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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

VU6007477

😃Good
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
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%
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Product Introduction

Bioactivity
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].
SynonymsVU-6007477, VU6007477, VU 6007477
Chemical Properties
Molecular Weight430.5
FormulaC24H26N6O2
Cas No.2220141-46-6
SmilesO=C(NC1CCOCC1)C=2N=C3C(C=CN3C)=C(C2)CC=4C=NC(=CC4)C=5C=NN(C5)C
ColorOrange
AppearanceSolid
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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