Catalog No.
Product Name
Application
Product Information
Citations
-
PPARγ Agonist
PPARγ Agonist 9 is a selective agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). This compound demonstrates significant biological activity by modulating PPARγ signaling pathways, which are critical in lipid metabolism and glucose homeostasis. It serves as a valuable tool in research applications focused on metabolic disorders, diabetes, and obesity-related studies. -
PPAR Activator
17(S)-HDHA is a pro-resolving mediator that functions as a partial activator of peroxisome proliferator-activated receptors (PPARs), specifically PPARγ, PPARα, and PPARδ. Its biological activity is linked to the resolution of inflammation and modulation of metabolic processes. This compound is utilized in research to explore the roles of PPAR activation in anti-inflammatory responses and metabolic regulation. -
Drug Metabolite
N-Desmethyl rosiglitazone is a drug metabolite resulting from the demethylation of Rosiglitazone via the cytochrome P450 enzyme system in liver microsomes. This compound exhibits partial agonist activity at the peroxisome proliferator-activated receptor gamma (PPARγ), making it valuable for research into the metabolism and pharmacokinetics of Rosiglitazone. It serves as a useful tool for examining the pharmacological effects and metabolic pathways associated with thiazolidinedione drugs. -
PPAR Agonist
PPARα/γ agonist 5 is a dual agonist targeting peroxisome proliferator-activated receptors alpha and gamma, demonstrating notable biological activity at low concentrations. With EC50 values of 0.358 μM and 1.21 μM for PPARα and PPARγ, respectively, this compound shows promise in addressing type 2 diabetes and lipid metabolism disorders. Its potent efficacy supports its potential application in clinical development for metabolic health research. -
PPARα/δ Agonist
(E/Z)-Elafibranor (also known as (E/Z)-GFT505) is a dual agonist of the peroxisome proliferator-activated receptors alpha (PPARα) and delta (PPARδ), exhibiting EC50 values of 45 nM and 175 nM, respectively. This compound plays a significant role in lipid metabolism and inflammation modulation, making it valuable for research in metabolic disorders, obesity, and non-alcoholic fatty liver disease (NAFLD). Its ability to simultaneously target multiple pathways positions (E/Z)-Elafibranor as a promising candidate for therapeutic interventions in metabolic diseases. -
PPARγ Agonist
17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid serves as a PPARγ agonist, primarily impacting inflammatory processes. This electrophilic oxo-derivative of docosahexaenoic acid (DHA) is produced in activated macrophages through a COX-2-catalyzed mechanism during inflammation. Its biological activity includes modulation of the NF-κB signaling pathway, inhibition of pro-inflammatory cytokine production, and reduction of nitric oxide synthesis, demonstrating significant anti-inflammatory properties. This compound is particularly valuable for research applications focused on inflammatory diseases and metabolic disorders. -
PPARα/PPARδ Agonist
GW 2433 is a dual agonist of peroxisome proliferator-activated receptors alpha (PPARα) and delta (PPARδ). This compound exhibits the ability to enhance fatty acid uptake and metabolism, making it relevant for research in type II diabetes and dyslipidemia. It provides valuable insights into metabolic regulation and potential therapeutic strategies for metabolic disorders. -
PPAR-α Agonist
ZINC17167211 is a potent agonist of peroxisome proliferator-activated receptor alpha (PPAR-α) with an EC50 of 0.16 nM. This compound is valuable for investigating metabolic disorders such as diabetes and hyperlipidemia, as well as inflammatory diseases. Its ability to activate PPAR-α makes it a useful tool for exploring therapeutic strategies aimed at modulating lipid metabolism and inflammation. -
PPAR-γ Inhibitor
