2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. LXR
  4. GSK3987

GSK3987 is a pan LXRα/β agonist with EC50s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellular cholesterol efflux and triglyceride accumulation.

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GSK3987 Chemical Structure

GSK3987 Chemical Structure

CAS No. : 264206-85-1

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Based on 1 publication(s) in Google Scholar

GSK3987 Related Antibodies

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Description

GSK3987 is a pan LXRα/β agonist with EC50s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellular cholesterol efflux and triglyceride accumulation[1].

IC50 & Target

EC50: 50 nM (LXRα); 40 nM (LXRβ)[1]
In Vitro

GSK3987 (compound 4) shows activity with EC50s of 0.08 µM, 50 nM, 40 nM for ABCA1, LXRα-SRC1, LXRβ-SRC1, respectively[1].
GSK3987 (30, 100, 300, 1000 nM) increases the expression of ABCA1 and induces cellular cholesterol efflux to apoA1 particles in a dose-dependent manner in primary human macrophages[1].
GSK3987 (6-1500 nM) increases the expression of SREBP-1c and induces triglyceride accumulation in human hepatoma (HepG2) cells in a dose-dependent manner[1].

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

GSK3987 Related Antibodies

RT-PCR[1]

Cell Line: HepG2 cells
Concentration: 6-1500 nM
Incubation Time:
Result: Increased the expression of SREBP-1c and induced triglyceride accumulation in human hepatoma (HepG2) cells in a dose-dependent manner.
Molecular Weight

384.43

Formula

C24H20N2O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N(C1=O)CC2=CC=CC=C2)C(NC3=CC=C(C=C3)OC)=C1C4=CC=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (260.13 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 2.6013 mL 13.0063 mL 26.0125 mL
5 mM 0.5203 mL 2.6013 mL 5.2025 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6013 mL 13.0063 mL 26.0125 mL 65.0313 mL
5 mM 0.5203 mL 2.6013 mL 5.2025 mL 13.0063 mL
10 mM 0.2601 mL 1.3006 mL 2.6013 mL 6.5031 mL
15 mM 0.1734 mL 0.8671 mL 1.7342 mL 4.3354 mL
20 mM 0.1301 mL 0.6503 mL 1.3006 mL 3.2516 mL
25 mM 0.1041 mL 0.5203 mL 1.0405 mL 2.6013 mL
30 mM 0.0867 mL 0.4335 mL 0.8671 mL 2.1677 mL
40 mM 0.0650 mL 0.3252 mL 0.6503 mL 1.6258 mL
50 mM 0.0520 mL 0.2601 mL 0.5203 mL 1.3006 mL
60 mM 0.0434 mL 0.2168 mL 0.4335 mL 1.0839 mL
80 mM 0.0325 mL 0.1626 mL 0.3252 mL 0.8129 mL
100 mM 0.0260 mL 0.1301 mL 0.2601 mL 0.6503 mL
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GSK3987 Related Classifications

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:

GSK3987264206-85-1GSK 3987GSK-3987LXRLiver X receptorHepG2 cellsABCA1SREBP-1ccellular cholesterolmacrophagestriglyceride accumulationInhibitorinhibitorinhibit

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