ASP8302
Based on 1 Customer Validation
ASP8302 is a positive and allosteric muscarinic M3 receptor modulator. ASP8302 improves voiding efficiency and reduced residual urine volume in two voiding dysfunction models. ASP8302 can be used for research of underactive bladder.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.95%
- No. CAS: 1839583-42-4
- Fòrmula: C26H32ClN7O3S2
- Peso molecular:590.16
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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mAChR3 |
ASP8302 (1-3 mg/kg; i.v.) reduces residual urine volume and improves voiding efficiency in female Wistar rats with voiding dysfunction induced by bladder outlet obstruction[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1839583-42-4
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Appearance Solid
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Peso molecular 590.16
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Fòrmula C26H32ClN7O3S2
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Color White to yellow
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SMILES
O=C(C1=NC=C(N2C[C@@H](N(CC2)CCC(O)=O)C)N=C1)NC(S3)=NC(C4=CC(Cl)=CS4)=C3CN5[C@@H](CCC5)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (169.45 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.
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: ≥ 2.5 mg/mL (4.24 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 (4.24 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.
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.
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Okimoto R, et al. Potentiation of Muscarinic M3 Receptor Activation through a New Allosteric Site with a Novel Positive Allosteric Modulator ASP8302. J Pharmacol Exp Ther. 2021 Oct;379(1):64-73. [Content Brief]
[2]. Okimoto R, et al. Muscarinic M3 positive allosteric modulator ASP8302 enhances bladder contraction and improves voiding dysfunction in rats. Low Urin Tract Symptoms. 2022 Jul;14(4):289-300. [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 | 1.6945 mL | 8.4723 mL | 16.9446 mL | 42.3614 mL |
| 5 mM | 0.3389 mL | 1.6945 mL | 3.3889 mL | 8.4723 mL | |
| 10 mM | 0.1694 mL | 0.8472 mL | 1.6945 mL | 4.2361 mL | |
| 15 mM | 0.1130 mL | 0.5648 mL | 1.1296 mL | 2.8241 mL | |
| 20 mM | 0.0847 mL | 0.4236 mL | 0.8472 mL | 2.1181 mL | |
| 25 mM | 0.0678 mL | 0.3389 mL | 0.6778 mL | 1.6945 mL | |
| 30 mM | 0.0565 mL | 0.2824 mL | 0.5648 mL | 1.4120 mL | |
| 40 mM | 0.0424 mL | 0.2118 mL | 0.4236 mL | 1.0590 mL | |
| 50 mM | 0.0339 mL | 0.1694 mL | 0.3389 mL | 0.8472 mL | |
| 60 mM | 0.0282 mL | 0.1412 mL | 0.2824 mL | 0.7060 mL | |
| 80 mM | 0.0212 mL | 0.1059 mL | 0.2118 mL | 0.5295 mL | |
| 100 mM | 0.0169 mL | 0.0847 mL | 0.1694 mL | 0.4236 mL |
ASP8302 Related Classifications
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