Search Result
Results for "
PPAR Agonist
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
25
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-U00340
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PPAR
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Metabolic Disease
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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.
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- HY-N0234
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7-O-Methylbavachin; Bavachinin A
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Amyloid-β
PPAR
HIF/HIF Prolyl-Hydroxylase
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Inflammation/Immunology
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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. .
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- HY-163443
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PPAR
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Others
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PPAR agonist 4 (Compound 12) is an orally active agonist for peroxisome proliferator-activated receptor (PPAR), which activates PPARα, PPARδ and PPARγ with EC50s of 0.7, 0.7 and 1.8 μM, respectively. PPAR agonist 4 exhibits anti-liver fibrosis efficacy .
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- HY-160003
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PPAR
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Metabolic Disease
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PPARγ agonist 9 is an agonist of PPARγ. PPARγ agonist 9 is the analogue of lysophosphatidic acid with an EC50 more than 10 μM for LPA3 receptor .
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- HY-148922
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PPAR
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Metabolic Disease
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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 .
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- HY-144111
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PPAR
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Inflammation/Immunology
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PPARα/δ agonist 1 is a potent PPARα/PPARδ dual agonist (PPARα EC50=7.0 nM; PPARδ EC50=8.4 nM). PPARα/δ agonist 1 is a high selectivity over PPARγ (PPARγ EC50=1316.1 nM). PPARα/δ agonist 1 has the potential for the research of nonalcoholic steatohepatitis .
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- HY-162123
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PPAR
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Inflammation/Immunology
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PPARα/γ agonist 4 (compound 14) is a potent PPARα and PPARδ agonist with EC50s of 3255 nM and 1475 nM for human PPARα and PPARβ/δ, respectively. PPARα/γ agonist 4 shows anti-inflammatory effects .
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- HY-146480
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PPAR
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Cancer
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PPARγ agonist 5 (Compound 1) is a potent and selective agonist of PPARγ. PPARγ agonist 5 has the potential for the research of cancer diseases .
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- HY-146482
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PPAR
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Cancer
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PPARγ agonist 6 (Compound 12) is a potent and selective agonist of PPARγ. PPARγ agonist 6 has the potential for the research of cancer diseases .
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- HY-146438
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PPAR
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Cancer
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PPARγ agonist 3 (Compound 18a) is a potent and selective agonist of PPARγ. PPARγ agonist 3 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 3 exerts antitumor potency only in combination with Imatinib .
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- HY-146439
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PPAR
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Cancer
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PPARγ agonist 4 (Compound 18b) is a potent and selective agonist of PPARγ. PPARγ agonist 4 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 4 exerts antitumor potency only in combination with Imatinib .
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- HY-143239
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PPAR
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Metabolic Disease
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PPARα/γ agonist 1 is a potent and dual PPARα/γ partial agonist with EC50 values of 28 nM and 69 nM for PPARα and PPARγ, respectively. PPARα/γ agonist 1 is a promising prototype for dyslipidemia and diabetes research .
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- HY-147511
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PPAR
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Others
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PPARγ agonist 7 (Compound 3a) is a potent and selective agonist of PPARγ. PPARγ agonist 7 promotes adiponectin production in human bone marrow mesenchymal stem cells (hBM-MSCs) as a novel PPARγ full agonist (EC50, 4.34 μM) .
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- HY-153982
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PPAR
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Metabolic Disease
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PPARγ agonist 8 is an agonist of PPARγ. PPARγ agonist 8 induces peroxisome proliferator response element (PPRE)-luciferase activity with an EC50 of 0.2 μM .
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- HY-162320
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PPAR
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Metabolic Disease
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PPARγ agonist 12 (compound 9i) is a potent and selective PPARγ agonist with EC50s of 3.98 and 15.42 μM against PPARγ and PPARδ, respectively. PPARγ agonist 12 improves insulin secretion and has anti-diabetic effect .
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- HY-146731
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PPAR
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Cardiovascular Disease
Metabolic Disease
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PPARγ agonist 1 (compound 15) is a potent agonist of PPARγ. PPARγ agonist 1 shows high efficacy to activate hPPARγ without raising a full agonism and probably avoiding adverse effects. PPARγ agonist 1 has the potential for the research of cardiovascular diseases associated with metabolic disorders .
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- HY-100120
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- HY-121542
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PPAR
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Metabolic Disease
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PPARδ agonist 10 (compound 7) is an orally active, selective, and partial agonist of PPARδ, with EC50 values of 0.053 μM and 0.30 µM for hPPARδ(LBD)-GAL4 and mPPARδ, respectively. PPARδ agonist 10 is a partial PPARδ agonist in transactivation assay but a full agonist on free fatty acids (FFA) oxidation in muscle cells both in vitro and in vivo. PPARδ agonist 10 can be used for dyslipidemia research .
