ChemicalBook CAS DataBase List 2919801-86-6

2919801-86-6

Name	Benzeneacetamide, N-[5-[[2-[[[4-[(ethylsulfonyl)amino]cyclohexyl]carbonyl]amino]-5-fluoro-6-benzothiazolyl]oxy]-2-fluorophenyl]-3-(trifluoromethyl)-
CAS	2919801-86-6
Molecular Formula	C31H29F5N4O5S2
Molecular Weight	696.71
MOL File	2919801-86-6.mol

Chemical Properties

density	1.49±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)
solubility	DMF: 15 mg/ml DMSO: 10 mg/ml
pka	9.86±0.70(Predicted)

Hazard Information

Uses

SZM-1209 is an orally active, potent and specific RIPK1 inhibitor, with a Kd of 85 nM. SZM-1209 exhibits high anti-necroptotic activity (EC50=22.4 ± 8.1 nM). SZM-1209 shows anti-SIRS (systemic inflammatory response syndrome), and anti-ALI (acute lung injury) effects[1].

in vivo

SZM-1209 (25-100 mg/kg, IG) can reverse mouse deaths with significant anti-inflammatory effects in a mTNF-α-induced systemic inflammatory response syndrome (SIRS) model^[1].
SZM-1209 (25-100 mg/kg, IP) significantly alleviates ALI (acute lung injury) by reducing pulmonary edema and pathological damage^[1].

Animal Model:	C57BL/6J mice (female, 6-8 weeks old, mTNF-α (intravenous injection)-induced SIRS model)^[1]
Dosage:	25, 50, and 100 mg/kg
Administration:	Intragastric administration
Result:	Dose-dependently improved survival rates of the SIRS mice to 30, 90, and 100%. Could effectively protect against mTNFα-induced SIRS in vivo. Serum levels of IL-6 and IL-1β were significantly decreased.

Animal Model:	C57BL/6J mice (female, 6-8 weeks old, NNK (HY-126477) (65 mg/kg) short-term intratracheal exposure-induced ALI model)^[1]
Dosage:	25, 50, and 100 mg/kg
Administration:	IP
Result:	Exhibited lower levels of IL-6 and TNF-α in BALF than those of model mice. Inhibited the expression of inflammatory genes of IL-6 and TNF-α in lung tissues of mice at a mRNA level. Significant reduced phosphorylation of RIPK1, and also completely blocked at a high dose of 100 mg/kg in lung tissue of ALI model mice.

IC 50

RIPK1: 85 nM (Kd); RIPK3: >10000 nM (Kd)

References

[1] Zhang X, et al. Targeting Receptor-Interacting Protein Kinase 1 by Novel Benzothiazole Derivatives: Treatment of Acute Lung Injury through the Necroptosis Pathway. J Med Chem. 2023 Apr 13;66(7):5261-5278. DOI:10.1021/acs.jmedchem.3c00197

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