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

LP-922761 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 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.

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LP-922761 Chemical Structure

LP-922761 Chemical Structure

CAS No. : 1454808-95-7

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Solid + Solvent
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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LP-922761 Related Antibodies

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Description

LP-922761 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 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].

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

410.47

Formula

C21H26N6O3
CAS No.
Appearance

Solid

Color

Off-white to gray

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (101.52 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4362 mL 12.1812 mL 24.3623 mL
5 mM 0.4872 mL 2.4362 mL 4.8725 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4362 mL 12.1812 mL 24.3623 mL 60.9058 mL
5 mM 0.4872 mL 2.4362 mL 4.8725 mL 12.1812 mL
10 mM 0.2436 mL 1.2181 mL 2.4362 mL 6.0906 mL
15 mM 0.1624 mL 0.8121 mL 1.6242 mL 4.0604 mL
20 mM 0.1218 mL 0.6091 mL 1.2181 mL 3.0453 mL
25 mM 0.0974 mL 0.4872 mL 0.9745 mL 2.4362 mL
30 mM 0.0812 mL 0.4060 mL 0.8121 mL 2.0302 mL
40 mM 0.0609 mL 0.3045 mL 0.6091 mL 1.5226 mL
50 mM 0.0487 mL 0.2436 mL 0.4872 mL 1.2181 mL
60 mM 0.0406 mL 0.2030 mL 0.4060 mL 1.0151 mL
80 mM 0.0305 mL 0.1523 mL 0.3045 mL 0.7613 mL
100 mM 0.0244 mL 0.1218 mL 0.2436 mL 0.6091 mL
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LP-922761 Related Classifications

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-9227611454808-95-7LP922761LP 922761AAK1Adaptor-associated Kinase 1AP2-associated kinase 1BIKEperipheralrestrictedpoorlybrain-penetrantInhibitorinhibitorinhibit

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