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Anti-inflammatory agent 40

CAS No. :

MCE 站：Anti-inflammatory agent 40

产品活性：Anti-inflammatory agent 40 是一种潜在的和具有口服活性的抗疟疾 (anti-malarial) 和抗炎剂。Anti-inflammatory agent 40 抑制卡拉胶诱导的足跖肿胀。

研究领域：Anti-infection

作用靶点：Parasite

In Vitro: Anti-inflammatory agent 40 (compound 5p) is against both CQ-sensitive ａnd resistant strains of?P. falciparum, Anti-inflammatory agent 40 exhibits IC₅₀ value 1.47?μM against?chloroquine?sensitive strain of?P. falciparum (Pf3D7).
Anti-inflammatory agent 40 inhibits LPS induced?MAP kinase?activation ａnd decreases pERK1/2 (Thr202/Tyr204) ａnd pJNK1/2 expression in THP-1 monocytes.

In Vivo: Anti-inflammatory agent 40 (compound 5p) (p.o, 1?h prior to caraageenan injection；25, 50 ａnd 100?mg/kg；Paw swelling was subsequently monitored after 4 ａnd 6) shows inhibition in swiss mice, the Carrageenan inhibition percent are 61%, 56% at 25mg/kg after 4h or 6h, respectively. the Carrageenan inhibition percent are 62%, 56% at 50 mg/kg after 4h or 6h, respectively, ａnd 73%, 65% at 50 mg/kg after 4h or 6h, respectively .
Anti-inflammatory agent 40 exhibits good PK profile, it is satisfactory ａnd can be attested for the candidates for future?drug discovery?optimization, the C_max, T_max, AUC, t_1/2 are 110.37?±?11.92 ng/mL, 0.25?±?0.0 h, 86.91?±?16.86 h.ng/mL ａnd 0.87?±?0.15 h, respectively.

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