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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-ASBT Transporter (SLC10A2)-Linerixibat
Linerixibat

Chemical Structure : Linerixibat

CAS No.: 1345982-69-5

Linerixibat (GSK-2330672, GSK2330672)

货号: PC-61384Not For Human Use, Lab Use Only.

Linerixibat (GSK2330672) is 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.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Linerixibat (GSK2330672) is 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.
Linerixibat (GSK2330672 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.

物理化学性质&存储条件

分子量 546.679
分子式 C28H38N2O7S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Wu Y, et al. J Med Chem. 2013 Jun 27;56(12):5094-114.

2. Nunez DJ, et al. Diabetes Obes Metab. 2016 Jul;18(7):654-62.

3. Hegade VS, et al. Lancet. 2017 Mar 18;389(10074):1114-1123.

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