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GSK5182 is a highly selective inverse estrogen-related receptor γ agonist (IC50 : 79 nM)

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $48 | In Stock | In Stock | |
| 2 mg | $68 | In Stock | In Stock | |
| 5 mg | $97 | In Stock | In Stock | |
| 10 mg | $155 | In Stock | In Stock | |
| 25 mg | $289 | In Stock | In Stock | |
| 50 mg | $438 | In Stock | In Stock | |
| 100 mg | $647 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $116 | In Stock | In Stock |
| Description | GSK5182 is a highly selective inverse estrogen-related receptor γ agonist (IC50 : 79 nM) |
| Targets&IC50 | ERRγ:79 nM (IC50) |
| In vitro | Small interfering RNA (siRNA)-mediated knockdown of ERRγ (siRNA-ERRγ) or an ERRγ inverse agonist, GSK5182, were also used to examine the effects of ERRγ inhibition on the proliferation and growth of a human hepatoma cell line, PLC/PRF/5[1]. |
| In vivo | a hyperinsulinemic-euglycemic clamp study and long-term studies of the antidiabetic effects of GSK5182, the ERRγ-specific inverse agonist, in db/db and DIO mice demonstrated that GSK5182 normalizes hyperglycemia mainly through inhibition of hepatic glucose production[2]. |
| Cell Research | Cell Line:The human hepatoma cell line PLC/PRF/5. Concentration:0 μM, 10 μM, 20 μM. Incubation Time:0 hour, 24 hours, 48 hours, 72 hours |
| Molecular Weight | 417.54 |
| Formula | C27H31NO3 |
| Cas No. | 877387-37-6 |
| Smiles | C(=C(/CCCO)\C1=CC=CC=C1)(\C2=CC=C(OCCN(C)C)C=C2)/C3=CC=C(O)C=C3 |
| Relative Density. | 1.132 g/cm3 (Predicted) |
| Storage | keep away from direct sunlight,store under nitrogen | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (191.6 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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