Motapizone
Based on 1 Customer Validation
Motapizone (NAT 05-239) is a selective PDE3 inhibitor. Motapizone moderately inhibits cytokine release in lipopolysaccharide (LPS)-induced alveolar macrophages. Motapizone also inhibits human platelet aggregation by increasing intracellular cAMP.
For research use only. We do not sell to patients.
- Purity : 96.25%
- CAS No.: 90697-57-7
- Formula: C12H12N4OS
- Molecular Weight:260.31
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PDE3 |
In Vitro
Motapizone (10 μM; 15 min before oxidants) results 20% inhibition rate for cytokine release in lipopolysaccharide (LPS)-induced alveolar macrophages with oxidative stress conditions, but the inhibitory effect is not affected by oxidative stress[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. 90697-57-7
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Appearance Solid
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Molecular Weight 260.31
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Formula C12H12N4OS
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Color Light yellow to yellow
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SMILES
CC(C1)C(C2=CC(N3C=CN=C3)=CS2)=NNC1=O
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Synonyms
NAT 05-239
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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
In Vitro:
DMSO : 100 mg/mL (384.16 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)
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 (9.60 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.60 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 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
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Data Sheet (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Milara J, et al. Oxidative stress-induced glucocorticoid resistance is prevented by dual PDE3/PDE4 inhibition in human alveolar macrophages. Clin Exp Allergy. 2011 Apr;41(4):535-46. [Content Brief]
[2]. Borbe HO, et al. Inhibition of human platelet aggregation by motapizone via an increase in intracellular cAMP. Agents Actions Suppl. 1986;20:249-57. [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 |
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| DMSO | 1 mM | 3.8416 mL | 19.2079 mL | 38.4157 mL | 96.0393 mL |
| 5 mM | 0.7683 mL | 3.8416 mL | 7.6831 mL | 19.2079 mL | |
| 10 mM | 0.3842 mL | 1.9208 mL | 3.8416 mL | 9.6039 mL | |
| 15 mM | 0.2561 mL | 1.2805 mL | 2.5610 mL | 6.4026 mL | |
| 20 mM | 0.1921 mL | 0.9604 mL | 1.9208 mL | 4.8020 mL | |
| 25 mM | 0.1537 mL | 0.7683 mL | 1.5366 mL | 3.8416 mL | |
| 30 mM | 0.1281 mL | 0.6403 mL | 1.2805 mL | 3.2013 mL | |
| 40 mM | 0.0960 mL | 0.4802 mL | 0.9604 mL | 2.4010 mL | |
| 50 mM | 0.0768 mL | 0.3842 mL | 0.7683 mL | 1.9208 mL | |
| 60 mM | 0.0640 mL | 0.3201 mL | 0.6403 mL | 1.6007 mL | |
| 80 mM | 0.0480 mL | 0.2401 mL | 0.4802 mL | 1.2005 mL | |
| 100 mM | 0.0384 mL | 0.1921 mL | 0.3842 mL | 0.9604 mL |
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