VU 0365114
Based on 1 publication(s) in Google Scholar
VU 0365114 is a selective mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM, and >30 μM for M1, M2, M3 and M4 receptors. VU 0365114 increases insulin secretion stimulated by ACh in human β-cells.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.34%
- CAS. Nr.: 1208222-39-2
- Formel: C22H14F3NO3
- Molecular Weight:397.35
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) VU 0365114
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Biologische Aktivität
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mAChR5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>30 μM
Compound: 6a
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Agonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilization
Agonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilization
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[PMID: 20004578] |
| CHO | EC50 |
1.6 μM
Compound: 4, VU0365114
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Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
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[PMID: 20801651] |
| CHO | EC50 |
2.7 μM
Compound: 6a
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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] |
Chemical Information
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CAS. Nr. 1208222-39-2
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Appearance Solid
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Molecular Weight 397.35
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Formel C22H14F3NO3
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Color Light yellow to orange
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SMILES
O=C1N(C2=CC=C(OC(F)(F)F)C=C2C1=O)CC3=CC=C(C4=CC=CC=C4)C=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
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
Lösungsmittel & Löslichkeit
DMSO : ≥ 77.5 mg/mL (195.04 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.58 mg/mL (6.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.58 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.8 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.
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.
Reinheit & Dokumentation
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Data Sheet (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Bridges TM, et al. Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5617-22. [Content Brief]
[2]. Molina J, et al. Control of insulin secretion by cholinergic signaling in the human pancreatic islet. Diabetes. 2014 Aug;63(8):2714-26. [Content Brief]
[3]. Bridges TM, et al. Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. Bioorg Med Chem Lett. 2010 Jan 15;20(2):558-62. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5167 mL | 12.5834 mL | 25.1667 mL | 62.9168 mL |
| 5 mM | 0.5033 mL | 2.5167 mL | 5.0333 mL | 12.5834 mL | |
| 10 mM | 0.2517 mL | 1.2583 mL | 2.5167 mL | 6.2917 mL | |
| 15 mM | 0.1678 mL | 0.8389 mL | 1.6778 mL | 4.1945 mL | |
| 20 mM | 0.1258 mL | 0.6292 mL | 1.2583 mL | 3.1458 mL | |
| 25 mM | 0.1007 mL | 0.5033 mL | 1.0067 mL | 2.5167 mL | |
| 30 mM | 0.0839 mL | 0.4194 mL | 0.8389 mL | 2.0972 mL | |
| 40 mM | 0.0629 mL | 0.3146 mL | 0.6292 mL | 1.5729 mL | |
| 50 mM | 0.0503 mL | 0.2517 mL | 0.5033 mL | 1.2583 mL | |
| 60 mM | 0.0419 mL | 0.2097 mL | 0.4194 mL | 1.0486 mL | |
| 80 mM | 0.0315 mL | 0.1573 mL | 0.3146 mL | 0.7865 mL | |
| 100 mM | 0.0252 mL | 0.1258 mL | 0.2517 mL | 0.6292 mL |
VU 0365114 Related Classifications
HY-107651 Related Classifications
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