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- HY-14817
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PPM 204
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PPAR
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Metabolic Disease
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Indeglitazar (PPM 204) is an orally available PPAR pan-agonist for all three PPARα, PPARδ and PPARγ .
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- HY-120596
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PPAR
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Neurological Disease
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PPARδ/γ agonist 1 sodium is a chemically unique and brain penetrant dual PPAR delta/gamma agonist. PPARδ/γ agonist 1 sodium can be used for the research of Alzheimer’s disease .
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- HY-146742
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PPAR
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Metabolic Disease
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PPARγ agonist 2 is a potent PPARγ partial agonist and can be used for metabolic disease research .
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- HY-116468
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- HY-107901
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PPAR
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Cardiovascular Disease
Metabolic Disease
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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.
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- HY-100428
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MCC-555; Isaglitazone
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Netoglitazone is a dual agonist of PPARα and PPARγ with antihyperglycemic activity .
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- HY-B0287
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PPAR
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Metabolic Disease
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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.
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- HY-141494
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PPAR
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Metabolic Disease
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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 .
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- HY-13928
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- HY-20019
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PPAR
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Metabolic Disease
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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.
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- HY-13861
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PPAR
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Cardiovascular Disease
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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.
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- HY-149429
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PPAR
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Metabolic Disease
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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%) .
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- HY-163294
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PPAR
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Metabolic Disease
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PPARγ agonist 10 (compound 33g) is a PPARγ agonist, and stimulats the insulin secretion, glucose uptake and insulin Sensitivity in βTC6 Cells .
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- HY-16086
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DRF 2593; NN 2344
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PPAR
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Metabolic Disease
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Balaglitazone is a selective partial PPARγ agonist with an EC50 of 1.351 μM for human PPARγ.
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- HY-N9333
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- HY-10678
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PPAR
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Cardiovascular Disease
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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.
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- HY-106266
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Carfloglitazar
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PPAR
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Metabolic Disease
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Chiglitazar (Carfloglitazar) is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.
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- HY-B0637
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BM15075
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PPAR
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Cardiovascular Disease
Metabolic Disease
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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.
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- HY-104049
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IVA337
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PPAR
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Metabolic Disease
Cancer
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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.
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- HY-143862
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PPAR
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Metabolic Disease
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Pparδ agonist 7 is a potent agonist of Pparδ. The peroxisome proliferator-activated receptor (PPAR) is a member of the intranuclear receptor transcription factor superfamily that plays a key role in the regulation of metabolic homeostasis, inflammation, cell growth and differentiation in vivo. Pparδ agonist 7 has the potential for the research of non-alcoholic fatty liver disease (NAFLD) (extracted from patent WO2019105234A1, compound TM4) .
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- HY-143863
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PPAR
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Metabolic Disease
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Pparδ agonist 8 is a potent agonist of Pparδ. The peroxisome proliferator-activated receptor (PPAR) is a member of the intranuclear receptor transcription factor superfamily that plays a key role in the regulation of metabolic homeostasis, inflammation, cell growth and differentiation in vivo. Pparδ agonist 8 has the potential for the research of non-alcoholic fatty liver disease (NAFLD) (extracted from patent WO2021169769A1, compound TM2) .
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- HY-16995
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Wy-14643
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PPAR
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Metabolic Disease
Inflammation/Immunology
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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.
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- HY-B0287S
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PPAR
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Metabolic Disease
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Clofibrate-d4 is the deuterium labeled Clofibrate. 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.
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- HY-162122
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PPAR
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Inflammation/Immunology
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PPARα/γ agonist 3 (Compound 4) is a dual agonist of PPARα/γ. PPARα/γ agonist 3 has anti-inflammatory activity, significantly reducing inflammatory markers such as IL-6 and MCP-1 on THP-1 macrophages through NF-κB activation. PPARα/γ agonist 3 can be used in the study of metabolic syndrome and metabolic dysfunction-related fatty liver disease (MAFLD) .
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- HY-146733
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- HY-B0287R
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PPAR
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Metabolic Disease
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Clofibrate (Standard) is the analytical standard of Clofibrate. This product is intended for research and analytical applications. 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.
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- HY-B0637S
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PPAR
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Cardiovascular Disease
Metabolic Disease
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Bezafibrate-d6 is the deuterium labeled Bezafibrate. 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.
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- HY-B0637S1
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BM15075-d4
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Isotope-Labeled Compounds
PPAR
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Cardiovascular Disease
Metabolic Disease
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Bezafibrate-d4 is deuterium labeled Bezafibrate. 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.
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- HY-101649
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TAK-559
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PPAR
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Cardiovascular Disease
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Imiglitazar (TAK559) is a potent and dual human PPARα and PPARγ1 agonist with EC50 values of 67 and 31 nM.
