Epaminurad


CAS No. : 1198153-15-9

(Synonyms: UR-1102; URC-102)

1198153-15-9
Price and Availability of CAS No. : 1198153-15-9
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Cat. No. : HY-111345
M.Wt: 414.05
Formula: C14H10Br2N2O3
Purity: >98 %
Solubility: DMSO : 100 mg/mL (ultrasonic)
Introduction of 1198153-15-9 :

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]. IC50 & 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

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