- Cat. No.
- A13346
MK 886
Synonyms: L-663,536; L663536
MK-886 is an inhibitor of leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes).
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- Cat. No.
- A15044
Choline Fenofibrate
Synonyms: ABT-335
Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia.
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- Cat. No.
- A17602
Cefminox Sodium (MT-141)
Synonyms: MT-141
Cefminox Sodium, also known as Meicelin and MT-141, is a penicillin binding protein inhibitor used to treat bacterial infection.
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- Cat. No.
- A19368
Azemiglitazone {MSDC-0602)
Synonyms: MSDC 0602
MSDC-0602, a PPARγ-sparing thiazolidinedione (TZD), interacts with the mitochondrial pyruvate carrier (MPC) and inhibits its activity and are effective for treatment of type 2 diabetes with reducing risk of PPARγ-mediated side effects.
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- Cat. No.
- A20815
Ertiprotafib
Synonyms: PTP 112
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
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- Cat. No.
- A24175
MTX-531
MTX-531 is an orally active small molecule that inhibits EGFR (IC50 = 14.7 nM) and multiple PI3K isoforms, with IC50 values of 6.4 nM (PI3Kα), 233 nM (PI3Kβ), 8.3 nM (PI3Kγ), and 1.1 nM (PI3Kδ), demonstrating potent antitumor activity. Additionally, MTX-531 functions as a weak PPARγ agonist (IC50 = 2.5 µM), which may mitigate PI3K inhibitor-induced hyperglycemia.
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- Cat. No.
- A24326
Auraptene
Auraptene is an orally active geranyloxycoumarin compound naturally found in plants of the *Brassicaceae* family. It exhibits a wide range of biological activities, including antibacterial, anti-pathogenic, antioxidant, anti-tumor, and neuroprotective effects. Auraptene has shown therapeutic potential in the management of various chronic conditions such as hypertension and cystic fibrosis, making it a valuable compound for pharmacological and nutraceutical research.
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- Cat. No.
- A29089
AZ0108
AZ0108 is a selective inhibitor of poly(ADP-ribose) polymerases (PARPs), including PARP1, PARP2, PARP3, PARP6, TNKS1, and TNKS2. It displays potent inhibitory activity with IC50 values of
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- Cat. No.
- A29120
AZD-9574-acid
AZD-9574-acid is a selective PPAR-1 inhibitor that serves as a crucial building block for the development of PROTAC molecules. Its inhibition of PPAR-1 demonstrates significant potential in the regulation of metabolic pathways and inflammatory responses. This compound is essential for researchers exploring targeted protein degradation and its applications in therapeutic development.
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- Cat. No.
- A30771
Soyasaponin Ab
Soyasaponin Ab is a potent PPARγ inhibitor with oral bioavailability. It effectively suppresses PPARγ transcriptional activity and induces apoptosis at elevated concentrations. This compound exhibits a range of biological activities, including anti-obesity, anti-oxidation, anti-inflammation, and anti-aging effects. Additionally, Soyasaponin Ab has been shown to mitigate memory impairment induced by Scopolamine, making it a valuable reagent for research in metabolic and neuroprotective applications.
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- Cat. No.
- A31416
Perfluorotetradecanoic acid
Synonyms: PFTeDA
Perfluorotetradecanoic acid (PFTeDA) is a potent PPARγ inhibitor, demonstrating a binding affinity to the human PPARγ ligand-binding domain with an IC50 of 22.8 μM and a Kd of 157.8 μM. It has been shown to impair Leydig cell function through the induction of oxidative stress and apoptosis. Additionally, PFTeDA stimulates corticosterone biosynthesis while inhibiting aldosterone production, making it a valuable tool for researching steroidogenesis and related metabolic pathways.
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- Cat. No.
- A39202
PIISVYWK
PIISVYWK is a potent PPARγ inhibitor that also acts as an activator of heme oxygenase-1 (HO-1) and nuclear factor erythroid 2-related factor 2 (Nrf2). This compound effectively modulates the HO-1/Nrf2 signaling pathway, contributing to the reduction of oxidative stress and inflammation, while also exhibiting anti-obesity properties. PIISVYWK is suitable for research applications focused on obesity and related metabolic disorders.
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- Cat. No.
- A39908
Bavachinin
Synonyms: 7-O-Methylbavachin; Bavachinin A
Bavachinin is a pan-peroxisome proliferator-activated receptor (PPAR) agonist and a HIF-1α inhibitor, demonstrating IC50 values of 21.043 μM, 12.819 μM, and 0.622 μM for PPAR-α, PPAR-β/δ, and PPAR-γ, respectively. This compound exhibits significant antitumor activity against non-small cell lung cancer through its modulation of PPAR-γ. Additionally, Bavachinin possesses notable anti-inflammatory and anti-angiogenic properties, making it a valuable tool for research in cancer and metabolic disorders. Its oral bioavailability further supports its utility in various biological studies.
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- Cat. No.
- A39919
PPARγ-IN-2
PPARγ-IN-2 is a selective PPARγ inhibitor that effectively reduces triglyceride accumulation in 3T3-L1 preadipocytes, with an EC50 of 0.106 μM. This compound demonstrates potential for mitigating obesity and associated metabolic syndrome, particularly in the context of a high-cholesterol diet. Its ability to diminish lipid accumulation in adipose tissue makes it a valuable tool for research focused on metabolic disorders and adipocyte biology.