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- HY-U00014
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PPAR
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Metabolic Disease
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AVE-8134 is a potent PPARα agonist, with EC50 values of 100 and 3000 nM for human and rodent PPARα receptor, respectively.
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- HY-19937
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PPAR
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Metabolic Disease
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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.
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- HY-106278
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PPAR
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Metabolic Disease
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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 .
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- HY-19937A
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PPAR
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Metabolic Disease
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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.
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- HY-19383
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PTP 112
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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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- HY-14792
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Efatutazone; CS-7017; RS5444
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PPAR
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Cancer
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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.
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- HY-14601
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U 72107A; AD 4833
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PPAR
Ferroptosis
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Metabolic Disease
Cancer
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Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
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- HY-111775
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PPAR
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Metabolic Disease
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LJ570 is a PPARα/PPARγ dual agonist with EC50s of 1.05 and 0.12 μM, respectively .
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- HY-17633
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NPS-005; SJP-0035
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PPAR
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Neurological Disease
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Fonadelpar is a PPARδ agonist, used in the research of neuroparalytic keratopathy.
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- HY-17618
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(R)-K-13675
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Pemafibrate is a highly selective PPARα agonist, with an EC50 of 1 nM.
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- HY-148351
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PPAR
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Cancer
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BAY-0069 is a potent and selective PPARγ inverse agonist with an IC50 value of 6.3 nM and 24 nM for human PPARγ and mouse PPARγ. BAY-0069 can be used to research cancer .
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- HY-147757
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PPAR
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Metabolic Disease
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PPARγ/δ modulator 1 (compound 3e) is a potent PPAR modulator. PPARγ/δ modulator 1 is a PPARδ antagonist and a PPARγ partial agonist , with Ki values of 14.4 nM and 5.31 μM, respectively. PPARγ/δ modulator 1 has the EC50 of 7.3 and 12.6 μM for PPARδ corepression and adiponectin production, respectively .
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- HY-14792B
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Efatutazone dihydrochloride; CS-7017 dihydrochloride; RS5444 dihydrochloride
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PPAR
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Cancer
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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.
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- HY-110118
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PPAR
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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 .
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- HY-116521
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- HY-19522A
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MBX-8025 sodium salt; RWJ-800025 sodium salt
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PPAR
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Metabolic Disease
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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.
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- HY-17445
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BMS-298585
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PPAR
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Metabolic Disease
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Muraglitazar is a PPAR α/γ dual agonist for the research of type 2 diabetes and associated dyslipidemia. Muraglitazar shows potent activity in vitro at human PPARα (EC50 = 320 nM) and PPARγ(EC50 = 110 nM) .
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- HY-117761
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PPAR
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Metabolic Disease
Cancer
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MHY908 is a potent dual agonist of PPARα and PPARγ . MHY908 also inhibits melanogenesis through inhibition of mushroom tyrosinase activity .
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- HY-116247
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PPAR
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Metabolic Disease
Inflammation/Immunology
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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 .
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- HY-117196
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- HY-50935S
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- HY-111068
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- HY-15655
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PPAR
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Neurological Disease
Metabolic Disease
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GW 1929 is an orally active peroxisome proliferator-activated receptor-γ (PPARγ) 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. GW 1929 (hydrochloride) has antidiabetic efficacy and neuroprotective potential .
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- HY-17444
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PPAR
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Metabolic Disease
Cancer
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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 .
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- HY-16421
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(-)-DRF 2725; NNC 61-0029
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PPAR
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Metabolic Disease
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Ragaglitazar is a PPARα and PPARγ agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. Ragaglitazar improves glycemic control and lipid profile in type 2 diabetic.
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- HY-10838
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- HY-106181
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R-106056
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PPAR
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Metabolic Disease
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Rivoglitazone is a thiazolidinedione-derivative PPARγ agonist for the research of type 2 diabetes mellitus.
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- HY-103034
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PPAR
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Metabolic Disease
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Sipoglitazar is an orally active agonist of PPAR. Sipoglitazar can be used to study diabetes .
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- HY-151963
-
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PPAR
Glucocorticoid Receptor
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Metabolic Disease
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PPARγ/GR modulator 1 is an orally active dual agonist of PPARγ and glucocorticoid receptor (GR), with Kis of 3.3 and 33.6 μM, respectively. PPARγ/GR modulator 1 can be used for the research of metabolic diseases, such as diabetes .
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- HY-50665
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LY-674
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PPAR
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Metabolic Disease
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LY518674 is a potent, selective PPARα agonist, 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 .
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- HY-13956S
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U 72107-d4
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PPAR
Ferroptosis
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Metabolic Disease
Cancer
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Pioglitazone-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[1].
