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LP-935509
- Soluble in DMSO
- MF: C20H24N6O3
- MW: 396.44
Description
LP-935509 is a potent, brain penetrant inhibitor of adapter protein-2 associated kinase 1 (AAK1) with a biochemical IC50 of 3.3 nM and a Ki of 0.9 nM. It displays IC50 values of 14 nM and 320 nM for the closely related BIKE and GAK enzymes, respectively. It shows excellent selectivity (IC50 > 30 μM) against μ- and κ-opioid receptors, as well as α2A- and α2C-adrenergic receptors. In SH-SY5Y cells, it blocks endocytic signaling by reducing AP2M1 phosphorylation. LP-935509 is antinociceptive in multiple rat models of neuropathic pain, but not acute pain.
AAK1 pharmacology is highly relevant to neuropathic pain pathways. As a selective tool compound, LP-935509 supports mechanistic studies of AAK1 and its AP2-dependent clathrin trafficking mechanisms across biochemical, cellular, and disease-model assays.
Key Features
- Orally active, potent and brain penetrant AAK1 inhibitor
- IC50 3.3 nM for AAK1 and 14 nM for the closely related BIKE enzyme
- Modulates AAK1-dependent signaling and biological activity
- Reduces neuropathic pain in rats without affecting acute pain
Applications
- AAK1 pharmacology and target-validation studies
- AAK1 pathway and signaling assays
- Disease-model research related to neuropathic pain
- Compound profiling, assay development and lead-optimization support
More Information
| Parent CAS No. | 1454555-29-3 |
|---|---|
| Chemical Name | isopropyl 4-(3-(2-methoxypyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine-1-carboxylate |
| SMILES | N1(C(OC(C)C)=O)CCN(C2C=CN3N=CC(C4=CC=CN=C4OC)=C3N=2)CC1 |
| MFCD | N.A. |
| InChi | InChI=1S/C20H24N6O3/c1-14(2)29-20(27)25-11-9-24(10-12-25)17-6-8-26-18(23-17)16(13-22-26)15-5-4-7-21-19(15)28-3/h4-8,13-14H,9-12H2,1-3H3 |
| InChiKey | GOOYSJIWTIHOGW-UHFFFAOYSA-N |
| CID | 86697436 |
| Short Description | AAK1 inhibitor |
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