GW-3965 hydrochloride

Cas No.:	405911-17-3
Chemical Name:	GW3965 HCl
Synonyms:	GW3965 HCl;2-(3-(3-((2-Chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride;2-[3-[3-[[2-Chloro-3-(trifluoromethyl)benzyl](2,2-diphenylethyl)amino]propoxy]phenyl]acetic acid hydrochloride;GW 3965 (hydrochloride);GW 3965 hydrochloride;2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methyl-(2,2-diphenylethyl)amino]propoxy]phenyl]acetic acid,hydrochloride;GW-3965 hydrochloride;3-[3-[N-(2-Chloro-3-trifluoromethylbenzyl)-(2,2-diphenylethyl)amino]propyloxy]phenylacetic acid hydrochloride;GW3965 hydrochloride;GW3965 (hydrochloride);GW3965 HCl;AK101044;2-(3-(3-((2-Chloro-3-(trif
SMILES:	ClC1C(C(F)(F)F)=C([H])C([H])=C([H])C=1C([H])([H])N(C([H])([H])C([H])([H])C([H])([H])OC1=C([H])C([H])=C([H])C(C([H])([H])C(=O)O[H])=C1[H])C([H])([H])C([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C1C([H])=C([H])C([H])=C([H])C=1[H].Cl[H]
Formula:	C33H32Cl2F3NO3
M.Wt:	618.5133
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	GW3965 hydrochloride is a potent and selective LXR agonist with EC50s of 190 and 30 nM for hLXRα and hLXRβ , respectively.
In Vivo:	GW3965 hydrochloride 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 hydrochloride 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 hydrochloride (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 hydrochloride (2 mg/kg, i.v.) increases bleeding time and modulated platelet thrombus formation in vivo[3].
In Vitro:	GW3965 hydrochloride promotes GBM cell death in vitro with enhanced efficacy in EGFRvIII-expressing tumor cells. GW3965 hydrochloride 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 hydrochloride (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 hydrochloride (10 μM) or T0901317 (40 μM), the levels of fibrinogen and P-selectin on the platelet surface are reduced[3].