XEN445 |
| カタログ番号GC10248 |
XEN445 は強力で選択的な EL 阻害剤 (IC50 = 0.237 uM) であり、良好な ADME および PK 特性を示し、マウスの血漿 HDLc 濃度を上昇させる in vivo 有効性を示しました。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1515856-92-4
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
XEN445 is a novel, highly selective and potent inhibitor of endothelial lipase(EL) with an IC 50 value of 0.237μM [1].
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, 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 [1].
References:
[1] Sun S1, Dean R, Jia Q, Zenova A, Zhong J, Grayson C, Xie C, Lindgren A, Samra P, Sojo L, van Heek M, Lin L, Percival D, Fu JM, Winther MD, Zhang Z. Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice. Bioorg Med Chem. 2013 Dec 15;21(24):7724-34.
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *