1. Membrane Transporter/Ion Channel
  2. URAT1
  3. Epaminurad

Epaminurad  (Synonyms: UR-1102)

Cat. No.: HY-111345
Handling Instructions

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.

For research use only. We do not sell to patients.

Epaminurad Chemical Structure

Epaminurad Chemical Structure

CAS No. : 1198153-15-9

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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].

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].

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

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

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

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.
Molecular Weight

414.05

Formula

C14H10Br2N2O3

CAS No.
SMILES

O=C(N1C2=C(OCC1)C=CN=C2)C3=CC(Br)=C(C(Br)=C3)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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