URAT1 inhibitor 2 是一种口服有效的URAT1和CYP isozyme抑制剂，对 URAT1 介导的14C-UA 吸收、CYP1A2、CYP2C9 的IC50分别为 1.36 μM、16.97 μM、5.22 μM。URAT1 inhibitor 2 在高尿酸血症和痛风的研究中是一个有前途的候选药物。

URAT1 inhibitor 2 is an orally active and potent URAT1 and CYP isozyme inhibitor, with IC 50 values of 1.36 μM, 16.97 μM, 5.22 μM for URAT1-mediated 14 C-UA uptake, CYP1A2 and CYP2C9, respectively. URAT1 inhibitor 2 is a promising drug candidate in the study of hyperuricemia and gout [1].

URAT1 inhibitor 2 (compound 23) (0-50 μM, 3-20 min) inhibits URAT1-mediated 14 C-UA uptake ( IC 50 = 1.36 μM) and CYP cells activity [1]. 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.

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. compound max (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 t 1/2 h 2.2 1.8 T max h 0.3 C max ng/mL 19185.0 CL mL/min/kg 2.2 F % 59.3 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.

C21H18BrN3O2S

456.36

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years