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K777 (tosylate)

K777 tosylate is a potent, orally active and irreversible cysteine protease inhibitor. K777 tosylate is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 tosylate irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 tosylate is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 tosylate inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively[1][2][3].

Product Specifications

CAS Number

502960-91-0

UNSPSC

12352005

Target

Cathepsin; CCR; Cytochrome P450; Filovirus; Parasite; SARS-CoV

Type

Reference compound

Related Pathways

Anti-infection; GPCR/G Protein; Immunology/Inflammation; Metabolic Enzyme/Protease

Field of Research

Cancer; Infection

Assay Protocol

https://www.medchemexpress.com/k777-tosylate.html

Smiles

O=S(O)(C1=CC=C(C=C1)C)=O.O=S(/C=C/[C@H](CCC2=CC=CC=C2)NC([C@@H](NC(N3CCN(CC3)C)=O)CC4=CC=CC=C4)=O)(C5=CC=CC=C5)=O

Molecular Formula

C39H46N4O7S2

Molecular Weight

746.94

References & Citations

[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 inhibition of chemotaxis by K777, a potent and selective CCR4 antagonist. Pharmacology. 2013;91 (5-6) :305-13.|[4]Ndao M, et al. A cysteine protease inhibitor rescues mice from a lethal Cryptosporidium parvum infection. Antimicrob Agents Chemother. 2013 Dec;57 (12) :6063-73.

Shipping Conditions

Room temperature

Scientific Category

Oligonucleotides

Clinical Information

No Development Reported

Frequently Asked Questions

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