GW3965

价格询价

品牌MedChemExpress(MCE)
产地美国
货号HY-10627
更新日期2025年07月12日

MedChemExpress LLC

品牌商

13 年钻石会员

GW3965

CAS No. : 405911-09-3

MCE 国际站：GW3965

产品活性：GW3965 是肝 X 受体 (LXR) 激动剂，对 hLXRα 和 hLXRβ 的 EC₅₀ 分别为 190 nM 和 30 nM。

研究领域：Metabolic Enzyme/Protease | Vitamin D Related/Nuclear Receptor

作用靶点：LXR

In Vitro: GW3965 promotes GBM cell death in vitro with enhanced efficacy in EGFRvIII-expressing tumor cells. GW3965 up-regulates expression of the cholesterol transporter gene ABCA1 and the E3 ubiquitin ligase IDOL and reduces LDLR levels. LXR ligands inhibits platelet aggregation and calcium mobilization stimulated by collagen or CRP. GW3965 (1 or 5 μM) displays a minor inhibitory effect on fibrinogen binding and P-selectin exposure, when platelets are stimulated with 1 μg/mL CRP. But using higher concentrations of GW3965 (10 μM) or T0901317 (40 μM), the levels of fibrinogen and P-selectin on the platelet surface are reduced.

In Vivo: GW3965 induces an increase of neuroactive steroids in the spinal cord, the cerebellum and the cerebral cortex of STZ-rats, but not in the CNS of non-pathological animals. GW3965 treatment induces an increase of dihydroprogesterone in the spinal cord of diabetic animals in association with an increase of myelin basic protein expression. GW3965 (40 mg/kg, p.o.) strongly induces ABCA1 expression and reduces LDLR expression, and this is accompanied by 59% inhibition of tumor growth, and a 25-fold increase in GBM cell apoptosis in vivo. GW3965 (2 mg/kg, i.v.) increases bleeding time and modulated platelet thrombus formation in vivo.