Catalog No.
Product Name
Application
Product Information
Citations
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Serine Aminopeptidase
Dipeptidyl Peptidase IV, Porcine Kidney is a serine aminopeptidase that plays a vital role in glucose metabolism. This enzyme specifically hydrolyzes gastric inhibitory peptide (GIP) and glucagon-like peptide-1 (GLP-1), which are key incretins involved in insulin release regulation. Its biological activity makes it a valuable tool for research in diabetes, metabolism, and related endocrine functions. -
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. -
Stable Isotope
Doxofylline-d4 is a deuterium-labeled derivative of Doxofylline, which functions primarily as an antagonist of the adenosine A1 receptor while also inhibiting phosphodiesterase IV. This reagent is valuable for studying pharmacokinetics and metabolic pathways in research involving adenosine receptor modulation and phosphodiesterase activity. Its stable isotope labeling allows for enhanced detection and quantification in various analytical applications. -
Adenosine Receptor Antagonist
Acefylline piperazine is an adenosine receptor antagonist known for its ability to activate peptidylarginine deiminase (PAD). This xanthine derivative exhibits significant bronchodilator and cardiac stimulant properties, while also inhibiting rat lung cAMP phosphodiesterase isoenzymes. As a result, Acefylline piperazine is a valuable tool in asthma research and studies exploring pulmonary function and cardiovascular effects. -
Stable Isotope
Rimonabant-d10 is a deuterium-labeled analog of Rimonabant, a highly potent and selective antagonist of the central cannabinoid receptor (CB1) with a Ki of 1.8 nM. This compound not only exhibits strong brain penetration but also inhibits Mycobacterial membrane protein Large 3 (MMPL3). Rimonabant-d10 serves as a valuable tool for studying cannabinoid receptor signaling and the role of CB1 in various biological processes, as well as for applications in mycobacterial research. -
Cannabinoid
O,O-Dimethyl-cannabigerol primarily targets cannabinoid receptors and is derived from Cannabis sativa. It exhibits antibacterial activity against drug-resistant strains of Staphylococcus aureus, demonstrating a minimum inhibitory concentration (MIC) of 1 to 2 μg/mL. As a nonpsychoactive constituent, O,O-Dimethyl-cannabigerol is valuable for research into therapeutic applications of cannabinoids, particularly in antimicrobial studies. -
Stable Isotope
(R)-Propranolol-d7 is a deuterated derivative of (R)-Propranolol, serving as a stable isotope-labeled compound. This reagent is invaluable for pharmacokinetic studies and metabolic pathway analysis, enabling the tracking of drug metabolism and distribution in biological systems. Researchers can utilize (R)-Propranolol-d7 in studies focused on cardiovascular research, anxiety treatments, and the mechanisms of action associated with beta-adrenergic receptors. -
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. -
CCK2R Antagonist
Ceclazepide is a cholecystokinin-2 receptor (CCK2R) antagonist that serves as an orally active inhibitor of Mycobacterium abscessus. This compound effectively reduces acid secretion in rat models and demonstrates significant suppression of both wild-type and multiple subspecies of M. abscessus. Importantly, Ceclazepide inhibits the growth of M. abscessus within macrophages while maintaining cell integrity, making it a valuable tool for research into mycobacterial infections and related therapeutic strategies. -
β-Adrenoceptor Blocker
Propranolol is a non-selective β-adrenoceptor antagonist that effectively crosses the blood-brain barrier. It exhibits high affinity for both β1 and β2 adrenergic receptors, with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol has demonstrated inhibitory activity against [3H]-DHA binding in rat brain membrane preparations, with an IC50 of 12 nM. This compound is commonly employed in research related to hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy. -
Somatostatin Receptor Activator
Reltecimod is a somatostatin receptor activator that modulates the immune response by targeting the CD28/B7-2 co-stimulatory pathway. This compound exhibits protective effects against various bacterial infections, their toxins, and ionizing radiation. Reltecimod is particularly relevant for research into necrotizing soft-tissue infections (NSTIs), providing insights into therapeutic interventions and immune modulation. -
α/β Adrenergic Receptor Blocker
