| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
Liver X receptor α (LXRα) and liver X receptor β (LXRβ). GSK3987 is a pan LXRα/β agonist that recruits steroid receptor coactivator 1 (SRC1) to human LXRα and LXRβ. LXR are nuclear receptors that regulate cholesterol homeostasis, lipid metabolism, and inflammation. Activation of LXR increases the expression of ABCA1, which promotes cholesterol efflux, and SREBP-1c, which induces triglyceride synthesis.
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| ln Vitro |
GSK3987 (compound 4) has EC50 activities of 0.08 μM, 50 nM, and 40 nM against ABCA1, LXRα-SRC1, and LXRβ-SRC1, respectively [1]. GSK3987 (30, 100, 300, and 1000 nM) in primary human macrophages increases ABCA1 expression and dose-dependently induces lysis to apoA1 particles [1]. In human template (HepG2), GSK3987 (6–1500 nM) induces triglyceride expression and dose-dependently increases SREBP-1c expression.
GSK3987 is a potent LXRα/β agonist with EC50 values of 50 nM for LXRα-SRC1 and 40 nM for LXRβ-SRC1. In primary human macrophages, GSK3987 (30-1000 nM) increases ABCA1 expression and dose-dependently induces lysis to apoA1 particles. In HepG2 cells, GSK3987 (6-1500 nM) induces triglyceride expression and dose-dependently increases SREBP-1c expression. The compound also has an EC50 of 0.08 μM against ABCA1. |
| ln Vivo |
Specific in vivo activity data for GSK3987 are not extensively reported in the available literature. As an LXR agonist, it would be expected to have effects on cholesterol metabolism and inflammation in vivo. The compound induces cellular cholesterol efflux and triglyceride accumulation, which are consistent with LXR activation. Specific animal model studies are not described in the available sources.
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| Enzyme Assay |
In vitro LXR activation assays for GSK3987 involve measuring the recruitment of SRC1 to LXRα and LXRβ in the presence of varying concentrations of the compound. These assays typically use fluorescence resonance energy transfer (FRET) or time-resolved fluorescence (TRF) technologies. The EC50 values are determined from dose-response curves.
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| Cell Assay |
RT-PCR[1]
Cell Types: HepG2 cells Tested Concentrations: 6-1500 nM Incubation Duration: Experimental Results: Increases the expression of SREBP-1c in human liver cancer (HepG2) cells and induces triglyceride accumulation [1]. dose-dependent manner. In vitro cell-based assays for GSK3987 assess its effects on LXR target gene expression in cultured cells. Cells such as primary human macrophages or HepG2 cells are treated with GSK3987, and the expression of ABCA1 or SREBP-1c is measured by RT-PCR or Western blotting. Triglyceride accumulation can also be quantified. The compound is soluble in DMSO at 77 mg/mL. |
| Animal Protocol |
Specific in vivo animal model protocols for GSK3987 are not described in the available literature. To evaluate its in vivo efficacy, GSK3987 could be administered to animal models of atherosclerosis or metabolic syndrome. Endpoints would include measurement of lipid profiles, cholesterol efflux, and inflammatory markers.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GSK3987 are not extensively reported in the available literature. As a small molecule with a molecular weight of 384.43 and a LogP of 4.35, it is expected to have reasonable oral bioavailability. The compound is typically stored as a powder at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Specific toxicological data for GSK3987 are not available in the searched literature. As a research compound, its safety profile has not been comprehensively characterized. LXR agonists can cause triglyceride accumulation and hepatic steatosis, which are potential toxicities of this class of compounds. The compound is for research use only.
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| References | |
| Additional Infomation |
GSK3987 is a research tool for studying LXR function and its role in lipid metabolism and inflammation. It is a pan LXRα/β agonist that increases the expression of ABCA1 and SREBP-1c. The compound induces cellular cholesterol efflux and triglyceride accumulation. It is not an approved therapeutic agent.
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| Molecular Formula |
C24H20N2O3
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|---|---|
| Molecular Weight |
384.427206039429
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| Exact Mass |
384.147
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| CAS # |
264206-85-1
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| Related CAS # |
264206-85-1 GSK3987
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| PubChem CID |
5288679
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
572.4±50.0 °C at 760 mmHg
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| Flash Point |
299.9±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.684
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| LogP |
4.35
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
624
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=C(C=C1)NC2=C(C(=O)N(C2=O)CC3=CC=CC=C3)C4=CC=CC=C4
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| InChi Key |
HLZMYWLMBBLASX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H20N2O3/c1-29-20-14-12-19(13-15-20)25-22-21(18-10-6-3-7-11-18)23(27)26(24(22)28)16-17-8-4-2-5-9-17/h2-15,25H,16H2,1H3
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| Chemical Name |
1-benzyl-3-(4-methoxyanilino)-4-phenylpyrrole-2,5-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~260.13 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2601 mL | 1.3006 mL | 2.6013 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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