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

URAT1 inhibitor 3 is a potent, orally active, selective URAT1 inhibitor with an IC50 value of 0.8 nM. URAT1 inhibitor 3 has urate-lowering efficacy. URAT1 inhibitor 3 can be used in research of gout and hyperuricemi.

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

URAT1 inhibitor 3 Chemical Structure

URAT1 inhibitor 3 Chemical Structure

CAS No. : 2850331-30-3

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Based on 1 publication(s) in Google Scholar

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  • Purity & Documentation

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Description

URAT1 inhibitor 3 is a potent, orally active, selective URAT1 inhibitor with an IC50 value of 0.8 nM. URAT1 inhibitor 3 has urate-lowering efficacy. URAT1 inhibitor 3 can be used in research of gout and hyperuricemi[1].

IC50 & Target

IC50: 0.8 nM (URAT1)[1]

In Vitro

URAT1 inhibitor 3 (0-400 μM; 24 and 72 h; HepG2 and HK2 cells) has low toxicity and inhibits cell viability at high concentrations[1].
URAT1 inhibitor 3 (0.01-100 μM) has lower inhibition on urate excretion transporters with IC50 values of 10.16 μM and 4.04 μM of OAT1 and ABCG2, respectively[1].

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

Cell Viability Assay[1]

Cell Line: HepG2 and HK2 cells
Concentration: 0, 100, 200, 300, and 400 μM
Incubation Time: 24 and 72 hours
Result: Had little cytotoxicity at 24 h and inhibition rate of 34.75% and 35.9% of HepG2 and HK2 cells, respectively.
In Vivo

URAT1 inhibitor 3 (1-4 mg/kg; i.g.; once) has urate lowering efficacy in a mouse model of hyperuricemia[1].
URAT1 inhibitor 3 (50 mg/kg; i.g.; daily, for 14 d) has no hepatic and renal toxicities in mice[1].
URAT1 inhibitor 3 (50 mg/kg; i.g.; once) induces GSH depletion in Kunming mice with hyperuricemia model[1].

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

Animal Model: Male Kunming (KM) mice with hyperuricemia model[1]
Dosage: 1, 2, and 4 mg/kg
Administration: Oral gavage; once
Result: Decreased the serum urate levels in a dose-dependent manner.
Animal Model: Male Kunming mice[1]
Dosage: 50 mg/kg
Administration: Oral gavage; daily, for 14 days
Result: Did not cause renal toxicity.
Animal Model: Male Kunming mice with hyperuricemia model[1]
Dosage: 50 mg/kg
Administration: Oral gavage; once
Result: Decreased the serum GSH levels from 42.23 μM to 20.39 μM.
Molecular Weight

307.13

Formula

C14H8Cl2N2O2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CC(Cl)=C(O)C(Cl)=C1)N2C=CC3=CC=CN=C32

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 (325.60 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 3.2560 mL 16.2798 mL 32.5595 mL
5 mM 0.6512 mL 3.2560 mL 6.5119 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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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    90% Corn Oil

    Solubility: ≥ 10 mg/mL (32.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown). 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 (100.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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 3.2560 mL 16.2798 mL 32.5595 mL 81.3988 mL
5 mM 0.6512 mL 3.2560 mL 6.5119 mL 16.2798 mL
10 mM 0.3256 mL 1.6280 mL 3.2560 mL 8.1399 mL
15 mM 0.2171 mL 1.0853 mL 2.1706 mL 5.4266 mL
20 mM 0.1628 mL 0.8140 mL 1.6280 mL 4.0699 mL
25 mM 0.1302 mL 0.6512 mL 1.3024 mL 3.2560 mL
30 mM 0.1085 mL 0.5427 mL 1.0853 mL 2.7133 mL
40 mM 0.0814 mL 0.4070 mL 0.8140 mL 2.0350 mL
50 mM 0.0651 mL 0.3256 mL 0.6512 mL 1.6280 mL
60 mM 0.0543 mL 0.2713 mL 0.5427 mL 1.3566 mL
80 mM 0.0407 mL 0.2035 mL 0.4070 mL 1.0175 mL
100 mM 0.0326 mL 0.1628 mL 0.3256 mL 0.8140 mL
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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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URAT1 inhibitor 3
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