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XEN445
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
XEN445图片
CAS NO:1515856-92-4
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
2-[(3S)-3-(2-吡啶基甲氧基)-1-吡咯烷基]-5-(三氟甲基)苯甲酸
XEN 445
XEN-445
产品介绍
XEN445 是一种内皮脂肪酶抑制剂(IC50:0.237 uM),具有显著的ADME和PK活性,可以增强小鼠血浆中高密度脂蛋白胆固醇浓度。

产品描述

XEN445, a potent and selective endothelial lipase(EL) inhibitor (IC50=0.237 uM), exhibitis good ADME and PK properties.

体外活性

XEN445 exhibits good specificity over LPL and HL, and great inhibition activity against EL.

激酶实验

In vitro PI3K lipid kinase assay: (1) For PI3Kγ: human PI3Kγ (100 ng) is incubated at RT with kinase buffer (10 mM MgCl2, 1 mM β-glycerophosphate, 1 mM DTT, 0.1 mM Na3VO4, 0.1% Na Cholate and 15 μM ATP/100 nCi γ[33P]ATP, final concentrations) and lipid vesicles containing 18 μM PtdIns and 250 μM of PtdSer (final concentrations), in the presence of AS-605240 or DMSO. Kinase reaction is stopped by adding 250 μg of Neomycin-coated Scintillation Proximity Assay (SPA) beads. (2) For PI3Kα, β, and δ: varying amounts of ATP are incubated with the different purified PI3K isoforms and saturating concentrations of PtdIns. Consequently, IC50 determinations with PI3Kα, β, and δ, to evaluate inhibitor selectivity are performed as follows: 60 ng of PI3Kα are incubated at RT with kinase buffer, as described for PI3Kγ (but containing 89 μM ATP/300 nCi γ[33P]ATP and no Na Cholate, instead) and lipid vesicles containing 212 μM PtdIns and 58 μM of PtdSer. 100 ng of PI3Kβ are incubated at RT with kinase buffer (containing 70 μM ATP/300 nCi γ[33P]ATP, 4 mM MgCl2 and no Na Cholate) and lipid vesicles containing 225 μM PtdIns and 45 μM of PtdSer. 90 ng of PI3Kδ are incubated with kinase buffer (containing 65 μM ATP/300 nCi γ[33P]ATP, 1 mM MgCl2, and no Na Cholate) and lipid vesicles containing 100 μM PtdIns and 170 μM of PtdSer. The reactions are stopped after 2 hours.

Cas No.

1515856-92-4

分子式

C18H17F3N2O3

分子量

366.34

别名

2-[(3S)-3-(2-吡啶基甲氧基)-1-吡咯烷基]-5-(三氟甲基)苯甲酸;XEN 445;XEN-445

储存和溶解度

Ethanol:36.6 mg/mL (100 mM)
DMSO:36.6 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years