URAT1/GLUT9-IN-1_product_DataBase

Bioactivity	URAT1/GLUT9-IN-1(compound 29) can inhibit both uric acid transporter 1(URAT1)(IC50=2.01 μM) and glucose transporter 9(GLUT9)(IC50=18.21 μM). URAT1/GLUT9-IN-1 exhibits favorable pharmacokinetic properties and oral bioavailability. URAT1/GLUT9-IN-1 can be uesd for gout and hyperuricemia research[1].
Invitro	URAT1/GLUT9-IN-1 对 urat1 介导的 14c-尿酸摄取具有最有效的抑制作用(IC50= 2.01 μM)，是 Lesinurad(HY-15258)(IC50= 5.54 μM) 的 3 倍左右[1]。URAT1/GLUT9-IN-1 (5 μM) 对 GLUT9 的体外抑制活性略优于 Benzbromarone(HY-B1135)， IC50 值为 18.21±1.03 μM[1]。URAT1/GLUT9-IN-1 (10 μM) 对 XOD 的抑制率小于 20%，表明其抑制作用可以忽略不计[1]。URAT1/GLUT9-IN-1 抑制 CYP(CYP2C9 (IC50= 2.00 μM) 和 CYP2C19 (IC50= 5.93 μM)) 药物代谢酶的抑制电位，表明具有较低的肝毒性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> URAT1/GLUT9-IN-1 相关抗体:
In Vivo	URAT1/GLUT9-IN-1 (0.25， 0.5， 1mg/kg， po) 对急性高尿酸血症小鼠模型的降低 SUA 活性最小有效剂量约为 0.5 mg/kg[1]。URAT1/GLUT9-IN-1 (2mg/kg， po) 显示出作为降低 SUA 活性的候选药物的巨大潜力，与 Lesinurad(HY-15258) 相比，其效力高约 1.8 倍在稳定的高尿酸血症大鼠模型中[1]。URAT1/GLUT9-IN-1 (100 mg/kg， 100 mg/kg，隔一天口服，为期 14 天) 较 Lesinurad(HY-15258) 组安全性显著提高在慢性高尿酸血症小鼠[1]。Pharmacokinetic Analysis in SD rats[1]Route
CAS	2883011-18-3
Formula	C23H21N3O2S2
Molar Mass	435.56
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Shi X, et al. Discovery of a Novel Thienopyrimidine Compound as a Urate Transporter 1 and Glucose Transporter 9 Dual Inhibitor with Improved Efficacy and Favorable Druggability[J]. Journal of Medicinal Chemistry, 2024, 67(6): 5032-5052.

PeptideDB

URAT1/GLUT9-IN-1

CAS: 2883011-18-3 F: C23H21N3O2S2 W: 435.56