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VU6007477
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Catalog No. T69780Cas No. 2220141-46-6
Alias VU-6007477, VU6007477, VU 6007477
VU6007477 is a brain-penetrant and selective M1 muscarinic receptor positive allosteric modulator (PAM) with an EC50 value of 230 nM, characterized by improved central nervous system penetration compared with hydroxylated congeners, moderate permeability as a human P-glycoprotein substrate, a pyranyl amide chemical scaffold, and strong suitability for experimental investigations into robust cholinergic seizure activity, central cholinergic signaling, and neurological disease models requiring reliable CNS exposure.
VU6007477
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Purity: 99.67%
Catalog No. T69780Alias VU-6007477, VU6007477, VU 6007477Cas No. 2220141-46-6
VU6007477 is a brain-penetrant and selective M1 muscarinic receptor positive allosteric modulator (PAM) with an EC50 value of 230 nM, characterized by improved central nervous system penetration compared with hydroxylated congeners, moderate permeability as a human P-glycoprotein substrate, a pyranyl amide chemical scaffold, and strong suitability for experimental investigations into robust cholinergic seizure activity, central cholinergic signaling, and neurological disease models requiring reliable CNS exposure.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $457 | - | In Stock | |
| 5 mg | $1,060 | - | In Stock | |
| 10 mg | $1,420 | - | In Stock | |
| 25 mg | $2,120 | - | In Stock | |
| 50 mg | $2,780 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.67%
Appearance:Solid
Color:Orange
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Product Introduction
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Chemical Properties
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| Description | VU6007477 is a brain-penetrant and selective M1 muscarinic receptor positive allosteric modulator (PAM) with an EC50 value of 230 nM, characterized by improved central nervous system penetration compared with hydroxylated congeners, moderate permeability as a human P-glycoprotein substrate, a pyranyl amide chemical scaffold, and strong suitability for experimental investigations into robust cholinergic seizure activity, central cholinergic signaling, and neurological disease models requiring reliable CNS exposure. |
| Targets&IC50 | PAM:230 nM |
| In vitro | Method: A series of M1 positive allosteric modulators based on a pyrrolo[2,3-b]pyridine core were generated via scaffold hopping and iterative parallel synthesis and evaluated in rat M1 receptor assays and in vivo CNS exposure and adverse event studies. Result: Removal of a secondary hydroxyl group yielded VU6007477, which showed good rat M1 PAM potency (EC50 = 230 nM, 93% ACh max), minimal agonist activity (agonist EC50 > 10 μM), good CNS penetration in rats and mice, and no cholinergic seizure liability[1]. |
| Synonyms | VU-6007477, VU6007477, VU 6007477 |
| Molecular Weight | 430.5 |
| Formula | C24H26N6O2 |
| Cas No. | 2220141-46-6 |
| Smiles | O=C(NC1CCOCC1)C=2N=C3C(C=CN3C)=C(C2)CC=4C=NC(=CC4)C=5C=NN(C5)C |
| 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, and a total of 10 animals are to be administered, using a formulation of 
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 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 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 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.
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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
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