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XEN445 

Cat. No.: HY-12246 Purity: 95.09%
Handling Instructions

XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.

For research use only. We do not sell to patients.

XEN445 Chemical Structure

XEN445 Chemical Structure

CAS No. : 1515856-92-4

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Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 77 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 130 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 700 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice. IC50 value: 0.237 uM [1] Target: Endothelial lipase inhibitor XEN445 can be readily prepared in good yield from commercial available chemicals, which was selected for further evaluation of this series of EL inhibitors. After a 30 min preincubation of EL-expressing HEK cells with XEN445, the IC50 value for XEN445 of 0.25 lM was obtained. This value was very similar to that determined in the cell-free assay. Wild-type mice were orally dosed with XEN445 at 30 mg/kg b.i.d. for 3 days and blood was taken on the morning of day 4, 16 h post final dose. At termination, the average plasma levels of XEN445 was 9.9 lM and the drug caused an 18% and 16% increase in total plasma cholesterol and HDLc, respectively.

Molecular Weight

366.33

Formula

C18H17F3N2O3

CAS No.
SMILES

O=C(O)C1=CC(C(F)(F)F)=CC=C1N2C[[email protected]@H](OCC3=NC=CC=C3)CC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 40 mg/mL (109.19 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7298 mL 13.6489 mL 27.2978 mL
5 mM 0.5460 mL 2.7298 mL 5.4596 mL
10 mM 0.2730 mL 1.3649 mL 2.7298 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Product Name:
XEN445
Cat. No.:
HY-12246
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