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- Cat. No.
- A39931
SR 16832
SR 16832 is a dual-site covalent inhibitor of peroxisome proliferator-activated receptor gamma (PPARγ). It functions by targeting both orthosteric and allosteric sites, leading to significant modulation of PPARγ activity. This compound is valuable for research applications related to metabolic disorders, obesity, and diabetes, particularly in studies investigating the downstream effects of PPARγ inhibition on gene expression and cellular metabolism.
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- Cat. No.
- A39936
FTX-6746
FTX-6746 is an orally active inhibitor of peroxisome proliferator-activated receptor gamma (PPARG). It demonstrates significant tumor inhibition in mouse xenograft models, making it a valuable tool for investigating the therapeutic potential of targeting PPARG in cancer research. Its specificity and efficacy in modulating PPARG activity support its use in studies related to metabolic disorders and cancer biology.
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- Cat. No.
- A39958
trans-Cinnamyl alcohol
trans-Cinnamyl alcohol is a selective PPARγ inhibitor that plays a significant role in regulating lipid metabolism and adipogenesis. As a metabolite derived from chestnut flowers, it exhibits anti-obesity activity by inhibiting PPARγ expression. This compound is valuable for research applications focused on obesity, metabolic disorders, and the modulation of fat cell differentiation.
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- Cat. No.
- A39998
PPARγ phosphorylation inhibitor 1
PPARγ phosphorylation inhibitor 1 is a selective inhibitor targeting Peroxisome Proliferator-Activated Receptor gamma (PPARγ). It effectively inhibits CDK5-mediated phosphorylation of PPARγ at Ser273 with an IC50 of 160 nM, demonstrating a binding affinity with an IC50 of 24 nM. This compound exhibits minimal PPARγ agonistic activity in reporter gene assays, making it a valuable tool for studying the role of PPARγ phosphorylation in metabolic disorders and antidiabetic research applications.
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- Cat. No.
- A40019
Anti-NASH agent 1
Anti-NASH agent 1 is a potent PPAR-α/δ inhibitor that effectively targets nonalcoholic steatohepatitis (NASH). This compound has demonstrated significant efficacy in improving hyperlipidemia, liver fat degeneration, and liver inflammation in a methionine-choline deficiency (MCD) induced NASH mouse model. Additionally, Anti-NASH agent 1 exhibits low liver toxicity while providing protective effects on liver health, making it a valuable tool for research into metabolic disorders and liver diseases.
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- Cat. No.
- A40023
Soyasaponin Aa
Soyasaponin Aa is a PPARγ inhibitor that demonstrates significant anti-obesity effects in 3T3-L1 adipocytes by downregulating the activity of peroxisome proliferator-activated receptor γ. Its biological activity supports research into mechanisms of adipogenesis and metabolic regulation. Soyasaponin Aa is useful in studies aimed at understanding the therapeutic potential of targeting PPARγ in obesity-related conditions.
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- Cat. No.
- A40036
BGT-002
Synonyms: 326E
BGT-002 is a potent dual inhibitor of ATP-citrate lyase (ACLY) and a peroxisome proliferator-activated receptor alpha (PPARα) agonist. This compound effectively reduces lipogenesis by inhibiting fatty acid synthesis and enhancing lipid efflux. BGT-002 has shown efficacy in improving metabolic dysfunction-related steatohepatitis and hyperlipidemia in vivo, making it a valuable reagent for research into hypercholesterolemia and related metabolic disorders.
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- Cat. No.
- A40124
Zaltoprofen sulfoxide
Zaltoprofen sulfoxide is a selective COX-2 inhibitor with an IC50 of 45.38 nM, as well as a PPAR-γ activator. This compound effectively inhibits NF-κB and MAPK inflammatory signaling pathways, making it a valuable tool in the study of inflammation and acute lung injury models. It is particularly relevant for research focused on LPS-induced acute lung injury.
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- Cat. No.
- A40151
Timcodar
Synonyms: VX-853
Timcodar is a selective PPAR inhibitor that effectively blocks adipogenic transcriptional regulators, specifically PPARγ and C/EBPα, thereby reducing fat accumulation. Its mechanism of action mirrors that of rapamycin but without inducing immunosuppression or glucose resistance. Timcodar's significant impact on adipogenesis may offer a promising therapeutic avenue for addressing obesity, a growing global health concern. This compound is ideally suited for research related to metabolic disorders and obesity treatment strategies.
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- Cat. No.
- A40153
PPARγ-IN-5
PPARγ-IN-5 is a selective inhibitor of PPARγ, a key regulator of adipocyte differentiation and lipid metabolism. This compound effectively reduces lipid accumulation in hepatocytes, demonstrating minimal cytotoxicity at concentrations up to 400 µM in HepG2 cells. PPARγ-IN-5 is suitable for investigations into non-alcoholic fatty liver disease and related metabolic disorders.
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- Cat. No.
- A40191
(±)-CBCQ
Synonyms: Cannabichromenquinone
(±)-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.
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