Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
CRTh2 Receptor Antagonist
AZ-11665362 is a selective antagonist of the CRTh2 (DP2) receptor, exhibiting a potent IC50 of 2.6 nM. While it demonstrates slight activity towards aldose reductase and the serotonin transporter, it shows negligible inhibition of COX-1 and COX-2 enzymes. This compound is primarily utilized in research focused on asthma and other inflammatory diseases, providing valuable insights into therapeutic pathways targeting eosinophilic inflammation. -
Dopamine-mimetic Probe
DAyne is a dopamine-mimetic probe that covalently interacts with proteins modified by dopamine oxidation products, such as dopaquinone, to create stable adducts. This compound is valuable for investigating the biochemical mechanisms underlying Parkinson’s disease, focusing on neurotoxicity and the modification of proteins. Its applications extend to exploring pathways affected by dopamine dysregulation, including endoplasmic reticulum stress and cytoskeletal instability. -
Glucagon-binding Fluorescent Probe
BD-105 is a glucagon-binding fluorescent probe with a dissociation constant (Ka) of 13.3 μM. This reagent displays significant changes in fluorescence intensity upon binding to glucagon, enabling the visualization of glucagon-secreting cells in various biological contexts. BD-105 selectively labels these cells while avoiding staining of insulin-secreting and non-endocrine control cells. It is an invaluable tool for imaging glucagon in live cells and tissues, facilitating studies in metabolic regulation and endocrine functions. -
Sigma Receptor Antagonist
NE-100 hydrochloride is a selective antagonist of the sigma-1 receptor, exhibiting an IC50 value of 4.16 nM. This compound demonstrates significant neuroprotective effects and has been shown to improve cognitive impairment, making it valuable in studies related to neurodegenerative disorders and psychiatric conditions. NE-100 hydrochloride is a useful tool for investigating the role of sigma receptors in the nervous system. -
Stable Isotope
Fluphenazine-d8 is a deuterium-labeled derivative of fluphenazine, functioning primarily as a dopamine receptor antagonist. It effectively inhibits postsynaptic dopamine-2 receptors in key neural pathways, including the mesolimbic, nigrostriatal, and tuberoinfundibular systems. This reagent is valuable in research areas such as psychosis and diabetic peripheral neuropathy, and it has shown potential in studies related to SARS-CoV-2 inhibition. Fluphenazine-d8 serves as a useful tool for elucidating the pharmacodynamics of dopaminergic activity and its downstream effects. -
Dopamine Receptor Antagonist
Fluphenazine hydrochloride functions as a potent dopamine receptor antagonist, primarily targeting postsynaptic dopamine-2 receptors within mesolimbic, nigrostriatal, and tuberoinfundibular pathways. This compound exhibits significant biological activity by blocking neuronal voltage-gated sodium channels, leading to effects on behavior, such as the antagonism of methylphenidate-induced stereotyped gnawing and inhibition of climbing behavior in murine models. Fluphenazine hydrochloride is valuable for research into psychotic disorders and painful peripheral neuropathy related to diabetes, and it has demonstrated potential for inhibition of SARS-CoV-2. -
Dopamine Receptor Antagonist
Fluphenazine dimaleate is a potent dopamine receptor antagonist primarily targeting postsynaptic dopamine-2 receptors in the mesolimbic, nigrostriatal, and tuberoinfundibular pathways. Its ability to antagonize neuronal voltage-gated sodium channels contributes to its effectiveness in modulating dopaminergic activity. Fluphenazine dimaleate is valuable in research addressing psychosis, diabetic neuropathy, and behavioral studies, including the inhibition of Methylphenidate-induced stereotyped behaviors in animal models. Emerging studies also suggest its potential in inhibiting SARS-CoV-2, positioning it as a multifaceted tool in scientific investigation. -
Dopamine Receptor Agonist
Mergocriptine is a dopamine receptor agonist that has been identified as a ligand for the SARS-CoV-2 main protease (Mpro). This compound plays a significant role in modulating ambulatory activity and may be utilized in research focused on neurological disorders and viral pathogenesis. Its dual action positions it as a valuable tool in studying dopamine-related pathways and potential antiviral mechanisms. -
