URAT1 inhibitor 3 是一种口服有效的选择性URAT1抑制剂，其IC50值为 0.8 nM。URAT1 inhibitor 3 具有降低尿酸的作用。URAT1 inhibitor 3 可用于痛风和高尿酸血症的研究。
| 生物活性 | URAT1 inhibitor3 is a potent, orally active, selectiveURAT1inhibitor with anIC50value of 0.8 nM.URAT1 inhibitor3 has urate-lowering efficacy.URAT1 inhibitor3 can be used in research of gout and hyperuricemi[1]. |
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体外研究
(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 IC50values of 10.16 μM and 4.04 μM of OAT1 and ABCG2, respectively[1].
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. |
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体内研究
(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].
| 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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