Linerixibat

Name: Linerixibat
Brand: TargetMol
SKU: T3978
Price: 828 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.98%

货号 T3978Cas号 1345982-69-5

别名 Iinerixibat, GSK2330672

Linerixibat (GSK2330672) 是高效的、不可吸收的、具有口服活性的顶端钠依赖性胆汁酸转运蛋白 (ASBT) 抑制剂，对人ASBT 的IC50为 42 nM。它是一种降脂剂，具有用于 2 型糖尿病和原发性胆源性胆管炎的研究潜力。

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Linerixibat

一键复制产品信息

很棒

纯度: 99.98%

货号 T3978 别名 Iinerixibat, GSK2330672Cas号 1345982-69-5

规格	价格	库存
1 mg	¥ 828	现货
2 mg	¥ 1,260	现货
5 mg	¥ 2,270	现货
10 mg	¥ 3,790	现货
25 mg	¥ 5,970	现货
50 mg	¥ 8,420	现货
1 mL x 10 mM (in DMSO)	¥ 2,730	现货

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产品介绍

Linerixibat AI Summary

Linerixibat exhibits bioactivities related to the inhibition of ASBT (Apical Sodium-dependent Bile Acid Transporter) and displays antidiabetic properties as well as antiviral activity. It shows potent inhibition of ASBT in rat, mouse, and human cell models with varying IC50 values, leading to increased fecal bile acid excretion and high drug recovery in rat feces. In Zucker diabetic fatty rats, it resulted in reduced non-fasted plasma glucose levels and blood HbA1c levels, demonstrating significant antidiabetic activity. The compound also inhibits taurocholate uptake with an IC50 of 43.0 nM and has favorable aqueous solubility and pharmacokinetic profiles in different animal models. Additionally, Linerixibat exhibits antiviral activity by inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 cells and VERO-6 cells with various inhibition rates and demonstrates SARS-CoV-2 3CL-Pro protease inhibition at 20µM. It also shows inhibitory activity against the human HDAC6 enzyme, suggesting potential as an HDAC6 inhibitor in enzymatic assays..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Linerixibat (GSK2330672) is a highly effective, nonabsorbable ASBT inhibitor (IC50: 42 ± 3 nM). It can lower glucose in an animal model of type 2 diabetes and shows excellent developability properties.
靶点活性	ASBT:42 ± 3 nM
别名	Iinerixibat, GSK2330672

化学信息

分子量	546.68
分子式	C₂₈H₃₈N₂O₇S
CAS No.	1345982-69-5
Smiles	CCCC[C@]1(CC)CS(=O)(=O)c2cc(CNC(CC(O)=O)CC(O)=O)c(OC)cc2[C@H](N1)c1ccccc1
密度	1.218 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 21.5 mg/mL (39.33 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8292 mL	9.1461 mL	18.2922 mL	91.4612 mL
5 mM	0.3658 mL	1.8292 mL	3.6584 mL	18.2922 mL
10 mM	0.1829 mL	0.9146 mL	1.8292 mL	9.1461 mL
20 mM	0.0915 mL	0.4573 mL	0.9146 mL	4.5731 mL