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Targets Recommended: PPAR
Results for "

PPAR

" in MCE Product Catalog:

146

Inhibitors & Agonists

1

Screening Libraries

43

Natural
Products

3

Recombinant Proteins

6

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-U00340
    PPAR agonist 1

    		PPAR Metabolic Disease
    PPAR agonist 1 is an agonist of PPAR α and PPAR γ, used for reducing blood glucose, lipid levels, lowering cholesterol and reducing body weight.
  • HY-107901
    Pparδ agonist 1

    		PPAR Metabolic Disease Cardiovascular Disease
    Pparδ agonist 1 is a PPAR-δ agonist, with an EC50 of 5.06 nM, used in the research of PPAR-delta related diseases, such as mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases.
  • HY-112597
    Pparδ agonist

    		PPAR Metabolic Disease
    PPARδ agonist is a PPARδ agonist extracted from patent US20180071304, compound example 10.
  • HY-100120
    Pparδ agonist 2

    		PPAR Metabolic Disease
    Pparδ agonist 2 is a PPARδ agonist extracted from patent WO 2016057656 A1.
  • HY-141494
    Pparδ agonist 5

    		PPAR Metabolic Disease
    Pparδ agonist 5, an orally active PPARδ-selective agonist (EC50=0.335 μM), is much greater than that of the prototypical standard GW0742. Pparδ agonist 5 promotes improvements in bone density and microarchitecture in vivo.
  • HY-U00068
    PPARα-MO-1

    		PPAR Metabolic Disease
    PPARα-MO-1 is a potent PPARα modulator extracted from patent WO/2004/110982A1, formula I.
  • HY-N1029
    Norathyriol

    Mangiferitin

    		 Glucosidase PPAR Cancer Infection Inflammation/Immunology
    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.
  • HY-B0637
    Bezafibrate

    BM15075

    		 PPAR Metabolic Disease Cardiovascular Disease
    Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
  • HY-13928
    GW0742

    GW610742

    		 PPAR Metabolic Disease Inflammation/Immunology Cardiovascular Disease Cancer
    GW0742 is a potent PPARβ and PPARδ agonist, with an IC50 of 1 nM for human PPARδ in binding assay, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.
  • HY-B0287
    Clofibrate

    		PPAR Metabolic Disease
    Clofibrate is an agonist of PPAR, with EC50s of 50 μM, ∼500 μM for murine PPARα and PPARγ, and 55 μM, ∼500 μM for human PPARα and PPARγ, respectively.
  • HY-16995
    Pirinixic acid

    Wy-14643

    		 PPAR Metabolic Disease Inflammation/Immunology
    Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.
  • HY-14817
    Indeglitazar

    PPM 204

    		 PPAR Metabolic Disease
    Indeglitazar (PPM 204) is an orally available PPAR pan-agonist for all three PPARα, PPARδ and PPARγ.
  • HY-20019
    L-165041

    		PPAR Metabolic Disease
    L-165041 is a cell permeable PPARδ agonist, with Kis of 6 nM and appr 730 nM for PPARδ and PPARγ, respectively, and induces adipocyte differentiation in NIH-PPARδ cells.
  • HY-13861
    GW7647

    		PPAR Cardiovascular Disease
    GW7647 is a potent PPARα agonist, with EC50s of 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ and PPARδ, respectively.
  • HY-106266
    Chiglitazar

    Carfloglitazar

    		 PPAR Metabolic Disease
    Chiglitazar (Carfloglitazar) is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.
  • HY-15655
    GW1929

    		PPAR Metabolic Disease Neurological Disease
    GW1929 is a potent PPAR-γ agonist, with a pKi of 8.84 for human PPAR-γ, and pEC50s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively.
  • HY-10678
    BMS-687453

    		PPAR Cardiovascular Disease
    BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.
  • HY-104049
    Lanifibranor

    IVA337

    		 PPAR Metabolic Disease Cancer
    Lanifibranor is a pan peroxisome proliferator-activated receptor (PPAR) agonist with EC50s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσ and PPARγ, respectively.
  • HY-15725
    CDDO-Im

