URAT1 inhibitor 2
URAT1 inhibitor 2 is an orally active and potent URAT1 and CYP isozyme inhibitor, with IC50 values of 1.36 μM, 16.97 μM, 5.22 μM for URAT1-mediated 14C-UA uptake, CYP1A2 and CYP2C9, respectively. URAT1 inhibitor 2 is a promising agent candidate in the study of hyperuricemia and gout.
For research use only. We do not sell to patients.
- CAS No.: 2803951-18-8
- Formula: C21H18BrN3O2S
- Molecular Weight:456.36
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 1.36 μM (URAT1-mediated 14C-UA uptake), 16.97 μM (CYP1A2), 5.22 μM (CYP2C9), >20 μM (CYP2C19), >20 μM (CYP2D6), and >20 μM (CYP3A4M)[1].
URAT1 inhibitor 2 (compound 23) (0-50 μM, 3-20 min) inhibits URAT1-mediated 14C-UA uptake (IC50 = 1.36 μM) and CYP cells activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human URAT1, CYP cells[1]
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Concentration:0, 0.05, 0.15, 0.5, 1.5, 5.0, 15, and 50 μM
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Incubation Time:3-20 min
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Result:Inhibited URAT1-mediated 14C-UA uptake and CYP cells activity.
URAT1 inhibitor 2 (4, 2, 1, 0.5, and 0.25 mg/kg; Orally) shows orally active and outstanding SUA-lowering activity with a dose-dependent manner in acute hyperuricemia mice[1].
URAT1 inhibitor 2 (1000 mg/kg, intragastric administration, once) shows favorable safety profiles and no obvious acute toxicity[1].
Pharmacokinetic Parameters of URAT1 inhibitor 2 in male Sprague-Dawley rats[1].
| parameter | unit | p.o. | i.v. |
| compoundmax (h) | 23 | 23 | |
| AUC (0-t) | ng/mL·h | 48754.6 | 16344.8 |
| AUC (0-∞) | ng/mL·h | 48781.5 | 16448.8 |
| MRT (0-∞) | h | 3.3 | 1.0 |
| t1/2 | h | 2.2 | 1.8 |
| Tmax | h | 0.3 | |
| Cmax | ng/mL | 19185.0 | |
| CL | mL/min/kg | 2.2 | |
| F | % | 59.3 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (n=10)[1]
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Dosage:2 mg/kg (intravenous) or 10 mg/kg (oral administration)
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Administration:Intravenous or oral administration
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Result:Achieved excellent pharmacokinetic properties with the oral bioavailability of 59.3%.
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Animal Model:Acute hyperuricemia mice[1]
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Dosage:4, 2, 1, 0.5, and 0.25 mg/kg
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Administration:Orally, once
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Result:Showed outstanding SUA-lowering activity.
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Animal Model:Kunming mice[1]
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Dosage:1000 mg/kg
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Administration:Itragastric administration, once
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Result:Showed favorable safety profiles and no obvious acute toxicity.
Chemical Information
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CAS No. 2803951-18-8
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Molecular Weight 456.36
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Formula C21H18BrN3O2S
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SMILES
O=C(C(C)(SC1=NC2=NC=CC=C2N1CC3=C4C=CC=CC4=C(C=C3)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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
URAT1 inhibitor 2 Related Classifications
HY-143906 Related Classifications
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