1. Metabolic Enzyme/Protease
  2. Cathepsin
  3. Z-Arg-Lys-AOMK

Z-Arg-Lys-AOMK is a cathepsin B inhibitor that can cross the blood-brain barrier. Z-Arg-Lys-AOMK reduces cytosolic cathepsin B activity in homogenates of mouse cerebral cortex and hippocampal tissues, and alleviates motor dysfunction associated with CCI-TBI. Z-Arg-Lys-AOMK can be used in the research of traumatic brain injury.

For research use only. We do not sell to patients.

Z-Arg-Lys-AOMK

Z-Arg-Lys-AOMK Chemical Structure

CAS No. : 2810056-57-4

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Description

Z-Arg-Lys-AOMK is a cathepsin B inhibitor that can cross the blood-brain barrier. Z-Arg-Lys-AOMK reduces cytosolic cathepsin B activity in homogenates of mouse cerebral cortex and hippocampal tissues, and alleviates motor dysfunction associated with CCI-TBI. Z-Arg-Lys-AOMK can be used in the research of traumatic brain injury[1].

In Vitro

Z-Arg-Lys-AOMK (1.7-5536 nM; 30 min) potently and selectively inhibits recombinant mouse cathepsin B at neutral pH 7.2 (IC50 = 25 nM) with 100-fold lower potency at acidic pH 4.6, and does not inhibit other mouse cysteine cathepsins (C, H, L, X) at relevant concentrations[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Z-Arg-Lys-AOMK (20 mg/kg; i.p.; once daily) reduces cathepsin B activity in the cytoplasm and homogenates of the cerebral cortex and hippocampus in mice induced by CCI-TBI, and restores motor function to 55% of the baseline level at 1 day post-injury[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice (female, adult, 4-5 months of age, traumatic brain injury CCI model)[1]
Dosage: 20 mg/kg
Administration: i.p.; daily; 7 consecutive days (starting 1 day pre-CCI-TBI through day 6 post-CCI-TBI)
Result: Reduced CCI-TBI-induced cytosolic cathepsin B activity in the ipsilateral brain cortex from ~400 pmol AMC/μg protein to ~275 pmol AMC/μg protein .
Reduced CCI-TBI-induced cytosolic cathepsin B activity in the contralateral cortex from ~200 pmol AMC/μg protein to ~220 pmol AMC/μg protein.
Reduced cathepsin B activity in ipsilateral brain cortex homogenates from ~1750 pmol AMC/μg protein to ~1000 pmol AMC/μg protein.
Reduced cathepsin B activity in ipsilateral hippocampus homogenates from ~1700 pmol AMC/μg protein to ~800 pmol AMC/μg protein.
Improved rotarod motor function on day 1 post-CCI-TBI, increasing latency from ~35% of baseline to ~55% of baseline.
Molecular Weight

582.70

Formula

C30H42N6O6

CAS No.
SMILES

C(OCC([C@@H](NC([C@@H](NC(OCC1=CC=CC=C1)=O)CCCNC(=N)N)=O)CCCCN)=O)(=O)C2=C(C)C=CC=C2C

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Z-Arg-Lys-AOMK
Cat. No.:
HY-183166
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