ChemicalBook > CAS DataBase List > LP-935509

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
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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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Axon Medchem
Product number
Axon2638
Product name
LP-935509
Purity
99%
Packaging
50mg
Price
$495
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
KIN0002499
Product name
LP-935509
Purity
95.00%
Packaging
5MG
Price
$503.18
Updated
2021/12/16
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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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LP-935509 Suppliers

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1454555-29-3, LP-935509Related Search:


  • LP-935509
  • 4-[3-(2-methoxy-pyridin-3-yl)-pyrazolo[1,5-a]pyrimidin-5-yl]-piperazine-1-carboxylicacid isopropyl 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
  • 1-Piperazinecarboxylic acid, 4-[3-(2-methoxy-3-pyridinyl)pyrazolo[1,5-a]pyrimidin-5-yl]-, 1-methylethyl ester
  • Isopropyl 4-(3-(2-methoxypyridin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)piperazine-1-carboxylate
  • LP-935509, 10 mM in DMSO
  • LP-935509 (LP935509
  • 1454555-29-3