Epaminurad

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Epaminurad

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1198153-15-9

UR-1102

Epaminurad (UR-1102) 是一种口服有效的和选择性的URAT1(尿酸转运体 1) 抑制剂，其K_i为 0.057 μM。Epaminurad 相当温和地抑制OAT1和OAT3(有机阴离子转运体)。Epaminurad 是一种促尿酸排泄剂。Epaminurad 可用于痛风和高尿酸血症的研究。

生物活性

Epaminurad (UR-1102) is an orally active, potent and selectiveURAT1(urate transporter 1) inhibitor, with aK_iof 0.057 μM. Epaminurad quite modestly inhibitsOAT1andOAT3(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].

体外研究
(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].

体内研究
(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
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

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.

分子量

414.05

Formula

C₁₄H₁₀Br₂N₂O₃

CAS 号

1198153-15-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.