-olide is a potent dipeptidyl peptidase 4 (DPP-4) inhibitor, targeting the serine protease class of enzymes. This clerodane diterpene demonstrates key biological activities, including the down-regulation of lipopolysaccharide (LPS)-induced ERK phosphorylation in myocytes and inhibition of glucagon-like peptide-1 (GLP-1) induced protein kinase A (PKA) expression. Additionally, it exhibits hypolipidemic, hepatoprotective, and hypoglycemic effects, making it a valuable compound for research in metabolic and cardiovascular diseases. -
DPP-IV Inhibitor
Carmegliptin hydrochloride is a potent DPP-IV inhibitor, exhibiting a human DPP-IV IC50 of 6.8 nM. By binding to the S1 pocket of DPP-IV, it prevents the degradation of GLP-1, leading to increased plasma insulin levels, improved glucose tolerance, and relief from hyperglycemia. This compound can serve as a valuable reagent for research into type 2 diabetes and non-insulin-dependent diabetes mellitus, providing insights into GLP-1 modulation and its effects on metabolic regulation. -
DPP-IV Inhibitor
TS-021 is a selective, orally active, reversible DPP-IV inhibitor with long-lasting effects. It demonstrates significant selectivity against DPP-8 and DPP-9, exceeding 600-fold and 1,200-fold, respectively, as well as a greater than 15,000-fold selectivity over other peptidases. With an IC50 value of 5.34 nM for DPP-IV inhibition in human plasma, TS-021 is effective in enhancing active GLP-1 levels and exhibits potent antihyperglycemic activity, making it valuable for research in diabetes and metabolic disorders. -
HIV Inhibitor
Schisantherin D is a dibenzocyclooctadiene lignan that exhibits significant anti-HIV activity with an EC50 of 0.5 μg/mL. This compound selectively inhibits endothelin receptor B (ETBR) and demonstrates hepatoprotective properties. Schisantherin D is valuable for research applications focused on HIV replication and the exploration of liver protective mechanisms. -
HIV-1 Entry Inhibitor
RPR103611 is a derivative of betulinic acid that functions as a potent HIV-1 entry inhibitor. It displays IC50 values of 80 nM for CCR5-tropic virus YU2, 0.27 nM for CXCR4-tropic virus NL4-3, and 0.17 nM for dual tropic virus 89.6. This compound is valuable for research focused on the mechanisms of HIV-1 entry and the development of antiviral therapies. -
CXCR Inhibitor
AMD 3329 octahydrobromide is a potent CXCR4 inhibitor that effectively reduces HIV-1 and HIV-2 viral replication. It demonstrates exceptional antiviral activity with EC50 values of 0.8 nM and 1.6 nM, surpassing the efficacy of related compounds. Additionally, AMD 3329 significantly obstructs the binding of specific CXCR4 monoclonal antibodies and inhibits SDF-1 alpha-induced Ca(2+) influx. This compound also disrupts virus-induced syncytium formation, with an EC50 of 12 nM, making it a valuable tool for HIV research and therapeutic development. -
Dopamine Receptor Inhibitor
7-Hydroxy-DPAT hydrobromide is a selective agonist for the D3 dopamine receptor, primarily impacting dopamine signaling pathways. This compound demonstrates significant biological activity in modulating locomotor behavior and influencing dopamine metabolism within the central nervous system. It serves as a valuable tool for research applications related to neuropharmacology and the study of dopamine-related disorders. -
Dopamine Receptor Inhibitor
GBR 12783 is a selective dopamine uptake inhibitor that targets dopamine receptors with high potency. It effectively inhibits [3H]dopamine uptake in striatal synaptosomes from rats and mice, exhibiting IC50 values of 1.8 nM and 1.2 nM, respectively. This compound has been shown to enhance memory performance and increase hippocampal acetylcholine release in rodent models, making it valuable for research in neuropharmacology and cognitive function studies. -
Dopamine Receptor Inhibitor
Cyclo(glycyl-L-leucyl) is a neuropeptide that specifically inhibits dopamine receptors, playing a crucial role in modulating dopaminergic signaling. This compound has been shown to down-regulate dopamine receptor activity and reduce dopaminergic supersensitivity, particularly in the context of morphine-induced analgesia in animal models. Cyclo(glycyl-L-leucyl) holds promise for potential therapeutic applications in preventing tardive dyskinesias and L-DOPA-induced dyskinesias, making it valuable for research in neuropharmacology and movement disorders. -
