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GW3965
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GW3965图片
CAS NO:405911-09-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

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

GW3965 is a potent, selectiveliver X receptor (LXR)agonist withEC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively[1][2][3].

IC50& Target

EC50: 190 nM (hLXRα), 30 nM (hLXRβ)

体外研究
(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[2]. 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[3].

体内研究
(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[1]. 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[2]. GW3965 (2 mg/kg, i.v.) increases bleeding time and modulated platelet thrombus formation in vivo[3].

分子量

582.05

Formula

C33H31ClF3NO3

CAS 号

405911-09-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.