Epaminurad (C09-1130-511)

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 researchIn VitroUR-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 VivoEpaminurad (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:SolidIC50& Target:Ki: 0.057 ± 0.036 μM (URAT1), 2.4 ± 0.2 μM (OAT3), 7.2 ± 0.8 μM (OAT1). Specification: 0.98 Molecular Formula: C14H10Br2N2O3 Molecular Weight: 414.05 PubChem CID: 44608229 Isomeric SMILES: C1COC2=C(N1C(=O)C3=CC(=C(C(=C3)Br)O)Br)C=NC=C2