Cat. No.: HY-111345

Epaminurad

(Synonyms: UR-1102; URC-102)

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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.

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Pureté: 99.75%
CAS No.: 1198153-15-9
Formule: C₁₄H₁₀Br₂N₂O₃
Masse moléculaire:414.05

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Epaminurad Chemical Structure

CAS No.: 1198153-15-9

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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.

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

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1198153-15-9
Appearance Solid
Masse moléculaire 414.05
Formule C₁₄H₁₀Br₂N₂O₃
Color White to off-white
SMILES

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

UR-1102; URC-102
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4152 mL

12.0758 mL

24.1517 mL

5 mM

0.4830 mL

2.4152 mL

4.8303 mL

10 mM

0.2415 mL

1.2076 mL

2.4152 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Ahn SO, et al. Stronger Uricosuric Effects of the Novel Selective URAT1 Inhibitor UR-1102 Lowered Plasma Urate in Tufted Capuchin Monkeys to a Greater Extent than Benzbromarone. J Pharmacol Exp Ther. 2016 Apr;357(1):157-66. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Epaminurad

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Epaminurad Related Classifications

HY-111345 Related Classifications