PPARα/δ antagonist-1
PPARα/δ antagonist-1 is an orally active, highly selective dual antagonist of PPARα/δ, with IC50 values of 0.113 μM and 0.025 μM against human PPARα and PPARδ, respectively. PPARα/δ antagonist-1 exhibits an excellent in vitro activity profile and preliminary efficacy in mouse tumor models. PPARα/δ antagonist-1 can be used in studies related to cancers (melanoma metastasis, ovarian cancer).
For research use only. We do not sell to patients.
- CAS No.: 1673590-38-9
- Formula: C34H29F4N3O4
- Molecular Weight:619.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PPARα 0.113 μM (IC50) |
PPARδ 0.025 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
30 μM
Compound: 11
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Cytotoxicity against CHO cells assessed as effect on cell viability
Cytotoxicity against CHO cells assessed as effect on cell viability
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[PMID: 30594433] |
PPARα/δ antagonist-1 (Compound 11) exhibits lower potency against mouse PPARα and PPARδ (with IC50 values of 1.28 μM and 0.96 μM, respectively) than against their human orthologs[1].
PPARα/δ antagonist-1 (1-10 μM) exhibits extremely low off-target activity against nuclear receptors and most CYPs, has low CYP3A4 induction potential, does not reduce CHO cell viability at concentrations up to 30 μM, and shows negligible hERG activity at 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57Bl/6 mice, 6-7 weeks old,[1]
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Dosage:10 and 30 mg/kg
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Administration:p.o., twice daily for 21 and 28 days
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Result:Significantly reduced the number of tumor nodules formed in the lungs of mice after intravenous injection of B16F10 cells.
Significantly inhibited the growth of SKOV-3 tumors in nude mice.
Chemical Information
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CAS No. 1673590-38-9
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Molecular Weight 619.61
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Formula C34H29F4N3O4
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SMILES
O=C(CC1=C(OCC)C=CC(C2=CC=C(CCCC3=NN(C4=CC=C(C(F)(F)F)C=C4)C(N3C5=C(F)C=CC=C5)=O)C=C2)=C1)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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PPARα/δ antagonist-1 Related Classifications
HY-182619 Related Classifications
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