VU 0238429
Based on 1 publication(s) in Google Scholar
VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
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- Purity: 99.56%
- CAS No.: 1160247-92-6
- 화학식: C17H12F3NO4
- 분자량:351.28
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보관: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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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) VU 0238429
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Biological Activity
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mAChR5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>30 μM
Compound: 3
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Agonist activity at rat muscarinic M2 expressed in CHO cells assessed as stimulation of calcium mobilization
Agonist activity at rat muscarinic M2 expressed in CHO cells assessed as stimulation of calcium mobilization
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[PMID: 20004578] |
| CHO | EC50 |
>30 μM
Compound: 3
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Agonist activity at rat muscarinic M4 expressed in CHO cells assessed as stimulation of calcium mobilization
Agonist activity at rat muscarinic M4 expressed in CHO cells assessed as stimulation of calcium mobilization
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[PMID: 20004578] |
| CHO | EC50 |
>30 μM
Compound: 42, (VU0238429)
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Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
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[PMID: 19438238] |
| CHO | EC50 |
>30 μM
Compound: 42, (VU0238429)
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Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
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[PMID: 19438238] |
| CHO | EC50 |
1.1 μM
Compound: 3
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Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
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[PMID: 20004578] |
| CHO | EC50 |
1.16 μM
Compound: 42, (VU0238429)
|
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
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[PMID: 19438238] |
Chemical Information
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CAS No. 1160247-92-6
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Appearance Solid
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분자량 351.28
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화학식 C17H12F3NO4
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Color Light yellow to orange
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SMILES
O=C1N(CC2=CC=C(OC)C=C2)C3=C(C=C(OC(F)(F)F)C=C3)C1=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Oncol
Repositioning VU-0365114 as a novel microtubule-destabilizing agent for treating cancer and overcoming drug resistance. [Abstract]2024 Feb;18(2):386-414. PMID: 37842807
용액&용해도
DMSO : ≥ 150 mg/mL (427.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (7.12 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.
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.
순도&문서
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Data Sheet (272 KB)
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SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 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 | 2.8467 mL | 14.2337 mL | 28.4673 mL | 71.1683 mL |
| 5 mM | 0.5693 mL | 2.8467 mL | 5.6935 mL | 14.2337 mL | |
| 10 mM | 0.2847 mL | 1.4234 mL | 2.8467 mL | 7.1168 mL | |
| 15 mM | 0.1898 mL | 0.9489 mL | 1.8978 mL | 4.7446 mL | |
| 20 mM | 0.1423 mL | 0.7117 mL | 1.4234 mL | 3.5584 mL | |
| 25 mM | 0.1139 mL | 0.5693 mL | 1.1387 mL | 2.8467 mL | |
| 30 mM | 0.0949 mL | 0.4745 mL | 0.9489 mL | 2.3723 mL | |
| 40 mM | 0.0712 mL | 0.3558 mL | 0.7117 mL | 1.7792 mL | |
| 50 mM | 0.0569 mL | 0.2847 mL | 0.5693 mL | 1.4234 mL | |
| 60 mM | 0.0474 mL | 0.2372 mL | 0.4745 mL | 1.1861 mL | |
| 80 mM | 0.0356 mL | 0.1779 mL | 0.3558 mL | 0.8896 mL | |
| 100 mM | 0.0285 mL | 0.1423 mL | 0.2847 mL | 0.7117 mL |
VU 0238429 Related Classifications
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