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PPAR Inhibitor

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194

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2

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36

Isotope-Labeled Compounds

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3

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0234
    Bavachinin
    3 Publications Verification

    7-O-Methylbavachin; Bavachinin A

    Amyloid-β PPAR HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology Cancer
    Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .
    Bavachinin
  • HY-147705

    PPAR Metabolic Disease
    PPARγ phosphorylation inhibitor 1 (Compound 10) is a potent PPARγ binder with the IC50 of 24 nM. PPARγ phosphorylation inhibitor 1 inhibits CDK5-mediated phosphorylation of PPARγ Ser273 with the IC50 of 160 nM. PPARγ phosphorylation inhibitor 1 displays negligible PPARγ agonism in a reporter gene assay. Antidiabetic effects .
    PPARγ phosphorylation inhibitor 1
  • HY-19383
    Ertiprotafib
    1 Publications Verification

    PTP 112

    Phosphatase IKK PPAR Metabolic Disease
    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.
    Ertiprotafib
  • HY-B0760

    FNF acid

    PPAR COX Metabolic Disease
    Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
    Fenofibric acid
  • HY-N11924

    AMPK PPAR Metabolic Disease
    Foenumoside B is a triterpene saponin isolated from Lysimachia foenum-graecum. Foenumoside B activates AMPK signaling, inhibits PPARγ-induced adipogenesis, and shifts lipid metabolism toward lipolysis. Foenumoside B can be used in the study of obesity and obesity-related metabolic diseases .
    Foenumoside B
  • HY-N0234R

    7-O-Methylbavachin (Standard); Bavachinin A (Standard)

    Amyloid-β Reference Standards PPAR HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    Bavachinin (Standard) is the analytical standard of Bavachinin. This product is intended for research and analytical applications. Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .
    Bavachinin (Standard)
  • HY-173622

    PPAR Metabolic Disease Endocrinology
    PPARγ agonist 18 (Compound (I)) is a PPARγ inhibitor (KD: 3.75 μM). PPARγ agonist 18 can inhibit CDK5-mediated phosphorylation of PPARγ at Ser245. PPARγ agonist 18 can be used in insulin resistance research .
    PPARγ agonist 18
  • HY-148922

    PPAR Metabolic Disease
    PPARα/γ agonist 2 is an orally active PPARα full agonist and PPARγ partial agonist. PPARα/γ agonist 2 activates PPARα and PPARγ with EC50 values of 0.95 μM and 0.91 μM respectively. PPARα/γ agonist 2 is also a PTP1B inhibitor. PPARα/γ agonist 2 is an anti-diabetic agent .
    PPARα/γ agonist 2
  • HY-172169

    PPAR Inflammation/Immunology
    PPARγ-IN-5 (Compound A3) is the inhibitor for PPARγ. PPARγ-IN-5 inhibits lipid accumulation in hepatocytes without significant cytotoxicity in HepG2 cell (400 µM). PPARγ-IN-5 can be used in research of non-alcoholic fatty liver disease .
    PPARγ-IN-5
  • HY-B0700

    BRL 49653 sodium

    PPAR TRP Channel Autophagy Metabolic Disease Inflammation/Immunology
    Rosiglitazone sodium is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone sodium is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
    Rosiglitazone sodium
  • HY-156010

    PPAR Metabolic Disease
    PPARγ-IN-2 (Compound 5a) is a PPARγ inhibitor. PPARγ-IN-2 inhibits TG accumulation in 3T3-L1 preadipocytes (EC50: 0.106 μM). PPARγ-IN-2 inhibits high-cholesterol diet (HFC)-induced obesity and related metabolic syndrome, and reduces lipid accumulation in adipose tissue .
    PPARγ-IN-2
  • HY-12483

    PPAR Metabolic Disease
    SR1664 is a PPARγ antagonist. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50=80 nM; Ki= 28.67 nM) .
    SR1664
  • HY-14600
    Rosiglitazone maleate
    Maximum Cited Publications
    115 Publications Verification

    BRL 49653C

    PPAR TRP Channel Autophagy Ferroptosis Metabolic Disease Inflammation/Immunology Cancer
    Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
    Rosiglitazone maleate
  • HY-163862

    PPAR Reactive Oxygen Species (ROS) Inflammation/Immunology
    PPARα agonist 3 (Compound A229) is a PPARα agonist (EC50: 590 nM). PPARα agonist 3 inhibits TBHP or 4-HNE (HY-113466)-induced production of ROS .
    PPARα agonist 3
  • HY-168719

