[CAS NO. 2850331-30-3] URAT1 inhibitor 3
PRODUCTS SPECIFICATIONS [2850331-30-3]
DESCRIPTION [2850331-30-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 307.13 |
| Molecular Formula | C14H8Cl2N2O2 |
| SMILES | O=C(C1=CC(Cl)=C(O)C(Cl)=C1)N2C=CC3=CC=CN=C32 |
Summary
URAT1 inhibitor 3 is a potent, orally active, selective URAT1 inhibitor with an IC 50 value of 0.8 nM. URAT1 inhibitor 3 has urate-lowering efficacy. URAT1 inhibitor 3 can be used in research of gout and hyperuricemi [1] .
IC50 & Target
IC50: 0.8 nM (URAT1) [1]
In Vitro
URAT1 inhibitor 3 (0-400 μM; 24 and 72 h; HepG2 and HK2 cells) has low toxicity and inhibits cell viability at high concentrations
[1]
.
URAT1 inhibitor 3 (0.01-100 μM) has lower inhibition on urate excretion transporters with IC
50
values of 10.16 μM and 4.04 μM of OAT1 and ABCG2, respectively
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | HepG2 and HK2 cells |
| Concentration: | 0, 100, 200, 300, and 400 μM |
| Incubation Time: | 24 and 72 hours |
| Result: | Had little cytotoxicity at 24 h and inhibition rate of 34.75% and 35.9% of HepG2 and HK2 cells, respectively. |
In Vivo
URAT1 inhibitor 3 (1-4 mg/kg; i.g.; once) has urate lowering efficacy in a mouse model of hyperuricemia
[1]
.
URAT1 inhibitor 3 (50 mg/kg; i.g.; daily, for 14 d) has no hepatic and renal toxicities in mice
[1]
.
URAT1 inhibitor 3 (50 mg/kg; i.g.; once) induces GSH depletion in Kunming mice with hyperuricemia model
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Kunming (KM) mice with hyperuricemia model [1] |
| Dosage: | 1, 2, and 4 mg/kg |
| Administration: | Oral gavage; once |
| Result: | Decreased the serum urate levels in a dose-dependent manner. |
| Animal Model: | Male Kunming mice [1] |
| Dosage: | 50 mg/kg |
| Administration: | Oral gavage; daily, for 14 days |
| Result: | Did not cause renal toxicity. |
| Animal Model: | Male Kunming mice with hyperuricemia model [1] |
| Dosage: | 50 mg/kg |
| Administration: | Oral gavage; once |
| Result: | Decreased the serum GSH levels from 42.23 μM to 20.39 μM. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.