Name | ST 2825 |
Synonyms | ST2825 ST 2825 (2R,4'R,8'aR)-1-[2-[4-[[2-(2,4-Dichlorophenoxy)acetyl]amino]phenyl]acetyl]tetrahydro-6'-oxospiro[pyrrolidine-2,7'(6'H)-[2H]pyrrolo[2,1-b][1,3]thiazine]-4'-carboxamide Spiro[pyrrolidine-2,7'(6'H)-[2H]pyrrolo[2,1-b][1,3]thiazine]-4'-carboxamide, 1-[2-[4-[[2-(2,4-dichlorophenoxy)acetyl]amino]phenyl]acetyl]tetrahydro-6'-oxo-, (2R,4'R,8'aR)- |
CAS | 894787-30-5 |
Molecular Formula | C27H28Cl2N4O5S |
Molar Mass | 591.51 |
Density | 1.51±0.1 g/cm3(Predicted) |
Boling Point | 939.0±65.0 °C(Predicted) |
Solubility | 10 mM in DMSO |
pKa | 12.86±0.70(Predicted) |
Storage Condition | -20℃ |
In vitro study | ST2825 blocks IL-1R/TLR signaling by interfering with MyD88 homodimerization. ST2825 inhibits this interaction in a concentration-dependent manner with ~40% inhibition of dimerization at 5 μM ST2825 and 80% inhibition at 10 μM ST2825. |
In vivo study | ST2825 dose-dependently inhibits IL-1β-induced production of IL-6 in treated mice after oral administration. The animals are administered orally with the appropriate vehicles or ST2825 at doses ranging from 50 to 200 mg/kg, 5 min prior to i.p. injection with 20 μg/kg IL-1β. ST2825 exertes a significant inhibition of IL-1β-stimulated production of IL-6 at 100 and 200 mg/kg. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.691 ml | 8.453 ml | 16.906 ml |
5 mM | 0.338 ml | 1.691 ml | 3.381 ml |
10 mM | 0.169 ml | 0.845 ml | 1.691 ml |
5 mM | 0.034 ml | 0.169 ml | 0.338 ml |
biological activity | ST 2825 is a specific MyD88 dimerization inhibitor. ST 2825 interferes with the recruitment of IRAK1 and IRAK4 by MyD88 and inhibits IL-1β-mediated NF-κB transcriptional activity. |
Target | MyD88 |
in vitro study | ST2825 blocks IL-1R/TLR signaling by interposing with MyD88 homodiderivation. ST2825 indications this interaction in a concentration-dependent manner with ~ 40% inhibition of differentiation at 5 μm ST2825 and 80% inhibition at 10 μm ST2825. |
in vivo study | ST2825 dose-dependently inhibits IL-1β-induced production of IL-6 in treated mice after oral administration. The animals are administered orally with the appropriate vehicles or ST2825 at orders ranging from 50 to 200 mg/kg, 5 min prior to I .p. injection with 20 μg/kg IL-1β. ST2825 exertes a significant inhibition of IL-1β-stimulated production of IL-6 at 100 and 200 mg/kg. |