K777

Research use only, not for human use.

K777 is an orally active and irreversible cysteine protease inhibitor. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry.

K777 is an orally active and irreversible cysteine protease inhibitor. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 is also a CYP3A4 inhibitor (IC50: 60 nM) and a CCR4 antagonist. K777 inhibits SARS-CoV and EBOV pseudovirus entry (IC50s: 0.68 nM and 0.87 nM). K777 irreversibly inhibits Cruzain, and cathepsins B and L.(In Vitro):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%. 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.(In Vivo):In C57BL/6 IFN-γR-KO mice, K777 ( 35-105 mg/kg; p.o.) rescues mice from otherwise lethal infections.

——

Animal Model:C57BL/6 IFN-γR-KO mice (6-8 weeks of age) injected with Cryptosporidium parvum Dosage:35 mg/kg, 70 mg/kg, and 105 mg/kg Administration:Oral administration; twice a day; for 10 days Result:Rescued mice from otherwise lethal infections.

APC-3316

Proteasome/Ubiquitin

Cysteine Protease

M1 muscarininc

——

——

233277-99-1

574.74

C32H38N4O4S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (173.99 mM)

CN1CCN(CC1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCc1ccccc1)\C=C\S(=O)(=O)c1ccccc1

——

(-20℃)

With Ice Pack

≥ 2 years