XEN 445

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Cat.No. 5839 - XEN 445 | C18H17F3N2O3 | CAS No. 1515856-92-4
Description: Selective endothelial lipase inhibitor; orally bioavailable
Chemical Name: 2-[(3S)-3-(2-Pyridinylmethoxy)-1-pyrrolidinyl]-5-(trifluoromethyl)benzoic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Selective endothelial lipase (EL) inhibitor (IC50 = 237 nM for human EL). Exhibits >20-fold selectivity for EL over lipoprotein lipase (LPL) and hepatic lipase (HL). Increases high density lipoprotein cholesterol (HDLc) plasma levels in mice. Orally bioavailable.

Technical Data

M. Wt 366.33
Formula C18H17F3N2O3
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1515856-92-4
PubChem ID 72736173
InChI Key NBGRERFNOKZQLO-AWEZNQCLSA-N
Smiles OC(C1=C(N2CC[C@H](OCC3=CC=CC=N3)C2)C=CC(C(F)(F)F)=C1)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36.63 100
ethanol 36.63 100

Preparing Stock Solutions

The following data is based on the product molecular weight 366.33. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.73 mL 13.65 mL 27.3 mL
5 mM 0.55 mL 2.73 mL 5.46 mL
10 mM 0.27 mL 1.36 mL 2.73 mL
50 mM 0.05 mL 0.27 mL 0.55 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Sun et al (2013) Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice. Bioorg.Med.Chem. 21 7724 PMID: 24211162


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Keywords: XEN445 Selective endothelial lipase EL inhibitors inhibits orally bioavailable Lipases

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