(±)-CBCQ is a potent inhibitor of PPAR-γ, exhibiting an EC50 value of 14.7 μM. This compound is of interest in research investigating the modulation of metabolic pathways and the potential therapeutic effects in obesity and diabetes. Its ability to interact with PPAR-γ makes it a valuable tool for studying the receptor's role in gene expression and lipid metabolism. -
PPARγ Agonist
4-Oxo Docosahexaenoic Acid is a potent PPARγ agonist with notable antiproliferative properties. This compound effectively inhibits the growth of several triple-negative breast cancer cell lines, such as MDA-MB-231 and BT549, at concentrations of 50-100 μM, although it shows increased proliferation in MCF-7 cells. It covalently binds to PPARγ, activating gene transcription, as demonstrated in luciferase reporter assays and dendritic cells, with an EC50 of approximately 8-16 μM. This makes 4-Oxo DHA a valuable tool for research into cancer biology and PPARγ-associated pathways. -
PPARα/γ Agonist
TZD18 is a potent dual agonist of PPARα and PPARγ, exhibiting IC50 values of 0.028 µM and 0.057 µM, respectively, while showing minimal activity toward PPARδ (>10 µM). This compound effectively reduces plasma glucose and triglyceride levels in diabetic mouse models. TZD18 holds promise for research into type 2 diabetes and related metabolic disorders. -
PPAR Agonist
AVE-8134 is a potent agonist of the peroxisome proliferator-activated receptor alpha (PPARα). It exhibits an EC50 of 100 nM for the human PPARα receptor and 3000 nM for the rodent counterpart. This compound is used in research applications focused on metabolic regulation, lipid metabolism, and the modulation of inflammatory processes, making it a valuable tool for studies related to cardiovascular disease and metabolic disorders. -
PPAR α/γ Agonist
CAY10514 is a dual agonist of peroxisome proliferator-activated receptors α (PPARα) and γ (PPARγ), exhibiting IC50 values of 0.173 μM and 0.642 μM, respectively. This compound is derived from 8(S)-HETE and demonstrates significant biological activity in modulating metabolic processes. CAY10514 is utilized in research applications related to metabolic disorders, obesity, and insulin sensitivity. -
PPAR-α Agonist
ZINC08438472 is a selective agonist of peroxisome proliferator-activated receptor alpha (PPAR-α), demonstrating an EC50 value of 12.1 nM. This compound exhibits significant biological activity, making it a valuable tool in research focused on diabetes, hyperlipidemia, and inflammatory disorders. Its potent action on PPAR-α pathways offers potential insights into lipid metabolism and related therapeutics. -
PPARα/PPARγ Activator
GW409544 is a highly potent activator of both PPARα and PPARγ, exhibiting EC50 values of 2.3 nM and 0.28 nM, respectively. This compound plays a significant role in the regulation of lipid metabolism and glucose homeostasis. GW409544 is instrumental for research investigating mechanisms underlying metabolic disorders and cardiovascular diseases, providing insights into potential therapeutic approaches. -
PPARγ Agonist
CLX-0921 is an orally active PPARγ agonist, with an IC50 of 1.54 μM. It exhibits potent antihyperglycemic activity, making it a valuable tool for research in type 2 diabetes. This compound aids in the investigation of metabolic regulation and related therapeutic strategies in glucose homeostasis. -
PPARα Agonist
N-Octadecyl-N'-propyl-sulfamide is a selective agonist of peroxisome proliferator-activated receptor alpha (PPARα), demonstrating an EC50 of 100 nM. As an analog of oleoylethanolamide (OEA), it activates PPARα, playing a critical role in lipid and glucose metabolism. In animal models, the compound significantly reduces food intake and body weight gain, with a notable effect observed in both free-feeding Wistar rats and obese Zucker (fa/fa) rats, particularly at doses of 1 mg/kg. Additionally, a dose of 10 mg/kg administered intraperitoneally effectively inhibits appetite and lowers plasma triglyceride levels. -
