1. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  2. Xanthine Oxidase BCRP GLUT
  3. Xanthine oxidase-IN-23

Xanthine oxidase-IN-23 (Compound BPF) 是一种具有口服活性的、可逆的、混合型 Xanthine oxidase 抑制剂,其 IC50 为 3.33 μM。Xanthine oxidase-IN-23 以可逆的混合型方式直接结合 XOD,从而抑制其催化活性。Xanthine oxidase-IN-23 可上调 ABCG2 并下调 GLUT9,以促进肾脏尿酸排泄。Xanthine oxidase-IN-23 可降低高尿酸血症小鼠的血清尿酸水平并改善其肾功能。Xanthine oxidase-IN-23 可用于高尿酸血症的研究。

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Xanthine oxidase-IN-23

Xanthine oxidase-IN-23 Chemical Structure

CAS No. : 3055112-52-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Xanthine oxidase-IN-23 (Compound BPF) is an orally active, reversible, mixed-type Xanthine oxidase inhibitor with an IC50 of 3.33 μM. Xanthine oxidase-IN-23 directly binds to XOD in a reversible mixed-type manner to inhibit its catalytic activity. Xanthine oxidase-IN-23 upregulates ABCG2 and downregulates GLUT9 to promote renal urate excretion. Xanthine oxidase-IN-23 reduces serum urate levels and improves renal function in hyperuricemic mice. Xanthine oxidase-IN-23 can be used in the research of hyperuricemia[1].

IC50 & Target[1]

GLUT9

 

体外研究
(In Vitro)

Xanthine oxidase-IN-23 (15 min) 可通过可逆的混合型抑制方式强效抑制纯化的黄嘌呤氧化酶,其 IC50 为 3.33 μM[1]
Xanthine oxidase-IN-23 (0.5-8 μM) 具有强效的 DPPH 自由基清除活性,在 2 μM 时清除率超过 50%[1]

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

体内研究
(In Vivo)

Xanthine oxidase-IN-23 (BPF) (100-200 mg/kg;口服) 可通过抑制肝脏 XOD 活性、调控肾脏尿酸转运体,剂量依赖性地降低高尿酸血症小鼠的血清尿酸水平,同时还能预防高尿酸血症诱导的肾损伤且不会造成肝损伤[1]

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

Animal Model: Kunming mice (male, 5 weeks old, 39.4 g)[1]
Dosage: 100 mg/kg; 200 mg/kg
Administration: p.o.; single dose
Result: Significantly reduced serum uric acid (SUA) levels compared to the hyperuricemia model group.
Significantly reduced hepatic uric acid levels and hepatic xanthine oxidase (XOD) activity compared to the model group (200 mg/kg dose).
Completely reversed the downregulation of renal uric acid secretion transporter ABCG2 while significantly downregulating renal uric acid reabsorption transporter GLUT9 (200 mg/kg dose).
Significantly restored elevated serum creatinine (CRE) levels to near normal and mitigated hyperuricemia-induced mild renal tubular dilation and eosinophilic material accumulation.
Increased urinary uric acid levels at early time points after modeling compared to the model group (200 mg/kg dose).
Caused no significant changes in hepatic index, serum alanine aminotransferase (ALT), or aspartate aminotransferase (AST) levels, indicating no liver injury.
分子量

456.08

Formula

C17H12Br2O5

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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产品名称:
Xanthine oxidase-IN-23
目录号:
HY-182000
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