    RTA-403; TP-235; CDDO-Imidazolide

    		 Keap1-Nrf2 PPAR Ferroptosis Cancer
    CDDO-Im (RTA-403) is an activator of Nrf2 and PPAR, with Kis of 232 and 344 nM for PPARα and PPARγ.
  • HY-106278
    GW 590735

    		PPAR Metabolic Disease
    GW 590735 is a potent and selective PPARα agonist. GW 590735 showsEC50=4 nM on PPARα and at least 500-fold selectivity versus PPARδ and PPARγ. GW 590735 can be used for the research of dyslipidemia.
  • HY-17444
    Tesaglitazar

    		PPAR Cancer Metabolic Disease
    Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively, and approximately 0.2 μM for both rat and human PPARγ. Tesaglitazar induces interstitial mesenchymal cell DNA synthesis and fibrosarcomas in subcutaneous tissues in rats.
  • HY-16578
    GW9662

    		PPAR Cancer
    GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
  • HY-19383
    Ertiprotafib

    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.
  • HY-B0760
    Fenofibric acid

    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.
  • HY-14600
    Rosiglitazone maleate

    BRL 49653C

    		 PPAR TRP Channel Autophagy Ferroptosis Cancer Metabolic Disease Inflammation/Immunology
    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).
  • HY-19937
    Saroglitazar

    		PPAR Metabolic Disease
    Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
  • HY-17386
    Rosiglitazone

    BRL 49653

    		 PPAR TRP Channel Autophagy Ferroptosis Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
    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.
  • HY-17386A
    Rosiglitazone hydrochloride

    BRL 49653 hydrochloride

    		 PPAR TRP Channel Autophagy Ferroptosis Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
    Rosiglitazone hydrochloride (BRL 49653 hydrochloride) is a selective, orally active PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone hydrochloride binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone hydrochloride is also an activator of TRPC5 (EC50=~30 μM) and an inhibitor of TRPM3.
  • HY-16086
    Balaglitazone

    DRF 2593; NN 2344

    		 PPAR Metabolic Disease
    Balaglitazone is a selective partial PPARγ agonist with an EC50 of 1.351 μM for human PPARγ.
  • HY-19937A
    Saroglitazar Magnesium

    		PPAR Metabolic Disease
    Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
  • HY-13956
    Pioglitazone

    U 72107

    		 PPAR Ferroptosis Metabolic Disease Cancer
    Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
  • HY-N9333
    Wistin

    		PPAR Cancer Metabolic Disease
    Wistin, isolated from Caragana sinica roots, is a PPARα and PPARγ agonist.
  • HY-12377
    GSK0660

    		PPAR Metabolic Disease
    GSK0660 is a potent antagonist of PPARβ and PPARδ, with IC50s of 155 nM for both isoforms.
  • HY-50935
    Troglitazone

    CS-045

    		 PPAR Autophagy Apoptosis Ferroptosis Cancer
    Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.
  • HY-19522A
    Seladelpar sodium salt

    MBX-8025 sodium salt; RWJ-800025 sodium salt

    		 PPAR Metabolic Disease
    Seladelpar sodium salt (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC50 of 2 nM, showing more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively.
  • HY-110118
    Edaglitazone

    		PPAR
    Edaglitazone is a potent, selective and orally active PPARγ agonist, with EC50s of 35.6 nM and 1053 nM for PPARα and PPARγ, respectively. Edaglitazone displays antiplatelet, antidiabetic and anti-hyperglycemic activity.
  • HY-12483
    SR1664

    		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).
  • HY-17386S
    Rosiglitazone-d3

    		PPAR TRP Channel Autophagy Ferroptosis Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
    Rosiglitazone-d3 (BRL 49653-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.
  • HY-101649
    Imiglitazar

    TAK-559

    		 PPAR Cardiovascular Disease
    Imiglitazar (TAK559) is a potent and dual human PPARα and PPARγ1 agonist with EC50 values of 67 and 31 nM.
  • HY-U00014
    AVE-8134

    		PPAR Metabolic Disease
    AVE-8134 is a potent PPARα agonist, with EC50 values of 100 and 3000 nM for human and rodent PPARα receptor, respectively.
  • HY-18756A
    NSC-87877 disodium

