Name | Amustaline Dihydrochloride |
Synonyms | Amustaline S-303 dihydrochloride AMUSTALINE DIHYDROCHLORIDE Amustaline Dihydrochloride |
CAS | 210584-54-6 |
Molecular Formula | C22H26Cl3N3O2 |
Molar Mass | 470.82 |
In vitro study | S‐303 (200 μM; 20 h) and glutathione (GSH; 20 mM) inactivates high titres of Chikungunya virus (CHIKV) in red blood cells (RBCs). S-303 (200 μM; 20 h) and GSH (2 mM) inactivates >6.5 logs of HIV, >5.7 logs of Bluetongue virus, >7.0 logs of Yersinia enterocolitica , 4.2 logs of Serratia marcescens , and 7.5 logs of Staphylococcus epidermidis in whole blood experiments . S-303 (200 μM; 20 h) and GSH (20 mM) inactivates approximately 5 logs or greater of Y. enterocolitica , E. coli , S. marcescens , S. aureus , HIV, bovine viral diarrhoea virus, bluetongue virus and human adenovirus 5 in RBC. S-303 (200 μM; 20 h) retains in vitro parameters of RBC function and physiology (including total ATP, extracellular potassium, hemolysis, glucose consumption, lactate production, and pH at 37 °C) compared to conventional RBC. |
In vivo study | S‐303 RBCs (a single transfusion) is well tolerated in rats (50 μmol/kg) and dogs (70 μmol/kg). S‐303 RBCs (repeated transfusions) is well tolerated in rats (10 μmol/kg) and dogs (10 μmol/kg) with no histopathologic evidence of organ toxicity. |
biological activity | Amustaline (S-303) dihydrochloride, an alkylating agent targeting nucleic acids, is an effective pathogen inactivator and can be used for blood components containing red blood cells. The Amustaline dihydrochloride has three components: acridine immobilizers (intercalators of non-covalently targeted nucleic acids), effectors (dialkyl groups that react with nucleophiles), and linkers (fine flexible carbon chains containing unstable ester bonds that hydrolyze at neutral pH to produce non-reactive decomposition products). |
in vitro study | S‐303 (200 μM; 20 h) and glutathione (GSH; 20 mM) inactivates high titers of Chikungunya virus (CHIKV) in red blood cells (RBCs). S-303 (200 μM; 20 h) and GSH (2 mM) inactivates >6.5 logs of HIV, >5.7 logs of Bluetongue virus, >7.0 logs of Yersinia enterocolitica , 4.2 logs of Serratia marcescens , and 7.5 logs of Staphylococcus epidermidis in whole blood experiments . S-303 (200 μ M; 20 h) and GSH (20 mM) inactivates approximately 5 logs or greater of Y. enterocolitica , E. coli , S. marcescens , S. aureus , HIV, bovine viral diarrhoea virus, bluetongue virus and human adenovirus 5 in RBC. S-303 (200 μM; 20 h) retains in vitro parameters of RBC function and physiology (including total ATP, extracellular potassium, hemolysis, glucose consumption, lactate production, and pH at 37 c) compared to conventional RBC. |
in vivo studies | s‐303 RBCs (a single transfusion) is well tolerated in rats (50 μmol/kg) and dogs (70 μmol/kg). s‐303 RBCs (repeated transfusions) is well tolerated in rats (10 μmol/kg) and dogs (10 μmol/kg) with no histopathologic evidence of organ toxicity. |