[CAS NO. 147859-80-1] CA-074 methyl ester (CA-074 Me)
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PRODUCTS SPECIFICATIONS [147859-80-1]
Store
Catalog
SLK-S7420
Brand
Selleck
CAS
147859-80-1
DESCRIPTION [147859-80-1]
Overview
| MDL | MFCD03452890 |
|---|---|
| Molecular Weight | 397.47 |
| Molecular Formula | C19H31N3O6 |
| SMILES | O=C(OC)[C@H]1N(C([C@H]([C@@H](C)CC)NC([C@H]2O[C@@H]2C(NCCC)=O)=O)=O)CCC1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5159 mL | 12.5796 mL | 25.1591 mL |
| 5 mM | 0.5032 mL | 2.5159 mL | 5.0318 mL |
| 10 mM | 0.2516 mL | 1.2580 mL | 2.5159 mL |
| 50 mM | 0.0503 mL | 0.2516 mL | 0.5032 mL |
Description
CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a membrane-permeable derivative of CA-074 and acts as an irreversible inhibitor.
Targets
| Cathepsin B [1] |
In vitro
CA-074Me is able to inhibit cathepsin L within living HL-60 cells and bloodstream forms of Trypanosoma brucei brucei, but does not inhibit cathepsin L in the absence of thiols. CA-074Me is converted into CA-074 by intracellular esterasesand is, therefore, able to inhibit cathepsin B in GSH-depleted HL-60 cell. It is suggested that CA-074 rather than CA-074Me should be used to selectively inhibit cathespsin B within living cells. Myotube size and number and induced levels of fusion-related creatine phosphokinase activity and myosin heavy-chain protein are reduced from 30 to 50% in CA074Me-treated myoblasts. These reductions are also dose related. Micromolar concentrations of CA074Me inhibit catB activity in differentiating myoblasts.
In vivo
Administration of CA074Me to the London APP mice results in significant improvement in memory deficit, reduces amyloid plaque load in brain, reduces levels of Aβ40 and Aβ42 in brain, and reduces C-terminal β-secretase fragment (CTFβ) derived from APP by β-secretase when compared with untreated control animals. It has no effect on any of these parameters in mice expressing the Swe mutant β-secretase site of APP (in Swedish/London APP mice). In vivo icv administration of CA074Me to normal guinea pigs results in substantial reduction of brain Aβ levels and inhibits β-secretase activity.
References
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