    PPAR Inflammation/Immunology
    PPARγ agonist 16 (Compound 4G) is the agonist for PPARγ, that competitively binds to LBD domain of PPARγ with IC50 of 1790 nM. PPARγ agonist 16 inhibits the ear swelling in mouse model, and exhibits anti-hyperglycemic in Streptozotocin (HY-13753)-induced mouse diabetes mellitus model .
    PPARγ agonist 16
  • HY-160937

    PARP Cancer
    AZD-9574-acid (70D), a PPAR-1 inhibitor, can be used for the synthesis of PROTAC (CAS 2923686-70-6) .
    AZD-9574-acid
  • HY-B0760R

    FNF acid (Standard)

    Reference Standards PPAR COX Metabolic Disease
    Fenofibric acid (Standard) is the analytical standard of Fenofibric acid. This product is intended for research and analytical applications. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
    Fenofibric acid (Standard)
  • HY-174278

    PPAR NO Synthase Inflammation/Immunology
    PPARδ agonist 12 (compound 25) is a PPARδ agonist that inhibits the production of inflammatory factors and nitric oxide. PPARδ agonist 12 can also effectively prevent macrophages from infiltrating inflammatory sites and can be used in inflammation research .
    PPARδ agonist 12
  • HY-161985

    PPAR Metabolic Disease
    PPARγ-IN-3 (compound 9ga) is a potent and orally active PPARγ inhibitor. PPARγ-IN-3 reduces triglyceride (TG) accumulation with low cytotoxicity. PPARγ-IN-3 preventes the excessive growth of body weight and lessened fat mass as well as liver mass, decreases lipid accumulation in the liver and blood. PPARγ-IN-3 has the potential for the research of diet-induced obesity .
    PPARγ-IN-3
  • HY-14600R

    BRL 49653C (Standard)

    Reference Standards PPAR TRP Channel Autophagy Ferroptosis Metabolic Disease Inflammation/Immunology Cancer
    Rosiglitazone (maleate) (Standard) is the analytical standard of Rosiglitazone (maleate). This product is intended for research and analytical applications. Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
    Rosiglitazone maleate (Standard)
  • HY-159146

    PPAR STING Reactive Oxygen Species (ROS) Neurological Disease Inflammation/Immunology
    PPARα agonist 4 (compound BH400) is a PPARα agonist (EC50= 1.2 μM). PPARα agonist 4 also inhibits STING (IC50: 8.1 μM). PPARα agonist 4 reduces the CoCl2-induced production of ROS and LPS-induced secretion of IL-6. The PPARα agonist 4 restores the decreased expression of PCG1α induced by LPS .
    PPARα agonist 4
  • HY-17386S

    Isotope-Labeled Compounds PPAR TRP Channel Autophagy Ferroptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Rosiglitazone-d3 is the deuterium labeled Rosiglitazone. Rosiglitazone (BRL 49653) is a selective, orally active PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone is also an activator of TRPC5 (EC50=~30 μM) and an inhibitor of TRPM3 .
    Rosiglitazone-d3
  • HY-117761

    PPAR Metabolic Disease Cancer
    MHY908 is a potent dual agonist of PPARα and PPARγ . MHY908 also inhibits melanogenesis through inhibition of mushroom tyrosinase activity .
    MHY908
  • HY-168376

    9(10)-Nitrated oleic acid

    PPAR Metabolic Disease Inflammation/Immunology
    9(10)-Nitrooleate (9(10)-Nitrated oleic acid) is a nitrated derivative of Oleic acid (HY-N1446). 9(10)-Nitrooleate can activate PPAR (PPARα, PPARβ/δ, and PPARγ), promoting fat formation and glucose uptake, inhibiting the function of neutrophils and platelets, and can be used in lipid metabolism and inflammation research .
    9(10)-Nitrooleate
  • HY-B0760S1

    FNF acid-13C8

    Isotope-Labeled Compounds COX PPAR Metabolic Disease
    Fenofibric acid- 13C8 (FNF acid- 13C8) is 13C labeled Fenofibric acid. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
    Fenofibric acid-13C8
  • HY-170874

    PPAR Metabolic Disease
    PPARγ modulator-2 (Compound (R)-2n) is the reversible modulator for PPARγ that inhibits PPARγ ligand-binding domain (LBD) with an IC50 of 41 nM. PPARγ modulator-2 reduces blood glucose, improves the glucose tolerance and insulin tolerance, and exhibits anti-diabetic efficacy in db/db mouse models .
    PPARγ modulator-2
  • HY-139175

