ZD-0892
Based on 1 Customer Validation
ZD-0892 is a selective and potent inhibitor of a neutrophil elastase with Kis of 6.7 and 200 nM for human neutrophil elastase and porcine pancreatic elastase, respectively.
For research use only. We do not sell to patients.
- Purity: 95.0%
- CAS No.: 171964-73-1
- Formula: C24H32F3N3O5
- Molecular Weight:499.52
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Ki: 6.7 nM (Human neutrophil elastase), 200 nM (Human neutrophil elastase)[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 171964-73-1
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Appearance Solid
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Molecular Weight 499.52
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Formula C24H32F3N3O5
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Color White to off-white
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SMILES
CC(C)[C@@H](C(N1[C@H](C(N[C@H](C(C(F)(F)F)=O)C(C)C)=O)CCC1)=O)NC(C2=CC=C(OC)C=C2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 250 mg/mL (500.48 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. 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. 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)
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: ≥ 2.08 mg/mL (4.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Protocol
Rats[2]
Adult male Sprague-Dawley rats (250-300 g in body weight) are induced pulmonary hypertension. In addition to a group of untreated rats, the experimental groups include rats that receive twice-daily gavage tube feedings of ZD0892, at a dose of 240 mg/kg per day or vehicle (5% polyethylene glycol or dimethyl sulfoxide). Rats are examined after 7 days of treatment.
Mice[1]
DBA/2 male mice 8 weeks old is used. ZD0892 is given in a dose of 60 mg/kg or 120 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Lee JK, et al. A serine elastase inhibitor reduces inflammation and fibrosis and preserves cardiac function after experimentally-induced murine myocarditis. Nat Med. 1998 Dec;4(12):1383-91. [Content Brief]
[2]. Cowan KN, et al. Complete reversal of fatal pulmonary hypertension in rats by a serine elastase inhibitor. Nat Med. 2000 Jun;6(6):698-702. [Content Brief]
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. 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 | 2.0019 mL | 10.0096 mL | 20.0192 mL | 50.0480 mL |
| 5 mM | 0.4004 mL | 2.0019 mL | 4.0038 mL | 10.0096 mL | |
| 10 mM | 0.2002 mL | 1.0010 mL | 2.0019 mL | 5.0048 mL | |
| 15 mM | 0.1335 mL | 0.6673 mL | 1.3346 mL | 3.3365 mL | |
| 20 mM | 0.1001 mL | 0.5005 mL | 1.0010 mL | 2.5024 mL | |
| 25 mM | 0.0801 mL | 0.4004 mL | 0.8008 mL | 2.0019 mL | |
| 30 mM | 0.0667 mL | 0.3337 mL | 0.6673 mL | 1.6683 mL | |
| 40 mM | 0.0500 mL | 0.2502 mL | 0.5005 mL | 1.2512 mL | |
| 50 mM | 0.0400 mL | 0.2002 mL | 0.4004 mL | 1.0010 mL | |
| 60 mM | 0.0334 mL | 0.1668 mL | 0.3337 mL | 0.8341 mL | |
| 80 mM | 0.0250 mL | 0.1251 mL | 0.2502 mL | 0.6256 mL | |
| 100 mM | 0.0200 mL | 0.1001 mL | 0.2002 mL | 0.5005 mL |