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LP-922761 

Cat. No.: HY-120179
Handling Instructions

LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with an in vitro IC50 of 4.8 nM and a cellular IC50 of 7.6 nM. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors.

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

LP-922761 Chemical Structure

LP-922761 Chemical Structure

CAS No. : 1454808-95-7

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Description

LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with an in vitro IC50 of 4.8 nM and a cellular IC50 of 7.6 nM. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors[1].

IC50 & Target

IC50: 4.8 nM (Adapter protein-2 associated kinase 1 (AAK1) in enzyme assays); 7.6 nM (AAK1 in cell assays); 24 nM (BMP-2-inducible protein kinase (BIKE))[1]

In Vivo

In mouse, LP-922761 has a brain to plasma ratio of 0.007, indicating that LP-922761 is essentially restricted to the peripheral compartment[1].

Molecular Weight

410.47

Formula

C₂₁H₂₆N₆O₃

CAS No.

1454808-95-7

SMILES

O=C(N(C)CCNC1=NN2C(C=C1)=NC=C2C3=CC=C(C=C3)C(N)=O)OC(C)(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

LP-922761LP922761LP 922761OthersAAK1BIKEperipheralrestrictedpoorlybrain-penetrantInhibitorinhibitorinhibit

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