产品
编 号：F167946
分子式：C20H24N6O3
分子量：396.44
分子式：C20H24N6O3
分子量：396.44
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1454555-29-3
产品详情
生物活性：
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.
体内研究：
LP-935509 (0-60 mg/kg; PO, single) causes a robust reduction in pain behavior.?LP-935509 (0.1-30 mg/kg; PO, single dosage) causes a dose-dependent reversal of thermal hyperalgesia in CCI model.?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.Animal Model:Male C57BL/6J mice (with SNL(spinal nerve ligation) injury, n=8-10 male mice per group)
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)
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
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.
体外研究：
LP-935509 inhibits μ2 phosphorylation with an IC50 value of 2.8 ± 0.4 nM, inhibits phosphorylation of a peptide derived from the μ2 protein with an IC50 value of 3.3 ± 0.7 nM.?LP-935509 exhibits a dose-dependent inhibition of the SARS-CoV-2 S-RBD internalization into host cells.
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.
体内研究：
LP-935509 (0-60 mg/kg; PO, single) causes a robust reduction in pain behavior.?LP-935509 (0.1-30 mg/kg; PO, single dosage) causes a dose-dependent reversal of thermal hyperalgesia in CCI model.?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.Animal Model:Male C57BL/6J mice (with SNL(spinal nerve ligation) injury, n=8-10 male mice per group)
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)
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
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.
体外研究：
LP-935509 inhibits μ2 phosphorylation with an IC50 value of 2.8 ± 0.4 nM, inhibits phosphorylation of a peptide derived from the μ2 protein with an IC50 value of 3.3 ± 0.7 nM.?LP-935509 exhibits a dose-dependent inhibition of the SARS-CoV-2 S-RBD internalization into host cells.
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