2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. PPARγ phosphorylation inhibitor 1

PPARγ phosphorylation inhibitor 1 (Compound 10) is a potent PPARγ binder with the IC50 of 24 nM. PPARγ phosphorylation inhibitor 1 inhibits CDK5-mediated phosphorylation of PPARγ Ser273 with the IC50 of 160 nM. PPARγ phosphorylation inhibitor 1 displays negligible PPARγ agonism in a reporter gene assay. Antidiabetic effects.

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PPARγ phosphorylation inhibitor 1 Chemical Structure

PPARγ phosphorylation inhibitor 1 Chemical Structure

CAS No. : 2882975-84-8

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PPARγ phosphorylation inhibitor 1 Related Antibodies

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Description

PPARγ phosphorylation inhibitor 1 (Compound 10) is a potent PPARγ binder with the IC50 of 24 nM. PPARγ phosphorylation inhibitor 1 inhibits CDK5-mediated phosphorylation of PPARγ Ser273 with the IC50 of 160 nM. PPARγ phosphorylation inhibitor 1 displays negligible PPARγ agonism in a reporter gene assay. Antidiabetic effects[1].

IC50 & Target[1]

PPARγ

24 nM (IC50)

In Vivo

PPARγ phosphorylation inhibitor 1 (compound 10) (100 μM/kg; i.g.; lean C57/BL6 mice) has a PK profile amenable to in vivo administration[1].
PPARγ phosphorylation inhibitor 1 (compound 10) (10-100 μM/kg; i.g.; daily, for 7 days) demonstrates a modest improvement of insulin sensitivity in ob/ob mice[1].

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

Animal Model: Lean C57/BL6 mice[1]
Dosage: 100 μM/kg
Administration: Oral gavage
Result: Exhibited good pharmacokinetic profiles with oral bioavailability (109%), Cmax (167 μM) and t1/2 (5 h).
Animal Model: ob/ob mouse model of diabetes[1]
Dosage: 10 and 100 μM/kg
Administration: Oral gavage; Daily, for 7 days
Result: Improved insulin sensitivity and did not impact the body weight.
Molecular Weight

441.26

Formula

C22H14Cl2N2O4
CAS No.
SMILES

O=C(C1=NN(C(C2=C1C=CC(OC3=CC=CC=C3)=C2)=O)CC4=CC(Cl)=C(C=C4)Cl)O
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PPARγ phosphorylation inhibitor 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:

PPARγ phosphorylation inhibitor 12882975-84-8PPARγ phosphorylation inhibitor1PPARγ phosphorylation inhibitor-1PPARPeroxisome proliferator-activated receptorsPPARγinsulin sensitizerPPARγ phosphorylation inhibitorPPARγ modulatorInhibitorinhibitorinhibit

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