PPAR agonist 7
PPAR agonist 7 is an orally active pan-PPAR agonist, demonstrating potent activation of all three subtypes, PPARα (EC50 = 1.51 μM), PPARδ (EC50 = 1.11 μM), and PPARγ (EC50 = 3.14 μM). PPAR agonist 7 significantly enhances glucose uptake in adipocytes while exhibiting minimal adipogenic activity. PPAR agonist 7 can suppress PPARγ Ser273 phosphorylation in white adipose tissue and upregulate insulin-sensitizing genes. PPAR agonist 7 does not cause weight gain or fluid retention in high-fat diet (HFD)/ Streptozotocin (HY-13753) (STZ)-induced type 2 diabetes mellitus (T2DM) models. PPAR agonist 7 has selective modulation of PPAR signaling pathways without activation of adipogenic gene programs. PPAR agonist 7 can be used for the study of diabetes.
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- CAS No.: 3122526-69-3
- Formula: C29H35NO5
- Molecular Weight:477.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
PPAR agonist 7 (Compound 1d) (1-10 μM, 24 h) has no significant effect on the viability of 3T3-L1 adipocytes and increases glucose uptake in mature adipocytes in a dose-dependent manner at the tested concentration[1].
PPAR agonist 7 (10 μM, 75 min) can significantly inhibit TNFα-induced phosphorylation of PPARγ at Ser273 in 3T3-L1 cells[1].
PPAR agonist 7 (1-10 μM, 24 h) significantly restores glucose uptake in HepG2 cells exposed to 30 mM glucose and 0.5 μM insulin[1].
PPAR agonist 7 (10 μM, 8 days) significantly reduces the number of lipid droplets in 3T3-L1, and the mRNA levels of key genes for adipogenesis (Ppary, Ap2, Cebpa, Fasn, Cd36, Lpl) are not significantly upregulated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:3T3-L1 adipocytes cells
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Concentration:1 μM, 5 μM, 10 μM
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Incubation Time:24 h
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Result:Showed no significant effect on the viability of 3T3-L1 adipocytes.
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Cell Line:TNF-α-induced 3T3-L1 cells
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Concentration:10 μM
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Incubation Time:Pretreated for 45 min, then stimulation with 50 ng/mL TNF-α for an additional 30 min
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Result:Significantly inhibited TNFα-induced phosphorylation of PPARγ at Ser273 in 3T3-L1 cells.
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Cell Line:3T3-L1 adipocytes cells
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Concentration:10 μM
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Incubation Time:8 days
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Result:Showed no significant effects on any of these adipogenesis-related genes (Ppary, Ap2, Cebpa, Fasn, Cd36, Lpl).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:The male C57BL/6J mice (18-22 g, 4-6 weeks) were fed a high-fat diet 12 weeks and then mice were received daily intraperitoneal injections of streptozotocin (STZ; 50 mg/kg) for five consecutive days, following this, the mice were fed for an additional three weeks to establish the STZ/HFD-induced T2DM model[1].
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Dosage:5 mg/kg, 10 mg/kg, 20 mg/kg
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Administration:P.o., once daily for 30 days
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Result:Significantly improved fasting blood glucose levels and reduced fasting insulin concentrations.
Demonstrated dose-dependent improvements in insulin resistance in this diabetic model.
Significantly elevated fasting plasma adiponectin levels in T2DM mice.
Did not cause significant body weight gain and no effect on hematocrit.
Significantly enhanced glucose clearance and insulin sensitivity.
Significantly reduced plasma TG, TC, LDL-C, and FFA; significantly increased plasma adiponectin levels.
Significantly alleviated hepatocellular steatosis and ballooning degeneration; reduced plasma AST and ALT levels.
Inhibited PPARγ Ser273 phosphorylation in WAT; upregulated insulin-sensitive genes (Adiponectin, Cyp2f2).
Selectively regulated insulin resistance-related genes (Glut4, Irs1), but did not activate adipogenesis genes (Ppary, Fasn).
Chemical Information
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CAS No. 3122526-69-3
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Molecular Weight 477.59
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Formula C29H35NO5
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SMILES
CC(C)(OC1=C(C)C=C(/C=C2OC3=CC(NCC4CC4)=CC=C3C\2=O)C=C1C)C(OC(C)(C)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Large-size fat particle sorting
Large-size fat particle sorting is widely used to isolate cells up to 200 μm in diameter. Single-cell flow sorting will allow greater insight into adipocyte heterogeneity by identifying gene expression, protein composition, and metabolic signatures at the single-cell level.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)