Iinerixibat-GSK2330672-DataSheet-生命科學試劑-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作靶點: Others作通路: Others儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據體外實驗 DMSO : 21.5 mg/mL (39.33 mM; Need ult

2、rasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內實驗 GSK2330672 is prepared in 1% methylcellulose3.BIOLOGICAL ACTIVITY物活性 Iinerixibat

3、(GSK2330672)效的, 不可吸收的ASBT抑制劑（IC50=423 nM ), 可于降低2型糖尿病的動物模型糖。IC50 & Target IC50: 423 nM (hASBT) 11/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 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體內研究 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戶使本產品發(fā)表的科研獻 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