Epaminurad

• CAT Number: I026910
• CAS Number: 1198153-15-9
• Purity: ≥95%
• Synonyms: (3,5-dibromo-4-hydroxyphenyl)-(2,3-dihydropyrido[4,3-b][1,4]oxazin-4-yl)methanone
• InChI: InChI=1S/C14H10Br2N2O3/c15-9-5-8(6-10(16)13(9)19)14(20)18-3-4-21-12-1-2-17-7-11(12)18/h1-2,5-7,19H,3-4H2
• InChIKey: ZMVGQIIOXCGAFV-UHFFFAOYSA-N
• SMILES: C1COC2=C(N1C(=O)C3=CC(=C(C(=C3)Br)O)Br)C=NC=C2

Epaminurad (UR-1102) is an orally active, potent and selective URAT1 (urate transporter 1) inhibitor, with a Ki 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[1].
UR-1102 (0-12 μM) inhibits urate and PAH (p-aminohippuric acid) uptake by HEK293 cells transiently expressing URAT1, OAT1, or OAT3[1].
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