VU0152100
Based on 1 publication(s) in Google Scholar
VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia.
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- Pureté: 98.98%
- CAS No.: 409351-28-6
- Formule: C18H19N3O2S
- Masse moléculaire:341.43
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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Publications Citing Use of MedChemExpress (MCE) VU0152100
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Activité biologique
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mAChR4 |
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Cell Line
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Type | Value | Description | References |
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| CHO-K1 | EC50 |
620 nM
Compound: ML108
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Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
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[PMID: 23177787] |
VU0152100 (10, 30, 56.6 mg/kg; i.p.; single) blocks amphetamine-induced disruption of the acquisition of contextual fear conditioning and prepulse inhibition of the acoustic startle reflex in rats[1].
VU0152100 reverses amphetamine-induced increases in extracellular dopamine levels in nucleus accumbens and caudate-putamen[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Sprague-Dawley rats (250-275 g; amphetamine-induced hyperlocomotion model)[1].
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Dosage:10, 30, 56.6 mg/kg
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Administration:Intraperitoneal injection; single (pre-treatment)
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Result:Produced a robust dose-dependent reversal of amphetamine-induced hyperlocomotion.
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Animal Model:Adult male Sprague-Dawley rats (250-275 g; amphetamine-induced)[1].
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Dosage:10, 30, 56.6 mg/kg
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Administration:Intraperitoneal injection; single (pre-treatment)
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Result:Blocked amphetamine-induced disruption of prepulse inhibition.
Dose-dependently reversed the disruptive effects of amphetamine on the acquisition of a context-dependent fear.
Chemical Information
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CAS No. 409351-28-6
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Appearance Solid
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Masse moléculaire 341.43
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Formule C18H19N3O2S
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Color Light yellow to khaki
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SMILES
CC1=C2C(SC(C(NCC3=CC=C(OC)C=C3)=O)=C2N)=NC(C)=C1
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Synonyms
VU152100
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
DMSO : ≥ 50 mg/mL (146.44 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (7.32 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 (7.32 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.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Byun NE, et al. Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100. Neuropsychopharmacology. 2014 Jun;39(7):1578-93. [Content Brief]
[2]. Brady AE, et al. Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. J Pharmacol Exp Ther. 2008 Dec;327(3):941-53. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9289 mL | 14.6443 mL | 29.2886 mL | 73.2215 mL |
| 5 mM | 0.5858 mL | 2.9289 mL | 5.8577 mL | 14.6443 mL | |
| 10 mM | 0.2929 mL | 1.4644 mL | 2.9289 mL | 7.3221 mL | |
| 15 mM | 0.1953 mL | 0.9763 mL | 1.9526 mL | 4.8814 mL | |
| 20 mM | 0.1464 mL | 0.7322 mL | 1.4644 mL | 3.6611 mL | |
| 25 mM | 0.1172 mL | 0.5858 mL | 1.1715 mL | 2.9289 mL | |
| 30 mM | 0.0976 mL | 0.4881 mL | 0.9763 mL | 2.4407 mL | |
| 40 mM | 0.0732 mL | 0.3661 mL | 0.7322 mL | 1.8305 mL | |
| 50 mM | 0.0586 mL | 0.2929 mL | 0.5858 mL | 1.4644 mL | |
| 60 mM | 0.0488 mL | 0.2441 mL | 0.4881 mL | 1.2204 mL | |
| 80 mM | 0.0366 mL | 0.1831 mL | 0.3661 mL | 0.9153 mL | |
| 100 mM | 0.0293 mL | 0.1464 mL | 0.2929 mL | 0.7322 mL |
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