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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Platelet Aggregation Inhibitor
SCH 38519 is a potent platelet aggregation inhibitor that effectively inhibits thrombin-induced aggregation of human platelets, exhibiting an IC50 of 68 μg/mL. In addition to its antiplatelet activity, SCH 38519 demonstrates antibacterial properties against both Gram-positive and Gram-negative bacteria. This compound is valuable for research applications focused on thrombosis, cardiovascular diseases, and bacterial infections. -
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 Biosynthesis Inhibitor
4-Chloro-L-phenylalanine is a potent inhibitor of serotonin (5-HT) biosynthesis, acting as a nonspecific antagonist of the tryptophan hydroxylase isoforms TPH1 and TPH2. This compound is valuable for studying serotonin-related pathways and their implications in psychiatric and neurological disorders. It serves as an important tool for researchers investigating the regulation of serotonin levels and the biochemical basis of 5-HT modulation. -
5-HT Uptake Inhibitor
Norfluoxetine hydrochloride is a potent 5-HT uptake inhibitor, serving as an active N-demethylated metabolite of Fluoxetine. It inhibits serotonin reuptake and has been shown to inhibit CaV3.3 T current with an IC50 of 5 μM. Due to its mechanism of action, Norfluoxetine hydrochloride is relevant in research focusing on mood disorders and anticonvulsant activity, providing insights into serotonin modulation and potential therapeutic applications. -
5-HT Receptor Inhibitor
Ansofaxine hydrochloride is a potent triple reuptake inhibitor that targets the serotonin, dopamine, and norepinephrine transporters. It demonstrates inhibition with IC50 values of 723 nM for serotonin, 491 nM for dopamine, and 763 nM for norepinephrine. This compound is primarily used in research to investigate the mechanisms underlying mood disorders and has potential applications in studies focused on neuropharmacology and the treatment of depression and anxiety. -
D2 Receptor Inhibitor, D3 Receptor Inhibitor, 5-HT1A Receptor Inhibitor, 5-HT2B Receptor Inhibitor
Desmethyl cariprazine is a potent inhibitor of the D2 and D3 dopamine receptors, as well as the 5-HT1A and 5-HT2B serotonin receptors. It demonstrates a pEC50 of 8.90 at D2 receptors, 8.09 at D3 receptors, and 6.28 at 5-HT1A receptors, significantly inhibiting forskolin-induced cAMP production and serotonin-induced Ca2+ release. This compound is valuable for research focused on psychiatric disorders such as schizophrenia and bipolar disorder type I. -
5-HT/SERT Inhibitor
Zimelidine dihydrochloride is a potent and selective inhibitor of serotonin uptake via the serotonin transporter (SERT). This compound exhibits significant antidepressant properties, making it valuable for research in the field of mood disorders and serotonin-related pathways. Its role in modulating serotonin levels can aid in the exploration of various neuropharmacological mechanisms. -
5-HT Receptor Inhibitor
Iprindole is a tricyclic indole compound that functions primarily as a 5-HT receptor inhibitor. It exhibits weak inhibitory effects on the reuptake of noradrenaline and serotonin (5-HT), making it relevant in the study of mood disorders and antidepressant mechanisms. This reagent is particularly useful in research applications focused on neuropharmacology and the modulation of serotonergic systems. -
NE/serotonin 5-HT Inhibitor
Ampreloxetine is a potent and orally bioavailable norepinephrine (NE) and serotonin 5-HT inhibitor. It exhibits significant potential for investigating neurogenic orthostatic hypotension and related disorders. This compound may facilitate research on neurotransmitter modulation and its effects on blood pressure regulation. -
5-HT Inhibitor
Antidepressant agent 10 is a selective 5-HT inhibitor, demonstrating IC50 values of 190 nM for 5-HT1A and 110 nM for 5-HT2. This orally active compound is valuable in the study of serotonin-related pathways and their implications in mental disorders. Researchers may utilize Antidepressant agent 10 to explore its potential effects on mood regulation and therapeutic applications in depression. -
NE/5-HT Inhibitor
