1. PI3K/Akt/mTOR
  2. PI3K
  3. PF-376304

PF-376304 是一种具有口服活性的非特异性 I 类磷酸肌醇 3-激酶 (PI3K) 抑制剂,其 PI3Kγ IC50 为 0.197 μM。PF‑376304 可致大鼠出现剂量依赖性糖脂代谢紊乱,高剂量下快速致死,低剂量下代谢异常可自行逆转。PF-376304 可用于代谢和炎症性疾病的研究。

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PF-376304

PF-376304 Chemical Structure

CAS No. : 851757-93-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体内研究
(In Vivo)

PF-376304 (0-1000 mg/kg; 灌胃; 7 d) 在Sprague‑Dawley 大鼠中诱导显著且可逆的葡萄糖代谢紊乱、酮尿与肌酸尿,≥300 mg/kg 可致 72 h 内快速死亡[1]

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.
分子量

388.43

Formula

C17H24N8O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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  • 稀释计算器

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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.

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产品名称:
PF-376304
目录号:
HY-107387
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