    		Phosphatase Apoptosis Cancer
    NSC-87877 disodium is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).
  • HY-18756
    NSC-87877

    		Phosphatase Apoptosis Others
    NSC-87877 is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).
  • HY-B0760S
    Fenofibric acid-d6

    		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.
  • HY-14601
    Pioglitazone hydrochloride

    U 72107A; AD 4833

    		 PPAR Ferroptosis Cancer Metabolic Disease
    Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
  • HY-14792
    Inolitazone

    Efatutazone; CS-7017; RS5444

    		 PPAR Cancer
    Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.
  • HY-14792B
    Inolitazone dihydrochloride

    Efatutazone dihydrochloride; CS-7017 dihydrochloride; RS5444 dihydrochloride

    		 PPAR Cancer
    Inolitazone dihydrochloride (Efatutazone dihydrochloride) is a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.
  • HY-111775
    LJ570

    		PPAR Metabolic Disease
    LJ570 is a PPARα/PPARγ dual agonist with EC50s of 1.05 and 0.12 μM, respectively.
  • HY-117727
    Leriglitazone

    Hydroxypioglitazone

    		 PPAR Metabolic Disease
    Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone. Leriglitazone (Hydroxypioglitazone) PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone (Hydroxypioglitazone) binds to the PPARγ C-terminal ligand-binding domain (LBD) with Ki of 1.2 μM，induces transcriptional efficacy of the PPARγ (LBD) with EC50 of 680 nM.
  • HY-100277
    Mifobate

    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.
  • HY-13956S
    Pioglitazone D4

    U 72107 D4

    		 PPAR Ferroptosis Cancer Metabolic Disease
    Pioglitazone D4 (U 72107 D4) is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
  • HY-112813
    TUG-1375

    		Others Metabolic Disease
    TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pKi of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ.
  • HY-N2025
    Oroxin A

    		PPAR Glucosidase Metabolic Disease
    Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity. Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence.
  • HY-114263
    NXT629

    		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.
  • HY-116699
    CP-868388 free base

    		PPAR Metabolic Disease Inflammation/Immunology Neurological Disease
    CP-868388 free base is a potent, selective and orally active PPARα agonist with a Ki value of 10.8 nM. CP-868388 free base has little or no affinity for PPARβ (Ki of 3.47 μM) and PPARγ. CP-868388 free base has hypolipidemic and anti-inflammatory actions.
  • HY-15372
    GW6471

    		PPAR Cancer
    GW6471 is a potent PPARα antagonist.
  • HY-13956S1
    Pioglitazone-d4 (alkyl)

    		PPAR Ferroptosis Metabolic Disease Cancer
    Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
  • HY-50665
    LY518674

    LY-674

    		 PPAR Metabolic Disease
    LY518674 is a potent, selective PPARα antagonist, with an EC50 of 42 nM for human PPARα. LY518674 reduces triglycerides in and increased HDL-C and is used for the treatment of atherosclerosis.
  • HY-13202
    T0070907

    		PPAR RAD51 Cancer
    T0070907 is a potent PPARγ antagonist with a Ki of 1 nM.
  • HY-N0019
    Daidzein

    		PPAR Endogenous Metabolite Endocrinology Cancer
    Daidzein is a soy isoflavone, which acts as a PPAR activator.
  • HY-124108
    Eicosatetraynoic acid

    ETYA

    		 COX PPAR Others
    Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively). Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 µM.
  • HY-17633
    Fonadelpar

    NPS-005; SJP-0035

    		 PPAR Neurological Disease
    Fonadelpar is a PPARδ agonist, used in the research of neuroparalytic keratopathy.
  • HY-14728
    Aleglitazar

    R1439; RO0728804

    		 PPAR Metabolic Disease
    Aleglitazar (R1439) is a potent dual PPARα/γ agonist, with IC50s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes.
  • HY-101292
    FK614

    		PPAR Metabolic Disease
    FK614 is an orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM). FK614 functions as a PPARγ agonist with potent anti-diabetic activity in vivo. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes.
  • HY-15721
    FH535

    		PPAR Wnt β-catenin Cancer
    FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities.
  • HY-19737A
    DG172 dihydrochloride