Ampreloxetine TFA is a potent inhibitor of norepinephrine (NE) and serotonin (5-HT) reuptake. This compound is primarily utilized in research targeting conditions such as neurogenic orthostatic hypotension. Its selective action on neurotransmitter pathways presents valuable insights into synaptic transmission and related disorders. -
5-HT Receptor Inhibitor
Davidigenin is a selective inhibitor of the 5-HT receptor, exhibiting significant antidiabetic properties along with antitumor, antispasmodic, and antioxidant activities. This compound effectively inhibits duodenal contractions triggered by acetylcholine or histamine, making it a valuable tool for research into gastrointestinal motility and related disorders. Its multifaceted biological activities suggest potential applications in studying metabolic and gastrointestinal diseases. -
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. -
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. -
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. -
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. -
Dopamine β-hydroxylase Inhibitor
A32390A is a potent inhibitor of dopamine β-hydroxylase, functioning primarily to decrease norepinephrine synthesis. This reduction can lead to lowered blood pressure, making A32390A valuable in studies related to hypertension, particularly in models such as DOCA hypertensive rats. Additionally, the compound's properties as a copper chelator allow for exploration in the context of bacterial infections and metabolic disorders, providing versatile applications in chemical research. -
AChE/Dopamine 2 Inhibitor
Itopride is a potent dopamine D2 receptor antagonist and an acetylcholinesterase (AChE) inhibitor. Itopride enhances gastric motility through its dual mechanisms of action, promoting both antidopaminergic and anti-acetylcholinesterase effects. This compound is primarily utilized in research related to gastrointestinal disorders, particularly gastroesophageal reflux disease (GERD), offering insights into prokinetic therapies. -
CCR5/CXCR3 Inhibitor
CCR5/CXCR3-IN-1 is a potent inhibitor of the chemokine receptors CXCR3 and CCR5. This compound effectively suppresses the chemotaxis of transformed cells expressing CCR5 and CXCR3, while exhibiting no inhibitory effect on CXCR4-expressing transfected cells. CCR5/CXCR3-IN-1 is valuable for research into chronic arthritic rheumatism and other conditions where modulation of these receptors is crucial. -
Cholecystokinin Receptor Inhibitor
Gastrazole free acid is a cholecystokinin receptor antagonist that demonstrates potential in inhibiting pancreatic cancer growth. By targeting gastrin receptors, this compound plays a crucial role in the modulation of gastric functions and may aid in the investigation of therapeutic strategies for gastrointestinal malignancies. Its utility in research provides insights into receptor-mediated pathways and cancer biology. -
CCK B Inhibitor
PD-135666 is a potent dipeptide inhibitor of cholecystokinin B (CCK B) receptors, demonstrating an IC50 of 0.1 nM in mouse cerebral cortex. Unlike its enantiomer, PD-140548, which selectively targets CCK A receptors in rat pancreas, PD-135666 primarily interacts with CCK B receptors. This compound has been shown to exhibit anxiolytic effects in various animal models, making it a valuable tool for studying anxiety-related disorders and CCK receptor biology. -
Cholecystokinin Receptor Inhibitor
CCK-A receptor inhibitor 1 is a selective inhibitor of the cholecystokinin A (CCK-A) receptor, exhibiting a binding IC50 of 340 nM. By modulating CCK-A receptor activity, this compound plays a crucial role in studying gastrointestinal physiology and related disorders. Its inhibitory properties make it useful for research applications focused on appetite regulation and the gastrointestinal system. -
ELR+CXCL-CXCR1/2 Inhibitor
CXCL-CXCR1/2-IN-1 is an orally active inhibitor of the ELR+CXCL-CXCR1/2 signaling pathway, exhibiting an EC50 of 42.7 nM for the CXCR2 receptor. This compound demonstrates significant anticancer and antiangiogenic properties, making it a valuable tool for research into tumor progression and vascularization. Its ability to target these pathways underscores its potential application in cancer biology and therapeutic development. -
CXCR4 Inhibitor
