LP-935509|cas:1454555-29-3|西域试剂

LP-935509,99.74%

产品编号：Bellancom-117626| CAS NO：1454555-29-3| 分子式：C₂₀H₂₄N₆O₃| 分子量：396.44

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-117626	￥950.00	杭州北京（现货）
Bellancom-117626	￥1650.00	杭州北京（现货）
Bellancom-117626	￥5950.00	杭州北京（现货）
Bellancom-117626	￥10500.00	杭州北京（现货）

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LP-935509

产品介绍

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 IC₅₀ of 3.3 nM and a K_i 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (126.12 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5224 mL	12.6122 mL	25.2245 mL
5 mM	0.5045 mL	2.5224 mL	5.0449 mL
10 mM	0.2522 mL	1.2612 mL	2.5224 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.25 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.25 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.25 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。