XEN445 |
| Catalog No.GC10248 |
XEN445는 강력하고 선택적인 EL 억제제(IC50=0.237 uM)로 우수한 ADME 및 PK 특성을 보여주고 마우스에서 혈장 HDLc 농도를 높이는 생체 내 효능을 입증했습니다.
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.
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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.
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