URAT1 inhibitor 3

• CAT Number: I042819
• CAS Number: 2850331-30-3
• Molecular Formula: C14H8Cl2N2O2
• Molecular Weight: 307.13
• Purity: ≥95%
• Synonyms: (3,5-dichloro-4-hydroxyphenyl)-pyrrolo[2,3-b]pyridin-1-ylmethanone
• InChI: InChI=1S/C14H8Cl2N2O2/c15-10-6-9(7-11(16)12(10)19)14(20)18-5-3-8-2-1-4-17-13(8)18/h1-7,19H
• InChIKey: HVYNCNZJQZOKFM-UHFFFAOYSA-N
• SMILES: C1=CC2=C(N=C1)N(C=C2)C(=O)C3=CC(=C(C(=C3)Cl)O)Cl

URAT1 inhibitor 3 is a potent, orally active, selective URAT1 inhibitor with an IC50 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].
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 IC50 values of 10.16 μM and 4.04 μM of OAT1 and ABCG2, respectively[1].
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].

Reference

[1]. Zhao Z, et, al. Discovery of novel benzbromarone analogs with improved pharmacokinetics and benign toxicity profiles as antihyperuricemic agents. Eur J Med Chem. 2022 Nov 15;242:114682.
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