货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
Y36331-10mg促销	98%	￥1300.00 ￥1000.00 Y36331-10mg ￥1000.00 3-5天	0 货期：3-5天	-	-	-	-
Y36331-25mg促销	98%	￥3000.00 ￥2295.00 Y36331-25mg ￥2295.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

Y36331-10mg促销

98%

￥1300.00 ￥1000.00

货期：3-5天

Y36331-25mg促销

98%

￥3000.00 ￥2295.00

货期：3-5天

产品描述：

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

体外研究：

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.

体内研究：

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.

参考文献：

1. Mitro, Nico., et al. LXR and TSPO as new therapeutic targets to increase the levels of neuroactive steroids in the central nervous system of diabetic animals. Neurochemistry International (2012), 60(6), 616-621.
2. Guo, Deliang., et al. An LXR Agonist Promotes Glioblastoma Cell Death through Inhibition of an EGFR/AKT/SREBP-1/LDLR-Dependent Pathway. Cancer Discovery (2011), 1(5), 442-456.
3. Spyridon, Michael., et al. LXR as a novel antithrombotic target. Blood (2011), 117(21), 5751-5761.

溶解性：

可溶于DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.718 ml	8.59 ml	17.181 ml
5 mM	0.344 ml	1.718 ml	3.436 ml
10 mM	0.172 ml	0.859 ml	1.718 ml
50 mM	0.034 ml	0.172 ml	0.344 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献(1篇)

1. [IF=5.6] Liu Sainan et al."Therapeutic Biomaterials with Liver X Receptor Agonists Based on the Horizon of Material Biology to Regulate Atherosclerotic Plaque Regression in Situ for Devices Surface Engineering."Regenerative Biomaterials.2024 Aug;:

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