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GW3965 hydrochloride Data Sheet
| Product Name: | GW3965 hydrochloride |
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|---|---|---|
| CAS No.: | 405911-17-3 | |
| Cat. No.: | HY-10627A | |
| MWt: | 618.51 | |
| Formula: | C33H32Cl2F3NO3 | |
| Purity : | >98% | |
| Solubility: | DMSO : 100 mg/mL (161.68 mM; Need ultrasonic); H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) | |
| Mechanisms: | Target: Cancer Cardiovascular Disease | |
| Biological Activity: | ||
| GW3965 hydrochloride is a potent and selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively[1][2][3]. IC50 & Target: EC50: 190 nM (hLXRα), 30 nM (hLXRβ)[4] 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]. 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]. | ||
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