K777 是一种有效的，口服活性且不可逆的半胱氨酸蛋白酶 (cysteine protease) 抑制剂，也是一种有效的 CYP3A4 抑制剂，IC₅₀ 为 60 nM，是一种选择性的 CCR4 拮抗剂，具有强的趋化性抑制作用。K777 不可逆地抑制锥虫（克鲁斯锥虫的主要半胱氨酸蛋白酶）和组织蛋白酶 B 和 L。K777 是一种广谱抗病毒药物，通过靶向组织蛋白酶介导的细胞进入。K777 抑制 SARS-CoV 和 EBOV 病毒的进入，IC₅₀ 值分别为 0.68 nM 和 0.87 nM。

K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC 50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC 50 values of 0.68 nM and 0.87 nM, respectively.

Solid

Cysteine protease
IC50: 60 nM (CYP3A4)
CCR4

K777 (K11777) can inhibit entry driven by other viral envelope proteins, HIV-based pseudotypes bearing spikes from coronaviruses (SARS-CoV, HCoV-229E, NL63, MERS-CoV) or glycoproteins from filoviruses (EBOV, SUDV, TAFV, RESTV, BEBOV and MARV) are examined. K777 inhibits SARS-CoV, HCoV-229E, NL63, MERS-CoV, EBOV, SUDV, TAFV, RESTV, BEBOV, MARV and Nipah pseudovirus entry with IC50 values of 0.68 nM, 1.48 nM, 6.78 nM, 46.12 nM, 0.87 nM, 1.14 nM, 2.26 nM, 3.37 nM, 5.91 nM, 1.9 nM and 0.42 nM, respectively. In contrast, 100 nM K777 does not inhibit infection mediated by envelope glycoproteins from an alphavirus (CHIKV), a rhabdovirus (VSV), a flavivirus (HCV), the retroviruses MLV-A and XMRV or two arenaviruses, Lassa and Junin virus.
Whether K777 displays antiviral activity in TMPRSS2 expressing cells are assessed. For this, the incubated target cells with Camostat

K777 (K11777; 35-105 mg/kg; oral administration; twice a day; for 10 days; C57BL/6 IFN-γR-KO mice) treatment rescues mice from otherwise lethal infections . has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；In solvent -80°C 6 months

[1]. Zhou Y, et al. Protease inhibitors targeting coronavirus and filovirus entry. Antiviral Res. 2015 Apr;116:76-84.
[2]. Jacobsen W, et al. In vitro evaluation of the disposition of A novel cysteine protease inhibitor. Drug Metab Dispos. 2000 Nov;28(11):1343-51.
[3]. Sato T, et al. Internalization of CCR4 and inhi

In Vitro: DMSO : 100 mg/mL (173.99 mM; Need ultrasonic)配制储备液