K777
K777
CAS: 233277-99-1
Molecular Formula: C32H38N4O4S
K777 - Names and Identifiers
K777 - Physico-chemical Properties
| Molecular Formula | C32H38N4O4S |
| Molar Mass | 574.73 |
| Density | 1.217±0.06 g/cm3(Predicted) |
| Boling Point | 861.0±65.0 °C(Predicted) |
| pKa | 12.48±0.20(Predicted) |
| Storage Condition | -20°C，干燥，密封 |
| MDL | MFCD14105618 |
| In vitro study | 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 IC 50 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, or a combination of K777 and Camostat and then infected with pseudoviruses bearing 229E-S. K777 alone demonstrates up to ~ 70% inhibition of 229E-S-mediated transduction. Simultaneous treatment with Camostat and K777 increases inhibition to ~ 90%. Similar inhibition patterns are obtained using the human intestinal epithelial cell line Caco-2, which express endogenous TMPRSS2 and cathepsins. K777 inhibits both CCL17 binding and CCL17-induced chemotaxis in Hut78 cells (IC 50 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. K777 does not inhibit CXCR4-induced chemotaxis or internalization and did not bring about Ca 2+ mobilization by itself. |
K777 - Reference Information
| biological activity | K777 is a potent, orally active and irreversible inhibitor of cysteine protease, it is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and is a selective CCR4 antagonist with strong chemotaxis inhibition. K777 irreversibly inhibits Trypanosoma (the major cysteine protease of Trypanosoma krusei) and cathepsin B and L. K777 is a broad-spectrum antiviral drug that targets cathepsin-mediated cell entry. K777 inhibited the entry of SARS-CoV and EBOV Virus with IC50 values of 0.68 nM and 0.87 nM, respectively. |
| Target | Cysteine protease IC50: 60 nM (CYP3A4) CCR4 |
| 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. |
Last Update：2024-04-09 21:11:58
Supplier List
Spot supply
Product Name: K777 Visit Supplier Webpage Request for quotationCAS: 233277-99-1
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: K777 Visit Supplier Webpage Request for quotationCAS: 233277-99-1
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: K777 Visit Supplier Webpage Request for quotationCAS: 233277-99-1
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
Product Name: K777 Visit Supplier Webpage Request for quotationCAS: 233277-99-1
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: K777 Visit Supplier Webpage Request for quotationCAS: 233277-99-1
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: K777 Visit Supplier Webpage Request for quotationCAS: 233277-99-1
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
View History
K777
L-Arginine,L-histidyl-L-methionyl-L-arginyl-L-seryl-L-alanyl-L-methionyl-L-serylglycyl-L-leucyl-L-histidyl-L-leucyl-L-valyl-L-lysyl-L-arginyl-
2-Pyrimidinamine,5-[2-(2,5-dibromophenyl)diazenyl]-4-methyl-6-phenyl-
(R)-2-(1-(tert-Butoxycarbonyl)azetidin-2-yl)acetic acid
N-[4-(1-azepanylsulfonyl)phenyl]-3-(2-thienyl)acrylamide
m-Xylene-2,5-diol
2-(2,4-dichlorophenoxy)-N-(4-fluorobenzyl)propanamide
8-Chloro-11,12-dimethoxy-4,7-diaza-9-thia-9H-indeno[2,1-c]phenanthrene
Surgicel (tn)
478031-21-9
L-Arginine,L-histidyl-L-methionyl-L-arginyl-L-seryl-L-alanyl-L-methionyl-L-serylglycyl-L-leucyl-L-histidyl-L-leucyl-L-valyl-L-lysyl-L-arginyl-
2-Pyrimidinamine,5-[2-(2,5-dibromophenyl)diazenyl]-4-methyl-6-phenyl-
(R)-2-(1-(tert-Butoxycarbonyl)azetidin-2-yl)acetic acid
N-[4-(1-azepanylsulfonyl)phenyl]-3-(2-thienyl)acrylamide
m-Xylene-2,5-diol
2-(2,4-dichlorophenoxy)-N-(4-fluorobenzyl)propanamide
8-Chloro-11,12-dimethoxy-4,7-diaza-9-thia-9H-indeno[2,1-c]phenanthrene
Surgicel (tn)
478031-21-9