CXCR4-IN-3 is a potent inhibitor of the CXCR4 receptor, demonstrating an IC50 of 3.2 nM. It exhibits significant antichemotactic effects, with an inhibition rate of 79.19±2.33%. This compound also displays anti-inflammatory properties, making it a valuable tool for research into inflammatory bowel disease (IBD) and related inflammatory conditions. -
CXCR4 Inhibitor
Peptide R is a cyclic peptide that functions as a specific antagonist of the CXCR4 receptor. It demonstrates significant efficacy in remodeling tumor stroma, making it a valuable tool for tumor research. Its ability to modulate the tumor microenvironment highlights its potential applications in cancer therapy and investigation into tumor progression mechanisms. -
CXCR4 Inhibitor
CXCR4-IN-1 is a selective inhibitor of the CXCR4 chemokine receptor, with an IC50 of 20 nM. This compound exhibits potential biological activity in modulating cellular responses associated with cancer progression, HIV infection, diabetic retinopathy, and inflammatory conditions. CXCR4-IN-1 is suitable for use in research applications focused on these disease processes, providing valuable insights into therapeutic targeting of the CXCR4 signaling pathway. -
CXCR2 Inhibitor
NVP CXCR2 20 is a selective inhibitor of the CXCR2 receptor, primarily involved in modulating pain pathways. It exhibits significant analgesic and antinociceptive effects, effectively reducing mechanical and thermal hypersensitivity in rat models of chronic constriction injury (CCI). Additionally, NVP CXCR2 20 diminishes CXCL3-induced hypersensitivity in naive mice and lowers CXCL3 protein levels in the spinal cord and dorsal root ganglia of CCI-exposed rats. This compound is valuable for research into neuropathic pain and chronic obstructive pulmonary disease (COPD). -
CXCL12 Inhibitor
4-Amino-D-phenylalanine is a potent CXCL12 inhibitor that targets the CXCR4 receptor. With an IC50 value of 0.1 μM, it effectively inhibits the binding of CXCL12 to its receptor. This compound is valuable for research applications focused on understanding CXCR4-related pathways and their implications in cancer, inflammation, and various other diseases. -
CXCR4 Inhibitor
vMIP-II (1-21) is a selective inhibitor of the chemokine receptor CXCR4. By competing with 125I-SDF-1R for binding sites, vMIP-II (1-21) effectively disrupts CXCR4 signaling, with an IC50 value of 190 nM. This compound is useful for research applications involving the study of chemokine receptors and their role in various biological processes, such as immune response and cancer metastasis. -
CXCR4 Inhibitor
TN14003 is a selective inhibitor of the CXCR4 receptor. It demonstrates significant antitumor activity by disrupting CXCR4-mediated signaling pathways, which are implicated in cancer cell survival, proliferation, and metastasis. This compound is primarily utilized in research focused on cancer treatment and understanding the role of the CXCR4 chemokine receptor in tumor progression. -
Phospholipase D Inhibitor
Halopemide is a potent inhibitor of phospholipase D (PLD), exhibiting IC50 values of 220 nM for human PLD1 and 310 nM for PLD2. In addition to its enzymatic inhibition, Halopemide functions as a dopamine receptor antagonist and exhibits psychotropic properties. This reagent is valuable for research applications exploring PLD-mediated signaling pathways and dopamine receptor interactions in various biological contexts. -
Dopamine Receptor Inhibitor
Clopenthixol is a thiaquinoline compound that acts as an antagonist of D1 and D2 dopamine receptors. It exhibits inhibitory effects comparable to those of phenothiazine antipsychotics, making it valuable in the treatment of schizophrenia and other mental disorders. This compound is primarily utilized in research related to psychiatric conditions and the exploration of dopamine regulation in the central nervous system. -
SR-2A/D2DR Inhibitor
Octoclothepin maleate salt is a dual inhibitor of the SR-2A and D2 dopamine receptors. This compound exhibits significant central depressant activity, demonstrated in various observational and instrumental studies using rodent models. Its properties make it a valuable tool in neuropharmacological research, particularly in the study of neuroleptic effects and dopaminergic signaling pathways. -
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.
