GW3965 hydrochloride

SKU: orb1225101

Description

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.

Images & Validation

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Key Properties

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CAS Number	405911-17-3
MW	618.5133
Purity	>98% (HPLC)
Formula	C₃₃H₃₂Cl₂F₃NO₃
SMILES	Cl.OC(=O)CC1=CC=CC(OCCCN(CC(C2=CC=CC=C2)C2=CC=CC=C2)CC2=CC=CC(=C2Cl)C(F)(F)F)=C1 \|c:6,18,20,25,27,33,35,42,t:4,16,23,31\|
Target	LXR
Solubility	10 mM in DMSO

Bioactivity

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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. 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. GW3965 hydrochloride (2 mg/kg, i. v.) increases bleeding time and modulated platelet thrombus formation In vivo.

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. 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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GW 3965 hydrochloride | GW-3965 hydrochloride

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Gene Symbol

LXR

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