VU0453595
Based on 2 publication(s) in Google Scholar
VU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140 nM) for the research of schizophrenia.
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- Pureza: 99.44%
- No. CAS: 1432436-13-9
- Fòrmula: C18H15FN4O
- Peso molecular:322.34
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) VU0453595
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Actividad biológica
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mAChR1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
1.9 μM
Compound: 5; VU0453595
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Positive allosteric modulation at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
Positive allosteric modulation at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
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[PMID: 27173801] |
| CHO | EC50 |
3.2 μM
Compound: 5; VU0453595
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Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
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[PMID: 27173801] |
Application of M1 PAM VU0453595 (3 μM) induces a transient increase in excitability of medium spiny neurons (MSNs)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
VU0453595 (1-10 mg/kg; i.p.) reverses behavioral deficits induced by repeated phencyclidine (PCP) administration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL6/J mice (8-9 weeks old)[1]
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Dosage:1, 3, or 10 mg/kg
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Administration:Intraperitoneal (i.p.); 10 mL/kg; administered 30 min before the social interaction test
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Result:Rescued deficits in social interaction observed in PCP-treated mice.
Chemical Information
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No. CAS 1432436-13-9
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Appearance Solid
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Peso molecular 322.34
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Fòrmula C18H15FN4O
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Color Off-white to light yellow
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SMILES
O=C1N(CC2=CC=C(C3=CN(C)N=C3)C=C2F)CC4=NC=CC=C41
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Neuropharmacology
Nicotine and a positive allosteric modulator of m1 muscarinic receptor increase NMDA/AMPA ratio in the hippocampus and medial prefrontal cortex. [Abstract]2024 Nov 8:262:110213. PMID: 39522675 -
Brain Res
Sex differences in interactions between the muscarinic-1 and orexin-1 receptors on cognitive flexibility in rats. [Abstract]2025 Nov 27:1872:150081. PMID: 41317779
Solvente y solubilidad
DMSO : 100 mg/mL (310.23 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)
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 (7.76 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.76 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 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.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. A Ghoshal, et al. Potentiation of M1 Muscarinic Receptor Reverses Plasticity Deficits and Negative and Cognitive Symptoms in a Schizophrenia Mouse Model. Neuropsychopharmacology. 2016 Jan;41(2):598-610. [Content Brief]
[2]. Sean P Moran, et al. M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition. Neuropsychopharmacology. 2018 Jul;43(8):1763-1771. [Content Brief]
[3]. Xiaohui Lv, et al. M1 muscarinic activation induces long-lasting increase in intrinsic excitability of striatal projection neurons. Neuropharmacology. 2017 May 15;118:209-222. [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 | 3.1023 mL | 15.5116 mL | 31.0231 mL | 77.5579 mL |
| 5 mM | 0.6205 mL | 3.1023 mL | 6.2046 mL | 15.5116 mL | |
| 10 mM | 0.3102 mL | 1.5512 mL | 3.1023 mL | 7.7558 mL | |
| 15 mM | 0.2068 mL | 1.0341 mL | 2.0682 mL | 5.1705 mL | |
| 20 mM | 0.1551 mL | 0.7756 mL | 1.5512 mL | 3.8779 mL | |
| 25 mM | 0.1241 mL | 0.6205 mL | 1.2409 mL | 3.1023 mL | |
| 30 mM | 0.1034 mL | 0.5171 mL | 1.0341 mL | 2.5853 mL | |
| 40 mM | 0.0776 mL | 0.3878 mL | 0.7756 mL | 1.9389 mL | |
| 50 mM | 0.0620 mL | 0.3102 mL | 0.6205 mL | 1.5512 mL | |
| 60 mM | 0.0517 mL | 0.2585 mL | 0.5171 mL | 1.2926 mL | |
| 80 mM | 0.0388 mL | 0.1939 mL | 0.3878 mL | 0.9695 mL | |
| 100 mM | 0.0310 mL | 0.1551 mL | 0.3102 mL | 0.7756 mL |
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