VU0467154
Based on 5 publication(s) in Google Scholar
VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.23%
- No. CAS: 1451993-15-9
- Fòrmula: C17H15F3N4O3S2
- Peso molecular:444.45
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
GPCR/G Protein Compound Library
HY-L006
-
Neuronal Signaling Compound Library
HY-L013
-
Neurotransmitter Receptor Compound Library
HY-L062
-
Targeted Diversity Library
HY-L099
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Allosteric Modulators (AMs) Compound Library
HY-L170
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Lactylation Compound Library
HY-L249
Publications Citing Use of MedChemExpress (MCE) VU0467154
More
Actividad biológica
|
mAChR4 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
17.8 nM
Compound: 5
|
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
|
[PMID: 27939174] |
| CHO | EC50 |
631 nM
Compound: 5
|
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay
|
[PMID: 27939174] |
| CHO-K1 | EC50 |
>30 μM
Compound: 5
|
Displacement of [3H]-N-Methylscopolamine from human M1 receptor expressed in CHOK1 cells
Displacement of [3H]-N-Methylscopolamine from human M1 receptor expressed in CHOK1 cells
|
[PMID: 27939174] |
| CHO-K1 | EC50 |
>30 μM
Compound: 5
|
Displacement of [3H]-N-Methylscopolamine from human M2 receptor expressed in CHOK1 cells
Displacement of [3H]-N-Methylscopolamine from human M2 receptor expressed in CHOK1 cells
|
[PMID: 27939174] |
| CHO-K1 | EC50 |
>30 μM
Compound: 5
|
Displacement of [3H]-N-Methylscopolamine from human M3 receptor expressed in CHOK1 cells
Displacement of [3H]-N-Methylscopolamine from human M3 receptor expressed in CHOK1 cells
|
[PMID: 27939174] |
VU0467154 is a positive allosteric modulators of the M4 muscarinic acetylcholine receptor (mAChR), robustly potentiates the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey (cyno) M4 receptor, respectively. VU0467154 does not potentiate the ACh response at rat and human M1, M2, M3, or M5[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
No. CAS 1451993-15-9
-
Appearance Solid
-
Peso molecular 444.45
-
Fòrmula C17H15F3N4O3S2
-
Color Light yellow to yellow
-
SMILES
O=C(C1=C(N)C2=C(C)C(C)=NN=C2S1)NCC3=CC=C(S(=O)(C(F)(F)F)=O)C=C3
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
-
Journal Impact Factor
-
Most Recent
-
Nature
2025 Oct;646(8083):180-189. PMID: 40836099 -
Nat Commun
Epigenetic regulation of cocaine intake through dopaminergic control of cholinergic interneurons in male mice. [Abstract]2025 Dec 9;16(1):10964. PMID: 41365875 -
Hepatology
Parallel regulation of goblet cell-associated antigen passages by reduced microbial sensing and mAChR4 signaling in Muc2 deficiency prevents ethanol-induced liver injury. [Abstract]2026 Mar 27. PMID: 41894257 -
iScience
2022 Oct 4;25(10):105263. PMID: 36274959 -
bioRxiv
Afferent-specific modulation of excitatory synaptic transmission by acetylcholine and serotonin in the prelimbic cortex. [Abstract]2025 May 5:2025.05.04.652144. PMID: 40488131
Solvente y solubilidad
DMSO : 13.89 mg/mL (31.25 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, 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: 1.39 mg/mL (3.13 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.39 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.9 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Protocolo
Rats[1]
To determine the relationship between in vivo efficacy of VU0467154 and brain concentrations in rats, the efficacy of VU0467154 (1, 3, 10, 30, and 56.6 mg/kg, PO; n ≥ 8 per dose level) in reversing amphetamine-induced hyperlocomotion is correlated to the brain concentrations of VU0467154 in the same animals upon study completion (1.5 h postadministration). In mice, the in vivo concentration-effect relationship for VU0467154 is determined by correlating the efficacy of VU0467154 in reversing amphetamine-induced hyperlocomotion (0.3, 1, 3, 10, and 30 mg/kg, IP) to the brain concentrations of VU0467154 in the same animals upon study completion (2.5 h postadministration). Terminal unbound brain concentrations for all treatment groups are plotted versus each animal’s efficacy in reversing amphetamine-induced hyperlocomotion. Nonlinear regression analysis of the plotted data are calculated to determine the in vivo EC50 value (nM) for VU0467154 in reversing amphetamine-induced hyperlocomotion in rats using GraphPad Prism 5.0[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
-
Ficha de datos (277 KB)
-
SDS (643 KB)
- English - EN (643 KB)
- Français - FR (643 KB)
- Deutsch - DE (643 KB)
- Norwegian - NO (643 KB)
- Español - ES (643 KB)
- Swedish - SV (643 KB)
- Italian - IT (643 KB)
- Korean - KR (643 KB)
- Portuguese - PT (643 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
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 | 2.2500 mL | 11.2499 mL | 22.4997 mL | 56.2493 mL |
| 5 mM | 0.4500 mL | 2.2500 mL | 4.4999 mL | 11.2499 mL | |
| 10 mM | 0.2250 mL | 1.1250 mL | 2.2500 mL | 5.6249 mL | |
| 15 mM | 0.1500 mL | 0.7500 mL | 1.5000 mL | 3.7500 mL | |
| 20 mM | 0.1125 mL | 0.5625 mL | 1.1250 mL | 2.8125 mL | |
| 25 mM | 0.0900 mL | 0.4500 mL | 0.9000 mL | 2.2500 mL | |
| 30 mM | 0.0750 mL | 0.3750 mL | 0.7500 mL | 1.8750 mL |
VU0467154 Related Classifications
HY-112209 Related Classifications
Powered by Bioz