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GSK3987

Catalog No. T27478   CAS 264206-85-1

GSK3987 is an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC50s of 40 nM.

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GSK3987 Chemical Structure
GSK3987, CAS 264206-85-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 97.00
5 mg In stock $ 255.00
10 mg In stock $ 413.00
25 mg In stock $ 692.00
50 mg In stock $ 985.00
100 mg In stock $ 1,330.00
500 mg In stock $ 2,660.00
1 mL * 10 mM (in DMSO) In stock $ 277.00
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Purity: 99.48%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK3987 is an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC50s of 40 nM.
Targets&IC50 LXRβ:40 nM(EC50), LXRα:40 nM(EC50)
In vitro In primary human macrophages, GSK3987 (30, 100, 300, 1000 nM) increased the expression of ABCA1 and induces cellular cholesterol efflux to apoA1 particles in a dose-dependent manner. In human hepatoma (HepG2) cells, GSK3987 (6-1500 nM) increases the expression of SREBP-1c and induces triglyceride accumulation in a dose-dependent manner[1]. GSK3987 showed activity with EC50s of 0.08 μM, 50 nM, 40 nM for ABCA1, LXRα-SRC1, LXRβ-SRC1, respectively[1].
Molecular Weight 384.43
Formula C24H20N2O3
CAS No. 264206-85-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/ml (130.06 mM)

TargetMolReferences and Literature

1. Ranganathan PV, et al. Netrin-1-treated macrophages protect the kidney against ischemia-reperfusion injury and suppress inflammation by inducing M2 polarization. Am J Physiol Renal Physiol. 2013 Apr 1;304(7):F948-57. 2. Lin HR. Paeoniflorin acts as a liver X receptor agonist. J Asian Nat Prod Res. 2013;15(1):35-45. 3. Jaye MC, et al. Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. J Med Chem. 2005 Aug 25;48(17):5419-22.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Metabolism Compound Library Nuclear Receptor Compound Library Bioactive Compounds Library Max

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Keywords

GSK3987 264206-85-1 Metabolism Liver X Receptor macrophages cellular cholesterol inhibit ABCA1 HepG2 cells Inhibitor SREBP-1c GSK-3987 LXR Liver X receptor triglyceride accumulation GSK 3987 inhibitor

 

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