GSK2330672 | CAS:1345982-69-5

Chemscene社は、高品質な低分子化合物を提供しているメーカーです。
Chemscene社のGSK2330672(CAS:1345982-69-5)をご紹介します。

※本製品は研究用です。研究用以外には使用できません。

Name:GSK2330672; linerixibat
Cat. No. :CS-5447
CAS No. :1345982-69-5
Formula:C28H38N2O7S
M. Wt. : 546.68
Solubility:DMSO: 21.5 mg/mL

GSK2330672 is a highly potent, nonabsorbable ASBT(apical sodium-dependent bile acid transporter) inhibitor (hASBT IC50=42 ± 3 nM) which lowers glucose in an animal model of type 2 diabetes and shows excellent developability properties for evaluating the potential therapeutic utility of a nonabsorbable ASBT inhibitor for treatment of patients with type 2 diabetes. IC50 value: 42 ± 3 nM [1]Target: hASBTin vitro: GSK2330672 is a highly potent, nonabsorbable ASBT inhibitor with excellent aqueous solubility, selectivity, and developability properties for evaluation in safety studies and ultimately humans. GSK2330672 will be a valuable clinical tool for exploring the therapeutic utility of a nonabsorbable ASBT inhibitor for treatment of patients with type 2 diabetes.[1]in vivo: GSK2330672 results in potent inhibition of ASBT and very low oral absorption in the rat. GSK2330672 shows potent mouse and rat ASBT activity and was stable in GI stability assays. GSK2330672 is stable in the rodent GI tract and potently induced fecal bile acid excretion in mice, leading us to select these three compounds for mechanistic and efficacy studies in vivo in lean rats and Zucker Diabetic Fatty (ZDF) rats, respectively.[1]

Nunez DJ, et al. Glucose and lipid effects of the ileal apical sodium-dependent bile acid transporter inhibitor GSK2330672: double-blind randomized trials with type 2 diabetes subjects taking metformin. Diabetes Obes Metab. 2016 Mar 4. doi: 10.1111/dom.12656. Wu Y, et al. Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes. J Med Chem. 2013 Jun 27;56(12):5094-114.