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.
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- CAS. Nr.: 2803951-18-8
- Formel: C21H18BrN3O2S
- Molecular Weight:456.36
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
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].
In Vitro
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. Further protocols information, click here.
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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.
In Vivo
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. Nr. 2803951-18-8
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Molecular Weight 456.36
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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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.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
URAT1 inhibitor 2 Related Classifications
HY-143906 Related Classifications
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