CA-074 methyl ester (CA-074 Me) - 10mM in DMSO , CAS No.147859-80-1

CAS: 147859-80-1 Cat. No.: C408263 Peso molecular: 397.47

GRADE & PURITY 10mM in DMSO

Synonyms

Cathepsin B Inhibitor IV | L-​Proline, N-​[[(2S,​3S)​-​3-​[(propylamino)​carbonyl]​-​2-​oxiranyl]​carbonyl]​-​L-​isoleucyl-​, methyl ester

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

CA-074 methyl ester (CA-074 Me) CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor.
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.
Cell Data

cell lines：Cultured human mast cells (CHMC)

Concentrations：100 μM

Incubation Time：2 h

Powder Purity:≥99%

Specifications

Sinónimos

Cathepsin B Inhibitor IV | L-​Proline, N-​[[(2S, ​3S)​-​3-​[(propylamino)​carbonyl]​-​2-​oxiranyl]​carbonyl]​-​L-​isoleucyl-​, methyl ester

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Tipo de acción

INHIBITOR

Nombres e identificadores

• Isómeros SMILES: CCCNC(=O)[C@@H]1[C@H](O1)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N2CCC[C@H]2C(=O)OC
• WGK Alemania: 3
• Peso molecular: 397.47
• Reaxy-Rn: 25187464
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25187464&ln=

Objetivos asociados (humanos)

CTSB Tchem Cathepsin B (1 Activities)

Discover Target: CTSB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 100 mg/mL (109.38 mM); Ethanol: 100 mg/mL (109.38 mM); Water: Insoluble
• Rotación específica [α]: -33.3 - -12.1°c = 1.4 in EtOH, 20° C