1. Metabolic Enzyme/Protease
  2. LXR
  3. GW3965 hydrochloride

GW3965 hydrochloride 

Cat. No.: HY-10627A Purity: 99.73%
Handling Instructions

GW3965 hydrochloride est un agoniste des récepteurs hépatiques X (LXR) qui est puissant et sélectif avec des EC50s de 190 nM et 30 nM pour hLXRα et hLXRβ, respectivement.

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.

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

GW3965 hydrochloride Chemical Structure

GW3965 hydrochloride Chemical Structure

CAS No. : 405911-17-3

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Solution
10 mM * 1 mL in DMSO USD 98 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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Solid
5 mg USD 72 In-stock
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10 mg USD 120 In-stock
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50 mg USD 468 In-stock
Estimated Time of Arrival: December 31
100 mg USD 804 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of GW3965 hydrochloride:

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Description

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].

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

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].

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

Molecular Weight

618.51

Formula

C₃₃H₃₂Cl₂F₃NO₃

CAS No.
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.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (161.68 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6168 mL 8.0839 mL 16.1679 mL
5 mM 0.3234 mL 1.6168 mL 3.2336 mL
10 mM 0.1617 mL 0.8084 mL 1.6168 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.04 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.04 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.04 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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 hydrochloride and before death. Two months after STZ injection, diabetic animals are treated once a week with Ro5-4864 (3 mg/kg) or GW3965 hydrochloride (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 hydrochloride 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

Purity: 99.73%

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Keywords:

GW3965GW 3965GW-3965LXRLiver X receptorInhibitorinhibitorinhibit

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GW3965 hydrochloride
Cat. No.:
HY-10627A
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