Name | Tetraethyl 2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethenyl-1,1-bisphosphonate SRL HTMT dimaleate 1ilh 4-[2,2-bis(diethoxyphosphoryl)ethenyl]-2,6-ditert-butylphenol |
Synonyms | SRL 1ilh SR12813 SR 12813 SR-12813 GW485801 GW 485801 GW-485801 HTMT dimaleate SR-12813(GW 485801) 4-[2,2-bis(diethoxyphosphoryl)ethenyl]-2,6-ditert-butylphenol Tetraethyl 2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethenyl-1,1-bisphosphonate [[3,5-Bis(1,1-dimethylethyl)-4-hydroxyphenyl]ethenylidene]bis-phosphonicacidtetraethylester Phosphonic acid, P,P'-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]ethenylidene]bis-, P,P,P',P'-tetraethyl ester |
CAS | 126411-39-0 |
Molecular Formula | C24H42O7P2 |
Molar Mass | 504.53 |
Melting Point | 119-121℃ |
Solubility | 10 mM in DMSO |
Appearance | solid |
Storage Condition | Sealed in dry,Room Temperature |
Target | IC50: 0.85 μM (HMG-CoA Reductase) |
In vitro study | SR12813 is a very potent activator of human and rabbit-derived PXR with EC50 of 200 nM and 700 nM, respectively. The activation of PXR in rats and mice is very weak. SR-12813 inhibited the integration of tritiated water into cholesterol with an IC50 of 1.2 μm, but had no effect on fatty acid synthesis. SR-12813 reduced intracellular HMG-CoA reductase activity, with an IC50 of 0.85 μm, it inhibited HMG-CoA reductase activity very rapidly, T1/2=10 min. |
In vivo study | SR12813 is able to lower cholesterol levels in many animals such as rats, dogs and primates. |
WGK Germany | 3 |
HS Code | 29319090 |
Reference Show more | 1. Berkhout T, et al. The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. J Biol Chem. 1996 Jun 14;271(24):14376-82.2. Jiang W, et al. Forward genetic screening for regulators involved in cholesterol synthesis using validation-based insertional mutagenesis. PLoS One. 2014 Nov 26;9(11):e112632.3. Sergio C Chai, et al. Small-molecule modulators of PXR and CAR. Biochim Biophys Acta.2016 Sep;1859(9):1141-1154. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.982 ml | 9.91 ml | 19.82 ml |
5 mM | 0.396 ml | 1.982 ml | 3.964 ml |
10 mM | 0.198 ml | 0.991 ml | 1.982 ml |
5 mM | 0.04 ml | 0.198 ml | 0.396 ml |
biological activity | SR-12813 is an agonist of pregnane X receptor (PXR). |
Target | Value |
pregnane X receptor | |
HMG-CoA reductase | 850 nM |