Dopamine Receptor Inhibitor
Fosopamine hydrochloride is a dopamine receptor D agonist, primarily targeting the dopamine receptor pathways. It has demonstrated significant utility in research related to hypertension, aiding in the exploration of cardiovascular mechanisms and blood pressure regulation. This compound may provide insights into both the physiological and pathological roles of dopamine signaling in hypertension-related studies. -
Dopamine Receptor Inhibitor
PD 128907 is a selective dopamine D3 receptor inhibitor that effectively modulates dopaminergic signaling. The active (+) enantiomer exhibits high affinity for rat D3 receptors and demonstrates significant inhibitory effects on neuronal firing in the ventral tegmental area and substantia nigra pars compacta, with EC50 values of 33 nM and 38 nM, respectively. Additionally, it inhibits dopamine release in the caudate putamen with an EC50 of 66 nM. While PD 128907 primarily targets D3 receptors, evidence suggests its actions may also involve D2 autoreceptors, making it a valuable tool for exploring dopamine receptor pharmacology and neurobehavioral research. -
Dopamine Receptor Inhibitor
ADTN is a dopamine receptor inhibitor that modulates dopamine neurotransmission. It demonstrates the ability to reduce dopamine-related signaling, which may help target conditions associated with excessive dopamine activity. ADTN is applicable in research focused on mental health disorders and cognitive function modulation, providing insights into therapeutic strategies for related pathologies. -
Dopamine Receptor Inhibitor
Metoclopramide dihydrochloride is a dopamine D2 receptor antagonist primarily used for its antiemetic effects. It demonstrates notable activity in managing nausea and vomiting, particularly in patients undergoing chemotherapy or surgery. This compound is also employed in research settings to explore the modulation of dopaminergic pathways and gastrointestinal motility. -
Dopamine Receptor Inhibitor
Bulbocapnine hydrochloride is a potent dopamine receptor inhibitor that plays a significant role in modulating dopaminergic activity. This aporphine alkaloid is known to inhibit dopamine synthesis and exhibits neuroleptic-like properties, alongside anticonvulsant and antinociceptive effects. Its pharmacological profile makes it a valuable tool in research related to neurological disorders and the exploration of dopamine-related pathways. -
Dopamine Receptor Inhibitor
Valbenazine dihydrochloride is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2) and primarily targets dopamine receptors. It is utilized in the treatment of tardive dyskinesia, offering therapeutic benefits for alleviating movement disorder symptoms linked to chronic dopamine receptor antagonism. Extensive preclinical studies support its efficacy, particularly in relation to the genetic factors contributing to tardive dyskinesia. -
Dopamine D1/D2 Receptor Inhibitor
(Z)-Flupenthixol decanoate is a potent antagonist of dopamine D1 and D2 receptors, functioning primarily to inhibit dopaminergic signaling. This compound exhibits significant antipsychotic activity, making it valuable in the study of psychiatric disorders and neuropharmacology. Research applications include investigations into the modulation of dopaminergic pathways and the evaluation of therapeutic strategies for schizophrenia and related conditions. -
Dopamine Receptor Inhibitor
Seproxetine hydrochloride is a dopamine receptor inhibitor known for its selective serotonin reuptake inhibitory activity. By specifically blocking the serotonin uptake transporter, it increases serotonin levels in the brain, while also exhibiting significant interactions with dopamine receptors. This compound is actively researched for its potential therapeutic applications in mood disorders and associated neurological conditions, showcasing enhanced biological activity and efficacy through its ability to form stable charge transfer complexes. -
Dopamine Receptor Inhibitor
