LP-935509|1454555-29-3|-陌孚医药/Medlife

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LP-935509

目录号: PL02347 纯度: ≥99%

CAS No. :1454555-29-3

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中文名称	LP-935509
中文别名	化合物LP-935509
英文名称	LP-935509
英文别名	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
Cas No.	1454555-29-3
分子式	C₂₀H₂₄N₆O₃
分子量	396.44
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	LP-935509 是一种口服有效的、选择性的、ATP 竞争性的和可透过血脑屏障的一种接头蛋白-2 相关激酶 1 (AAK1) 抑制剂，其 IC₅₀ 为 3.3 nM，K_i 为 0.9 nM。LP-935509 也是 BIKE 的有效抑制剂 (IC₅₀=14 nM) 和 GAK 的中度抑制剂 (IC₅₀=320 nM)。LP-935509 具有镇痛活性。LP-935509 可用于神经性疼痛和 SARS-CoV-2 的研究。
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 IC 50 of 3.3 nM and a K i of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC 50 =14 nM) and a modest inhibitor of GAK (IC 50 =320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research.
性状	Solid
IC50 & Target[1][2]	IC50: 3.3 ± 0.7 nM (AAK1), 14 nM (BIKE), 320 ± 40 nM (GAK)
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[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. [2]. Mushtaq, et al. Role Of Endocytic Machinery Regulators in EGFR Traffic and Viral Entry (2021). Theses & Dissertations. 532.

溶解度数据	In Vitro: DMSO : 50 mg/mL (126.12 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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