产品
编 号:F067270
分子式:C14H10Br2N2O3
分子量:414.05
产品类型
结构图
CAS No: 1198153-15-9
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产品详情
生物活性:
Epaminurad (UR-1102) is an orally active, potent and selective URAT1 (urate transporter 1) inhibitor, with a Ki of 0.057 μM. Epaminurad quite modestly inhibits OAT1 and OAT3 (organic anion transporter). Epaminurad is a uricosuric agent. Epaminurad can be used for gout and hyperuricemia research.
体内研究:
Epaminurad (0-30 mg/kg, Orally, once a day for 3 consecutive days) shows uricosuric and urate-lowering effects.Epaminurad (3-30 mg/kg, Orally, once) shows a good pharmacokinetic profile, increases the fractional excretion of urinary uric acid, and reduces plasma uric acid more effectively.Pharmacokinetic Parameters of Epaminurad (UR-1102) in tufted capuchin monkeys.Group3 mg/kg 10 mg/kg 30 mg/kg
Cmax (μg/mL)8.96 ± 1.7442.4 ± 12.892.9 ± 21.0
Tmax (h)0.6 ± 0.20.5 ± 0.00.8 ± 0.3
T1/2 (h)4.7 ± 0.94.2 ± 1.13.3 ± 0.8
AUC0-inf (mg*h/mL)26.2 ± 8.1108 ± 51257 ± 60
Animal Model:Tufted capuchin monkeys
Dosage:0, 3, 10, and 30 mg/kg
Administration:Orally, once a day, for 3 consecutive days
Result:Showed good uricosuric and urate-lowering effects at 3 mg/kg, the lowest dose, which were comparable to those of benzbromarone at 100 mg/kg, the highest dose, with maximum efficacy.
Animal Model:Tufted capuchin monkeys
Dosage:0, 3, 10, and 30 mg/kg
Administration:Orally, once
Result:Showed a good pharmacokinetic profile. Exhibited both good systemic exposure and significantly great plasma urate-lowering at 3 mg/kg.
体外研究:
UR-1102 (0-12 μM) inhibits urate and PAH (p-aminohippuric acid) uptake by HEK293 cells transiently expressing URAT1, OAT1, or OAT3.