GW3965

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服活性的 LXR 激动剂，可在无细胞配体感应测定中将类固醇受体辅激活剂 1 招募到 LXRα 上，EC50 为 125 nM。

A potent, selective, orally active LXR agonist that recruits the steroid receptor coactivator 1 to human LXRα in a cell-free ligand-sensing assay with an EC50 of 125 nM; acts as a full agonist on hLXRα and hLXRβ in cell-based reporter gene assays with EC50 of 190 and 30 nM, respectively; increases expression of ABCA1 in the small intestine and peripheral macrophages in C57BL/6 mice at 10 mg/kg.Asthma Discontinued.

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.

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.

GW 3965 | GW-3965

Nuclear Receptor/Transcription Factor

LXR

LXR

Inflammation/Immunology

Asthma

405911-09-3

582.0524

C33H31ClF3NO3

>98% (HPLC)

10 mM in DMSO

C1=CC=C(C=C1)C(CN(CCCOC2=CC=CC(=C2)CC(=O)O)CC3=C(C(=CC=C3)C(F)(F)F)Cl)C4=CC=CC=C4

Benzeneacetic acid, 3-[3-[[[2-chloro-3-(trifluoromethyl)phenyl]methyl](2,2-diphenylethyl)amino]propoxy]-

(-20℃)

With Ice Pack

≥ 2 years