VU6007678
Based on 1 Customer Validation
VU6007678 is a CNS-penetrant muscarinic acetylcholine receptor (mAChR) modulator. VU6007678 potentiates acetylcholine-mediated signaling at human M1, M3, M5 and rat M1, M3, M4, M5 muscarinic acetylcholine receptors. VU6007678 is applicable to research related to Alzheimer's disease, schizophrenia, and ischemic stroke.
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- Pureza : 96.08%
- No. CAS: 2222737-15-5
- Fòrmula: C25H29FN4O3S
- Peso molecular:484.59
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
In Vitro
VU6007678 (0-30 μM) potently acts as a positive allosteric modulator of human M5 receptors expressed in CHO cells, with an EC50 of 41 nM and a maximum response of 74% of acetylcholine's peak activity[1].
VU6007678 (0-30 μM) acts as a positive allosteric modulator of rat M5 receptors expressed in CHO cells, with an EC50 of 74 nM and a maximum response of 76% of acetylcholine's peak activity[1].
VU6007678 (0-30 μM) acts as a positive allosteric modulator of human M1 receptors expressed in CHO cells, with an EC50 of 1034 nM and a maximum response of 67% of acetylcholine's peak activity[1].
VU6007678 (0-30 μM) acts as a positive allosteric modulator of human M3 receptors expressed in CHO cells, with an EC50 of 466 nM and a maximum response of 71% of acetylcholine's peak activity[1].
VU6007678 (0-30 μM) acts as a positive allosteric modulator of rat M1 receptors expressed in CHO cells, with an EC50 of 904 nM and a maximum response of 69% of acetylcholine's peak activity[1].
VU6007678 (0-30 μM) acts as a positive allosteric modulator of rat M3 receptors expressed in CHO cells, with an EC50 of 772 nM and a maximum response of 51% of acetylcholine's peak activity[1].
VU6007678 (0-30 μM) weakly acts as a positive allosteric modulator of rat M4 receptors expressed in CHO cells, with an EC50 of 3913 nM and a maximum response of 49% of acetylcholine's peak activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
Chemical Information
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No. CAS 2222737-15-5
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Appearance Solid
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Peso molecular 484.59
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Fòrmula C25H29FN4O3S
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Color White to off-white
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SMILES
N(C(=O)C1CCN(S(=O)(=O)C=2C=C3C(=CC2)NN=C3)CC1)(CCC)[C@H]4C=5C(CC4)=C(F)C=CC5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (206.36 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (5.16 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 (sealed storage, away from moisture). 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 | 2.0636 mL | 10.3180 mL | 20.6360 mL | 51.5900 mL |
| 5 mM | 0.4127 mL | 2.0636 mL | 4.1272 mL | 10.3180 mL | |
| 10 mM | 0.2064 mL | 1.0318 mL | 2.0636 mL | 5.1590 mL | |
| 15 mM | 0.1376 mL | 0.6879 mL | 1.3757 mL | 3.4393 mL | |
| 20 mM | 0.1032 mL | 0.5159 mL | 1.0318 mL | 2.5795 mL | |
| 25 mM | 0.0825 mL | 0.4127 mL | 0.8254 mL | 2.0636 mL | |
| 30 mM | 0.0688 mL | 0.3439 mL | 0.6879 mL | 1.7197 mL | |
| 40 mM | 0.0516 mL | 0.2580 mL | 0.5159 mL | 1.2898 mL | |
| 50 mM | 0.0413 mL | 0.2064 mL | 0.4127 mL | 1.0318 mL | |
| 60 mM | 0.0344 mL | 0.1720 mL | 0.3439 mL | 0.8598 mL | |
| 80 mM | 0.0258 mL | 0.1290 mL | 0.2580 mL | 0.6449 mL | |
| 100 mM | 0.0206 mL | 0.1032 mL | 0.2064 mL | 0.5159 mL |
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