    		PPAR Cancer
    DG172 dihydrochloride is a selective PPARβ/δ antagonist, with an IC50 of 27 nM.
  • HY-111068
    KD-3010

    		PPAR Metabolic Disease
    KD-3010 is a potent, orally active, and selective PPARδ agonist.
  • HY-101738A
    Peliglitazar racemate

    BMS 426707-01 racemate

    		 PPAR Metabolic Disease
    Peliglitazar racemate is the racemate of Peliglitazar. Peliglitazar is a novel dual α/γ PPAR activator.
  • HY-108523
    LG100754

    UVI 2112

    		 RAR/RXR Metabolic Disease
    LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR.
  • HY-117103
    AMG131

    INT131

    		 PPAR Metabolic Disease
    AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM).
  • HY-108022
    Azemiglitazone

    MSDC-0602

    		 Mitochondrial Metabolism Metabolic Disease
    Azemiglitazone (MSDC-0602), a PPARγ-sparing thiazolidinedione (TZD), interacts with the mitochondrial pyruvate carrier (MPC) and inhibits its activity and has the potential for type 2 diabetes study with reducing risk of PPARγ-mediated side effects.
  • HY-128671
    6-​Thioinosine

    6TI; 6-Mercaptopurine riboside

    		 Nucleoside Antimetabolite/Analog Metabolic Disease
    6-​Thioinosine (6TI) is a purine antimetabolite, acts as an anti-adipogenesis agent, downregulates mRNA levels of PPAR γ and C/EBPα, as well as PPAR γ target protein such as LPL, CD36, aP2, and LXRα.
  • HY-124581
    DS-6930

    		PPAR Metabolic Disease
    DS-6930 is a potent and selective agonist of PPARγ, with an EC50 of 41 nM. DS-6930 could robust reduce plasma glucose (PG), and with fewer PPARγ-related adverse effects than Rosiglitazone. DS-6930 can be used for the research of diabetes.
  • HY-114739
    MA-0204

    		PPAR Metabolic Disease
    MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD).
  • HY-10838
    GW 501516

    GW 1516; GSK-516

    		 PPAR Autophagy Metabolic Disease Cancer
    GW 501516 (GW 1516) is a PPARδ agonist with an EC50 of 1.1 nM.
  • HY-107542
    Oleoylethanolamide

    N-Oleoylethanolamide; Oleamide MEA; Oleic acid monoethanolamide

    		 Endogenous Metabolite PPAR Metabolic Disease Cardiovascular Disease
    Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
  • HY-16737
    Elafibranor

    GFT505

    		 PPAR Metabolic Disease
    Elafibranor (GFT505) is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively.
  • HY-N8122
    24-Methylenecycloartanyl ferulate

    		Akt Cancer
    24-Methylenecycloartanyl ferulate is a γ-oryzanol compound. 24-Methylenecycloartanyl ferulate promotes parvin-beta expression in human breast cancer cells. 24-Methylenecycloartanyl ferulate is a potential ATP-competitive Akt1 inhibitor (EC50= 33.3μM).
  • HY-15577
    GSK3787

    		PPAR Cancer
    GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.
  • HY-N0625A
    Alpinetin

    		PPAR Inflammation/Immunology Cancer
    Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity.
  • HY-Y0078
    Cinnamyl Alcohol

    		PPAR Metabolic Disease
    Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, with anti-obesity activity.
  • HY-14831
    Arhalofenate

    MBX 102; JNJ 39659100

    		 PPAR Metabolic Disease
    Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.
  • HY-N0783
    Eupatilin

    		PPAR Autophagy Inflammation/Immunology Neurological Disease Cancer
    Eupatilin, a lipophilic flavonoid isolated from Artemisia species, is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.
  • HY-101746
    GSK376501A

    		PPAR Metabolic Disease
    GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.
  • HY-B1026
    Adelmidrol

    		NF-κB COX PPAR Inflammation/Immunology
    Adelmidrol exerts important anti-inflammatory effects that are partly dependent on PPARγ. Adelmidrol reduces NF-κB translocation, and COX-2 expression.
  • HY-N2209
    Angeloylgomisin H

