2. Neuronal Signaling
  3. AAK1
  4. LP-922761 hydrate

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.

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LP-922761 hydrate Chemical Structure

LP-922761 hydrate Chemical Structure

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LP-922761 hydrate Related Antibodies

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

414.98

Formula

C21H26N6O3.1/4H2O
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: ≥98.0%

COA (250 KB)

Handling Instructions (2659 KB)
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LP-922761 hydrate Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LP-922761LP922761LP 922761AAK1Adaptor-associated Kinase 1AP2-associated kinase 1BIKEperipheralrestrictedpoorlybrain-penetrantInhibitorinhibitorinhibit

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LP-922761 hydrate
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