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- HY-112813
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- HY-124244
-
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PPARδ/γ Agonist 1
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PPAR
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Neurological Disease
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DB-959 (PPARδ/γ agonist 1) is a potent dual PPAR delta/gamma inhibitor. DB-959 can be used for Alzheimer’s disease research .
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- HY-50935
-
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CS-045
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PPAR
Autophagy
Apoptosis
Ferroptosis
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Metabolic Disease
Cancer
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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.
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- HY-119248
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MK-0767
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PPAR
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Metabolic Disease
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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.
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- HY-19937S1
-
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Isotope-Labeled Compounds
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Others
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Saroglitazar-d4 is the deuterium-labeled Saroglitazar (HY-19937). Saroglitazar-d4 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.
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- HY-17386S
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- HY-14728
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R1439; RO0728804
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PPAR
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Metabolic Disease
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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 .
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- HY-113473
-
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PPAR
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Metabolic Disease
Inflammation/Immunology
Cancer
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10-Nitrolinoleic acid is a potent peroxisome proliferator-activated receptor γ (PPARγ) agonist. 10-Nitrolinoleic acid competes with [ 3H]Rosiglitazone for binding to PPAR-γ, with an IC50 of 0.22 μM .
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- HY-13956
-
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U 72107
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PPAR
Ferroptosis
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Metabolic Disease
Cancer
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Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) 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. Pioglitazone can be used in diabetes research .
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- HY-116699
-
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PPAR
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
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-13956B
-
|
U 72107 potassium
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
|
Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research .
|
-
- HY-16737
-
|
GFT505
|
PPAR
|
Metabolic Disease
|
|
Elafibranor (GFT505) is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively.
|
-
- HY-107542
-
-
- HY-105074
-
|
GI262570; GI262570X
|
PPAR
|
Metabolic Disease
|
|
Farglitazar is a PPARγ agonist that has significant therapeutic benefits such as glycemic control in type 2 diabetic patients.
|
-
- HY-148352
-
|
|
PPAR
|
Cancer
|
|
BAY-4931 is a potent, covalent and selective PPARγ inverse-agonist with an IC50 of 0.17 nM .
|
-
- HY-110022
-
|
|
PPAR
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
GW1929 hydrochloride is an orally active peroxisome proliferator-activated receptor-γ (PPARγ) 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. GW1929 hydrochloride has antidiabetic efficacy and neuroprotective potential. GW1929 hydrochloride suppresses neuronal apoptosis and shows anti-inflammatory potential .
|
-
- HY-108572
-
|
|
PPAR
|
Cardiovascular Disease
Metabolic Disease
|
|
S26948 is a specific peroxisome proliferator-activated receptor γ (PPARγ) modulator (EC50=8.83 nM) with potent antidiabetes and antiatherogenic effects. S26948 is a specific high-affinity agonist for PPARγ .
|
-
- HY-118514
-
|
|
PPAR
|
Metabolic Disease
|
|
CAY10514 is an aromatic of 8(S)-HETE. CAY10514 acts as a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ with IC50 of 0.173 and 0.642 μM, respectively .
|
-
- HY-14601R
-
|
U 72107A (Standard); AD 4833 (Standard)
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
|
Pioglitazone (hydrochloride) (Standard) is the analytical standard of Pioglitazone (hydrochloride). This product is intended for research and analytical applications. 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-N6869
-
|
|
Antibiotic
PPAR
Bacterial
Fungal
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice .
|
-
- HY-13956S1
-
|
|
Isotope-Labeled Compounds
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[1][2].
|
-
- HY-108523
-
|
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
-
|
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-108571
-
|
|
PPAR
|
Metabolic Disease
|
|
CP-775146 is a selective PPARα agonist that binds strongly to the PPARα ligand. CP-775146 efficiently alleviates obesity-induced liver damage, prevents lipid accumulation by activating the liver fatty acid β-oxidation pathway .
|
-
- HY-N2025
-
|
|
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-117727
-
|
MIN-102; Hydroxypioglitazone
|
PPAR
|
Metabolic Disease
|
|
Leriglitazone (MIN-102; Hydroxypioglitazone), a metabolite of pioglitazone. Leriglitazone 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 binds to the PPARγ C-terminal ligand-binding domain (LBD) with a Ki of 1.2 μM，Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an EC50 of 680 nM .
|
-
- HY-117727A
-
|
MIN-102 hydrochloride; Hydroxypioglitazone hydrochloride
|
PPAR
|
Metabolic Disease
|
|
Leriglitazone (MIN-102; Hydroxypioglitazone) hydrochloride, a metabolite of pioglitazone. Leriglitazone hydrochloride 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 hydrochloride binds to the PPARγ C-terminal ligand-binding domain (LBD) with a Ki of 1.2 μM，Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an EC50 of 680 nM .
|
-
- 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 .
