GW3965

Name: GW3965
Brand: MedChemExpress
SKU: HY-10627
Rating: 5.0 (26 reviews)

Cat. No.: HY-10627 Purity: 99.80%: Data Sheet
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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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 405911-09-3

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무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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고객리뷰

Based on 26 publication(s) in Google Scholar

Other Forms of GW3965:

GW3965 hydrochloride In-stock
GW3965 (Standard) 견적 받기

26 Publications Citing Use of MCE GW3965

Cell Imaging/Staining

Cell Proliferation/Viability Assay

Apoptosis Analysis

Others

RT-PCR

IHC

: GW3965 purchased from MedChemExpress. Usage Cited in: Environ Int. 2024 Nov 26:194:109168. [Abstract]; Representative images of Oil red O straining of HepG2 cells after treated with different concentrations of GW3965 (0, 1, and 10 μM; 72 h).

: GW3965 purchased from MedChemExpress. Usage Cited in: Environ Int. 2024 Nov 26:194:109168. [Abstract]; Total triglycerides (TG) and total cholesterol (T-CHO) contents of HepG2 cells after treated with GW3965 (1-10 μM; 72 h).

: GW3965 purchased from MedChemExpress. Usage Cited in: Environ Int. 2024 Nov 26:194:109168. [Abstract]; Expression of the genes in HepG2 cells measured by qRT-PCR after treated with GW3965 (1-10 μM).

: GW3965 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 May 14;23(1):542. [Abstract]; Control or Ethidium Bromide treated (100-200 ng/mL; 7 d) CCRF-CEM and MOLT-4 cells, were treated with the indicated concentrations of GW3965 (0.5-10 μM; 24 h) and the accumulation of P-gp and β-actin was visualized as above.

: GW3965 purchased from MedChemExpress. Usage Cited in: Respir Res. 2024 Nov 7;25(1):399. [Abstract]; MLE12 cells were cultured under normoxia (NOX) or hyperoxia (HYX) conditions with different doses of GW3965 (1-10 μM) for 24 h, and cell viability was determined by CCK-8 assays.

: GW3965 purchased from MedChemExpress. Usage Cited in: Respir Res. 2024 Nov 7;25(1):399. [Abstract]; MLE12 cells were cultured under normoxia (NOX) or hyperoxia (HYX) conditions with different doses of GW3965 (1-15 μM) for 24 h, and detected relative mRNA expression of Abca1 normalized to Gapdh.

: GW3965 purchased from MedChemExpress. Usage Cited in: Respir Res. 2024 Nov 7;25(1):399. [Abstract]; Representative pictures of MLE12 cells exposed to NOX or HYX for 24 h treated with or without 5 µM GW3965 stained by Filipin III and the quantification of the mean fluorescence intensity of Filipin III staining.

: GW3965 purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jul 11;10(19):8834-8850. [Abstract]; Flow cytometry showed the combination of sorafenib and GW3965 (1, 2 μM) could induce apoptosis in Huh7-SR and HCCLM3-SR.

: GW3965 purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jul 11;10(19):8834-8850. [Abstract]; Colony-formation efficiency showed the emergency of Huh7-SR coloines which treated with Sorafenib and GW3965 (1, 2 μM) was less than that treated with Sorafenib alone.

: GW3965 purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jul 11;10(19):8834-8850. [Abstract]; WB showed IGF1R were upregulated in combination along with their common downstream target pERK/p-AKT and combination treatment also could induce apoptosis treated with GW3965 (1, 2 μM).

: GW3965 purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jul 11;10(19):8834-8850. [Abstract]; The impact of Sorafenib, GW3965 and the combination therapy on cell viability in Huh7-SR and HCCLM3-SR cells were determined by CCK8 assay.

: GW3965 purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jul 11;10(19):8834-8850. [Abstract]; Immunohistochemistry showed Sorafenib and GW3965 (30 mg/kg) combination therapy could suppress HCC proliferation and IGF1R level in vivo.

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Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

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	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]
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	100 % Compound: GW-3965	Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay relative to GW-3965 Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay relative to GW-3965	[PMID: 17587573]
HepG2	EC₅₀	2002 nM Compound: 2, GW-3965	Effect on triglyceride accumulation in human HepG2 cells Effect on triglyceride accumulation in human HepG2 cells	[PMID: 18973288]
HepG2	EC₅₀	210 nM Compound: 2, GW-3965	Effect on SREBP1c gene expression in human HepG2 cells Effect on SREBP1c gene expression in human HepG2 cells	[PMID: 18973288]
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	0.01 μM Compound: GW-3965	Induction of cholesterol efflux in THP1 cells Induction of cholesterol efflux in THP1 cells	[PMID: 17587573]
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	EC₅₀	31 nM Compound: 2, GW-3965	Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL	[PMID: 18973288]
THP-1	EC₅₀	434 nM Compound: 2, GW-3965	Effect on ABCA1 gene expression in human differentiated THP1 cells Effect on ABCA1 gene expression in human differentiated THP1 cells	[PMID: 18973288]
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.

분자량

582.05

화학식

C₃₃H₃₁ClF₃NO₃

CAS No.

405911-09-3

Appearance

Solid

Color

White to off-white

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

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

DMSO : 100 mg/mL (171.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7181 mL	8.5903 mL	17.1807 mL
5 mM	0.3436 mL	1.7181 mL	3.4361 mL
10 mM	0.1718 mL	0.8590 mL	1.7181 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기
농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (8.59 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.80%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (257 KB) HNMR (138 KB) RP-HPLC (214 KB) LCMS (233 KB)

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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7181 mL	8.5903 mL	17.1807 mL	42.9516 mL
	5 mM	0.3436 mL	1.7181 mL	3.4361 mL	8.5903 mL
	10 mM	0.1718 mL	0.8590 mL	1.7181 mL	4.2952 mL
	15 mM	0.1145 mL	0.5727 mL	1.1454 mL	2.8634 mL
	20 mM	0.0859 mL	0.4295 mL	0.8590 mL	2.1476 mL
	25 mM	0.0687 mL	0.3436 mL	0.6872 mL	1.7181 mL
	30 mM	0.0573 mL	0.2863 mL	0.5727 mL	1.4317 mL
	40 mM	0.0430 mL	0.2148 mL	0.4295 mL	1.0738 mL
	50 mM	0.0344 mL	0.1718 mL	0.3436 mL	0.8590 mL
	60 mM	0.0286 mL	0.1432 mL	0.2863 mL	0.7159 mL
	80 mM	0.0215 mL	0.1074 mL	0.2148 mL	0.5369 mL
	100 mM	0.0172 mL	0.0859 mL	0.1718 mL	0.4295 mL

GW3965 Related Classifications

Cardiovascular Disease

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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GW3965

고객리뷰

Other Forms of GW3965:

GW3965 Related Antibodies

26 Publications Citing Use of MCE GW3965

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

순도&문서

References

고객리뷰

GW3965 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

GW3965 Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

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