2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. 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).

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PPARα/δ antagonist-1

PPARα/δ antagonist-1 Chemical Structure

CAS No. : 1673590-38-9

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PPARα/δ antagonist-1 Related Antibodies

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Description

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)[1].

IC50 & Target[1]

PPARα

0.113 μM (IC50)

PPARδ

0.025 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
30 μM
Compound: 11
Cytotoxicity against CHO cells assessed as effect on cell viability
Cytotoxicity against CHO cells assessed as effect on cell viability
[PMID: 30594433]
In Vitro

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.

PPARα/δ antagonist-1 Related Antibodies
In Vivo

PPARα/δ antagonist-1 (Compound 11) (10-30 mg/kg, p.o., twice daily for 21-28 days) exhibits significant anti-tumor activity in mouse B16F10 melanoma lung metastasis models and SKOV-3 ovarian cancer xenograft models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C57Bl/6 mice, 6-7 weeks old,[1]
Dosage: 10 and 30 mg/kg
Administration: p.o., twice daily for 21 and 28 days
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.
Molecular Weight

619.61

Formula

C34H29F4N3O4
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PPARα/δ antagonist-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PPARα/δ antagonist-11673590-38-9PPARPeroxisome proliferator-activated receptorsmouse PPAR isoformsovarian cancerhuman PPARαPPARδperoxisome proliferator-activated receptor alphaCHO cellPPARαmelanoma metastasishuman PPARδperoxisome proliferator-activated receptor deltaInhibitorinhibitorinhibit

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