耗材描述
SARS-CoV-2-IN-34
产品活性:SARS-CoV-2-IN-34 (S-20-1) 是一种具有广谱抑制活性的,可穿透血脑屏障的 pan-coronavirus (CoV) fusion 抑制剂。SARS-CoV-2-IN-34 有效抑制伪型和真型 SARS-CoV-2 和其伪型变体 (VOCs) 的感染效应。SARS-CoV-2-IN-34 对 SARS-CoV-2 S1 和 S2 蛋白的 HR1 和 RBD 结构域具有高度亲和性。SARS-CoV-2-IN-34 可用于感染的研究。
产品来源: https://www.medchemexpress.cn/sars-cov-2-in-34.html
研究领域:Anti-infection
作用靶点:SARS-CoV
In Vitro: SARS-CoV-2-IN-34 (0.1-100 μM; 30 min) inhibits infection by PsV of SARS variants on Huh-7 and Caco-2 cells with IC50s values ranging from 0.54 to 10.23 μM and inhibits infection of pseudotyped SARS-CoV, MERS-CoV, HCoV-229E, HCoV-NL63, and bat SARSr-CoV WIV1 with IC50s ranging from 1.30 to 12.02 μM.
SARS-CoV-2-IN-34 (0.1-100 μM; 30 min) inhibits the replication of authentic SARS-CoV 2 on Caco-2 cell line with an IC50 value of 8.14 μM and inhibits authentic HCoV-OC43 and HCoV-229E infection in RD cells and Huh-7 cells with IC50s of 6.25 and 9.46 μM, respectively.
SARS-CoV-2-IN-34 (0.1-100 μM; 2-4 h) potently inhibits cell-cell fusion mediated by S protein of SARS-CoV-2, SARS-CoV, MERS CoV, HCoV-229E and HCoV-NL63 with IC50s ranging from 1.47 to 5.44 μM.
SARS-CoV-2-IN-34 (50 μM; 1 h) inhibits SARS-CoV-2 infection at the early stage of viral entry.
SARS-CoV-2-IN-34 (0-2 μM) shows binding effects to S1, RBD and HR with Kd value of 67, 61 and 277 nM, respectively.
In Vivo: SARS-CoV-2-IN-34 (60 and 80 mg/kg; intranasal route 0.5 h pre- or post-challenge with HCoV-OC43 and SARS-CoV-2 Delta) effectively protects mice from infection.
SARS-CoV-2-IN-34 (50 mg/kg; i.p. and p.o. once ) shows good oral bioavailability and higher absorption rate under fed conditionsis, it is expected to have potential oral bioavailability.
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