PPARα Agonist
NS-220 is a potent and selective agonist of PPARα, exhibiting an EC50 value of 1.9 × 10^-8 M for PPARα, while demonstrating significantly lower affinity for PPARγ and PPARδ (9.6 × 10^-6 M and >10^-4 M, respectively). This compound is instrumental in research focused on hyperlipidemia and metabolic disorders associated with type-2 diabetes, aiding in the exploration of therapeutic strategies targeting lipid metabolism and glucose homeostasis. -
PPARα/γ/δ Agonist
PPARα/γ/δ Agonist 1 is a potent agonist of the peroxisome proliferator-activated receptors α, γ, and δ, exhibiting an IC50 of 70 nM for PPARγ. This compound is primarily utilized in research focused on type 2 diabetes, facilitating studies on metabolic regulation and potential therapeutic strategies. Its ability to activate multiple PPAR subtypes makes it a valuable tool for investigating lipid metabolism and glucose homeostasis. -
PPARgamma Activator
BM152054 is a potent PPARgamma activator that enhances insulin action and promotes glucose utilization in peripheral tissues. This compound is crucial for research focused on metabolic disorders and diabetes, offering insights into the regulatory mechanisms of lipid and glucose metabolism. Its ability to modulate PPARgamma activity makes it a valuable tool for investigating therapeutic strategies targeting insulin sensitivity and metabolic health. -
PPAR Modulator
PPARα-MO-1 is a potent modulator of peroxisome proliferator-activated receptor alpha (PPARα), contributing to lipid metabolism and glucose homeostasis. This compound has potential applications in the study of metabolic disorders, including obesity and type 2 diabetes, by regulating gene expression involved in fatty acid oxidation and inflammation. It serves as an important tool for researchers investigating the role of PPARα in metabolic pathways and therapeutic strategies. -
AhR Activator
ANI-7 is an aryl hydrocarbon receptor (AhR) activator that exhibits significant cytotoxicity against various cancer cell lines. It selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 activates the AhR pathway, leading to the induction of CYP1-metabolizing mono-oxygenases, DNA damage, kinase activation, and S-phase cell cycle arrest, ultimately resulting in cell death in sensitive breast cancer cell lines. -
JNK/CYP Inhibitor
JNK-IN-14 is a potent inhibitor of the c-Jun N-terminal kinase (JNK) family, demonstrating IC50 values of 1.81 nM for JNK1, 12.7 nM for JNK2, and 10.5 nM for JNK3. This compound effectively induces early apoptosis and causes cell cycle arrest in the G2/M phase. Additionally, JNK-IN-14 exhibits a modest inhibition of beclin-1 expression in K562 leukemia cells, indicating its potential application in cancer research and therapeutic strategies targeting JNK signaling pathways. -
INK Inhibitor
SET-171 is a selective JNK (c-Jun N-terminal kinase) inhibitor that demonstrates notable anticancer properties and regulation of lipid metabolism through the suppression of liver pyruvate kinase (PKL) expression. In vitro studies reveal IC50 values of 8.82 μM and 2.97 μM against HepG2 and Huh7 cell lines, respectively, showcasing its potent cytotoxic effects. Furthermore, SET-171 has been shown to significantly decrease triacylglycerol (TAG) levels and inhibit steatosis-related protein expression, highlighting its potential utility in the study of hepatocellular carcinoma (HCC) and non-alcoholic fatty liver disease (NAFLD). -
Anti-Inflammatory Agent
Rhamnocitrin is an anti-inflammatory and antioxidant agent that targets the STIM-1, NFATc3, and MAPK pathways. It effectively scavenges free radicals and exhibits a specific inhibitory effect on oxidative stress and inflammatory responses in vascular endothelial cells and neurons. Through upregulation of miR-185, Rhamnocitrin inhibits STIM-1-mediated store-operated calcium entry, which prevents NFATc3 translocation to the nucleus and reduces the expression of downstream inflammatory factors. Additionally, it induces heme oxygenase HO-1 expression and modulates the ERK/p38 MAPK pathway, mitigating the production of pro-inflammatory cytokines and adhesion molecules. Rhamnocitrin is suitable for research focused on endothelial-related inflammatory diseases and neuroprotection. -
