製品番号: HY-111345

Epaminurad

(別名: UR-1102; URC-102)

カスタマーレビュー

Based on 1 Customer Validation

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.75%
CAS 番号: 1198153-15-9
分子式: C₁₄H₁₀Br₂N₂O₃
分子量:414.05

保管条件:

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

Epaminurad 構造式

CAS 番号: 1198153-15-9

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
- 臨床実験
化学情報
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

Ki: 0.057 ± 0.036 μM (URAT1), 2.4 ± 0.2 μM (OAT3), 7.2 ± 0.8 μM (OAT1)^[1].

体外実験

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.

体内実験

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.

臨床実験

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

化学情報

CAS 番号 1198153-15-9
性状 Solid
分子量 414.05
分子式 C₁₄H₁₀Br₂N₂O₃
Color White to off-white
SMILES

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

UR-1102; URC-102
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
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- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

生物活性

化学情報

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

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

生物活性

化学情報

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Epaminurad 関連分類

HY-111345 関連分類