Primidolol is an orally active α/β Adrenergic Receptor blocker that exhibits antihypertensive properties. This compound demonstrates significant antibacterial and antioxidant activities, making it relevant in studies focused on both cardiovascular diseases and infectious processes. Its dual mechanism of action positions Primidolol as a valuable tool for research aimed at understanding the interplay between adrenergic signaling and microbial resistance. -
β2-Drenergic Receptor Agonist
Terbutaline is an orally active β2-adrenergic receptor agonist that effectively stimulates the β2-adrenergic receptors. Its primary biological activity includes bronchodilation, making it relevant for research on asthma symptoms and respiratory disorders. Terbutaline is commonly used in studies investigating the therapeutic effects of β2-agonists in pulmonary conditions. -
β2-Drenergic Receptor Agonist
Terbutaline sulfate is an orally active β2-adrenergic receptor agonist, primarily utilized in the treatment of asthma and other bronchospastic conditions. As an active metabolite of bambuterol, it promotes bronchodilation by relaxing smooth muscle in the airways. This compound is essential for research applications focused on respiratory pharmacology and the therapeutic evaluation of β2-adrenergic systems in asthma symptom management. -
Antibiotic
Kendomycin ((−)-TAN 2162) is a polyketide antibiotic primarily targeting bacterial growth inhibition. It exhibits significant antibacterial activity, particularly against methicillin-resistant Staphylococcus aureus (MRSA) with a minimum inhibitory concentration (MIC) of 5 μg/mL. In addition to its antibacterial properties, Kendomycin acts as a potent antagonist of the endothelin receptor and a calcitonin receptor agonist, highlighting its potential applications in anti-osteoporotic research. -
Endothelin Receptor Antagonist
Sulfisoxazole diethanolamine is an endothelin receptor antagonist, exhibiting IC50 values of 0.60 μM and 22 μM for endothelin receptor A and endothelin receptor B, respectively. This sulfonamide antibacterial compound, characterized by its oxazole substituent, demonstrates significant inhibition of breast cancer exosome release through the selective targeting of endothelin receptor A. Its mechanism of action holds potential for applications in cancer research and related therapeutic studies. -
5-HT2A Regulator
2-Bromo-LSD D-Tartrate is a selective 5-HT2A receptor partial agonist and competitive antagonist. It exhibits significant biological activity, displaying an EC50 of 0.81 nM for Gq dissociation and a KB of 0.18 nM, making it a valuable tool for studying serotonergic signaling pathways. Additionally, it promotes dendritogenesis and spinogenesis while effectively reversing the behavioral impacts of chronic stress in animal models, enhancing active coping behaviors. This compound is suitable for research involving neurological and behavioral studies related to serotonin modulation. -
5-HT2A/5-HT2C Receptor Agonist
DOI hydrochloride is a potent agonist of the serotonin 5-HT2A and 5-HT2C receptors, exhibiting Ki values of 0.7 nM and 2.4 nM, respectively, while also targeting the 5-HT2B receptor with a Ki of 20 nM. This compound effectively crosses the blood-brain barrier, making it valuable for neurological research. DOI hydrochloride has been shown to induce head twitches in murine models, providing insight into its psychotropic effects and facilitating the study of serotonergic signaling pathways. -
5-HT2B Agonist
BW-723C86 is a selective agonist of the 5-HT2B receptor, demonstrating significant anxiolytic-like effects. In animal models, it has been shown to induce hyperphagia and decrease grooming behavior in rats. Additionally, BW-723C86 exhibits the ability to dilate pulmonary arteries and inhibit gastric accommodation following liquid meal intake, making it a useful reagent for research into anxiety, appetite regulation, and gastrointestinal physiology. -
5-HT4 Receptor Antagonist
GR 113808 is a potent and highly selective antagonist of the 5-HT4 receptor, exhibiting a pKb of 8.8. It demonstrates substantial selectivity, being 300-fold more effective against the 5-HT4 receptor compared to 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C, and 5-HT3 receptors. This compound is widely utilized in research applications focusing on gastrointestinal motility and cognitive function related to serotonin signaling pathways. -
5-HT2B Antagonist
SB 204741 is a selective high-affinity antagonist of the 5-HT2B receptor, exhibiting a pKi value of 7.1. This compound is utilized in research exploring the role of 5-HT2B in various physiological and pathological processes. Its antagonistic properties make it valuable for studies on cardiac function, pulmonary effects, and potential therapeutic interventions in diseases related to serotonergic dysregulation. -