|
-
- HY-14831
-
|
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-129683
-
|
|
PPAR
|
Metabolic Disease
|
|
AM3102 is an oleoylethanolamide (OEA) analog. AM3102 is an endogenous high-affinity PPAR-alpha agonist. AM3102 resists enzymatic hydrolysis, activates PPAR-alpha with high potency in vitro, and persistently reduces feeding when administered in vivo either parenterally or orally .
|
-
- HY-19522
-
|
MBX-8025
|
|
|
|
Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist .
|
-
- HY-N6807S
-
-
- HY-124581
-
|
|
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-117422
-
|
11-Oxo-prosta-5Z,12E,14Z-trien-1-oic acid
|
PPAR
|
Cancer
|
|
CAY10410 (11-Oxo-prosta-5Z), a 15d-PGJ2 analog, is a potent PPARγ agonist. CAY10410 has the ability to activate PPARγ in human B cells without killing B lymphocytes .
|
-
- HY-101292
-
|
|
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-123654
-
|
|
PPAR
|
Neurological Disease
|
|
L-796449 is a potent PPARγ agonist. L-796449 shows neuroprotective. L-796449 has the potential for the research of stroke .
|
-
- HY-156977
-
|
|
PPAR
|
Cardiovascular Disease
|
|
Sitofibrate is a Clofibrate (HY-B0287) derivative. Sitofibrate is aperoxisome proliferator activated receptor-α (PPAR-α) agonist. Sitofibrate is an antihyperlipidemic agent .
|
-
- HY-N0783
-
-
- HY-107542S2
-
-
- HY-107542S
-
-
- HY-16737A
-
|
(E/Z)-GFT505
|
PPAR
|
Metabolic Disease
|
|
(E/Z)-Elafibranor ((E/Z)-GFT505) is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively .
|
-
- HY-117727S
-
|
MIN-102-d4; Hydroxypioglitazone-d4
|
Isotope-Labeled Compounds
PPAR
|
Metabolic Disease
|
|
Leriglitazone-d4 (MIN-102-d4; Hydroxypioglitazone-d4) is deuterium labeled Leriglitazone. 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-B1415
-
|
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-U00450
-
|
|
PPAR
NF-κB
|
Inflammation/Immunology
Cancer
|
|
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
-
|
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 lentiscus var. Chia . Methyl oleanonate is a modified oleanolic acid derivative with anti-cancer effects .
|
-
- HY-160161
-
|
|
PPAR
|
Cancer
|
|
BAY-5094 is a PPAR gamma (PPARG) inverse agonist. BAY-5094 has oral activity. BAY-5094 can be used in the research of luminal bladder cancer .
|
-
- HY-N0163
-
-
- HY-U00036A
-
|
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-121900
-
|
|
PPAR
|
Metabolic Disease
Endocrinology
|
|
LT175, a dual PPARα/γ ligand, is an orally active partial agonist against PPARγ(hPPARα:EC50=0.22 μm; mPPARα:EC50=0.26 μm; hPPARγ:EC50=0.48 μm). LT175 interacts with PPARγ and affects the recruitment of the coregulators cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1). LT175 interacts with PPARγ in a hydrophobic region called “diphenyl pocket”. LT175 has potent insulin-sensitizing effects and reduced adipogenic properties .
|
-
- HY-120160
-
|
CP-86325
|
PPAR
|
Neurological Disease
Metabolic 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-U00036
-
|
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-128344
-
|
|
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-120160A
-
|
CP 86325 Sodium
|
PPAR
|
Neurological Disease
Metabolic Disease
|
|
Darglitazone Sodium, a thiazolidinedione, is an orally active, potent, and selective PPAR-γ (peroxisome proliferator-activated receptor) agonist. Darglitazone Sodium is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research .
|
-
- HY-113631
-
|
|
PPAR
|
Neurological Disease
Metabolic Disease
|
|
Amorfrutin B is a highly potent natural peroxisome proliferation-activated receptor γ (PPARγ) agonist with oral activity with Ki values of 19 nM and EC50 values of 73 nM, respectively. Amorfrutin B has hypoglycemic and neuroprotective activities .
|
-
- HY-N7687
-
|
|
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-N0783R
-
|
|
PPAR
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Eupatilin (Standard) is the analytical standard of Eupatilin. This product is intended for research and analytical applications. Eupatilin, a lipophilic flavonoid isolated from Artemisia argyi Lévl. et Van., is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.
|
-
- HY-15027
-
-
- HY-B1415S
-
|
Chlorofibrinic acid-d4
|
PPAR
Drug Metabolite
|
Others
|
|
Clofibric acid-d4 is the deuterium labeled Clofibric acid. 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[1][2][3].