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. -
NMDA Receptor Antagonist
Ifenprodil is a noncompetitive antagonist of the NMDA receptor, with a strong affinity for the NR1A/NR2B subunit (IC50 = 0.34 μM) compared to NR1A/NR2A (IC50 = 146 μM). This compound also acts as an α1 adrenergic receptor antagonist and inhibits GIRK channels, reducing basal inward currents. Additionally, Ifenprodil demonstrates antiviral activity against A/H1N1 strains (EC50 = 6.6 µM) and possesses neuroprotective, anticonvulsant, and antinociceptive properties. It is suitable for research in cerebrovascular diseases and peripheral arterial obliterative disease. -
GPCRs/Adenosine Modulator
SCH-202676 is an allosteric modulator of G protein-coupled receptors (GPCRs), specifically targeting adenosine receptors (AR). This compound exhibits antiviral properties and effectively inhibits the 3CLpro enzyme in a time-dependent manner, with an IC50 value of 0.655 µM. SCH-202676 is valuable for research applications focusing on GPCR signaling pathways and the development of antiviral therapeutic strategies. -
CXCR4 Antagonist
Mavorixafor trihydrochloride is a potent and selective antagonist of the CXCR4 receptor, exhibiting an IC50 of 13 nM in inhibiting CXCR4 125I-SDF binding. This compound has demonstrated significant antiviral activity by inhibiting the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs, with IC50 values of 1 nM and 9 nM, respectively. Mavorixafor trihydrochloride is applicable in research studying WHIM syndrome and various CXCR4-related biological processes. -
CCR7 and CXCR2 Antagonist
Cosalane is a dual antagonist of the chemokine receptors CCR7 (IC50 = 2.43 μM) and CXCR2 (IC50 = 0.66 μM). This compound effectively inhibits HIV replication across a variety of strains, including HIV-1, HIV-2, Rauscher murine leukemia virus, as well as herpes simplex viruses HSV-1 and HSV-2, and human cytomegalovirus. Cosalane disrupts the interaction between gp120 and CD4, inhibiting signaling downstream of CCR7 in response to its ligands CCL19 and CCL21. Research applications include studies on HIV and the potential modulation of acute graft-versus-host disease in allogeneic hematopoietic stem cell transplantation. -
CXCR4 Antagonist
TC14012 is a peptidomimetic antagonist targeting the chemokine receptor CXCR4, exhibiting a high level of selectivity with an IC50 of 19.3 nM. In addition, TC14012 acts as a potent agonist for CXCR7, demonstrating an EC50 of 350 nM in β-arrestin 2 recruitment assays. This compound is utilized in research focused on HIV and cancer therapy, showcasing its potential in modulating chemokine signaling pathways. -
CXCR4 Antagonist
FC131 TFA is a potent CXCR4 antagonist that effectively inhibits the binding of [125I]-SDF-1 to CXCR4, demonstrating an IC50 value of 4.5 nM. This compound exhibits significant anti-HIV activity, making it a valuable tool for research in HIV treatment and other CXCR4-related studies. Its ability to disrupt CXCR4 signaling can be explored in various biological contexts, including cancer metastasis and immune response regulation. -
CXCR4 Antagonist
AMD 3465 is a potent antagonist of the CXCR4 chemokine receptor. It effectively inhibits the binding of both the 12G5 monoclonal antibody and CXCL12AF647 to CXCR4, demonstrating IC50 values of 0.75 nM and 18 nM in SupT1 cells, respectively. Additionally, AMD 3465 significantly impedes the replication of X4-tropic HIV strains, with IC50 values ranging from 1 to 10 nM, while showing no activity against CCR5-using (R5) viruses. This compound is suitable for research applications focusing on HIV treatment and CXCR4-related signaling pathways. -
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. -
CXCR4 Antagonist
KRH-3955 hydrochloride is a potent CXCR4 antagonist that effectively inhibits the binding of SDF-1α to CXCR4 with an IC50 of 0.61 nM. This compound demonstrates strong selectivity and efficacy against X4 HIV-1, with an EC50 ranging from 0.3 to 1.0 nM. KRH-3955 hydrochloride is suitable for research applications focused on HIV-1 pathogenesis and CXCR4-related signaling pathways. -
CXCR4 Antagonist
FC131 is a potent antagonist of the CXCR4 chemokine receptor. It effectively inhibits the binding of [125I]-SDF-1 to CXCR4 with an IC50 value of 4.5 nM. Due to its mechanism of action, FC131 demonstrates significant anti-HIV activity, making it a valuable tool for research into HIV pathogenesis and potential therapeutic interventions. -
