Iinerixibat-GSK2330672-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIinerixibatCat. No.: HY-16643CAS No.: 1345982-69-5Synonyms: GSK2330672分式: CHNOS分量: 546.68作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 21.5 mg/mL (39.33 mM; Need ult

2、rasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.8292 mL 9.1461 mL 18.2922 mL5 mM 0.3658 mL 1.8292 mL 3.6584 mL10 mM 0.1829 mL 0.9146 mL 1.8292 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 GSK2330672 is prepared in 1% methylcellulose3.BIOLOGICAL ACTIVITY物活性 Iinerixibat

3、(GSK2330672)效的, 不可吸收的ASBT抑制剂（IC50=423 nM ), 可于降低2型糖尿病的动物模型糖。IC50 & Target IC50: 423 nM (hASBT) 11/2 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 Iinerixibat (GSK2330672) is a highly potent, nonabsorbable ASBT inhibitor with excellent aqueous solubility,selectivity, and developability properties

4、 for evaluation in safety studies and ultimately humans. Iinerixibat willbe a valuable clinical tool for exploring the therapeutic utility of a nonabsorbable ASBT inhibitor for treatmentof patients with type 2 diabetes.1体内研究 Iinerixibat (GSK2330672) results in potent inhibition of ASBT and very low

5、oral absorption in the rat.Iinerixibat shows potent mouse and rat ASBT activity and was stable in GI stability assays. Iinerixibat isstable in the rodent GI tract and potently induced fecal bile acid excretion in mice, leading us to select thesethree compounds for mechanistic and efficacy studies in

6、 vivo in lean rats and Zucker Diabetic Fatty (ZDF)rats, respectively.1户使本产品发表的科研献 Gene Expr. 2018 Aug 22;18(3):187-196.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Wu Y, et al. Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibito

7、r (GSK2330672) fortreatment of type 2 diabetes. J Med Chem. 2013 Jun 27;56(12):5094-114.2. Nunez DJ, et al. Glucose and lipid effects of the ileal apical sodium-dependent bile acid transporter inhibitor GSK2330672: double-blindrandomized trials with type 2 diabetes subjects taking metformin. Diabetes Obes Metab. 2016 Mar 4. doi: 10.1111/dom.12656.3. Wang Y, et al. HNF4 Regulates CSAD to Couple Hepatic Taurine Production to Bile Acid Synthesis in Mice. Gene Expr. 2018 Aug22;18(3):187-196.McePdfHeightCaution: Product has not been fully validated for medical applications.For