894787-30-5
894787-30-5 structure
- Name: ST 2825
- Chemical Name: (4R,7R,8aR)-1'-[2-[4-[[2-(2,4-dichlorophenoxy)acetyl]amino]phenyl]acetyl]-6-oxospiro[3,4,8,8a-tetrahydro-2H-pyrrolo[2,1-b][1,3]thiazine-7,2'-pyrrolidine]-4-carboxamide
- CAS Number: 894787-30-5
- Molecular Formula: C27H28Cl2N4O5S
- Molecular Weight: 591.50600
- Catalog: Signaling Pathways Immunology/Inflammation MyD88
- Create Date: 2016-06-27 01:54:40
- Modify Date: 2024-01-09 22:31:58
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ST 2825 is a MyD88 dimerization inhibitor.
| Name | (4R,7R,8aR)-1'-[2-[4-[[2-(2,4-dichlorophenoxy)acetyl]amino]phenyl]acetyl]-6-oxospiro[3,4,8,8a-tetrahydro-2H-pyrrolo[2,1-b][1,3]thiazine-7,2'-pyrrolidine]-4-carboxamide |
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| Synonyms |
cs-0797
st 2825 st 2825||st-2825 |
| Description | ST 2825 is a MyD88 dimerization inhibitor. |
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| Related Catalog | |
| Target |
MyD88[1] |
| In Vitro | 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[1]. |
| In Vivo | 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[1]. |
| Cell Assay | HeLa cells are seeded at 105 cells/mL in a 96-well tissue-culture plate. After incubating overnight, the medium is discarded, and the cells are added with tissue culture medium, 10% FBS, containing ST2825 at concentrations ranging from 0.1 to 10 μM and DMSO at 0.1% final concentration. The cells are incubated for 6 and 18 h and then added with the yellow XTT (0.3 mg/mL) for further 2 h of incubation. At the end of the incubation periods, reactions are quantified by using a Sirio S Seac microplate reader[1]. |
| Animal Admin | Mice[1] Mice (female C57Bl/6) are divided into experimental groups of 15 mice. They are injected i.p. with saline (control animals) or recombinant murine IL-1β (20 μg/kg). A time-course analysis of IL-6 production established that the peak of cytokine is reached 2 h after IL-1β injection. ST2825, administered orally as 0.5% suspension in carboxymethylcellulose (CMC) or CMC alone, is supplied to the experimental mice groups. Two hours after IL-1β injection, the animals are killed, and sera are collected to assay IL-6 levels. Mice, which are treated orally with 100 and 200 mg/kg ST2825, shows lower levels of IL-6 versus CMC-treated mice. |
| References |
| Molecular Formula | C27H28Cl2N4O5S |
|---|---|
| Molecular Weight | 591.50600 |
| Exact Mass | 590.11600 |
| PSA | 148.33000 |
| LogP | 4.56230 |
| Storage condition | 2-8℃ |