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 适度地抑制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。

Epaminurad (UR-1102) is an orally active, potent and selective URAT1 (urate transporter 1) inhibitor, with a Ki of 0.057 μM. Epaminurad inhibits OAT1 and OAT3 (organic anion transporter) quite modestly. Epaminurad is a uricosuric agent which can be used for gout and hyperuricemia research [1].

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

Epaminurad (0-30 mg/kg, Orally, once a day for 3 consecutive days) exhibits strong 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 C max (μg/mL) 8.96 ± 1.74 42.4 ± 12.8 92.9 ± 21.0 T max (h) 0.6 ± 0.2 0.5 ± 0.0 0.8 ± 0.3 T 1/2 (h) 4.7 ± 0.9 4.2 ± 1.1 3.3 ± 0.8 AUC 0-inf (mg*h/mL) 26.2 ± 8.1 108 ± 51 257 ± 60

1198153-15-9

C14H10Br2N2O3

414.05

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years