1198153-15-9

1198153-15-9 structure

Name: UR-1102
Chemical Name: (3,5-Dibromo-4-hydroxyphenyl)(2,3-dihydro-4H-pyrido[4,3-b][1,4]oxazin-4-yl)methanone
CAS Number: 1198153-15-9
Molecular Formula: C₁₄H₁₀Br₂N₂O₃
Molecular Weight: 414.049
Catalog: Signaling Pathways Membrane Transporter/Ion Channel URAT1
Create Date: 2018-06-25 14:27:51
Modify Date: 2025-08-25 16:15:36
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].

Name	(3,5-Dibromo-4-hydroxyphenyl)(2,3-dihydro-4H-pyrido[4,3-b][1,4]oxazin-4-yl)methanone
Synonyms	(3,5-Dibromo-4-hydroxyphenyl)(2,3-dihydro-4H-pyrido[4,3-b][1,4]oxazin-4-yl)methanone

Description	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].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> URAT1 Research Areas >> Inflammation/Immunology Research Areas >> Metabolic Disease
Target	Ki: 0.057 ± 0.036 μM (URAT1), 2.4 ± 0.2 μM (OAT3), 7.2 ± 0.8 μM (OAT1)[1].
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].
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.
References	[1]. Ahn SO, et al. Stronger Uricosuric Effects of the Novel Selective URAT1 Inhibitor UR-1102 Lowered Plasma Urate in Tufted Capuchin Monkeys to a Greater Extent than Benzbromarone. J Pharmacol Exp Ther. 2016 Apr;357(1):157-66.

Density	1.9±0.1 g/cm3
Boiling Point	530.0±50.0 °C at 760 mmHg
Molecular Formula	C₁₄H₁₀Br₂N₂O₃
Molecular Weight	414.049
Flash Point	274.3±30.1 °C
Exact Mass	411.905792
LogP	3.05
Vapour Pressure	0.0±1.5 mmHg at 25°C
Index of Refraction	1.691

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