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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.
相关产品：T0901317 | GW3965 hydrochloride | GSK2033 | 27-Hydroxycholesterol | LXR-623 | SR9243 | (20S)-Protopanaxatriol | SR9238 | Saikosaponin A | DMHCA | 24-Hydroxycholesterol | AZ876 | RGX-104 | XL041 | GSK3987 | Larsucosterol (trimethylamine) | BMS-779788 | Rovazolac | IMB-808 | Acetyl podocarpic acid anhydride | FITC-GW3965 | GW6340 | Nagilactone B | Yamogenin | 22(R)-Hydroxycholesterol | BE1218 | GAC0001E5 | GAC0003A4
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文献和实验magichunter 我在文献中查到，PPARr拮抗剂GW9662可以抑制药物的抗炎作用，前提是药物是通过激活PPARr来实现其抗炎作用的。即炎症细胞中的炎症因子（如：NO）升高，加入抗炎药物后，NO水平降低，当同时给予GW9662和该抗炎药物时，该药物的抗炎作用被抑制，NO水平再次升高。以上是文献的报道，但是我在实验时发现，加入了抗炎药物+GW9662后，NO的水平不但没有升高，反而降低了（与单独抗炎药物组相比），不知这是怎么回事？ chp
. A new drug candidate belonging to the family of the peroxisome proliferator-activated receptor-delta agonists termed GW1516 (also referred to as GW501516) has been prohibited by the World Anti-Doping Agency in 2009
有一种胖，反而有利于心血管健康！「肥胖悖论」新证据，源于脂肪
-HFD 喂养的 adipo-FtMT 小鼠心脏组织的蛋白质羰基化水平显著升高，且线粒体 H2O2 产生水平较对照小鼠显著增加。研究者根据这些数据提出大胆假设，即体内存在一种内分泌机制将促氧化信号从脂肪细胞传递到心肌。接下来，研究者通过纳米粒子追踪分析测量，发现食用 dox-HFD 3 周的 Adipo-FtMT 小鼠的循环 sEV 水平显著升高。进一步，利用中性鞘磷脂酶抑制剂 GW4869 阻断外泌体的产生，实验结果表明 dox-HFD 喂食 4 小时后，GW4869 完全阻止了 adipo
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