1. GPCR/G Protein Neuronal Signaling
  2. mAChR
  3. VU0467154

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.

For research use only. We do not sell to patients.

VU0467154 Chemical Structure

VU0467154 Chemical Structure

CAS No. : 1451993-15-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 133 In-stock
Solution
10 mM * 1 mL in DMSO USD 133 In-stock
Solid
5 mg USD 121 In-stock
10 mg USD 165 In-stock
25 mg USD 319 In-stock
50 mg USD 539 In-stock
100 mg USD 935 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE VU0467154

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

IC50 & Target

pEC50: of 7.75 (Rat M4 receptor), 6.2 (Human M4 receptor), 6 (Cynomolgus monkey M4 receptor)[1]

In Vitro

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.

In Vivo

VU0467154 (1-56.6 mg/kg, p.o. or i.p.) reverses amphetamine-induced hyperlocomotion in rats. VU0467154 (0.3-30 mg/kg, i.p.) reverses amphetamine- and MK-801-induced hyperlocomotion in wild-type but not M4 KO mice. VU0467154 alone also enhances the acquisition of both contextual and cue-mediated fear conditioning in wild-type mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

444.45

Formula

C17H15F3N4O3S2

CAS No.
Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2500 mL 11.2499 mL 22.4997 mL
5 mM 0.4500 mL 2.2500 mL 4.4999 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.56%

References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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, 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
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VU0467154 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
VU0467154
Cat. No.:
HY-112209
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