    		PPAR Metabolic Disease
    Angeloylgomisin H, as a major lignin extract of Schisandra rubriflora, has the potential to improve insulin-stimulated glucose uptake by activating PPAR-γ.
  • HY-19522
    Seladelpar

    MBX-8025

    		 PPAR Metabolic Disease
    Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist.
  • HY-N0604
    Ginsenoside Rh1

    Prosapogenin A2; Sanchinoside B2; Sanchinoside Rh1

    		 PPAR TNF Receptor Interleukin Related Endogenous Metabolite Inflammation/Immunology
    Ginsenoside Rh1 (Prosapogenin A2) inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
  • HY-N1426
    Raspberry ketone

    Frambione; 4-(4-Hydroxyphenyl)-2-butanone

    		 PPAR Metabolic Disease Cardiovascular Disease
    Raspberry ketone is a major aromatic compound of red raspberry, widely used as a fragrance in cosmetics and as a flavoring agent in foodstuff; also shows PPAR-α agonistic activity.
  • HY-119964
    Cetaben

    		Others Cardiovascular Disease
    Cetaben is a PPARα-independent peroxisome proliferator. Cetaben is a non-fibrate hypolipidemic drug and potently reduces the concentration of cholesterol and triglycerides.
  • HY-N4194
    Glabrone

    		PPAR Metabolic Disease
    Glabrone is an isoflavone isolated from Glycyrrhiza glabra roots. Glabrone exhibits anti-influenza activity and significant PPAR-γ ligand-binding activity.
  • HY-N0704
    Agrimol B

    		Sirtuin PPAR Metabolic Disease
    Agrimol B is a polyphenol derived from Agrimonia pilosa Ledeb, suppresses adipogenesis via inducing SIRT1 translocation and expression, and reducing PPARγ expression.
  • HY-15027
    5-Aminosalicylic Acid

    Mesalamine; 5-ASA; Mesalazine

    		 PPAR PAK NF-κB Endogenous Metabolite Inflammation/Immunology Cancer
    5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-N0014
    Icariin

    Ieariline

    		 Phosphodiesterase (PDE) PPAR Autophagy Inflammation/Immunology Cardiovascular Disease Cancer
    Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.
  • HY-14739
    Choline Fenofibrate

    ABT-335

    		 PPAR COX Cardiovascular Disease
    Choline Fenofibrate (ABT-335), a choline salt of Fenofibric acid (HY-B0760), releases free Fenofibric acid in the gastrointestinal tract. Fenofibric acid is a PPAR activator with antihyperlipidemic effect.
  • HY-133615
    8(14)-Abietenic acid

    		Others Others
    8(14)-Abietenic acid is an abietane diterpenoid. Abietenic acid is racemic of 8(14)-Abietenic acid. Abietenic acid acts as a PPARα/γ dual activator.
  • HY-U00450
    4-O-Methyl honokiol

    		PPAR NF-κB Cancer Inflammation/Immunology
    4-O-Methyl honokiol is a natural neolignan isolated from Magnolia officinalis, acts as a PPARγ agonist, and inhibtis NF-κB activity, used for cancer and inflammation research.
  • HY-N7624
    Methyl oleanonate

    3-Oxoolean-12-en-28-oic acid methyl ester

    		 PPAR Cancer
    Methyl oleanonate is a natural triterpene PPARγ agonist isolated from the species of Pistacia. Methyl oleanonate is a modified oleanolic acid derivative with anti-cancer effects.
  • HY-B1415
    Clofibric acid

    Chlorofibrinic acid

    		 PPAR Drug Metabolite Others
    Clofibric acid (Chlorofibrinic acid), the pharmaceutically active metabolite of lipid regulators Clofibrate, Etofibrate and Etofyllinclofibrate, is a PPARα agonist which exhibits hypolipidemic effects. Clofibric acid also is an herbicide.
  • HY-128400
    4'-Methoxychalcone

    		PARP Metabolic Disease Cancer
    4'-Methoxychalcone regulates adipocyte differentiation through PPARγ activation. 4'-Methoxychalcone modulates the expression and secretion of various adipokines in adipose tissue that are involved in insulin sensitivity.
  • HY-N0163
    Magnolol

