| Identification | Back Directory | [Name]
2-Thiophenecarboxylic acid, 5-[[[4-[3-[2-[[4-(trifluoromethoxy)phenyl]amino]-4-pyridinyl]-1,2,4-oxadiazol-5-yl]phenyl]amino]sulfonyl]-, methyl ester | [CAS]
2521624-67-7 | [Synonyms]
2-Thiophenecarboxylic acid, 5-[[[4-[3-[2-[[4-(trifluoromethoxy)phenyl]amino]-4-pyridinyl]-1,2,4-oxadiazol-5-yl]phenyl]amino]sulfonyl]-, methyl ester | [Molecular Formula]
C26H18F3N5O6S2 | [MOL File]
2521624-67-7.mol | [Molecular Weight]
617.58 |
| Chemical Properties | Back Directory | [Boiling point ]
750.2±70.0 °C(predicted) | [density ]
1.523±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [pka]
5.63±0.50(predicted) |
| Hazard Information | Back Directory | [Uses]
GSK-3β inhibitor 17 (compound 5 n) is a potent GSK-3β inhibitor. GSK-3β inhibitor 17 decreases cisplatin (HY-17394) induced p-p65, KIM-1 protein and mRNA expression. GSK-3β inhibitor 17 decreases cisplatin induced TNF-α, IL-1β, IL-6 and MCP-1 mRNA expression. GSK-3β inhibitor 17 shows anti-inflammation effect and has the potential for the research of acute kidney injury[1]. | [in vivo]
GSK-3β inhibitor 17 (12.5, 25, 50 mg/kg; i.p.) reduces cisplatin (HY-17394) induced NF-κB signaling activation and inflammatory cytokine release, thereby reducing kidney injury[1]. | Animal Model: | 6-8 weeks, 20-22 g, Male C57/BL6 mice (cisplatin 20 mg/kg i.p. for 3 days)[1] | | Dosage: | 12.5, 25, 50 mg/kg | | Administration: | I.p.; 24 h before the modeling | | Result: | Inhibited cisplatin-induced renal glycogen accumulation and tubular necrosis, 5n significantly reduced the protein level of p-P65 in cisplatin treatment, significantly downregulated mRNA levels of TNF-α, IL-1β, IL-6 and MCP-1. |
| [IC 50]
GSK-3β | [References]
[1] Cai YT, et al. A novel GSK3β inhibitor 5n attenuates acute kidney injury. Heliyon. 2024 Apr 12;10(8):e29159. |
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