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  3. PF-376304

PF-376304 is an orally active non-specific class I phosphoinositide 3-kinase (PI3K) inhibitor with an IC50 of 0.197 μM against PI3Kγ. PF-376304 induces dose-dependent glucose and lipid metabolic disorders in rats, causes rapid death at high doses, and leads to metabolic abnormalities that are self-reversible at low doses. PF-376304 is applicable to the research of metabolic and inflammatory diseases.

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PF-376304

PF-376304 Chemical Structure

CAS No. : 851757-93-2

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Description

PF-376304 is an orally active non-specific class I phosphoinositide 3-kinase (PI3K) inhibitor with an IC50 of 0.197 μM against PI3Kγ. PF-376304 induces dose-dependent glucose and lipid metabolic disorders in rats, causes rapid death at high doses, and leads to metabolic abnormalities that are self-reversible at low doses. PF-376304 is applicable to the research of metabolic and inflammatory diseases[1][2].

IC50 & Target

PI3Kγ

0.197 μM (IC50)

In Vivo

PF-376304 (0-1000 mg/kg; i.g.; 7 d) induces significant and reversible glucose metabolism disorders, ketonuria and creatinuria in Sprague-Dawley rats, while doses of ≥300 mg/kg cause rapid death within 72 h[1].

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

Animal Model: Sprague-Dawley [Crl:CD(SD)BR] rats (6-8 weeks old; males 194-228 g, females 164-182 g)[1]
Dosage: 0, 30, 100, 300, 1000 mg/kg
Administration: i.g.; daily; once daily for up to 7 consecutive days
Result: Caused dose-dependent hyperglycemia, hyperinsulinemia, elevated serum corticosterone, reduced triglycerides, profound transient glucosuria, increased urinary β-hydroxybutyrate and creatine, and decreased citrate.
Led to rapid mortality within 72 h at doses ≥300 mg/kg , while metabolic effects mostly reversed within 72 h despite continued dosing at 100 mg/kg.
Molecular Weight

388.43

Formula

C17H24N8O3

CAS No.
SMILES

O=C(NC1=NN=NN1)C2=CN=C(N=C2OC3CCCCCC3)N4CCOCC4

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    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.

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Product Name:
PF-376304
Cat. No.:
HY-107387
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