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. -
Dopamine Receptor Antagonist
Spiperone is a potent antagonist of dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A receptors. With its capability to enhance intracellular calcium levels and inhibit the Wnt signaling pathway, Spiperone serves as a valuable tool in the study of neurological disorders. Its role as a labeled ligand for neuroleptic receptors further underscores its utility in receptor binding studies and neurotransmitter research. This compound is particularly relevant for investigating the mechanisms underlying various neuropsychiatric conditions. -
5-HT2C Receptor Agonist
Bexicaserin is a selective agonist of the 5-HT2C receptor, primarily involved in the regulation of appetite and mood. This compound demonstrates potential therapeutic applications in the study of obesity and psychiatric disorders, such as epilepsy. Its unique mechanism of action makes it a valuable tool for researchers investigating the role of serotonin receptors in these conditions. -
5-HT Receptor Agonist
8-OH-DPAT hydrobromide is a potent and selective 5-HT1A receptor agonist with a high pIC50 of 8.19. This compound demonstrates exceptional selectivity, being nearly 1000 times more selective for the 5-HT1A subtype compared to other serotonin receptor subtypes. It is primarily utilized in neuropharmacological research to investigate serotonin-mediated signaling pathways and to explore its effects on various neurological conditions. -
5-HT1A Agonist
Gepirone is a selective 5-HT1A agonist that binds specifically to the 5-HT1A receptor binding site. Its primary biological activity includes acting as an antidepressant, making it a valuable tool in research related to anxiety and major depressive disorders. Gepirone can be utilized to explore the underlying mechanisms of these conditions and aid in the development of new therapeutic strategies. -
5-HT2A Receptor Antagonist
Lumateperone is a potent 5-HT2A receptor antagonist with a Ki of 0.54 nM, exhibiting dual action as a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM). Additionally, it modulates dopamine D1 receptors. This compound demonstrates significant antipsychotic properties and supports research in schizophrenia and bipolar depression, while also presenting potential anticancer activity. -
5-HT Receptor Agonist
2-Methyl-5-HT is a selective agonist for the 5-HT3 receptor. This compound exhibits significant biological activity, particularly in demonstrating anti-depressive-like effects in preclinical models. It is utilized in research to explore serotonergic pathways and contribute to studies on mood regulation and anxiety disorders. -
5-HT Receptor Agonist
Bretisilocin is a selective agonist for the 5-HT2A receptor and functions as a serotonin releaser. This compound demonstrates significant antidepressant activity, making it an important tool for the investigation of depression and related neuropsychiatric disorders. Its role in modulating serotonin pathways provides valuable insights into the underlying mechanisms of mood regulation and potential therapeutic approaches. -
Dopamine D1/D5 Receptor Antagonist
SKF-83566 is a selective antagonist of the D1-like dopamine receptors, specifically targeting the dopamine D1 and D5 receptors. This compound exhibits potent inhibition of the dopamine transporter (DAT) with an IC50 of 5.7 μM, and shows competitive antagonism at the vascular 5-HT2 receptor. In addition, SKF-83566 selectively inhibits adenylyl cyclase 2 (AC2) over AC1 and AC5, making it relevant for research into neurological disorders such as Parkinson's disease and studies focused on alleviating nicotine cravings. -
5-HT3 Receptor Agonist
SR 57227A is a potent, orally active selective agonist of the 5-HT3 receptor, capable of crossing the blood-brain barrier. This compound exhibits binding affinities (IC50) ranging from 2.8 to 250 nM for 5-HT3 receptor sites in rat cortical membranes and NG 108-15 cell membranes. SR 57227A is primarily utilized in research focused on neuropharmacology and has demonstrated potential anti-depressant effects. -
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-HT4 Receptor Agonist
RS 67333 hydrochloride is a selective partial agonist of the 5-HT4 receptor, demonstrating a pKi of 8.7 in guinea pig striatum. This compound exhibits lower affinities for various other receptors, including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2, and muscarinic M1-M3 receptors. RS 67333 hydrochloride is known for its neuroprotective properties, making it a valuable tool for research in Alzheimer's disease and related neurodegenerative disorders. -
