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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- CAS. Nr.: 851757-93-2
- Formel: C17H24N8O3
- Molecular Weight:388.43
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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PI3Kγ 0.197 μM (IC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley [Crl:CD(SD)BR] rats (6-8 weeks old; males 194-228 g, females 164-182 g)[1]
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Dosage:0, 30, 100, 300, 1000 mg/kg
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Administration:i.g.; daily; once daily for up to 7 consecutive days
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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.
Chemical Information
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CAS. Nr. 851757-93-2
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Molecular Weight 388.43
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Formel C17H24N8O3
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SMILES
O=C(NC1=NN=NN1)C2=CN=C(N=C2OC3CCCCCC3)N4CCOCC4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Robertson DG, et al. Metabonomic evaluation of metabolic dysregulation in rats induced by PF 376304, a novel inhibitor of phosphoinositide 3-kinase. Chem Res Toxicol. 2007;20(12):1871-1877. [Content Brief]
[2]. Ameriks MK, et al. Small molecule inhibitors of phosphoinositide 3-kinase (PI3K) delta and gamma. Curr Top Med Chem. 2009;9(8):738-53. [Content Brief]
Calculators
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