Xanthine oxidase-IN-6 (Compound 6c) 是一种强效的、具有口服活性的黄嘌呤氧化酶 (XOD) 混合型抑制剂，其IC50值为1.37 μM。Xanthine oxidase-IN-6 具有很强的抗高尿酸血症 (anti-hyperuricemia) 和肾保护活性。
| 生物活性 | Xanthine oxidase-IN-6 (Compound 6c) is a potent, orally active, mixed-typexanthine oxidase(XOD) inhibitor with anIC50value of 1.37 μM. Xanthine oxidase-IN-6 shows stronganti-hyperuricemiaand renal protective activity[1]. |
| IC50& Target | NF-κB | TLR4 | XOD 1.37 μM (IC50) |
|
体外研究
(In Vitro) | Xanthine oxidase-IN-6 (Compound 6c) is a mixed-type XOD inhibitor, preferentially bound to the free enzyme and not the enzyme substrate complex[1].
Xanthine oxidase-IN-6 is stable in simulated gastrointestinal digestion, with hydrolysis half-life more than 4 h[1].
Xanthine oxidase-IN-6 (0-100 μM) exhibits an obvious anti-inflammatory effect by reducing the level of inflammatory factors (TGF-β, TNF-α and IL-1β) in a dose-dependent manner[1].
Xanthine oxidase-IN-6 (0-100 μM, 48 h) inhibits HK-2 cell epithelial mesenchymal transition under high level of uric acid[1].
Western Blot Analysis[1] | Cell Line: | HK-2 cells | | Concentration: | 12.5, 25, 50, and 100 μM | | Incubation Time: | 48 h | | Result: | Reduced the protein levels of α-SMA and Collagen I in a dose-dependent manner |
|
体内研究
(In Vivo) | Xanthine oxidase-IN-6 (Compound 6c) (0-20 mg/kg; i.g.; once daily for 2 weeks) shows anti-hyperuricemic effects, alleviates kidney damage, and inhibits XOD activity in a dose-dependent manner[1].
Xanthine oxidase-IN-6 (0-20 mg/kg; i.g.; once daily for 2 weeks) effectively reduces renal fibrosis and inflammation[1].
| Animal Model: | Kunming mice (male, weight 20 ± 2 g). Hyperuricemic mouse model established by administering 0.5% CMC-Na (10 mL/kg), adenine (200 mg/kg) and potassium oxonate (500 mg/kg); oral gavage once daily for 2 or 4 weeks[1]. | | Dosage: | 5, 10 and 20 mg/kg | | Administration: | Gavage, once daily for 2 weeks | | Result: | Effectively decreased the levels of SUA, Cr, and BUN, effectively inhibited XOD activity and urate accumulation in a dose-dependent manner. Remarkedly improved the morphologic lesions with less fibrosis in the interstitium. Reduced the production of multiple cytokines (TNF-α, IL-8, and IL-1β). Reduced the expression of α-SMA, collagen I, TLR4, NF-κB, IκBα and TNF-α. |
|
| 分子量 | |
| Formula | |
| 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. |
