URAT1/GLUT9-IN-1
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.
For research use only. We do not sell to patients.
- CAS No.: 2883011-18-3
- Formula: C23H21N3O2S2
- Molecular Weight:435.56
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
GLUT9 18.21 μM (IC50) |
URAT1/GLUT9-IN-1 possesses the most effective inhibition of URAT1-mediated 14C-uric acid uptake (IC50=2.01 μM), which is about three times more potent than Lesinurad(HY-15258) (IC50=5.54 μM)[1].
URAT1/GLUT9-IN-1 (5 μM) compares to Benzbromarone(HY-B1135) at a concentration of 5 μM and demonstrated an IC50 value of 18.21±1.03 μM[1].
URAT1/GLUT9-IN-1 (10 μM) inhibits to xanthine oxidase(XOD) less than 20%, indicating its negligible inhibitory activity[1].
URAT1/GLUT9-IN-1 inhibits the inhibitory potential of CYP drug metabolizing enzymes(CYP2C9 (IC50= 2.00 μM) and CYP2C19 (IC50= 5.93 μM)) and exhibits a low potential for inducing hepatotoxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
URAT1/GLUT9-IN-1 (2mg/kg, po.) exhibits significant potential as a SUA reduction drug, demonstrating approximately 1.8-fold higher potency compared to Lesinurad(HY-15258) in a stable hyperuricemia rat model[1].
URAT1/GLUT9-IN-1 (100 mg/kg, po.; every other day for a period of 14 days) displays significantly enhanced safety profiles compared to Lesinurad(HY-15258) in Mice with Chronic Hyperuricemia[1].
Pharmacokinetic Analysis in AD rats[1]
| Route | Dose (mg/kg) | AUC0_t (ng•h/mL) | AUC0_INF (ng•h/mL) | MRT0_INF (h) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | Cl (L•h/kg) | F (%) |
| p.o. | 2 | 1813.4 | 7929.1 | 2.5 | 1.8 | 0.25 | 1272.7 | / | 20.1 |
| i.v. | 2 | 1903.7 | 1922.9 | 0.5 | 1.6 | 0.083 | 6591.8 | 17.5 | / |