Linerixibat - 10mM in DMSO , Ileal bile acid transporter inhibitor, CAS No.1345982-69-5, Ileal bile acid transporter inhibitor

CAS: 1345982-69-5 Cat. No.: L655600 分子式: C₂₈H₃₈N₂O₇S 分子量: 546.68 EC番号: 876-203-0 PubChem CID: 53492727

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Linerixibat (GSK2330672) is a highly potent, nonabsorbable and orally active apical sodium-dependent bile acid transporter (ASBT) inhibitor with an IC 50 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

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.

IC50& Target:IC50: 42 nM (Apical sodium-dependent bile acid transporter (ASBT))

Specifications

仕様と純度

10mM in DMSO

生化学的・生理学的メカニズム

Linerixibat (GSK2330672) is a highly potent, nonabsorbable and orally active apical sodium-dependent bile acid transporter (ASBT) inhibitor with an IC 50 of 42 nM human ASBT . Linerixibat can be used as lipid-lowering agent. Linerixibat has the potential

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

アクションタイプ

INHIBITOR

作用メカニズム

Ileal bile acid transporter inhibitor

製品の性質

• ALogP: -1.6

名前と識別子

• 異性体SMILES: CCCC[C@@]1(CS(=O)(=O)C2=C(C=C(C(=C2)CNC(CC(=O)O)CC(=O)O)OC)[C@H](N1)C3=CC=CC=C3)CC
• 代替CAS番号: 1345982-69-5
• PubChem CID: 53492727
• MeSH用語: 3-((((3R,5R)-3-butyl-3-ethyl-7-(methyloxy)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,4-benzothiazepin-8-yl)methyl)amino)pentanedioic acid;GSK2330672
• 分子量: 546.68

関連ターゲット（人間）

SLC10A2 Tclin Ileal sodium/bile acid cotransporter (2 Activities)

Discover Target: SLC10A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

よくある質問

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1345982-69-5, the molecular formula is C28H38N2O7S, and the molecular weight is 546.68 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.