5-HT Receptor Agonist
CP94253 hydrochloride is a selective agonist of the 5-HT1B receptor, demonstrating a Ki value of 2 nM in radioligand binding assays. It exhibits lower affinity for other serotonin receptor subtypes, with Ki values of 89 nM for 5-HT1A, 49 nM for 5-HT1D, 860 nM for 5-HT1C, and 1600 nM for 5-HT2. This compound is known for its central activity when administered systemically in vivo, making it valuable for research in neuropharmacology and the study of serotonin-related pathways. -
5-HT3 Agonist
m-CPBG hydrochloride is a selective agonist of the 5-HT3 receptor, influencing serotonin signaling pathways. It has demonstrated potential in research related to neurological diseases, allowing for the investigation of serotonin's role in various neurophysiological processes. This compound is valuable for studies aiming to elucidate the mechanisms underlying anxiety, depression, and other psychiatric conditions. -
D2R Agonist
UNC9994 hydrochloride is a functionally selective agonist of the dopamine D2 receptor (D2R), exhibiting β-arrestin–biased signaling and selectively activating β-arrestin recruitment. With a binding affinity of Ki 79 nM for D2R, it functions as an antagonist of Gi-mediated cAMP production and a partial agonist for D2R/β-arrestin-2 interactions. This compound demonstrates antipsychotic-like effects, making it a valuable tool for research in neuropharmacology and the study of dopamine receptor signaling pathways. -
5-HT Receptor Agonist
TCB2 is a potent agonist of the serotonin 5-HT2A receptor. It demonstrates significant activation of this receptor, crucial for mediating various psychological and physiological responses. TCB2 is utilized in research exploring the role of 5-HT2A activation in neuropsychiatric disorders and receptor signaling pathways. -
5-HT7 Receptor Antagonist
SB 258719 is a selective antagonist of the 5-HT7 receptor, exhibiting a high affinity with a pKi value of 7.5. This compound demonstrates significant potential in the research of various neurological disorders and cancer. Its targeted mechanism allows for the exploration of 5-HT7 receptor signaling pathways, contributing to a deeper understanding of their role in these diseases. -
5-HT2C Receptor Agonist
(Rac)-WAY-161503 is a selective agonist of the 5-HT2C receptor, exhibiting a Ki of 4 nM and an EC50 of 12 nM. This compound demonstrates significantly higher affinity for the 5-HT2C receptor compared to the 5-HT2A and 5-HT2B receptors. Due to its biological activity, (Rac)-WAY-161503 is valuable for research applications aimed at understanding obesity and depressive disorders. -
5-HT2C Receptor Antagonist
RS-102221 hydrochloride is a selective antagonist of the 5-HT2C receptor, exhibiting a Ki value of 10 nM. This compound demonstrates approximately 100-fold selectivity over the 5-HT2A and 5-HT2B receptors. RS-102221 hydrochloride has been shown to stimulate the differentiation of new nerve cells and is associated with increased food intake and weight gain in rodent models, making it a useful tool for research in neurobiology and appetite regulation. -
5HT4 Agonist
Mosapride is a selective 5HT4 agonist known for its gastroenterokinetic properties. This compound enhances gastrointestinal motility and is used in research related to gastrointestinal diseases. Additionally, Mosapride acts as a CYP inducer and exhibits a concentration-dependent inhibitory effect on Kv4.3 with an IC50 value of 15.2 μM. Its pharmacological profile makes it a valuable tool for investigating gut-related disorders. -
Dopamine D3 Receptor Antagonist
SB-277011 hydrochloride is a selective antagonist of the dopamine D3 receptor (D3R), demonstrating potent inhibition with Ki values of 10.7 nM in rodents and 11.2 nM in humans. This compound exhibits significant selectivity, with an 80- to 100-fold preference for D3R over other dopamine receptors, including D2, 5-HT1B, and 5-HT1D. Due to its ability to penetrate the brain and oral bioavailability, SB-277011 hydrochloride is valuable in research investigating the role of D3R in various neurological and psychiatric disorders. -
Dopamine/5-HT2A Antagonist
Paliperidone palmitate is a competitive antagonist of dopamine D2 and 5-hydroxytryptamine 2A (5-HT2A) receptors with the capability to cross the blood-brain barrier. By binding to these receptors, it modulates the activity of dopamine and serotonin, thereby exerting antipsychotic effects. This compound is primarily utilized in research related to schizophrenia and other neuropsychiatric disorders, contributing to the understanding of antipsychotic mechanisms and therapeutic strategies.