Substrate For ALDH, Precursor Compound for Phenolic Compounds
3-Hydroxybenzaldehyde serves as a substrate for aldehyde dehydrogenase (ALDH) and acts as a precursor for diverse phenolic compounds, including Protocatechuic aldehyde. This compound exhibits vasculoprotective properties, demonstrating potential in both in vitro and in vivo studies. Research applications primarily focus on its role in atherosclerosis, making it a valuable reagent for biochemical investigations related to cardiovascular health. -
Carboxylesterase Notum Inhibitor
Carboxylesterase-IN-3 is a highly potent inhibitor of Carboxylesterase Notum, exhibiting an IC50 of 10 nM or lower. Notum plays a critical role as a negative regulator of Wnt signaling by hydrolyzing palmitoleoylate esters necessary for Wnt activity. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating the modulation of Wnt signaling pathways. -
Carboxylesterase Notum Inhibitor
Carboxylesterase-IN-2 is a highly potent inhibitor of Carboxylesterase Notum, exhibiting an IC50 of 10 nM or lower. Notum functions as a negative regulator of Wnt signaling by hydrolyzing palmitoleoylate esters, which are essential for Wnt activity. This compound is valuable for investigating the role of Notum in cancer biology and the modulation of Wnt signaling pathways. -
Carboxylesterase Inhibitor
WZU-13 is a potent inhibitor of carboxylesterase (CES), demonstrating significant inhibition of 77% at a concentration of 100 μM. This compound is valuable for research applications aimed at studying the role of CES in drug metabolism and detoxification processes. WZU-13 can aid in elucidating the enzymatic mechanisms and biological functions of CES in various physiological and pathological contexts. -
SMO Inhibitor
IPI-269609 is a potent inhibitor of Smoothened (SMO), specifically targeting the Hedgehog (Hh) signaling pathway. This compound has demonstrated significant efficacy in reducing the ALDH-bright cell population, identified as cancer stem cells in pancreatic cancer. IPI-269609 effectively inhibits both the migration and colony formation of pancreatic cancer cells, and has shown effectiveness in mitigating pancreatic cancer metastasis in preclinical mouse models. Its application is invaluable for research focused on pancreatic cancer and the underlying mechanisms of tumor progression. -
5-LO/COX-2/DPP-4 Inhibitor
Timosaponin A1 is a natural steroidal saponin that acts as an inhibitor of 5-lipoxygenase (5-LO), cyclooxygenase-2 (COX-2), and dipeptidyl peptidase 4 (DPP-4), with IC50 values of 3.29 µM, 36.43 µM, and 33.25 µM, respectively. This compound exhibits anti-inflammatory properties and is relevant for research on conditions such as asthma and diabetes. Its inhibitory effects on key enzymes involved in inflammatory pathways make it a valuable tool for exploring therapeutic strategies in related biological studies. -
Triterpenoid
Cyclocarin A is a triterpenoid compound isolated from the leaves of Cyclocarya paliurus. This compound exhibits weak inhibitory activity against several enzymes, including α-glucosidase, lipase, DPP-IV, and aldose reductase, along with limited effects on human cancer cell lines (IC50 > 10 μM). Despite its modest biological activity, Cyclocarin A may serve as a useful tool for research in enzyme inhibition and cancer biology. -
Cathepsin C Inhibitor
