Identification | Back Directory | [Name]
1-Piperazinecarboxamide, 4-[(3-bromophenyl)sulfonyl]-N-[(1S)-1-(2-thienyl)ethyl]- | [CAS]
2437475-16-4 | [Synonyms]
1-Piperazinecarboxamide, 4-[(3-bromophenyl)sulfonyl]-N-[(1S)-1-(2-thienyl)ethyl]- | [Molecular Formula]
C17H20BrN3O3S2 | [MDL Number]
MFCD30532664 | [MOL File]
2437475-16-4.mol | [Molecular Weight]
458.39 |
Hazard Information | Back Directory | [Uses]
T6167923 is a selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with IC50s of 2.7 μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively[1][2]. | [in vivo]
T6167923 (0.17 and 1 mg; i.p. once) survives the mice from intoxication with SEB and LPS injection[2]. Animal Model: | 16-20 week-old BALB/c mice with LPS potentiation model[2] | Dosage: | 0.17 and 1 mg | Administration: | Intraperitoneal injection; 0.17 and 1 mg once | Result: | Dose-dependently showed a therapeutic efficacy against SEB intoxication. |
| [References]
[1] Saqib U, et al. Identifying the inhibition of TIR proteins involved in TLR signalling as an anti-inflammatory strategy. SAR QSAR Environ Res. 2018 Apr;29(4):295-318. DOI:10.1080/1062936X.2018.1431308 [2] Olson MA, et al. Discovery of small molecule inhibitors of MyD88-dependent signaling pathways using a computational screen. Sci Rep. 2015 Sep 18;5:14246. DOI:10.1038/srep14246 |
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InvivoChem
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MedChemExpress
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