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2437475-16-4

2437475-16-4 Structure

2437475-16-4 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[density ]

1.530±0.06 g/cm3(Predicted)
[form ]

Solid
[pka]

12.87±0.20(Predicted)
[color ]

White to off-white
Hazard InformationBack 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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