Epaminurad UR-1102|cas:1198153-15-9|西域试剂

Epaminurad UR-1102,98.05%

产品编号：Bellancom-111345| CAS NO：1198153-15-9| 分子式：C₁₄H₁₀Br₂N₂O₃| 分子量：414.05

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货号	价格	库存与货期
Bellancom-111345	￥3800.00	杭州北京（现货）
Bellancom-111345	￥6200.00	杭州北京（现货）
Bellancom-111345	￥12500.00	杭州北京（现货）

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Epaminurad UR-1102

产品介绍

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 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 research.

体外研究

UR-1102 (0-12 μM) inhibits urate and PAH (p-aminohippuric acid) uptake by HEK293 cells transiently expressing URAT1, OAT1, or OAT3.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Epaminurad (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

西域 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.

体内研究

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

西域 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.