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Epaminurad
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Epaminurad图片
CAS NO: 1198153-15-9
包装与价格：
包装 价格(元)
100mg 电议
250mg 电议
500mg 电议

半岛bd体育手机客户端 名称
UR-1102
半岛bd体育手机客户端 介绍
Epaminurad (UR-1102) 是一种口服有效的和选择性的 URAT1(尿酸转运体 1) 抑制剂，其 Ki为 0.057 μM。Epaminurad 相当温和地抑制 OAT1和 OAT3(有机阴离子转运体)。Epaminurad 是一种促尿酸排泄剂。Epaminurad 可用于痛风和高尿酸血症的研究。
生物活性

Epaminurad (UR-1102) is an orally active, potent and selectiveURAT1(urate transporter 1) inhibitor, with aKiof 0.057 μM. Epaminurad quite modestly inhibitsOAT1andOAT3(organic anion transporter). Epaminurad is a uricosuric agent. Epaminurad can be used for gout and hyperuricemia research[1].
IC50& Target

Ki: 0.057 ± 0.036 μM (URAT1), 2.4 ± 0.2 μM (OAT3), 7.2 ± 0.8 μM (OAT1)[1].
体外研究
(In Vitro)

UR-1102 (0-12 μM) inhibits urate and PAH (p-aminohippuric acid) uptake by HEK293 cells transiently expressing URAT1, OAT1, or OAT3[1].
体内研究
(In Vivo)

Epaminurad (0-30 mg/kg, Orally, once a day for 3 consecutive days) shows uricosuric and urate-lowering effects[1].
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[1].
Pharmacokinetic Parameters of Epaminurad (UR-1102) in tufted capuchin monkeys[1].

Group 3 mg/kg 10 mg/kg 30 mg/kg
Cmax(μg/mL) 8.96 ± 1.74 42.4 ± 12.8 92.9 ± 21.0
Tmax(h) 0.6 ± 0.2 0.5 ± 0.0 0.8 ± 0.3
T1/2(h) 4.7 ± 0.9 4.2 ± 1.1 3.3 ± 0.8
AUC0-inf(mg*h/mL) 26.2 ± 8.1 108 ± 51 257 ± 60

Animal Model: Tufted capuchin monkeys[1]
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[1]
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.
分子量

414.05
Formula

C14H10Br2N2O3
CAS 号

1198153-15-9
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.
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