TISCH is a potent and selective iodinated ligand that targets CNS D1 dopamine receptors, demonstrating a high affinity with a Kd value of 0.205 nM in rat striatal tissue. Its ability to cross the blood-brain barrier allows for effective distribution in regions with substantial D1 receptor density, making it a valuable pharmacological tool for characterizing these receptors. Additionally, TISCH, when labeled with I-123, has potential applications as an in vivo imaging agent for studying D1 dopamine receptor function in the central nervous system. -
Dopamine Receptor Inhibitor
Opromazine hydrochloride is a dopamine receptor inhibitor known for its sedative and antiemetic effects. It primarily reduces dopaminergic activity by blocking dopamine receptors in the brain, making it useful in the treatment of psychiatric disorders such as schizophrenia and psychosis. Additionally, studies have investigated its metabolites through various microsomal enzymes, highlighting differences in formation rates and the variability of drug-metabolizing enzymes in human liver and placenta microsomes, which is essential for understanding its pharmacokinetic profile. -
Adrenergic Receptor Inhibitor
Cetamolol hydrochloride acts as a potent β1-adrenergic receptor inhibitor, exhibiting intrinsic sympathomimetic activity and cardioselectivity. It demonstrates a prolonged inhibitory effect on heart rate and myocardial contractility at low to moderate doses, making it a valuable reagent for cardiovascular research. Its unique profile allows for exploration in studies evaluating hypertension, arrhythmias, and other cardiac conditions. -
β-Adrenergic Receptor Inhibitor
Bufetolol is a selective β-adrenergic receptor inhibitor that modulates cardiac activity by decreasing the maximum rate of depolarization during action potentials. Its antiarrhythmic properties make it a valuable tool for research into the mechanisms of cardiac rhythm disorders. Bufetolol is utilized in studies aimed at exploring therapeutic strategies for arrhythmias and related cardiovascular conditions. -
Adrenergic Receptor Inhibitor
Teoprolol is a selective β-adrenergic receptor inhibitor that effectively modulates adrenergic signaling pathways. It exhibits key biological activities including the reduction of heart rate and myocardial contractility, making it valuable for cardiovascular research. Teoprolol is widely used in studies investigating hypertension, anxiety, and heart failure, contributing to our understanding of adrenergic receptor function and pharmacological interventions. -
α1/β1-Adrenergic Receptor Inhibitor
Amosulalol hydrochloride functions as a dual inhibitor of α1 and β1-adrenergic receptors, demonstrating pronounced antihypertensive effects. By inhibiting α1-adrenergic receptors, it effectively lowers blood pressure, while β1-adrenergic receptor inhibition reduces reflexive increases in heart rate and plasma renin activity. This compound is particularly useful in studies involving spontaneously hypertensive rats, providing valuable insights into cardiovascular mechanisms and potential therapeutic interventions in hypertension. -
AR Inhibitor
Amidephrine hydrochloride is an adrenergic receptor (AR) agonist that functions primarily by stimulating adrenergic signaling pathways. It demonstrates key biological activities relevant to neurological research, making it a valuable reagent for studying various neurological diseases and disorders. Its effects on AR modulation can facilitate investigations into therapeutic interventions and pharmaceutical development in the field of neuroscience. -
Adrenergic Receptor Inhibitor
Tropodifene is an α-adrenergic receptor inhibitor that modulates adrenergic signaling pathways. It is primarily utilized in research related to cardiovascular pharmacology and the study of sympathetic nervous system functions. Its unique mechanism of action makes it valuable for investigating the role of adrenergic receptors in various physiological and pathological conditions. -
Adrenergic Receptor Inhibitor
Benzquinamide is an adrenergic receptor inhibitor that selectively binds to the α2A, α2B, and α2C adrenergic receptors, exhibiting Ki values of 1,365, 691, and 545 nM, respectively. This compound demonstrates antiemetic properties and is utilized in research applications relating to nausea and vomiting. Its mechanism of action involves modulation of adrenergic signaling pathways, making it a valuable tool for studying the role of adrenergic receptors in various physiological and pathological conditions.
