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| 【主 题】 ： |
GW3965 |
| 【联系人名】 ： |
Linna Green |
| 【电子邮件】 ： |
account@bocsci.com |
| 【联系电话】 ： |
15166698109 |
| 【发布日期】 ： |
2016-9-6 |
| 【详细说明】 ： |
GW3965 is a potent, selective LXR agonist for hLXRα
and hLXRβ. When screened against a panel of nuclear
receptors, it cross-reacted with only the pregnane X
receptor (PXR).
In Vitro: Recruit the steroid receptor coactivator 1
to human LXRα with EC50 of 125 nM in a cell-free
ligand-sensing assay;
Potent antagonistic activity against hLXRα
and hLXRβ in cell-based assays with EC50 of 190 nM
and 30 nM, respectively;
In human islets, GW3965 (1 μM) reduces
expression of selected pro-inflammatory cytokines
including IL-8, monocyte chemotactic protein-
1 and tissue factor
In Vivo: At a dose of 10 mg/kg upregulates ABCA1
expression 8-fold and raises circulating levels of
HDL by 30% with Cmax of 12.7 μg/mL and t1/2 of 2
hours.http://www.bocsci.com/gw3965-cas-405911-09-3-
item-84-241846.html
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English
