VU0467319
Based on 1 Customer Validation
VU0467319 (Compound VU319) is a highly selective and blood-brain-permeable, orally active M1 positive allosteric modulator (PAM) (EC50: 492 nM). VU0467319 is selective (EC50 > 30 μM) versus M2-5 for both human and rat. VU0467319 improves cognitive impairment in Alzheimer's disease (AD) through central M1 muscarinic receptors. VU0467319 does not induce cholinergic adverse reactions and has potential in AD research.
For research use only. We do not sell to patients.
- Purity: 98.53%
- CAS No.: 1432438-14-6
- Formula: C22H16F2N4O
- Molecular Weight:390.39
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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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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mAChR1 492 nM (EC50) |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1432438-14-6
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Appearance Solid
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Molecular Weight 390.39
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Formula C22H16F2N4O
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Color White to off-white
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SMILES
O=C1N(CC2=C(F)C=C(C3=CC=CC4=NN(C)C=C43)C=C2F)CC5=NC=CC=C51
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Synonyms
VU319
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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
DMSO : 50 mg/mL (128.08 mM; ultrasonic and warming and heat to 60°C; 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (12.81 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Purity & Documentation
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Data Sheet (275 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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 | 2.5615 mL | 12.8077 mL | 25.6154 mL | 64.0385 mL |
| 5 mM | 0.5123 mL | 2.5615 mL | 5.1231 mL | 12.8077 mL | |
| 10 mM | 0.2562 mL | 1.2808 mL | 2.5615 mL | 6.4039 mL | |
| 15 mM | 0.1708 mL | 0.8538 mL | 1.7077 mL | 4.2692 mL | |
| 20 mM | 0.1281 mL | 0.6404 mL | 1.2808 mL | 3.2019 mL | |
| 25 mM | 0.1025 mL | 0.5123 mL | 1.0246 mL | 2.5615 mL | |
| 30 mM | 0.0854 mL | 0.4269 mL | 0.8538 mL | 2.1346 mL | |
| 40 mM | 0.0640 mL | 0.3202 mL | 0.6404 mL | 1.6010 mL | |
| 50 mM | 0.0512 mL | 0.2562 mL | 0.5123 mL | 1.2808 mL | |
| 60 mM | 0.0427 mL | 0.2135 mL | 0.4269 mL | 1.0673 mL | |
| 80 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8005 mL | |
| 100 mM | 0.0256 mL | 0.1281 mL | 0.2562 mL | 0.6404 mL |
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