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XEN445

Catalog No. T2249 CAS 1515856-92-4

Synonyms: XEN-445, 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

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

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XEN445, CAS 1515856-92-4

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	XEN445, a potent and selective endothelial lipase(EL) inhibitor (IC50=0.237 uM), exhibitis good ADME and PK properties.
Targets&IC50	endothelial lipase:0.237 μM
In vitro	XEN445 exhibits good specificity over LPL and HL, and great inhibition activity against EL.
Kinase Assay	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.

Synonyms	XEN-445, 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
Molecular Weight	366.34
Formula	C18H17F3N2O3
CAS No.	1515856-92-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: 36.6 mg/mL (100 mM)

DMSO: 36.6 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Sun S, et al. Bioorg Med Chem. 2013, 21(24), 7724-7734.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Obesity Compound Library Inhibitor Library Anti-Metabolism Disease Compound Library Fluorochemical Library Bioactive Lipid Compound Library Protease Inhibitor Library Anti-Aging Compound Library Bioactive Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

XEN445 1515856-92-4 代谢 Lipase Inhibitor inhibit XEN-445 XEN 445 inhibitor

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