URAT1/GLUT9-IN-2
URAT1/GLUT9-IN-2 is a selective, orally active URAT1/GLUT9 inhibitor, with an IC50 of 2.81 μM against URAT1 and an IC50 of 12.53 μM against GLUT9. URAT1/GLUT9-IN-2 reduces serum uric acid levels and protects renal function. URAT1/GLUT9-IN-2 can be used in research related to hyperuricemia and hyperuricemic nephropathy.
For research use only. We do not sell to patients.
- CAS No.: 3051509-32-8
- Formula: C25H21N3O5S
- Molecular Weight:475.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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]|
GLUT9 12.53 μM (IC50) |
URAT1 2.81 μM (IC50) |
In Vitro
URAT1/GLUT9-IN-2 (Compound 42) (30 min) potently inhibits URAT1 in HEK293T cells expressing hURAT1, with an IC50 of 2.81 μM[1].
URAT1/GLUT9-IN-2 inhibits GLUT9 in HEK293T cells expressing hGLUT9, with an IC50 value of 12.53 μM[1].
URAT1/GLUT9-IN-2 (10 μM; 15 min) shows no significant xanthine oxidase (XOD) inhibitory activity, with an inhibition rate of only 14.43% at a concentration of 10 μM[1].
URAT1/GLUT9-IN-2 (30 min) inhibits OAT1-mediated transport in HEK293T cells expressing hOAT1, with an IC50 of 7.83 μM. Compared with ZS-24, it exhibits weaker off-target activity and improved selectivity[1].
URAT1/GLUT9-IN-2 (0-50 μM; 3-20 min) does not inhibit CYP1A2, CYP2C19 or CYP2D6, but moderately inhibits CYP2C9 and CYP3A4M, with IC50 values of 1.12 μM and 1.38 μM, respectively[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/GLUT9-IN-2 (2 mg/kg; p.o.; single administration) exhibits potent hypouricemic activity in acute hyperuricemic SD rats, reducing serum uric acid (SUA) by 89.25% at an oral dose of 2 mg/kg[1].
URAT1/GLUT9-IN-2 (2 mg/kg; i.p.; once daily; for 7 consecutive days) reduces serum uric acid levels and protects renal function in hyperuricemic nephropathy KM mice[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) mice (male)[1]
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Dosage:1 mg/kg; 0.5 mg/kg
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Administration:p.o.; single dose
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Result:Reduced SUA with a DR of 80.25% at 1 mg/kg.
Reduced SUA with a DR of 11.98% at 0.5 mg/kg.
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Animal Model:Sprague-Dawley (SD) rats[1]
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Dosage:2 mg/kg
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Administration:p.o.; single dose
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Result:Reduced SUA with a DR of 89.25%.
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Animal Model:Kunming (KM) mice (male)[1]
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Dosage:2 mg/kg
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Administration:i.p.; daily; 7 days
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Result:Significantly reduced SUA levels.
Decreased BUN and CRE levels.
Reduced kidney mass and kidney/body weight ratio.
Prevented renal edema/whitening compared to the model group.
Chemical Information
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CAS No. 3051509-32-8
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Molecular Weight 475.52
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Formula C25H21N3O5S
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SMILES
O=C(NS(=O)(C1=CC=CC([N+]([O-])=O)=C1)=O)C2=CC=CN2CC3=C4C=CC=CC4=C(C=C3)C5CC5
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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/GLUT9-IN-2 Related Classifications
HY-183543 Related Classifications
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