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LP-922761 hydrate 

Cat. No.: HY-120179A
Handling Instructions

LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less 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 hydrate Chemical Structure

LP-922761 hydrate Chemical Structure

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Description

LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less 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].

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

Molecular Weight

414.98

Formula

C₂₁H₂₆N₆O₃.₁/₄H₂O

SMILES

O=C(N(C)CCNC1=NN2C(C=C1)=NC=C2C3=CC=C(C=C3)C(N)=O)OC(C)(C)C.[H]O[H].[1/4]

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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Product Name:
LP-922761 hydrate
Cat. No.:
HY-120179A
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