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

Epaminurad  (Synonyms: UR-1102; URC-102)

Cat. No.: HY-111345 Purity: 99.75%
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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

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 418 In-stock
Solution
10 mM * 1 mL in DMSO USD 418 In-stock
Solid
5 mg USD 380 In-stock
10 mg USD 620 In-stock
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Based on 1 publication(s) in Google Scholar

Epaminurad Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

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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].

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

Epaminurad Related Antibodies
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

MedChemExpress (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.
Clinical Trial
Molecular Weight

414.05

Formula

C14H10Br2N2O3
CAS No.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (241.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4152 mL 12.0758 mL 24.1517 mL
5 mM 0.4830 mL 2.4152 mL 4.8303 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (6.04 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.04 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4152 mL 12.0758 mL 24.1517 mL 60.3792 mL
5 mM 0.4830 mL 2.4152 mL 4.8303 mL 12.0758 mL
10 mM 0.2415 mL 1.2076 mL 2.4152 mL 6.0379 mL
15 mM 0.1610 mL 0.8051 mL 1.6101 mL 4.0253 mL
20 mM 0.1208 mL 0.6038 mL 1.2076 mL 3.0190 mL
25 mM 0.0966 mL 0.4830 mL 0.9661 mL 2.4152 mL
30 mM 0.0805 mL 0.4025 mL 0.8051 mL 2.0126 mL
40 mM 0.0604 mL 0.3019 mL 0.6038 mL 1.5095 mL
50 mM 0.0483 mL 0.2415 mL 0.4830 mL 1.2076 mL
60 mM 0.0403 mL 0.2013 mL 0.4025 mL 1.0063 mL
80 mM 0.0302 mL 0.1509 mL 0.3019 mL 0.7547 mL
100 mM 0.0242 mL 0.1208 mL 0.2415 mL 0.6038 mL
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Epaminurad Related Classifications

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.

Keywords:

Epaminurad1198153-15-9UR-1102 URC-102UR1102UR 1102URC102URC 102URC-102URAT1Urate transporter 1SLC22A12HEK293 cellsUricosuricgouthyperuricemiap-aminohippuric acidurateInhibitorinhibitorinhibit

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