Z-Arg-Lys-AOMK diTFA
Z-Arg-Lys-AOMK diTFA is a cathepsin B inhibitor that can cross the blood-brain barrier. Z-Arg-Lys-AOMK diTFA 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 diTFA can be used in the research of traumatic brain injury.
For research use only. We do not sell to patients.
- Formula: C34H44F6N6O10
- Molecular Weight:810.74
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
In Vitro
Z-Arg-Lys-AOMK (1.7-5536 nM; 30 min) diTFA 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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Molecular Weight 810.74
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Formula C34H44F6N6O10
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SMILES
O=C(OCC1=CC=CC=C1)N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN)C(COC(C2=C(C=CC=C2C)C)=O)=O)=O.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (61.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (1.54 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (1.54 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2334 mL | 6.1672 mL | 12.3344 mL | 30.8360 mL |
| 5 mM | 0.2467 mL | 1.2334 mL | 2.4669 mL | 6.1672 mL | |
| 10 mM | 0.1233 mL | 0.6167 mL | 1.2334 mL | 3.0836 mL | |
| 15 mM | 0.0822 mL | 0.4111 mL | 0.8223 mL | 2.0557 mL | |
| 20 mM | 0.0617 mL | 0.3084 mL | 0.6167 mL | 1.5418 mL | |
| 25 mM | 0.0493 mL | 0.2467 mL | 0.4934 mL | 1.2334 mL | |
| 30 mM | 0.0411 mL | 0.2056 mL | 0.4111 mL | 1.0279 mL | |
| 40 mM | 0.0308 mL | 0.1542 mL | 0.3084 mL | 0.7709 mL | |
| 50 mM | 0.0247 mL | 0.1233 mL | 0.2467 mL | 0.6167 mL | |
| 60 mM | 0.0206 mL | 0.1028 mL | 0.2056 mL | 0.5139 mL |
Z-Arg-Lys-AOMK diTFA Related Classifications
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