|
-
- HY-113827
-
|
|
Nuclear Hormone Receptor 4A/NR4A
|
Inflammation/Immunology
|
|
THPN is a potent Nur77 agonist. THPN specifically binds the LBD of Nur77 (TR3) but not that of retinoic acid receptor α and PPARγ with a Kd of 270 nM. THPN leads to Nur77 translocation to the mitochondria to induce autophagic cell death in melanoma .
|
-
- HY-112597
-
|
REN001 free acid; HPP593 free acid; PPARδ Agonist
|
PPAR
|
Metabolic Disease
|
|
Mavodelpar free acid is a PPARδ agonist extracted from patent US20180071304, compound example 10. Mavodelpar (free acid) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-131265
-
|
|
PPAR
PAK
NF-κB
|
Inflammation/Immunology
Cancer
|
|
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-111616
-
|
|
PPAR
Angiotensin Receptor
|
Others
|
|
GSK1820795A, as a telmisartan analog, is a selective hGPR132a antagonist. GSK1820795A blocks activation of yeast cells expressing hGPR132a by N-acylamides . GSK1820795A is also a angiotensin II antagonists and partial PPARγ agonists (compound 38) .
|
-
- HY-B1415R
-
|
Chlorofibrinic acid (Standard)
|
PPAR
Drug Metabolite
|
Others
|
|
Clofibric acid (Standard) is the analytical standard of Clofibric acid. This product is intended for research and analytical applications. 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-15027S
-
-
- HY-17386
-
-
- HY-N6642
-
|
|
PPAR
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Ankaflavin, isolated from Monascus-Fermented red rice, is an orally active PPARγ agonist. Ankaflavin exhibits selective cytotoxic effect and induces cell death through apoptosis on cancer cells. Ankaflavin has anti-inflammatory, anti-cancer, antiatherosclerotic, and hypolipidemic effects .
|
-
- HY-17386A
-
|
BRL 49653 hydrochloride
|
|
|
|
Rosiglitazone (BRL 49653) hydrochloride is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone hydrochloride is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone hydrochloride can be used in the research of obesity and diabetes, senescence, ovarian cancer .
|
-
- HY-17386B
-
-
- HY-B0205
-
|
CV 11974
|
Angiotensin Receptor
PPAR
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Candesartan (CV 11974) is an orally active angiotensin II AT1-Receptor blocker and PPAR-γ agonist. Candesartan has potent and long-lasting antihypertensive effects. Candesartan can be used for the research of hypertension, chronic heart failure (CHF) and Traumatic brain injury (TBI) .
|
-
- HY-15027S1
-
-
- HY-130120
-
|
|
Free Fatty Acid Receptor
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-15027S2
-
|
Mesalamine-13C6; 5-ASA-13C6; Mesalazine-13C6
|
PPAR
PAK
NF-κB
Endogenous Metabolite
|
|
|
5-Aminosalicylic acid- 13C6 is the 13C labeled 5-Aminosalicylic Acid[1]. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[2][3][4].
|
-
- HY-108568
-
|
15d-PGJ2; 15-Deoxy-Δ12,14-PGJ2
|
PPAR
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
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-N9768
-
|
9-oxo-ODA
|
Fungal
PPAR
|
Infection
|
|
(10E,12E)-9-Oxo-10,12-octadecadienoic acid (9-oxo-ODA) is a PPARα agonist that can be isolated from the basidiomycete Gomphus floccosus. (10E,12E)-9-Oxo-10,12-octadecadienoic acid enhances fatty acid oxidation through PPARα activation, thereby inhibiting triglyceride accumulation. (10E,12E)-9-Oxo-10,12-octadecadienoic acid also has antifungal (Fungal) activity .
|
-
- HY-14649
-
|
Vitamin A acid; all-trans-Retinoic acid; ATRA
|
Organoid
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-128872
-
|
EHP-101; VCE-004.8
|
PPAR
Cannabinoid Receptor
HIF/HIF Prolyl-Hydroxylase
|
Metabolic Disease
Inflammation/Immunology
|
|
Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity .
|
-
- HY-128932
-
|
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-139230
-
|
|
Cannabinoid Receptor
PPAR
|
Metabolic Disease
|
|
OLHHA is a dual CB1 receptor antagonist and PPARα agonist. OLHHA also is a alcohol intake inhibitor with an EC50 value of 0.2 mg/kg. OLHHA reduces both hepatic lipid accumulation and circulating triglyceride levels. OLHHA shows anti-steatotic activity and has the potential for the research of non-alcoholic fatty liver disease (NAFLD) .
