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编 号:F128766
分子式:C28H38N2O7S
分子量:546.68
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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生物活性:
Linerixibat (GSK2330672) is a highly potent, nonabsorbable and orally active apical sodium-dependent bile acid transporter (ASBT) inhibitor with an IC50 of 42 nM human ASBT. Linerixibat can be used as lipid-lowering agent. Linerixibat has the potential for type 2 diabetes and Primary Biliary Cholangitis treatment.

体内研究:
Linerixibat (GSK2330672;0.05-10 mg/kg;口服强饲法;每天两次;持续 14 天;雄性 ZDF 大鼠) 处理可降低 2 型糖尿病动物模型中的葡萄糖。Animal Model:Male Zucker Diabetic Fatty (ZDF) rat
Dosage:0.05 mg/kg, 0.1 mg/kg, 0.5 mg/kg, 1 mg/kg, 5 mg/kg, 10 mg/kg
Administration:Oral gavage; twice daily; for 14 days
Result:Led to a 1.30-1.64% reduction in hemoglobin A1c (HbA1c), a greater than 50% reduction in nonfasted plasma glucose to below 200 mg/dL, and statistically significant higher plasma insulin.

体外研究:
Linerixibat (化合物 56) 的两性离子、非吸湿性结晶盐形式在 pH 7.4 下显示出良好的水溶性 (>7 mg/mL)、出色的热稳定性,并且不会产生反应性或人特异性代谢物。
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