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Purity: ≥98%
GSK5182 is an orally bioactive, novel, potent, highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. In hepatocellular carcinoma, GSK5182 also causes the production of reactive oxygen species (ROS).
| Targets |
Reactive Oxygen Species; ERRγ (IC50 = 79 nM)
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| ln Vitro |
GSK5182 (0-20 μM; 0-hours; PLC/PRF/5 cells) treatment reduces the number of proliferating PLC/PRF/5 cells significantly and dose-dependently[1].
GSK5182 (0-20 μM; 24 hours; PLC/PRF/5 cells) treatment also results in a decrease in the amount of phosphorylated retinoblastoma protein (p-pRb) and a dose-dependent increase in the expression of p21 and p27[1]. GSK5182 (10-20 μM; PLC/PRF/5 cells) treatment causes a dose-dependent decrease in the proportion of cells in the S phase by causing cell cycle arrest at the G1 phase[1]. |
| ln Vivo |
GSK5182 (40 mg/kg; intraperitoneal injection; every day; 25 or 30 days; db/db mice, diet-induced obesity mice) specifically inhibits ERRγ's transcriptional activity and reduces the amount of glucose produced in the liver by blocking hepatic gluconeogenesis. GSK5182 inhibits the hepatic gluconeogenesis program in mouse models to produce anti-diabetic effects. GSK5182 primarily normalizes hyperglycemia by preventing the liver from producing glucose[3].
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| Cell Assay |
The experiment involved culturing mouse articular chondrocytes (3×105) for two days, followed by an infection with different Ad-Esrrg adenovirus concentrations [200 800 MOI (multiplicity of infection)] for two hours, and an additional twenty-four hours of culture in the presence or absence of GSK5182 (2.5-10 μM). Several inflammatory cytokines, including TNF-α (10-50 ng/mL), IL-6 (10-50 ng/mL), and IL-1β (0.1-1 ng/mL), were applied to the cells for a full day.
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| Animal Protocol |
db/db mice (male, 7-12-week-old), diet-induced obesity (DIO) mice[3]
40 mg/kg Intraperitoneal injection; every day; 30 days for db/db mice, 25 days for DIO mice |
| References |
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| Molecular Formula |
C27H31NO3
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|---|---|
| Molecular Weight |
417.55
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| Exact Mass |
417.2304
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| Elemental Analysis |
C, 77.67; H, 7.48; N, 3.35; O, 11.49
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| CAS # |
877387-37-6
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| Related CAS # |
(E/Z)-GSK5182;2699724-40-6
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| Appearance |
Solid powder
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| SMILES |
CN(C)CCOC1=CC=C(C=C1)/C(=C(/CCCO)\C2=CC=CC=C2)/C3=CC=C(C=C3)O
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| InChi Key |
ZVSFNBNLNLXEFQ-RQZHXJHFSA-N
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| InChi Code |
InChI=1S/C27H31NO3/c1-28(2)18-20-31-25-16-12-23(13-17-25)27(22-10-14-24(30)15-11-22)26(9-6-19-29)21-7-4-3-5-8-21/h3-5,7-8,10-17,29-30H,6,9,18-20H2,1-2H3/b27-26-
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| Chemical Name |
4-[(Z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol
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| Synonyms |
GSK5182; GSK-5182; GSK 5182
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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: 25~84 mg/mL (59.9~201.2 mM)
Ethanol: ~84 mg/mL (~201.2 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 | 2.3949 mL | 11.9746 mL | 23.9492 mL | |
| 5 mM | 0.4790 mL | 2.3949 mL | 4.7898 mL | |
| 10 mM | 0.2395 mL | 1.1975 mL | 2.3949 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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