Molecular Formula | C19H31N3O6 |
Molar Mass | 397.47 |
Density | 1.212±0.06 g/cm3(Predicted) |
Melting Point | 153-155°C |
Boling Point | 666.3±55.0 °C(Predicted) |
Solubility | Soluble in DMSO |
Appearance | Solid |
Color | White to Off-White |
pKa | 13.38±0.40(Predicted) |
Storage Condition | -20°C |
In vitro study | CA-074Me inhibits cathepsin L in HL-60 cells and in the blood form of Trypanosoma brucei, but does not act in the absence of thiols. CA-074Me is transformed into CA-074 under the action of intracellular esterases and thus inhibits cathepsin B in GSH-depleted HL60 cells. CA-074, but not CA-074Me, selectively inhibits cathespsin B in living cells. Myotube size, number, and induced fusion-related creatine phosphokinase activity and myosin heavy chain protein were reduced in CA074Me-treated myoblasts, and the degree of reduction correlated with concentration. In differentiating myoblasts, micromolar concentrations of CA-074Me inhibit catB activity. |
In vivo study | Administration of CA074Me to London APP mice significantly improved their memory deficits, reduced the levels of amyloid plaque load, Aβ40 and Aβ42 in the brain, and reduced APP-derived ctfβ. There was no such effect in Swedish/London APP mice. Intraventricular injection of CA074Me in normal guinea pigs resulted in A large decrease in intracerebral Aβ and inhibition of β-secretase activity. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.516 ml | 12.58 ml | 25.159 ml |
5 mM | 0.503 ml | 2.516 ml | 5.032 ml |
10 mM | 0.252 ml | 1.258 ml | 2.516 ml |
5 mM | 0.05 ml | 0.252 ml | 0.503 ml |
biological activity | CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a CA-074 derivative of permeable membranes, it is an irreversible inhibitor of cathepsin B. |
Target | Value |