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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)
中文名称
Epaminurad
英文名称
Epaminurad
中文别名
伊巴米努拉德
英文别名
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号
1198153-15-9
分子式
C14H10Br2N2O3
分子量
414.05 g/mol
精确质量
≥98%
PSA
62.700 Ų
Logp
2.600
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Epaminurad 5mg

品牌:阿拉丁
货号:E646798-5mg
级别: ≥98%
货期:30天
已售 986 件
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