Stable Isotope
Plerixafor-d4 is a deuterated derivative of Plerixafor, a selective antagonist of the CXCR4 receptor with an IC50 of 44 nM. This compound serves as an immunostimulant and is known for its ability to mobilize hematopoietic stem cells (HSCs). Additionally, Plerixafor has demonstrated efficacy in inhibiting HIV-1 and HIV-2 replication, with an EC50 ranging from 1 to 10 nM. Plerixafor-d4 is useful in research applications requiring stable isotopes for tracking and quantification purposes. -
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. -
CXCR4 Antagonist
CXCR4 antagonist 7 is a potent CXCR4 antagonist with an IC50 of 9.3 nM. It effectively inhibits CXCR4 receptor activity, making it a valuable tool in the investigation of HIV infection, inflammatory diseases, cancer, and WHIM syndrome. This compound provides essential insights into the roles of CXCR4 signaling in various pathological conditions. -
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. -
Adenosine Analog
N6-Benzoyl-7'-O-DMT-morpholino adenine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits notable biological activities, including smooth muscle vasodilation and the potential inhibition of cancer progression. It is commonly utilized in research applications related to cardiovascular studies and cancer therapeutics, contributing valuable insights into adenosine signaling and its effects on physiological processes. -
Adenosine Analog
2-Cyanomethylthioadenosine is an adenosine analog that primarily targets adenosine receptors. This compound demonstrates potent vasodilatory effects on smooth muscle tissue and has shown potential in inhibiting cancer progression. It serves as a valuable tool in research applications focusing on vascular biology and cancer therapeutics. -
Adenosine Analog
3’-β-C-Ethynyladenosine is an adenosine analog that primarily targets adenosine receptors. It exhibits smooth muscle vasodilatory effects and has been implicated in the inhibition of cancer progression. Additionally, this compound serves as a click chemistry reagent, featuring an alkyne group that allows it to undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating bioconjugation applications in chemical biology and drug development. -
Adenosine Analog
7'-O-DMT-morpholino thymine is an adenosine analog primarily known for its role in modulating adenosine receptors. It exhibits biological activities such as smooth muscle vasodilation and may play a role in inhibiting cancer progression. This compound is valuable for research applications in cardiovascular studies and cancer biology, providing insights into cellular signaling pathways and therapeutic strategies. -
Adenosine Analog
N6,N6-Dimethyl-2’-β-C-methyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant vasodilatory effects on smooth muscle and has been implicated in inhibiting cancer progression. It serves as a valuable tool for research in cardiovascular studies and cancer biology, providing insights into the modulation of adenosine signaling pathways. -
Adenosine Analog
N6-(3-Methoxybenzyl)-2’-C-methyl adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant biological activity as a smooth muscle vasodilator and demonstrates potential anti-cancer properties. It is suitable for research applications focused on vascular biology and cancer therapeutics. -
Adenosine Analog
N6-Methyl-2’-β-C-methyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound has demonstrated vasodilatory effects on smooth muscle and exhibits potential in inhibiting cancer progression. Its unique structure allows for various research applications related to adenosine signaling pathways and therapeutic interventions. -
Adenosine Analog
5’-O-(4,4’-Dimethoxytrityl)-N6-phenoxyacetyl adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant smooth muscle vasodilatory effects and has been implicated in the inhibition of cancer progression. It is a valuable reagent for research focused on vascular biology, immunology, and oncology, facilitating investigations into the therapeutic potential of nucleotide derivatives. -
Adenosine Analog
5'-O-[Bis(4-methoxyphenyl)phenylmethyl]-adenosine is an adenosine analog that primarily acts as a smooth muscle vasodilator. This compound has demonstrated potential in inhibiting cancer progression, making it valuable for cancer research. It serves as a useful tool in studies focused on adenosine receptor modulation and vascular biology.