    		RAR/RXR PPAR Autophagy Bacterial Cancer Inflammation/Immunology Neurological Disease Cardiovascular Disease
    Magnolol, a natural lignan isolated from the stem bark of Magnolia officinalis, is a dual agonist of both RXRα and PPARγ, with EC50 values of 10.4 µM and 17.7 µM, respectively.
  • HY-N6642
    Ankaflavin

    		PPAR Cancer Inflammation/Immunology
    Ankaflavin, isolated from Monascus-Fermented red rice, is a PPARγ agonist with anti-inlfammatory activity. Ankaflavin exhibits selective cytotoxic effect and induces cell death on cancer cells.
  • HY-U00036A
    Naveglitazar

    LY519818

    		 PPAR Metabolic Disease
    Naveglitazar (LY519818) is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models.
  • HY-120160
    Darglitazone

    CP-86325

    		 PPAR Metabolic Disease Neurological Disease
    Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research.
  • HY-128344
    BR102375

    		PARP Apoptosis Metabolic Disease
    BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC50 value of 0.28 μM and Amax ratio of 98%.
  • HY-U00036
    Naveglitazar racemate

    LY519818 racemate

    		 PPAR Metabolic Disease
    Naveglitazar racemate (LY519818 racemate) is the racemate of Naveglitazar. Naveglitazar is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models.
  • HY-N3026
    Soyasaponin Ab

    		Others Metabolic Disease
    Soyasaponin Ab is a soyasaponin that exerts an anti-obesity effect in 3T3-L1 adipocytes through downregulation of peroxisome proliferator-activated receptor γ (PPARγ).
  • HY-N3027
    Soyasaponin Aa

    		Others Metabolic Disease
    Soyasaponin Aa is a soyasaponin that exerts an anti-obesity effect in 3T3-L1 adipocytes through downregulation of peroxisome proliferator-activated receptor γ (PPARγ).
  • HY-N0364
    Falcarindiol

    		Apoptosis Autophagy PPAR Cancer Infection Metabolic Disease Inflammation/Immunology
    Falcarindiol, an orally active polyacetylenic oxylipin, activates PPARγ and increases the expression of the cholesterol transporter ABCA1 in cells. Falcarindiol induces apoptosis and autophagy. Falcarindiol has anti-inflammatory, antifungal, anticancer and antidiabetic properties.
  • HY-N7687
    Caulophyllogenin

    		PPAR Metabolic Disease Inflammation/Immunology
    Caulophyllogenin is a triterpene saponin extracted from M. polimorpha. Caulophyllogenin is a partial PPARγ agonist, with an EC50 of 12.6 μM. Caulophyllogenin can be used for the research of type-2 diabetes, obesity, metabolic syndrome and inflammation.
  • HY-108568
    15-Deoxy-Δ-12,14-prostaglandin J2

    15d-PGJ2; 15-Deoxy-Δ12,14-PGJ2

    		 PPAR Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM.
  • HY-101491
    SR-18292

    		PGC-1α Autophagy Metabolic Disease
    SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.
  • HY-B0963
    Cloxiquine

    5-Chloro-8-quinolinol

    		 Bacterial Fungal Parasite PPAR Cancer Infection
    Cloxiquine (5-Chloro-8-quinolinol) is an antibacterial, antifungal and antiamoebic agent. Cloxiquine can be used for the research of tuberculosis and dermatoses. Cloxiquine suppresses the growth and metastasis of melanoma cells through activation of PPARγ.
  • HY-131265
    Mesalamine impurity P

    		PPAR PAK NF-κB Cancer Inflammation/Immunology
    Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-B0258
    Gemfibrozil

    CI-719

    		 PPAR Cytochrome P450 Metabolic Disease Cardiovascular Disease
    Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering drug; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
  • HY-N0393
    Glabridin

