VU10010
Based on 1 Customer Validation
VU10010 is a potent, highly selective and allosteric M4 mAChR potentiator with an EC50 of 400 nM. VU10010 binds to an allosteric site on M4 mAChR and increases affinity for acetylcholine and coupling to G proteins. VU10010 increases carbachol-induced depression of transmission at excitatory but not inhibitory synapses in the hippocampus.
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- Pureté : 98.04%
- CAS No.: 633283-39-3
- Formule: C17H16ClN3OS
- Masse moléculaire:345.85
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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mAChR4 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
400 nM
Compound: 20j, VU10010
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Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
Allosteric activation of rat recombinant muscarinic M4 receptor expressed in CHO cells assessed as potentiation of 10 uM acetylcholine-induced calcium mobilization after 1 hr by fluorescence assay
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[PMID: 18059262] |
In Vitro
VU10010 potentiates the M4 response to acetylcholine 47-fold while having no activity at other mAChR subtypes (rM1, rM2, rM3 or rM5). VU10010 causes an increase in affinity for ACh and M4-mediated [35S]GTPγS binding[1].
VU10010 (10 μM) has no agonist, antagonist or allosteric potentiator activity at P2Y1R or mGluR5[1].
The EC50 values are 33 and 0.7 nM for ACh in the absence and presence of VU10010, respectively[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. 633283-39-3
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Appearance Solid
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Masse moléculaire 345.85
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Formule C17H16ClN3OS
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Color White to off-white
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SMILES
O=C(C1=C(N)C2=C(C)C=C(C)N=C2S1)NCC3=CC=C(Cl)C=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 125 mg/mL (361.43 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: ≥ 2.08 mg/mL (6.01 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.
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.
Pureté et documentation
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Fiche technique (273 KB)
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SDS (416 KB)
- English - EN (416 KB)
- Français - FR (416 KB)
- Deutsch - DE (416 KB)
- Norwegian - NO (416 KB)
- Español - ES (416 KB)
- Swedish - SV (416 KB)
- Italian - IT (416 KB)
- Korean - KR (416 KB)
- Portuguese - PT (416 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.8914 mL | 14.4571 mL | 28.9143 mL | 72.2857 mL |
| 5 mM | 0.5783 mL | 2.8914 mL | 5.7829 mL | 14.4571 mL | |
| 10 mM | 0.2891 mL | 1.4457 mL | 2.8914 mL | 7.2286 mL | |
| 15 mM | 0.1928 mL | 0.9638 mL | 1.9276 mL | 4.8190 mL | |
| 20 mM | 0.1446 mL | 0.7229 mL | 1.4457 mL | 3.6143 mL | |
| 25 mM | 0.1157 mL | 0.5783 mL | 1.1566 mL | 2.8914 mL | |
| 30 mM | 0.0964 mL | 0.4819 mL | 0.9638 mL | 2.4095 mL | |
| 40 mM | 0.0723 mL | 0.3614 mL | 0.7229 mL | 1.8071 mL | |
| 50 mM | 0.0578 mL | 0.2891 mL | 0.5783 mL | 1.4457 mL | |
| 60 mM | 0.0482 mL | 0.2410 mL | 0.4819 mL | 1.2048 mL | |
| 80 mM | 0.0361 mL | 0.1807 mL | 0.3614 mL | 0.9036 mL | |
| 100 mM | 0.0289 mL | 0.1446 mL | 0.2891 mL | 0.7229 mL |
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