LP-935509
- Product Name
- LP-935509
- CAS No.
- 1454555-29-3
- Chemical Name
- LP-935509
- Synonyms
- LP-935509;LP-935509 (LP935509;LP-935509, 10 mM in DMSO;Isopropyl 4-(3-(2-methoxypyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine-1-carboxylate;4-[3-(2-methoxy-pyridin-3-yl)-pyrazolo[1,5-a]pyrimidin-5-yl]-piperazine-1-carboxylicacid isopropyl ester;1-Piperazinecarboxylic acid, 4-[3-(2-methoxy-3-pyridinyl)pyrazolo[1,5-a]pyrimidin-5-yl]-, 1-methylethyl ester;orally active,AP2-associated kinase 1,LP 935509,Inhibitor,brain-penetrant,SARS coronavirus,LP-935509,pain,spinal nerve ligation,SARS-CoV,Cyclin G-associated Kinase (GAK),Antinociceptive,AAK1,infection,LP935509,chronic constriction injury,inhibit,streptozotocin,formalin,Auxilin 2,ATP-competitive,SNL,Adaptor-associated Kinase 1
- CBNumber
- CB73159379
- Molecular Formula
- C20H24N6O3
- Formula Weight
- 396.44
- MOL File
- 1454555-29-3.mol
LP-935509 Property
- Density
- 1.34±0.1 g/cm3(Predicted)
- solubility
- DMSO: Soluble
- pka
- 1.73±0.12(Predicted)
- form
- Solid
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- Axon2638
- Product name
- LP-935509
- Purity
- 99%
- Packaging
- 50mg
- Price
- $495
- Updated
- 2021/12/16
- Product number
- KIN0002499
- Product name
- LP-935509
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $503.18
- Updated
- 2021/12/16
LP-935509 Chemical Properties,Usage,Production
Description
LP-935509 is a potent inhibitor of the Adapter protein-2 Associated Kinase 1 (AAK1).
Uses
LP-935509 is an orally active, potent, selective, ATP-competitive and brain-penetrant inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research[1].
in vivo
LP-935509 (0-60 mg/kg; PO, single) causes a robust reduction in pain behavior[1].
?
LP-935509 (0.1-30 mg/kg; PO, single dosage) causes a dose-dependent reversal of thermal hyperalgesia in CCI model[1].
?
LP-935509 (IV (1 mg/kg) or orally (10 mg/kg); once) has 100% oral bioavailability and a plasma half life of 3.6 hours[1].
| Animal Model: | Male C57BL/6J mice (with SNL(spinal nerve ligation) injury, n=8-10 male mice per group)[1] |
| Dosage: | 0, 10, 30 and 60 mg/kg (10 ml/kg) |
| Administration: | PO, single |
| Result: | Caused a dose-dependent reduction in phase II paw flinches that was significantly lower than the vehicle-treated animals; exhibited a dose-dependent reversal of the mechanical allodynia; Caused a robust reduction in pain behavior. |
| Animal Model: | Male Sprague-Dawley rats (CCI (chronic constriction injury)-operated rats)[1] |
| Dosage: | 0, 0.1, 0.3, 1, 3, 10, or 30 mg/kg |
| Administration: | PO, two daily, for 5 days |
| Result: | Caused a dose-dependent reversal of thermal hyperalgesia, cold allodynia, mechanical allodynia, and mechanical hyperalgesia in CCI animals. Reversed the behavioral deficits, with ED50 values ranging from 2 mg/kg to 10 mg/kg. |
| Animal Model: | Male Sprague-Dawley rats[1] |
| Dosage: | 1 mg/kg (IV), 10 mg/kg (PO) |
| Administration: | IV, PO; once (Pharmacokinetic Analysis) |
| Result: | Had 100% oral bioavailability and a plasma half life of 3.6 hours; The Cmax for the 10 mg/kg oral dose was 5.2 μM at 0.5-hour postdose; had a plasma-free fraction of 2.6% in mice. Brain drug levels exceeded plasma drug levels with a brain/plasma drug ratio typically between 3 and 4, showing that LP-935509 was highly brain-penetrant. |
References
[1] Kostich W, et al. Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain. J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. DOI:10.1124/jpet.116.235333
[2] Mushtaq, et al. Role Of Endocytic Machinery Regulators in EGFR Traffic and Viral Entry (2021). Theses & Dissertations. 532.
[3] QINFANG LIU. Dysregulation of the AP2M1 phosphorylation cycle by LRRK2 impairs endocytosis and leads to dopaminergic neurodegeneration[J]. Science Signaling, 2021, 14 693. DOI: 10.1126/scisignal.abg3555
LP-935509 Preparation Products And Raw materials
Raw materials
Preparation Products
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