[CAS NO. 2699724-40-6] (E/Z)-GSK5182
PRODUCTS SPECIFICATIONS [2699724-40-6]
DESCRIPTION [2699724-40-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 417.54 |
| Molecular Formula | C27H31NO3 |
| SMILES | OCCC/C(C1=CC=CC=C1)=C(C2=CC=C(C=C2)OCCN(C)C)\C3=CC=C(C=C3)O |
Summary
(E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC 50 of 79 nM [1] . GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma [1] [2] [3] .
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 75 mg/mL ( 179.62 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3950 mL | 11.9749 mL | 23.9498 mL |
| 5 mM | 0.4790 mL | 2.3950 mL | 4.7900 mL |
| 10 mM | 0.2395 mL | 1.1975 mL | 2.3950 mL |
References
- [1] Kim JH, et al. Estrogen-related receptor γ is upregulated in liver cancer and its inhibition suppresses livercancer cell proliferation via induction of p21 and p27. Exp Mol Med. 2016 Mar 4;48:e213.
- [2] Misra J, et al. ERRγ: a Junior Orphan with a Senior Role in Metabolism. Trends Endocrinol Metab. 2017 Apr;28(4):261-272.
- [3] Kim DK, et al. Inverse agonist of nuclear receptor ERRγ mediates antidiabetic effect through inhibition of hepatic gluconeogenesis. Diabetes. 2013 Sep;62(9):3093-102.
