VU6000918

Name: VU6000918
Brand: TargetMol
SKU: T39543
Rating: 4.5 (1 reviews)

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Catalog No. T39543Cas No. 2101737-32-8

VU6000918 is a positive allosteric modulator that targets the muscarinic acetylcholine receptor subtype M4. It exhibits a half maximal effective concentration (EC50) of 19 nM for the human M4 receptor.

VU6000918

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Catalog No. T39543Cas No. 2101737-32-8

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Product Introduction

Bioactivity

Description	VU6000918 is a positive allosteric modulator that targets the muscarinic acetylcholine receptor subtype M4. It exhibits a half maximal effective concentration (EC50) of 19 nM for the human M4 receptor.
Targets&IC50	M4 (human):19 nM (EC50)
In vitro	VU6000918 significantly reverses AHL by 18% at a minimal oral dosage of 0.03 mg/kg and achieves peak reversal of 74% with a 3 mg/kg dosage, yielding an in vivo plasma EC50 of 74 nM (0.66 nM unbound) according to terminal concentrations observed in study animals 1.5 hours after administering compound 17j[1].

Chemical Properties

Molecular Weight	389.42
Formula	C₁₈H₁₇F₂N₅OS
Cas No.	2101737-32-8
Smiles	Cc1nnc2sc(C(=O)NC3CN(C3)c3cccc(F)c3F)c(N)c2c1C

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc