Epaminurad (UR-1102) is an orally active, potent and selective URAT1 (urate transporter 1) inhibitor, with a K i 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 In Vitro UR-1102 (0-12 μM) inhibits urate and PAH (p-aminohippuric acid) uptake by HEK293 cells transiently expressing URAT1, OAT1, or OAT3. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . 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 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:Ki: 0.057 ± 0.036 μM (URAT1), 2.4 ± 0.2 μM (OAT3), 7.2 ± 0.8 μM (OAT1)
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Epaminurad
CAS number：1198153-15-9 molecular formula：C14H10Br2N2O3
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| Chinese alias | 伊巴米努拉德 | ||
| English alias | EX-A4697 | UNII-0YP1ME85GH | Epaminurad;UR-1102;UR1102 | (3,5-dibromo-4-hydroxyphenyl)(2H-pyrido[4,3-b][1,4]oxazin-4(3H)-yl)methanone | AKOS040748326 | UR-1102 | BCP30414 | UR 1102 | MS-27164 | (3,5-Dibromo-4-hydroxyphenyl)(2,3-dihydro-4H-pyrido(4,3-b)-1, | ||
| CAS number | 1198153-15-9 | molecular formula | C14H10Br2N2O3 |
| molecular weight | 414.05 g/mol | Exact mass | ≥98% |
| PSA | 62.700 Ų | logp | 2.600 |
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