product name XEN445
Description: XEN445 is a potent and selective endothelial lipase inhibitor with IC50 of 0.237 μM. vitro, XEN445 has been reported to selectively inhibit EL with IC50 values of 0.237μM, 20μM and 9.5μM for hEL, hLPL and hHL, respectively. In addition, XEN445 has been revealed to suppress EL in EL-transfected HEK cells with an IC50 value of 0.25μM which is very similar to that tested in cell-free assay. Besides, XEN445 has shown significantly high oral bioavailability and low clearance rates in C57BL6 mice. In vivo, XEN445 has been evidenced to increase plasma HDLc in wild-type mice. Moreover, XEN445 has exhibited the HDL-raising effect because of on-target inhibition by using the EL knockout mice.
References: Bioorg Med Chem. 2013 Dec 15;21(24):7724-34.
366.33
Formula
C18H17F3N2O3
CAS No.
1515856-92-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 80 mg/mL (218.4 mM)
Water: <1 mg/mL
Ethanol: 34 mg/mL (92.8 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: XEN445 shows good in vitro inhibitory potency against EL, and high selectivity over LPL and HL. Kinase Assay: Cell Assay: In vitro, XEN445 has been reported to selectively inhibit EL with IC50 values of 0.237μM, 20μM and 9.5μM for hEL, hLPL and hHL, respectively. In addition, XEN445 has been revealed to suppress EL in EL-transfected HEK cells with an IC50 value of 0.25μM which is very similar to that tested in cell-free assay. Besides, XEN445 has shown significantly high oral bioavailability and low clearance rates in C57BL6 mice. |
|---|---|
| In Vivo | In vivo, XEN445 displays good ADME and PK properties. In mice, XEN445 (30 mg/kg, p.o.) raises plasma HDL-cholesterol concentration. |
| Animal model | Male EL knockout mice and age-matched wild-type male C57BL6 mice |
| Formulation & Dosage | Formulated in 0.2% Tween-20/1% carboxymethyl-cellulose; 30 mg/kg bid; p.o. |
| References | Bioorg Med Chem. 2013 Dec 15;21(24):7724-34. |