|
-
- HY-17386S1
-
-
- HY-112597A
-
|
REN001; HPP593
|
PPAR
|
Inflammation/Immunology
|
|
Mavodelpar (REN001) is a selective PPARδ agonist. Mavodelpar suppresses glomerular injury and renal fibrosis. Mavodelpar can be used for the research of primary mitochondrial myopathies (PMM) and long-chain fatty acid oxidation disorders (LC-FAOD) . Mavodelpar is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-154985
-
|
|
PPAR
Bombesin Receptor
ERK
|
Metabolic Disease
|
|
DSO-5a is a potent, selective, orally active BB3 agonist. DSO-5a is a representative DMAKO-00 derivative compound. DSO-5a upregulates ppar-γ activity through BB3 and activates ERK1/2 phosphorylation. DSO-5a can be used in diabetes-related research .
|
-
- HY-B0205R
-
|
CV 11974 (Standard)
|
Angiotensin Receptor
PPAR
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Candesartan (Standard) is the analytical standard of Candesartan. This product is intended for research and analytical applications. Candesartan (CV 11974) is an orally active angiotensin II AT1-Receptor blocker and PPAR-γ agonist. Candesartan has potent and long-lasting antihypertensive effects. Candesartan can be used for the research of hypertension, chronic heart failure (CHF) and Traumatic brain injury (TBI) .
|
-
- HY-15027S3
-
|
Mesalamine-d3 disodium; 5-ASA-d3 disodium; Mesalazine-d3 disodium
|
PPAR
NF-κB
Endogenous Metabolite
PAK
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
|
5-Aminosalicylic acid-d3 disodium is deuterated labeled 5-Aminosalicylic Acid (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
|
-
- HY-17356
-
|
|
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-W011220
-
|
ADD-3878; U-63287
|
PPAR
|
Cardiovascular Disease
Cancer
|
|
Ciglitazone is a potent and selective PPARγ agonist (EC50=3 μM). Ciglitazone inhibits proliferation and differentiation of th17 cells. Ciglitazone is a hypoglycemic agent orally active in the obese-hyperglycemic animal models. Ciglitazone induces apoptosis accompanied by activation of p38 MAPK and nuclear translocation of apoptosis inducing factor (AIF) in opossum kidney (OK) renal epithelial cells .
|
-
- HY-120327
-
KY-226
1 Publications Verification
|
Phosphatase
|
Neurological Disease
Metabolic 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
1 Publications Verification
|
COX
PPAR
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
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-14649R
-
|
Vitamin A acid (Standard); all-trans-Retinoic acid (Standard); ATRA (Standard)
|
RAR/RXR
PPAR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
Retinoic acid (Standard) is the analytical standard of Retinoic acid. This product is intended for research and analytical applications. 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-17356S
-
-
- HY-155525
-
|
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
|
Anti-NASH agent 1 (compound 3d)，a derivative of Elafibranor (HY-16737)，is a potent agonist of PPAR-α/δ，targeting to nonalcoholic steatohepatitis (NASH). Anti-NASH agent 1 (3-10 mg/kg; 4 weeks) improves hyperlipidemia，liver fat degeneration and liver inflammation in Methionine-choline deficiency (MCD) induced NASH mice model. Anti-NASH agent 1 shows low liver toxicity and potent liver protection effect .
|
-
- HY-101676
-
|
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-14649S2
-
|
|
RAR/RXR
PPAR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
11-cis-Retinoic Acid-d5 is the deuterium labeled Retinoic acid. 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[1][2].
|
-
- HY-17356S1
-
|
|
PPAR
Autophagy
Cytochrome P450
|
|
|
Fenofibrate-d4 is the deuterium labeled Fenofibrate[1]. 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[2][3].
|
-
- HY-14649S4
-
|
Vitamin A acid-d5; all-trans-Retinoic acid-d5; ATRA-d5
|
Isotope-Labeled Compounds
RAR/RXR
PPAR
|
Cancer
|
|
Retinoic acid-d5 is the the deuterium labeled Retinoic acid (HY-14649). 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-17356R
-
|
|
PPAR
Cytochrome P450
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Fenofibrate (Standard) is the analytical standard of Fenofibrate. This product is intended for research and analytical applications. 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-108568S
-
|
15d-PGJ2-d4; 15-Deoxy-Δ12,14-PGJ2-d4
|
PPAR
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
15-Deoxy-Δ-12,14-prostaglandin J2-d4 is the deuterium labeled 15-Deoxy-Δ-12,14-prostaglandin J2. 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[1][2].
|
-
- HY-15589
-
GW9508
4 Publications Verification
|
Free Fatty Acid Receptor
Potassium Channel
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
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-14649S3
-
|
Vitamin A acid-d6; all-trans-Retinoic acid-d6; ATRA-d6
|
RAR/RXR
PPAR
Autophagy
Endogenous Metabolite
|
Cancer
|
|
Retinoic acid-d6 is the deuterium labeled Retinoic acid[1]. 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[2][3][4][5][6][7].