Verducatib is an orally active inhibitor of cathepsin C, also known as Dipeptidyl Peptidase I (DPP1). By inhibiting the activation of neutrophil serine proteases, Verducatib restores the balance of proteases and inhibitors, thereby reducing pulmonary inflammation and enhancing responses to infection. This compound has demonstrated efficacy in decreasing the frequency and severity of acute exacerbations in bronchiectasis, while also improving lung function and quality of life. Its safety profile is comparable to placebo, with a slight increase in mild-to-moderate cutaneous adverse events at higher doses, indicating potential for clinical application. -
DPP-4 Inhibitor
2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one is a natural compound that functions as a dipeptidyl peptidase-4 (DPP-4) inhibitor. It exhibits significant binding affinities to both DPP-4 and α-Amylase, suggesting its potential role in the regulation of glucose metabolism. This compound may offer beneficial effects in antidiabetic research, making it a valuable tool for studies focused on diabetes management and therapeutic development. -
Antidiabetic Compound
Lupinalbin A, a dipeptidyl peptidase 4 (DPP4) and α-glucosidase inhibitor, demonstrates effective inhibition with IC50 values of 45.2 µM and 53.4 µM, respectively. This compound exhibits notable antidiabetic activity, making it a valuable tool for research in diabetes management and metabolic studies. Its dual inhibition profile supports investigations into glucose metabolism and insulin sensitivity. -
PDE1A1 Inhibitor
PDE1-IN-11 is a potent and selective inhibitor of phosphodiesterase 1A1 (PDE1A1). This compound enhances intracellular levels of cAMP and cGMP, thereby activating the PKA-CREB and NO-cGMP-PKG signaling pathways, which in turn promotes osteoblast differentiation and supports bone formation while inhibiting osteoclastogenesis and bone resorption. PDE1-IN-11 is a valuable tool for investigating postmenopausal osteoporosis and other disorders related to bone metabolism. -
Phosphodiesterase (PDE) Inhibitor
PDE10-IN-6 is a selective inhibitor of phosphodiesterase-10 (PDE10), which plays a crucial role in the degradation of cyclic AMP (cAMP) and cyclic GMP (cGMP). By inhibiting PDE10, this compound enhances the levels of these important second messengers, thereby affecting various signaling pathways. PDE10-IN-6 is primarily utilized in neurological research, specifically in studies related to cognitive function and neurodegenerative diseases. -
PDE-5 Inhibitor
BL-122 is a selective phosphodiesterase-5 (PDE-5) inhibitor that elevates cGMP levels in tissues, enhancing the expression of nitric oxide (NO) and facilitating smooth muscle relaxation. This reagent is primarily utilized in research related to inflammation, immunology, and cardiovascular diseases, including conditions such as asthma and hypertension. Its ability to modulate cGMP signaling pathways makes it a valuable tool for investigating therapeutic strategies in these areas. -
PDE5 Inhibitor
UK 343664 is a selective inhibitor of phosphodiesterase 5 (PDE5), demonstrating significant potency and oral bioavailability. This compound has been shown to partially reverse thromboxane-induced pulmonary hypertension, indicating its potential therapeutic applications in treating cardiovascular disorders associated with pulmonary hypertension. -
PDE4 Inhibitor
CP-220629 is a potent inhibitor of phosphodiesterase 4 (PDE4), demonstrating an IC50 of 0.44 μM. This compound is effective in mitigating airway obstruction, as evidenced by an ED50 of 2.0 mg/kg in guinea pig models using aerosolized antigen. CP-220629 is utilized in research aimed at exploring therapeutic strategies for respiratory conditions related to PDE4 activity. -
PDE10A Antagonist
AMG580 is a selective antagonist of phosphodiesterase 10A (PDE10A) with subnanomolar affinity across rat, primate, and human isoforms. This compound demonstrates significant biological activity in modulating intracellular signaling pathways associated with PDE10A inhibition. AMG580 is particularly useful in research applications involving noninvasive radiotracers, aiding in the exploration of brain imaging and neuropharmacology. -
PDE2 Agonist
