URAT1-IN-18
URAT1-IN-18 is an orally effective URAT1 inhibitor. URAT1-IN-18 inhibits URAT1-mediated urate transport and renal urate reabsorption. URAT1-IN-18 exhibits low cytotoxicity in vitro, with less apoptosis and loss of mitochondrial membrane potential. URAT1-IN-18 shows moderate metabolic stability in rat liver microsomes. URAT1-IN-18 reduces serum uric acid levels in a hyperuricemia mouse model, protects renal tubular structure, and has good biosafety. URAT1-IN-18 can be used for research related to hyperuricemia.
For research use only. We do not sell to patients.
- CAS No.: 3133114-23-2
- Formula: C14H7Cl2NO3S
- Molecular Weight:340.18
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
111.4 μM
|
Cytotoxicity against human embryonic kidney 293 T cells assessed as viability reduction after 72 hrs by CCK-8 assay.
Cytotoxicity against human embryonic kidney 293 T cells assessed as viability reduction after 72 hrs by CCK-8 assay.
|
42743610 |
| HepG2 | IC50 |
319.8 μM
|
Cytotoxicity against human hepatocellular carcinoma HepG2 cells assessed as viability reduction after 72 hrs by CCK-8 assay.
Cytotoxicity against human hepatocellular carcinoma HepG2 cells assessed as viability reduction after 72 hrs by CCK-8 assay.
|
42743610 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human embryonic kidney 293 T cells and human hepatocellular carcinoma HepG2 cells
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Concentration:100 μM
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Incubation Time:24 h
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Result:Induced minimal apoptosis in 293 T cells (1.3%) and HepG2 cells (3.8%).
Parmacokinetics
In Vivo
URAT1-IN-18 (2 mg/kg; p.o.; once daily; days 1-14 and days 15-19) reduced serum uric acid in a chronic hyperuricemia Kunming mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kunming (male; 3-week-old; 19-21 g)[1]
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Dosage:2 mg/kg
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Administration:p.o. (gavage); once daily; for 5 consecutive days
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Result:Reduced serum uric acid to 613.7 μM, corresponding to a 48.1% decrease rate.
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Animal Model:Kunming (male; 3-week-old; 19-21 g)[1]
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Dosage:2 mg/kg
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Administration:p.o. (gavage); once daily; days 1-14 and days 15-19
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Result:Reduced serum uric acid to 421 μM, corresponding to a 64.1% decrease rate.
The renal tubule structures were more intact and arranged more regularly.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Mitochondrial membrane-potential fluorescent assay
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Fluorescent plasma-membrane potential dye assay
- Mitochondrial membrane-potential and mitochondrial mass staining
- Apoptosis Solutions
- Cell Viability Determination by MTT Colorimetric Assay
- How to Choose the Right Model Animal
Chemical Information
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CAS No. 3133114-23-2
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Molecular Weight 340.18
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Formula C14H7Cl2NO3S
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SMILES
O=C1SC2=CC=CC=C2N1C(C3=CC(Cl)=C(O)C(Cl)=C3)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)