|
-
- HY-17356G
-
|
|
Cytochrome P450
PPAR
Autophagy
|
Cardiovascular Disease
|
|
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 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-15697
-
TUG-770
2 Publications Verification
|
Free Fatty Acid Receptor
|
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 . TUG-770 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-143704S
-
|
Mesalamine-13C6 hydrochloride; 5-ASA-13C6 hydrochloride; Mesalazine-13C6 hydrochloride
|
PPAR
NF-κB
PAK
|
Metabolic Disease
|
|
5-Aminosalicylic acid-13C6 hydrochloride?(Mesalamine-13C6 hydrochloride; 5-ASA-13C6 hydrochloride; Mesalazine-13C6 hydrochloride) is the 13C labeled 5-Aminosalicylic Acidhydrochloride. 5-Aminosalicylic acid-13C6 hydrochloride?acts as a PPARγ agonist, and also inhibits p21-activated kinase 1 (PAK1) and NF-κB .
|
-
- HY-148418
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes . TUG-499 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-17356G
-
|
|
Fluorescent Dye
|
|
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 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.
|
| Cat. No. |
Product Name |
Type |
-
- HY-17356G
-
|
|
Biochemical Assay Reagents
|
|
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 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.
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0637S
-
|
|
|
Bezafibrate-d6 is the deuterium labeled Bezafibrate. 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-13956S
-
|
|
|
Pioglitazone-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[1].
|
-
-
- HY-B0287S
-
|
|
|
Clofibrate-d4 is the deuterium labeled Clofibrate. 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-B0637S1
-
|
|
|
Bezafibrate-d4 is deuterium labeled Bezafibrate. 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-50935S
-
|
|
|
Troglitazone-d4 is deuterium labeled Troglitazone. Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.
|
-
-
- HY-19937S1
-
|
|
|
Saroglitazar-d4 is the deuterium-labeled Saroglitazar (HY-19937). Saroglitazar-d4 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-17386S
-
|
|
|
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[1][2][3][4].
|
-
-
- HY-13956S1
-
|
|
|
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[1][2].
|
-
-
- HY-N6807S
-
|
|
|
Elemicin-d3 is deuterated labeled Pemafibrate (HY-17618). Pemafibrate is a highly selective PPARα agonist, with an EC50 of 1 nM.
|
-
-
- HY-107542S2
-
|
|
|
Oleoylethanolamide-d2 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
|
-
-
- HY-107542S
-
|
|
|
Oleoylethanolamide-d4 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
|
-
-
- HY-117727S
-
|
|
|
Leriglitazone-d4 (MIN-102-d4; Hydroxypioglitazone-d4) is deuterium labeled Leriglitazone. 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-B1415S
-
|
|
|
Clofibric acid-d4 is the deuterium labeled Clofibric acid. 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[1][2][3].
|
-
-
- HY-15027S
-
|
|
|
5-Aminosalicylic Acid-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-15027S1
-
|
|
|
5-Aminosalicylic acid-d3 is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[1][2][3][4].
|
-
-
- HY-15027S2
-
|
|
|
5-Aminosalicylic acid- 13C6 is the 13C labeled 5-Aminosalicylic Acid[1]. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[2][3][4].
|
-
-
- HY-17386S1
-
|
|
|
Rosiglitazone-d4 is deuterated labeled Rosiglitazone (HY-17386). Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer .
|
-
-
- HY-15027S3
-
|
|
|
5-Aminosalicylic acid-d3 disodium is deuterated labeled 5-Aminosalicylic Acid (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
|
-
-
- HY-17356S
-
|
|
|
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-14649S2
-
|
|
|
11-cis-Retinoic Acid-d5 is the deuterium labeled Retinoic acid. 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[1][2].
|
-
-
- HY-17356S1
-
|
|
|
Fenofibrate-d4 is the deuterium labeled Fenofibrate[1]. 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[2][3].
|
-
-
- HY-14649S4
-
|
|
|
Retinoic acid-d5 is the the deuterium labeled Retinoic acid (HY-14649). 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-108568S
-
|
|
|
15-Deoxy-Δ-12,14-prostaglandin J2-d4 is the deuterium labeled 15-Deoxy-Δ-12,14-prostaglandin J2. 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[1][2].
|
-
-
- HY-14649S3
-
|
|
|
Retinoic acid-d6 is the deuterium labeled Retinoic acid[1]. 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[2][3][4][5][6][7].
|
-
-
- HY-143704S
-
|
|
|
5-Aminosalicylic acid-13C6 hydrochloride?(Mesalamine-13C6 hydrochloride; 5-ASA-13C6 hydrochloride; Mesalazine-13C6 hydrochloride) is the 13C labeled 5-Aminosalicylic Acidhydrochloride. 5-Aminosalicylic acid-13C6 hydrochloride?acts as a PPARγ agonist, and also inhibits p21-activated kinase 1 (PAK1) and NF-κB .
|
-
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