5,6-DCl-cBIMP is a cyclic adenosine monophosphate (cAMP) analog that functions as an agonist of phosphodiesterase 2 (PDE2). This compound significantly enhances the hydrolytic activity of PDE2 on both cAMP and cGMP, making it a valuable tool for studying signal transduction pathways. Its potency and specificity position it as a useful reagent in research related to cardiovascular, neurological, and metabolic disorders. -
PDE4 Inhibitor
MK-0952 sodium is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor, demonstrating an IC50 of 0.53 nM. This compound exhibits potential therapeutic effects in modulating inflammatory responses and cognitive functions, making it a valuable tool in Alzheimer’s disease research. MK-0952 sodium can be utilized to study the role of PDE4 in neurodegenerative disorders. -
PDE4 Inhibitor
UK-500001 is a selective inhibitor of phosphodiesterase 4 (PDE4), demonstrating high potency with IC50 values of 0.28 nM for PDE4D3, 22.8 nM for PDE4B2, 26.1 nM for PDE4A4, and 271 nM for PDE4C2. This compound exhibits significant anti-inflammatory properties by effectively inhibiting the release of TNF-α and IFN-γ in both human and rodent macrophagic cell lines at nanomolar concentrations. UK-500001 holds potential for research applications in chronic obstructive pulmonary disease (COPD) and asthma treatment. -
PDE Inhibitor
Dazonone is a selective phosphodiesterase III (PDE3) inhibitor, exhibiting an IC50 of 1.68 μM. This compound enhances intracellular levels of cyclic AMP, leading to increased vasodilation and improved cardiac function. Dazonone is utilized in research on cardiovascular diseases and for investigating cellular signaling pathways involving cAMP modulation. -
PDE5 Inhibitor
N-Desethyl-N-methyl vardenafil is a potent PDE5 inhibitor, exhibiting an IC50 value of 0.14 μM. This compound is primarily utilized in pharmacological research focused on the modulation of erectile dysfunction and related cardiovascular conditions. Its capacity to inhibit PDE5 facilitates increased levels of cyclic GMP, thus enhancing vascular smooth muscle relaxation and blood flow. -
PDE Inhibitor
5,5′-(1,3-Propanediyl)bis-1,3,4-oxadiazole-2(3H)-thione is identified as a phosphodiesterase (PDE) inhibitor, specifically targeting both snake venom and human recombinant PDE 1 with IC50 values of 429 μM and 467 μM, respectively. Additionally, it exhibits weak inhibition of mushroom tyrosinase, with a calculated Ki of 1.9 μM. This compound can be utilized in biochemical research related to enzyme inhibition and potential pharmacological applications concerning PDE activity. -
PDE5 Inhibitor
Xanthoanthrafil is a potent phosphodiesterase-5 (PDE5) inhibitor, exhibiting an IC50 value of 3.95 ng/mL. This compound is primarily utilized in research related to erectile dysfunction, offering valuable insights into its mechanisms and potential therapeutic applications. -
Phosphodiesterase (PDE) Inhibitor
Hedgehog IN-8 is a potent phosphodiesterase (PDE) inhibitor that modulates hedgehog signaling pathways. This compound demonstrates significant biological activity in disrupting aberrant hedgehog signaling, which is often implicated in various cancers and developmental disorders. Hedgehog IN-8 is valuable for research applications aimed at understanding the role of hedgehog signaling in tumorigenesis and developing potential therapeutic interventions. -
PDE1/PDE5 Inhibitor
SCH 51866 is a potent and selective inhibitor of phosphodiesterase 1 (PDE1) and phosphodiesterase 5 (PDE5), with IC50 values of 70 nM and 60 nM, respectively. This compound effectively inhibits collagen-induced aggregation of human washed platelets with an IC50 of 10 μM and demonstrates protective effects against neointimal formation in balloon catheter-injured carotid arteries in spontaneously hypertensive rats. Additionally, SCH 51866 has been shown to reduce blood pressure in this model, making it a valuable tool for research in hypertension and related vascular disorders.
