K777 是一种具有口服活性且不可逆的半胱氨酸蛋白酶抑制剂，对 CYP3A4 的 IC50 为 60 nM。 K777 是一种 CCR4 拮抗剂并抑制趋化性。

K777 is an orally active and irreversible inhibitor of cysteine protease with an IC50 of 60 nM for CYP3A4. K777 is a CCR4 antagonist and inhibits chemotaxis.

K777 is a broad-spectrum antiviral and 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. K777 alone demonstrates up to 70% inhibition of 229E-S-mediated transduction in TMPRSS2 expressing cells. Simultaneous treatment with Camostat and K777 increases inhibition to ~ 90%[1]. K777 inhibits both CCL17 binding and CCL17-induced chemotaxis in Hut78 cells with IC50s of 57 and 8.9 nM, respectively. The K777-mediated inhibition of chemotaxis is potent even in the presence of a 10-fold higher concentration of CCL17. K777 induces CCR4 internalization with a 50% reduction of cell surface CCR4[3].

In C57BL/6 IFN-γR-KO mice, K777 ( 35-105 mg/kg; p.o.) rescues mice from otherwise lethal infections[4].

233277-99-1

C32H38N4O4S

574.73

APC-3316

DMSO:90mg/mL (156.6mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years