URAT1-IN-17
URAT1-IN-17 is an orally active URAT1 inhibitor with an IC50 of 5.32 μM in HEK293T cells. URAT1-IN-17 inhibits URAT1-mediated uric acid reabsorption in the renal proximal tubule, thereby reducing serum uric acid levels. URAT1-IN-17 weakly inhibits OAT1-mediated organic anion transport. URAT1-IN-17 can be used for research on hyperuricemia.
For research use only. We do not sell to patients.
- CAS No.: 3129164-13-9
- Formula: C20H16BrN3O2S
- Molecular Weight:442.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
URAT1 5.32 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HK-2 | CC50 |
168.56 μM
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Cytotoxicity against human HK-2 cells assessed as reduction in cell viability by CCK-8 assay.
Cytotoxicity against human HK-2 cells assessed as reduction in cell viability by CCK-8 assay.
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42720468 |
In Vitro
URAT1-IN-17 (compound 17) (30 min) potently inhibits URAT1-mediated uric acid uptake in HEK293T cells with an IC50 of 5.32 μM[1].
URAT1-IN-17 (30 min) weakly inhibits OAT1 in HEK293T cells with an IC50 of 30.11 μM and an inhibition rate of 48.2% at 10 μM[1].
URAT1-IN-17 (0-200 μM) exhibits low cytotoxicity in HK-2 cells, with a CC50 of 168.56 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
In Vivo
URAT1-IN-17 (1000 mg/kg; gavage; single administration) does not cause death or obvious toxic reactions in mice at the high dose of 1000 mg/kg, indicating its low acute toxicity[1].
URAT1-IN-17 (50 mg/kg; p.o.; every other day; 14 days) shows good tolerability and a low subacute toxicity profile at a dose of 50 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kunming (KM) (male, acute hyperuricemia model)[1]
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Dosage:0.5 mg/kg; 1 mg/kg; 2 mg/kg
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Administration:p.o.; single dose; 3 h before induction
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Result:Reduced SUA levels with DR values of 42.0% at 0.5 mg/kg, 68.1% at 1 mg/kg, and 79.8% at 2 mg/kg.
Reduced SUA concentrations to 678 μM, 420 μM, and 305 μM at 0.5 mg/kg, 1 mg/kg, and 2 mg/kg, respectively.
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Animal Model:Kunming (KM) (male and female, healthy)[1]
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Dosage:1000 mg/kg
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Administration:i.g.; single dose
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Result:All male and female mice survived within 7 days after administration, with no death or abnormal behaviors.
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Animal Model:Kunming (KM) (male and female, healthy)[1]
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Dosage:50 mg/kg
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Administration:p.o.; every other day; 14 days
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Result:No animal death occurred.
No significant difference in body weight growth curves was found.
Histopathological analysis revealed no conspicuous pathological lesions in the heart, spleen, or lungs, with only slight reversible kidney injury occasionally found.
Chemical Information
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CAS No. 3129164-13-9
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Molecular Weight 442.33
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Formula C20H16BrN3O2S
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SMILES
OC(C(SC1=NC=NC2=C1N(C=C2)CC3=CC=C(C4=C3C=CC=C4)Br)C)=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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
URAT1-IN-17 Related Classifications
HY-189427 Related Classifications
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