    PPAR Others
    ZLY032 is a dual FFA1/PPARδ agonist with the activity of improving glucose and lipid metabolism, alleviating liver fibrosis, and potentially inhibiting metabolic disorders.
    ZLY032
  • HY-B0760S

    PPAR COX Metabolic Disease
    Fenofibric acid-d6 (FNF acid-d6) is the deuterium labeled Fenofibric acid. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 µM, 1.47 µM, and 1.06 µM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
    Fenofibric acid-d6
  • HY-B0760S2

    FNF acid-d4

    Isotope-Labeled Compounds Metabolic Disease
    Fenofibric acid-d4 (FNF acid-d4) is deuterium labeled Fenofibric acid. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
    Fenofibric acid-d4
  • HY-173166

    PPAR Cancer
    PPARγ agonist 17 (Compound C1) is a PPARγ agonist. PPARγ agonist 17 enhances PPARγ activity and blocks the cell cycle in G2/M phase, inhibits cell migration and induces apoptosis in HT-29 cells. PPARγ agonist 17 has a broad spectrum anti-proliferative activity in cancer cells with relatively low toxicity in normal cells which cannot cross the blood-brain barrier .
    PPARγ agonist 17
  • HY-169404

    PPAR Metabolic Disease
    PPARγ agonist 15 (Compound 7c) is an agonist for PPARγ. PPARγ agonist 15 inhibits the expression of alpha-amylase (HPA) and alpha-glucosidase (HLAG) with IC50 of 28.35 µM and 26.21 µM. PPARγ agonist 15 enhances glucose uptake in the L6 myotube cell. PPARγ agonist 15 improves glucose homeostasis, insulin sensitivity, and lipid metabolism in rat Streptozotocin (HY-13753)-induced diabetes model .
    PPARγ agonist 15
  • HY-149429

    PPAR Metabolic Disease
    PPARδ agonist 9 (compound 21) is a PPARδ agonist (EC50: 3.6 nM). PPARδ agonist 9 has in vivo efficacy, reducing serum levels of MCP-1 in mice and significantly inhibiting atherosclerosis progression in the LDLr-KO model (inhibition rate: 50-60%) .
    PPARδ agonist 9
  • HY-N1029
    Norathyriol
    1 Publications Verification

    Mangiferitin

    Glycosidase PPAR Infection Inflammation/Immunology Cancer
    Norathyriol (Mangiferitin) is a natural metabolite of Mangifera. Norathyriol inhibits α-glucosidase in a noncompetitive manner with an IC50 of 3.12 μM . Norathyriol inhibits PPARα, PPARβ, and PPARγ with IC50s of 92.8 µM, 102.4 µM, and 153.5 µM, respectively . Antioxidant, anticancer, antimicrobial, anti-inflammatory, anti-bacterial activities.
    Norathyriol
  • HY-100277
    Mifobate
    1 Publications Verification

    SR-202

    PPAR Metabolic Disease
    Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
    Mifobate
  • HY-167950

    PPAR Metabolic Disease
    PPARα/γ agonist 5 is a dual PPARα/γ agonist with significant biological activity exhibited at low concentrations. The EC50 of PPARα/γ agonist 5 are 0.358μM and 1.21μM respectively, showing its potential in inhibiting type 2 diabetes and lipid metabolism disorders. PPARα/γ agonist 5 was selected for clinical development due to its high efficacy .
    PPARα/γ agonist 5
  • HY-114263
    NXT629
    3 Publications Verification

    PPAR Cancer
    NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively . NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models .
    NXT629
  • HY-50935
    Troglitazone
    20+ Cited Publications

    CS-045

    PPAR Autophagy Apoptosis Ferroptosis Metabolic Disease Cancer
    Troglitazone is an orally active PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.
    Troglitazone
  • HY-119248

    MK-0767

    PPAR Metabolic Disease
    KRP-297 is a PPARα and PPARγ agonist potentially for the research of type 2 diabetes and dyslipidemia. KRP-297 restores reduced lipid oxidation, and inhibits of enhanced lipogenesis and triglyceride accumulation in the liver.
    KRP-297
  • HY-14928

    PPAR ERK JNK TGF-beta/Smad NO Synthase COX NF-κB Interleukin Related Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    Lobeglitazone is a new type of thiazolidinedione. Lobeglitazone is the orally active agonist for PPAR with EC50 of 137.4 nM and 546.3 nM for PPARγ and PPARα. Lobeglitazone is the inhibitor for ERK/JNK/Smad/NF-κB signaling pathway. Lobeglitazone exhibits anti-inflammatory, anti-diabetic, anti-fibrotic and anti-atherosclerotic properties .
    Lobeglitazone
  • HY-159944

