Linerixibat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种高效、选择性、回肠顶端钠依赖性胆汁酸转运蛋白 (ASBT) 抑制剂，对小鼠/大鼠 ASBT 的 IC50 分别为 2.1/1.9 nM。

A highly potent, selective, ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor with IC50 of 2.1/1.9 nM for mouse/rat ASBT, respectively; lowers glucose in an animal model of type 2 diabetes, shows excellent developability properties for evaluating the potential therapeutic utility of a nonabsorbable ASBT inhibitor for treatment of patients with type 2 diabetes.Diabetes Phase 2 Clinical(In Vitro):The zwitterionic, nonhygroscopic, crystalline salt form of Linerixibat (Compound 56) shows good aqueous solubility at pH 7.4 (>7 mg/mL), excellent thermal stability, and did not generate reactive or humanspecific metabolite, characteristics.(In Vivo):Linerixibat (GSK2330672; 0.05-10 mg/kg; oral gavage; twice daily; for 14 days; male ZDF rat) treatment lowers glucose in an animal model of type 2 diabetes.

——

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.

GSK-2330672 | GSK2330672

Membrane Transporter/Ion Channel

ASBT Transporter

hASBT

Metabolic Disease

Diabetes

1345982-69-5

546.679

C28H38N2O7S

>98% (HPLC)

DMSO: 21.5 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C(O)CC(NCC1=C(OC)C=C(C2=C1)[C@@H](C3=CC=CC=C3)N[C@](CC)(CCCC)CS2(=O)=O)CC(O)=O

3-[[[(3R,5R)-3-Butyl-3-ethyl-2,3,4,5-tetrahydro-7-methoxy-1,1-dioxido-5-phenyl-1,4-benzothiazepin-8-yl]methyl]amino]pentanedioic acid

(-20℃)

With Ice Pack

≥ 2 years