BKI-1369

BKI-1369 是一种 bumped kinase 抑制剂 (BKI)。 BKI-1369 增加人类 Ether-a-go-go-related 相关基因 (hERG) 的抑制活性，IC50 为 1.52 μM。BKI-13699 降低了生殖猪模型中的寄生虫负担和疾病严重程度。BKI-1369 已经充分表征了效力，稳定性，代谢，毒性和药代动力学，并且可以有效抑制感染的小鼠和小牛中的微小隐孢子虫 (C. parvum)。

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Background

BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves[1]. IC50: 1.52 μM (hERG)[1]

[1]. Lee S, et al. Therapeutic Efficacy of Bumped Kinase Inhibitor 1369 in a Pig Model of Acute Diarrhea Caused by Cryptosporidium hominis. Antimicrob Agents Chemother. 2018 Jun 26;62(7).