    PPAR Neurological Disease Metabolic Disease Inflammation/Immunology
    PPARγ agonist 14 (compound 3) is a PPARy agonist (EC50=2.4 μM) with anti-diabetic activity. PPARγ agonist 14 can improve intracellular glucose uptake, promote insulin release, and lower blood sugar. In addition, PPARγ agonist 14 also improves mitochondrial function, reduces oxidative stress, and inhibits inflammatory factors. PPARγ agonist 14 can be used in the study of neurodegenerative diseases, neuroinflammatory diseases, and other diseases .
    PPARγ agonist 14
  • HY-15721
    FH535
    10+ Cited Publications

    PPAR Wnt β-catenin Cancer
    FH535 is an inhibitor of Wnt/β-catenin and PPAR with anti-tumor activities .
    FH535
  • HY-111254

    PPAR Metabolic Disease
    GQ-16 is a moderate affinity ligand for the ligand-binding domain (LBD) of PPARγ, exhibiting a Ki of 160 nM. GQ-16 is an effective inhibitor of Cdk5-mediated phosphorylation of PPARγ. GQ-16 is a partial agonist of PPARγ with reduced adipogenic actions. GQ-16 promotes insulin Sensitization without weight gain .
    GQ-16
  • HY-116247

    PPAR Metabolic Disease Inflammation/Immunology
    ST247 a potent PPARβ/δ inverse agonist. ST247 has a higher affinity to PPARβ/δ. ST247 modulates expression of the activation marker CCL2 in the opposite direction. ST247 efficiently induces the interaction with corepressors. ST247 inhibits the agonist-induced transcriptional activity of PPARβ/δ .
    ST247
  • HY-100277R

    SR-202 (Standard)

    Reference Standards PPAR Metabolic Disease
    Mifobate (Standard) is the analytical standard of Mifobate. This product is intended for research and analytical applications. Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
    Mifobate (Standard)
  • HY-14928A

    PPAR ERK JNK TGF-beta/Smad NO Synthase COX NF-κB Interleukin Related Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    Lobeglitazone sulfate is a new type of thiazolidinedione. Lobeglitazone sulfate is the orally active agonist for PPAR with EC50 of 137.4 nM and 546.3 nM for PPARγ and PPARα. Lobeglitazone sulfate is the inhibitor for ERK/JNK/Smad/NF-κB signaling pathway. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic and anti-atherosclerotic properties .
    Lobeglitazone sulfate
  • HY-116259

    PPAR Metabolic Disease
    PT-S58, a GSK0660 derivative, is a PPARβ/δ full antagonist with an IC50 value of 98 nM. PT-S58 inhibits the agonist-induced transcriptional activity of PPARβ/δ in vitro .
    PT-S58
  • HY-P10873

    Nuclear Hormone Receptor 4A/NR4A Mitochondrial Metabolism Cancer
    ST-CY14 is an inhibitor for Nur77-PPARγ interaction with an EC50 of 3.15 μM, that binds to Nur77 (Kd=32 nM), blocks Nur77 from being ubiquitinated and degraded by PPARγ, reduces fatty acid uptake and mitochondrial respiration, and inhibits the transcription of CD36 and FABP4. ST-CY14 inhibits the proliferation and migration of cancer cell MCF7 and MDA-MB-231. ST-CY14 inhibits tumor growth and bone metastasis in mouse models .
    ST-CY14
  • HY-112247

    PPAR Metabolic Disease
    SR 16832 is a dual site covalent PPARγ inhibitor that acts at orthosteric and allosteric sites .
    SR 16832
  • HY-168049

    PPAR Akt Metabolic Disease
    ZLY06 is an orally active dual agonist of peroxisome proliferator-activated receptor (PPAR) δ and γ (PPAR δ: EC50=341 nM; PPAR γ: EC50=237 nM). ZLY06 induces hepatic lipid accumulation by inhibiting the phosphorylation of AKT1, mediating the upregulation of CD36. In addition, ZLY06 significantly improves glucose and lipid metabolism without increasing body weight, and alleviates fatty liver by promoting β-oxidation of fatty acids and inhibiting hepatic lipogenesis .
    ZLY06
  • HY-50935R

    CS-045 (Standard)

    Reference Standards PPAR Autophagy Apoptosis Ferroptosis Metabolic Disease Cancer
    Troglitazone (Standard) is the analytical standard of Troglitazone. This product is intended for research and analytical applications. Troglitazone is an orally active PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.
    Troglitazone (Standard)

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