2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. VU 0365114

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.

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VU 0365114 Chemical Structure

VU 0365114 Chemical Structure

CAS No. : 1208222-39-2

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10 mM * 1 mL in DMSO
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 USD 121 In-stock
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10 mM * 1 mL in DMSO USD 121 In-stock
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10 mg USD 154 In-stock
50 mg USD 484 In-stock
100 mg USD 759 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

VU 0365114 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE VU 0365114

View All mAChR Isoform Specific Products:

View All Isoforms
mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].

IC50 & Target

mAChR5

 

Cellular Effect
Cell Line Type Value Description References
CHO EC50
1.6 μM
Compound: 4, VU0365114
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
[PMID: 20801651]
In Vitro

VU 0365114 (10 μM) increases insulin secretion stimulated by ACh in human β-cells[2].
VU 0365114 (10 μM) does not alter somatostatin secretion stimulated by ACh in human β-cells[2].

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

VU 0365114 Related Antibodies
Molecular Weight

397.35

Formula

C22H14F3NO3
CAS No.
Appearance

Solid

Color

Light yellow to orange

SMILES

O=C1N(C2=CC=C(OC(F)(F)F)C=C2C1=O)CC3=CC=C(C4=CC=CC=C4)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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5167 mL 12.5834 mL 25.1667 mL
5 mM 0.5033 mL 2.5167 mL 5.0333 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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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

×
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: ≥ 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.58 mg/mL (6.49 mM); Clear solution; Need warming

    This protocol yields a clear solution of 2.58 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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
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, 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
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VU 0365114 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.

Keywords:

VU 03651141208222-39-2VU0365114VU-0365114mAChRMuscarinic acetylcholine receptorβ-cellsinsulin secretionInhibitorinhibitorinhibit

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