KP496
Based on 1 Customer Validation
KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.79%
- CAS. Nr.: 217799-03-6
- Formel: C31H34ClN3O7S3
- Molecular Weight:692.27
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
LTD4 |
TXA2 Receptor |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 217799-03-6
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Appearance Solid
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Molecular Weight 692.27
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Formel C31H34ClN3O7S3
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Color White to off-white
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SMILES
O=C(O)C1=CC=CC=C1S(=O)(N(CCCCNS(=O)(C2=CC=C(Cl)C=C2)=O)CC3=CC=CC(OCC4=NC(C(C)C)=CS4)=C3)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (144.45 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.5 mg/mL (3.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Protokoll
Animal Administration[1]
Male mice (9 weeks old, 33 to 42g are used) BLM solution (15 mg/mL) is intravenously injected into mice (0.1 mL/10 g of body weight) on day 0. Mice are sacrificed on day 7 or 21. They are exposed to an aerosol of KP496 (KP-496) solution (0.5%) for 30 min using a pressure nebulizer 1 h before and 3 h after BLM-injection on day 0. From day 1 to the day before sacrificed, mice are exposed to KP496 (0.5%) for 30 min morning and evening[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (273 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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Kurokawa S, et al. Effect of inhaled KP-496, a novel dual antagonist of the cysteinyl leukotriene and thromboxane A2 receptors, on a bleomycin-induced pulmonary fibrosis model in mice. Pulm Pharmacol Ther. 2010 Oct;23(5):425-31. [Content Brief]
[2]. Ishimura M, et al. Effects of KP-496, a novel dual antagonist for cysteinyl leukotriene receptor 1 and thromboxane A2 receptor, on Sephadex-induced airway inflammation in rats. Biol Pharm Bull. 2009 Jun;32(6):1057-61. [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 | 1.4445 mL | 7.2226 mL | 14.4452 mL | 36.1131 mL |
| 5 mM | 0.2889 mL | 1.4445 mL | 2.8890 mL | 7.2226 mL | |
| 10 mM | 0.1445 mL | 0.7223 mL | 1.4445 mL | 3.6113 mL | |
| 15 mM | 0.0963 mL | 0.4815 mL | 0.9630 mL | 2.4075 mL | |
| 20 mM | 0.0722 mL | 0.3611 mL | 0.7223 mL | 1.8057 mL | |
| 25 mM | 0.0578 mL | 0.2889 mL | 0.5778 mL | 1.4445 mL | |
| 30 mM | 0.0482 mL | 0.2408 mL | 0.4815 mL | 1.2038 mL | |
| 40 mM | 0.0361 mL | 0.1806 mL | 0.3611 mL | 0.9028 mL | |
| 50 mM | 0.0289 mL | 0.1445 mL | 0.2889 mL | 0.7223 mL | |
| 60 mM | 0.0241 mL | 0.1204 mL | 0.2408 mL | 0.6019 mL | |
| 80 mM | 0.0181 mL | 0.0903 mL | 0.1806 mL | 0.4514 mL | |
| 100 mM | 0.0144 mL | 0.0722 mL | 0.1445 mL | 0.3611 mL |