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.
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- CAS No.: 2810056-57-4
- Formule: C30H42N6O6
- Masse moléculaire:582.70
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (female, adult, 4-5 months of age, traumatic brain injury CCI model)[1]
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Dosage:20 mg/kg
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Administration:i.p.; daily; 7 consecutive days (starting 1 day pre-CCI-TBI through day 6 post-CCI-TBI)
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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.
Chemical Information
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CAS No. 2810056-57-4
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Masse moléculaire 582.70
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Formule C30H42N6O6
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Z-Arg-Lys-AOMK Related Classifications
HY-183166 Related Classifications
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