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].
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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. |
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| 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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