ML417|cas:1386162-69-1|西域试剂

ML417,99.65%

产品编号：Bellancom-136390| CAS NO：1386162-69-1| 分子式：C₂₂H₂₅N₃O₃| 分子量：379.45

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货号	价格	库存与货期
Bellancom-136390	￥900.00	杭州北京（现货）
Bellancom-136390	￥1500.00	杭州北京（现货）
Bellancom-136390	￥4500.00	杭州北京（现货）

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ML417

产品介绍

ML417 是一种选择性的，可透过血脑屏障的 D3 多巴胺受体 (D3R) 激动剂，EC₅₀ 为 38 nM。ML417 促进 D3R 介导的 β-arrestin 易位、G 蛋白介导的信号传导和 pERK 磷酸化，对其他 GPCR 介导的信号传导影响最小。ML417 对毒素诱导的多巴胺能神经元变性具有神经保护作用。

生物活性

ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC₅₀ of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons.

体外研究

ML417 exhibits a K_i for the D3R of 1.24 µM. ML417 is a full and potent agonist for multiple signaling pathways associated with D3R activation.
ML417 potently inhibits cAMP accumulation with an EC₅₀ of 86 nM and an efficacy identical to that of dopamine. ML417 exhibits submicromolar affinity for only three of the targets, the β1-adrenergic, 5-HT2B serotoninergic, and σ-1 receptors. ML417 stimulates β-arrestin recruitment to the D3R-WT with an EC₅₀ of 1.4 nM.
ML417 protects (0.005-5 μM; 24 hours) D3R-expressing dopaminergic neurons from 6-OHDA induced cell death.

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

体内研究

In vivo pharmacokinetics experiments in mice (using 20 mg/kg; i.p.) reveals that ML417 is brain penetrant and exhibits a plasma half-life of 3.44 hours and a brain half-life of 4.23 hours. ML417 displays a plasma T_max of 0.5 hours and C_max of 6500 ng/ml, and a brain T_max of 0.25 hours and C_max of 28000 ng/ml.

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

Animal Model:	6-8 week old male C57BL/6 mice
Dosage:	20 mg/kg
Administration:	I.p. (Pharmacokinetic Analysis)
Result:	Brain penetrant and exhibits a plasma half-life of 3.44 hours and a brain half-life of 4.23 hours. Displayed a plasma T_max of 0.5 hours and C_max of 6500 ng/ml, and a brain T_max of 0.25 hours and C_max of 28000 ng/ml.

体内研究

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

Animal Model:	6-8 week old male C57BL/6 mice
Dosage:	20 mg/kg
Administration:	I.p. (Pharmacokinetic Analysis)
Result:	Brain penetrant and exhibits a plasma half-life of 3.44 hours and a brain half-life of 4.23 hours. Displayed a plasma T_max of 0.5 hours and C_max of 6500 ng/ml, and a brain T_max of 0.25 hours and C_max of 28000 ng/ml.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (131.77 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6354 mL	13.1770 mL	26.3539 mL
5 mM	0.5271 mL	2.6354 mL	5.2708 mL
10 mM	0.2635 mL	1.3177 mL	2.6354 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 90% corn oil
Solubility: ≥ 5 mg/mL (13.18 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (13.18 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 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。