GW3965

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GW3965 is a potent, selective liver X receptor (LXR) agonist with EC₅₀s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (GW3965 hydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

GW3965 Chemical Structure

CAS No. : 405911-09-3

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Other In-stock Forms of GW3965:

GW3965 hydrochloride

Other Forms of GW3965:

GW3965 hydrochloride In-stock

12 Publications Citing Use of MCE GW3965

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Description

GW3965 is a potent, 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)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	410 nM Compound: 2, GW-3965	Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay	[PMID: 17034119]
CHO-K1	EC₅₀	0.42 μM Compound: 2, GW3965	Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 25677664]
CHO-K1	EC₅₀	1.3 μM Compound: 2, GW3965	Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 25677664]
COS-7	EC₅₀	0.015 μM Compound: GW-3965	Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay	[PMID: 17587573]
COS-7	EC₅₀	0.015 μM Compound: GW-3965	Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay	[PMID: 17416521]
Huh-7	EC₅₀	0.31 μM Compound: 2, GW-3965	Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 18973288]
Huh-7	EC₅₀	0.66 μM Compound: 2, GW-3965	Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 18973288]
Platelet	IC₅₀	30 nM Compound: GW3965	Inhibition of collagen-induced platelet aggregation in human platelet suspension preincubated for 10 mins followed by collagen stimulation by light transmission-based assay Inhibition of collagen-induced platelet aggregation in human platelet suspension preincubated for 10 mins followed by collagen stimulation by light transmission-based assay	[PMID: 32463237]
RAW264.7	EC₅₀	29 nM Compound: 2	Induction of [3H]cholesterol efflux in mouse RAW264.7 cells loaded with acetylated-LDL after 24 hrs Induction of [3H]cholesterol efflux in mouse RAW264.7 cells loaded with acetylated-LDL after 24 hrs	[PMID: 19717304]
SH-SY5Y	EC₅₀	0.13 μM Compound: 3, GW-3965	Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay	[PMID: 19264481]
SH-SY5Y	EC₅₀	0.31 μM Compound: 3, GW-3965	Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay	[PMID: 19264481]
THP-1	EC₅₀	0.01 μM Compound: GW-3965	Induction of cholesterol efflux in THP1 cells after 18 hrs Induction of cholesterol efflux in THP1 cells after 18 hrs	[PMID: 17416521]
THP-1	EC₅₀	0.027 μM Compound: 1, GW-3965	Agonist activity at GAL-linked human LXRbeta expressed in THP1 cells assessed as stimulation of co-activator recruitment by FRET assay Agonist activity at GAL-linked human LXRbeta expressed in THP1 cells assessed as stimulation of co-activator recruitment by FRET assay	[PMID: 17665897]
THP-1	EC₅₀	0.097 μM Compound: 1, GW-3965	Agonist activity at GAL-linked human LXRalpha expressed in THP1 cells assessed as stimulation of coactivator recruitment by FRET assay Agonist activity at GAL-linked human LXRalpha expressed in THP1 cells assessed as stimulation of coactivator recruitment by FRET assay	[PMID: 17665897]
THP-1	IC₅₀	20 nM Compound: 2, GW-3965	Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA	[PMID: 18800767]
U-87MG ATCC	IC₅₀	3.65 μM Compound: GW3965	Antiproliferative activity against human U87 cells overexpressing EGFR variant III measured after 7 days by CCK8 assay Antiproliferative activity against human U87 cells overexpressing EGFR variant III measured after 7 days by CCK8 assay	[PMID: 32248003]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

582.05

Formula

C₃₃H₃₁ClF₃NO₃

CAS No.

405911-09-3

SMILES

ClC1=C(C(F)(F)F)C=CC=C1CN(CC(C2=CC=CC=C2)C3=CC=CC=C3)CCCOC4=CC(CC(O)=O)=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Mitro, Nico., et al. LXR and TSPO as new therapeutic targets to increase the levels of neuroactive steroids in the central nervous system of diabetic animals. Neurochemistry International (2012), 60(6), 616-621. [Content Brief]

[2]. Guo, Deliang., et al. An LXR Agonist Promotes Glioblastoma Cell Death through Inhibition of an EGFR/AKT/SREBP-1/LDLR-Dependent Pathway. Cancer Discovery (2011), 1(5), 442-456.

[3]. Spyridon, Michael., et al. LXR as a novel antithrombotic target. Blood (2011), 117(21), 5751-5761. [Content Brief]

Cell Assay ^[2]	Cells are seeded in 96 wells and are treated after 24 hours with different drugs indicated in each experiment in medium containing 1% FBS or lipoprotein deficient serum. Relative proliferation is determined using Cell Proliferation Assay Kit. Cells are incubated 1.5 hrs after adding tetrazolium salt WST-1 [2-(4-iodophenyl)-3- (4-nitrophenyl)-5-(2, 4-disulfo-phenyl)-2H-tetrazolium, monosodium salt] at 5% CO₂, 37ºC and the absorbance of the treated and untreated cells are measured using a microplate reader at 420 to 480 nm. Cells seeded in 12 well plates are counted using a hemocytometer, and dead cells are assessed using trypan blue exclusion assays. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Diabetes is induced in two-month-old male rats by a single i.p. injection of freshly prepared STZ (65 mg/kg) in 0.09 M citrate buffer, pH 4.8. Control animals are injected with 0.09 mol/L citrate buffer at pH 4.8. Hyperglycemia is confirmed 48 h after streptozotocin injection by measuring tail vein blood glucose levels using a glucometer OneTouch Ultra2. Only animals with mean plasma glucose levels over 300 mg/mL are classified as diabetic. Glycemia is also assessed before treatment with Ro5-4864 or GW3965 and before death. Two months after STZ injection, diabetic animals are treated once a week with Ro5-4864 (3 mg/kg) or GW3965 (50 mg/kg). Thus, they receive four subcutaneous injections in a month. Control diabetic rats receive 200 μL of vehicle (sesame oil). Four-month-old non-diabetic male rats are injected, following the same experimental schedule, with Ro5-4864, GW3965 or vehicle. Rats are killed 24 h after the last treatment. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Mitro, Nico., et al. LXR and TSPO as new therapeutic targets to increase the levels of neuroactive steroids in the central nervous system of diabetic animals. Neurochemistry International (2012), 60(6), 616-621. [Content Brief] [2]. Guo, Deliang., et al. An LXR Agonist Promotes Glioblastoma Cell Death through Inhibition of an EGFR/AKT/SREBP-1/LDLR-Dependent Pathway. Cancer Discovery (2011), 1(5), 442-456. [3]. Spyridon, Michael., et al. LXR as a novel antithrombotic target. Blood (2011), 117(21), 5751-5761. [Content Brief]

GW3965 Related Classifications

Cardiovascular Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GW3965405911-09-3GW 3965GW-3965LXRLiver X receptorInhibitorinhibitorinhibit

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