1. Membrane Transporter/Ion Channel
  2. URAT1
  3. URAT1 inhibitor 2

URAT1 inhibitor 2 

Cat. No.: HY-143906
Handling Instructions

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 drug candidate in the study of hyperuricemia and gout.

For research use only. We do not sell to patients.

URAT1 inhibitor 2 Chemical Structure

URAT1 inhibitor 2 Chemical Structure

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Description

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 drug candidate in the study of hyperuricemia and gout[1].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line: Human URAT1, CYP cells[1]
Concentration: 0, 0.05, 0.15, 0.5, 1.5, 5.0, 15, and 50 μM
Incubation Time: 3-20 min
Result: Inhibited URAT1-mediated 14C-UA uptake and CYP cells activity.
In Vivo

URAT1 inhibitor 2 (Intravenous at 2 mg/kg or orally at 10 mg/kg) has excellent pharmacokinetic properties with the oral bioavailability of 59.3%[1].
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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (n=10)[1]
Dosage: 2 mg/kg (intravenous) or 10 mg/kg (oral administration)
Administration: Intravenous or oral administration
Result: Achieved excellent pharmacokinetic properties with the oral bioavailability of 59.3%.
Animal Model: Acute hyperuricemia mice[1]
Dosage: 4, 2, 1, 0.5, and 0.25 mg/kg
Administration: Orally, once
Result: Showed outstanding SUA-lowering activity.
Animal Model: Kunming mice[1]
Dosage: 1000 mg/kg
Administration: Itragastric administration, once
Result: Showed favorable safety profiles and no obvious acute toxicity.
Molecular Weight

456.36

Formula

C21H18BrN3O2S

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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URAT1 inhibitor 2
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HY-143906
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