Z-FF-FMK
Based on 1 Customer Validation
Z-FF-FMK (Z-Phe-Phe-FMK) is a cell-permeable, irreversible, and cysteine protease inhibitor targeting cathepsin-L. Z-FF-FMK inhibits angiotensin II-induced MEK activation in vascular walls, aortic medial remodeling, blood pressure elevation, and upregulation of cystatin C in aortic walls. Z-FF-FMK prevents β-amyloid-mediated caspase-3 activation, poly (ADP-ribose) polymerase cleavage, DNA fragmentation, and apoptosis of cortical neurons (apoptosis). Z-FF-FMK can be used in research related to hypertension and Alzheimer's disease.
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- Pureté: 95.98%
- CAS No.: 105608-85-3
- Formule: C27H27FN2O4
- Masse moléculaire:462.51
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Stockage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
|
cathepsin L |
Caspase 3 |
Z-FF-FMK (10 μM; 6 h) potently inhibits basal and Aβ-stimulated cathepsin-L activity in primary cultured rat cortical neurones, reducing basal activity to near undetectable levels and eliminating the 6 h Aβ-induced activity increase[2].
Z-FF-FMK (10 μM; 24 h) completely prevents Aβ1-40-induced caspase-3 activation in primary cultured rat cortical neurones after 24 h of co-incubation[2].
Z-FF-FMK (10 μM; 24 h) fully blocks Aβ1-40-stimulated caspase-3 activity in primary cultured rat cortical neurones after 24 h of co-incubation[2].
Z-FF-FMK (10 μM) completely inhibits Aβ1-40-induced PARP cleavage in primary cultured rat cortical neurones[2].
Z-FF-FMK (10 μM; 72 h) fully prevents Aβ1-40-induced DNA fragmentation in primary cultured rat cortical neurones after 72 h of co-incubation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 wild-type (8-12 weeks old; angiotensin II-induced hypertension model)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every other day; 28 days
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Result:Almost completely blocked angiotensin II-induced aortic artery media remodeling, reducing media thickness from a 2.1-fold increase (vs. control) to a 1.3-fold increase (vs. control).
Prevented angiotensin II-induced systolic blood pressure elevation, maintaining systolic blood pressure near baseline (~100 mmHg) compared to the ~160 mmHg peak in angiotensin II-only mice.
Suppressed angiotensin II-induced increases in aortic p-MEK expression, reducing from a 3.2-fold increase vs. control to a 1.2-fold increase vs. control.
Suppressed angiotensin II-induced increases in cystatin C expression, reducing from a 0.8-fold increase vs. control to a 0.4-fold increase vs. control.
Normalized angiotensin II-induced elevated arterial cathepsin L activity to control levels.
Chemical Information
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CAS No. 105608-85-3
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Appearance Solid
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Masse moléculaire 462.51
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Formule C27H27FN2O4
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Color White to off-white
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Synonyms
Z-Phe-Phe-FMK
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Sequence
Z-Phe-Phe-FMK
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Sequence Shortening
Z-FF-FMK
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 100 mg/mL (216.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1621 mL | 10.8106 mL | 21.6212 mL | 54.0529 mL |
| 5 mM | 0.4324 mL | 2.1621 mL | 4.3242 mL | 10.8106 mL | |
| 10 mM | 0.2162 mL | 1.0811 mL | 2.1621 mL | 5.4053 mL | |
| 15 mM | 0.1441 mL | 0.7207 mL | 1.4414 mL | 3.6035 mL | |
| 20 mM | 0.1081 mL | 0.5405 mL | 1.0811 mL | 2.7026 mL | |
| 25 mM | 0.0865 mL | 0.4324 mL | 0.8648 mL | 2.1621 mL | |
| 30 mM | 0.0721 mL | 0.3604 mL | 0.7207 mL | 1.8018 mL | |
| 40 mM | 0.0541 mL | 0.2703 mL | 0.5405 mL | 1.3513 mL | |
| 50 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0811 mL | |
| 60 mM | 0.0360 mL | 0.1802 mL | 0.3604 mL | 0.9009 mL | |
| 80 mM | 0.0270 mL | 0.1351 mL | 0.2703 mL | 0.6757 mL | |
| 100 mM | 0.0216 mL | 0.1081 mL | 0.2162 mL | 0.5405 mL |