An endothelial lipase inhibitor
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XEN445

Item No. 19144

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(3S)-3-(2-pyridinylmethoxy)-1-pyrrolidinyl]-5-(trifluoromethyl)-benzoic acid
CAS Number
1515856-92-4
Molecular Formula
C18H17F3N2O3
Formula Weight
366.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 25 mg/mlEthanol: 14 mg/ml
λmax
274, 329 nm
SMILES
OC(C1=CC(C(F)(F)F)=CC=C1N2CC[C@H](OCC3=NC=CC=C3)C2)=O
InChi Code
InChI=1S/C18H17F3N2O3/c19-18(20,21)12-4-5-16(15(9-12)17(24)25)23-8-6-14(10-23)26-11-13-3-1-2-7-22-13/h1-5,7,9,14H,6,8,10-11H2,(H,24,25)/t14-/m0/s1
InChi Key
NBGRERFNOKZQLO-AWEZNQCLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    Endothelial lipase, a member of the triglyceride lipase gene family expressed in endothelial cells, prefers phospholipid-enriched high-density lipoprotein (HDL) over triglyceride as a substrate. XEN445 is an endothelial lipase inhibitor (IC50 = 237 nM) that demonstrates selectivity for endothelial lipase compared to lipoprotein and hepatic lipases (IC50s = 20 and 9.5 µM, respectivley).1 An oral dose of 30 mg/kg XEN445 is reported to increase HDL cholesterol concentrations by 16% after three days and by 30% after nine days dosing in wild-type mice.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sun, S., Dean, R., Jia, Q., et al. Discovery of XEN445: A potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice. Bioorg. Med. Chem. 21(24), 7724-7734 (2013).