    		PPAR Reactive Oxygen Species Bacterial Cancer Infection Inflammation/Immunology
    Glabridin is a natural isoflavan from Glycyrrhiza glabra, binds to and activates PPARγ, with an EC50 of 6115 nM. Glabridin exhibits antioxidant, anti-bacterial, anti-nephritic, anti-diabetic, anti-fungal, antitumor, anti-inflammatory, antiosteoporotic, cardiovascular protective, neuroprotective and radical scavenging activities.
  • HY-N0368
    Linalool

    		iGluR Apoptosis Endogenous Metabolite Cancer Cardiovascular Disease
    Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity.Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome.
  • HY-N0479
    Licarin B

    (-)-Licarin B

    		 PPAR GLUT Metabolic Disease
    Licarin B, a nitric oxide production inhibitor extracted from the component of the seeds of Myristica fragrans, improves insulin sensitivity via PPARγ and activation of GLUT4 in the IRS-1/PI3K/AKT pathway.
  • HY-N1990
    Gypenoside XLIX

    		PPAR Inflammation/Immunology Cardiovascular Disease
    Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells.
  • HY-121538
    CUDA

    		Epoxide Hydrolase PPAR Cardiovascular Disease
    CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease.
  • HY-15027S
    5-Aminosalicylic Acid-D3 hydrochloride

    Mesalamine-D3 hydrochloride; 5-ASA-D3 hydrochloride; Mesalazine-D3 hydrochloride

    		 PPAR PAK NF-κB Endogenous Metabolite Inflammation/Immunology Cancer
    5-Aminosalicylic Acid-D3 (Mesalamine-D3) hydrochloride is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) hydrochloride acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
  • HY-122716
    PTGR2-IN-1

    		Others Others
    PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC50 of ~0.7 μM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells.
  • HY-130120
    HWL-088

    		GPR40 PPAR Metabolic Disease
    HWL-088 is a highly potent and orally active free fatty acid receptor 1 (FFA1/GPR40) agonist (EC50 of 18.9 nM) with moderate PPARδ activity (EC50 of 570.9 nM) . HWL-088 improves glucose and lipid metabolism, and has anti-diabetic effects.
  • HY-N1280
    Semilicoisoflavone B

    		Amyloid-β Neurological Disease
    Semilicoisoflavone B, an isoflavone, mainly derived from Glycyrrhiza uralensis Fisch.. Semilicoisoflavone B reduces amyloid β (Aβ) secretion by inhibiting β-secretase-1 (BACE1) expression and activity. Semilicoisoflavone B decreases BACE1 expression mainly through increasing PPARγ expression and inhibiting STAT3 phosphorylation.
  • HY-N1967
    Dihydrocurcumin

    		Fatty Acid Synthase (FASN) Metabolic Disease
    Dihydrocurcumin, a major metabolites of curcumin, reduces lipid accumulation and oxidative stress. Dihydrocurcumin regulates mRNA and protein expression levels of SREBP-1C, PNPLA3 and PPARα, increases protein expression levels of pAKT and PI3K, and reduced the levels of cellular NO and ROS via Nrf2 signaling pathways.
  • HY-14166
    MK-886

    L 663536

    		 FLAP Leukotriene Receptor PPAR Apoptosis Cancer
    MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis.
  • HY-14649
    Retinoic acid

    Vitamin A acid; all-trans-Retinoic acid; ATRA

    		 RAR/RXR PPAR Endogenous Metabolite Autophagy Cancer
    Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
  • HY-N0292
    Oleuropein

    		PPAR Apoptosis Aromatase Cancer Inflammation/Immunology Cardiovascular Disease
    Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase.
  • HY-113884B
    (S)-Coriolic acid

    13(S)-HODE

    		 PPAR Mitochondrial Metabolism Cancer Inflammation/Immunology
    (S)-Coriolic acid (13(S)-HODE), the product of 15-lipoxygenase (15-LOX) metabolism of linoleic acid, functions as the endogenous ligand to activate PPARγ. (S)-Coriolic acid is an important intracellular signal agent and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial injury.
  • HY-N5097
    13-Oxo-9E,11E-octadecadienoic acid

    		PPAR Metabolic Disease
    13-Oxo-9E,11E-octadecadienoic acid, an isomer of 9-oxo-ODA, is a potent PPARα activator derived from tomato juice. 13-Oxo-9E,11E-octadecadienoic acid decreases plasma and hepatic triglyceride in obese diabetic mice.
  • HY-128932
    Cefminox sodium

    MT-141

    		 Bacterial PPAR Prostaglandin Receptor Antibiotic Infection Cardiovascular Disease Endocrinology
    Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity. Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension.
  • HY-B2163
    Astaxanthin

    		PPAR Reactive Oxygen Species Cancer Cardiovascular Disease
    Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is a modulator of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity. Astaxanthin has potential in the study of various diseases, such as cancers and Parkinson’s disease, cardiovascular disease. Due to its bright red colour, Astaxanthin could be used as a food colorant in animal feeds.
  • HY-128872
    EHP-101

    VCE-​004.8

    		 PPAR Cannabinoid Receptor HIF/HIF Prolyl-Hydroxylase Metabolic Disease Inflammation/Immunology
    EHP-101 (VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. EHP-101 inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. EHP-101, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. EHP-101 attenuates adipogenesis and prevents diet-induced obesity.
  • HY-N4103
    Fucosterol

    		PARP Endogenous Metabolite Cancer Metabolic Disease
    Fucosterol is a sterol isolated from algae, seaweed or diatoms. Fucosterol exhibits various biological activities, including antioxidant, anti-adipogenic, blood cholesterol reducing, anti-diabetic and anti-cancer activities. Fucosterol regulates adipogenesis via inhibition of PPARα and C/EBPα expression and can be used for anti-obesity agents development research.
  • HY-17356
    Fenofibrate

    		PPAR Cytochrome P450 Autophagy Cardiovascular Disease Cancer
    Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
  • HY-100348
    EPI-001

    		Androgen Receptor PPAR Apoptosis Cancer
    EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer.
  • HY-N0222
    Avicularin

    		Others Cancer Inflammation/Immunology
    Avicularin is a bio-active flavonoid from plants, anti-inflammatory, anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities. Avicularin exhibits anti-inflammatory activity through the suppression of ERK signaling pathway in LPS-stimulated RAW 264.7 macrophage cells. Avicularin ameliorates human hepatocellular carcinoma via the regulation of NF κB (p65), COX 2 and PPAR γ activities.
  • HY-120327
    KY-226

    		Phosphatase Metabolic Disease Neurological Disease
    KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury.
  • HY-W010983
    SC-236

    		COX PPAR Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    SC-236 is an orally active COX-2 specific inhibitor (IC50 = 10 nM) and a PPARγ agonist. SC-236 suppresses activator protein-1 (AP-1) through c-Jun NH2-terminal kinase. SC-236 exerts anti-inflammatory effects by suppressing phosphorylation of ERK in a murine model.
  • HY-N2453
    Convallatoxin

    		PPAR NF-κB P-glycoprotein Cancer Inflammation/Immunology
    Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties.
  • HY-15697
    TUG-770

    		GPR40 Metabolic Disease
    TUG-770 is a potent, selective and orally active GPR40/FFA1 agonist with an EC50 of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research.
  • HY-17356S
    Fenofibrate-d6

    		PPAR Cytochrome P450 Autophagy Cardiovascular Disease Cancer
    Fenofibrate-d6 is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
  • HY-101676
    RG-12525

    NID 525

    		 Leukotriene Receptor PPAR Cytochrome P450 Metabolic Disease
    RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.
  • HY-N2118
    Bilobetin

    		PPAR PKA Metabolic Disease
    Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.
  • HY-123986
    CTPI-2

    		Mitochondrial Metabolism Cancer Inflammation/Immunology
    CTPI-2 is a third-generation mitochondrial citrate carrier SLC25A1 inhibitor with a KD of 3.5 μM. CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. CTPI-2 halts salient alterations of NASH reverting steatosis, preventing the evolution to steatohepatitis, reducing inflammatory macrophage infiltration in the liver and adipose tissue, and starkly mitigating obesity induced by a high-fat diet. Antitumor activity.
  • HY-15589
    GW9508

    		GPR40 Potassium Channel Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.
  • HY-N0515
    Ophiopogonin D

    		PPAR NF-κB Calcium Channel Inflammation/Immunology Cardiovascular Disease
    Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca 2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.