Piromelatine - CAS:946846-83-9

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Piromelatine (Synonyms:Neu-P11)

目录号 : KM2638 CAS No. : 946846-83-9

Data Sheet 产品使用指南

Piromelatine (Neu-P11) 是褪黑素受体 MT1/MT2 的激动剂，是 5-HT_1A 和 5-HT_1D 的激动剂，也是 5-HT_2B 的拮抗剂。Piromelatine (Neu-P11) 有用于促进睡眠、缓解疼痛、抗神经退行性和抗抑郁等研究的潜能。Piromelatine (Neu-P11) 还具有抑制疼痛相关靶点 P2X3、TRPV1和 Nav1.7 通道的活性。

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50mg		In-stock
100mg		In-stock
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500mg	询价	In-stock

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生物活性

Piromelatine (Neu-P11) is a melatonin MT₁/MT₂ receptor agonist, serotonin 5-HT_1A/5-HT_1D agonist, and serotonin 5-HT_2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.

体内研究

Piromelatine (20 mg/kg, ip, daily) treatment prevents insulin resistance induced by sleep restriction.
Piromelatine (5-50 mg/kg, ip, daily) decreases plasma glucose significantly.
Piromelatine (100 mg/kg) decreases thermal hyperalgesia and mechanical allodynia in PSL (partial sciatic nerve ligation) mice.

Animal Model:	Twenty four male Sprague-Dawley rats (3 months old, weighing 250-300 g).
Dosage:	20 mg/kg.
Administration:	IP, daily at 8:00 p.m.
Result:	Resulted in significantly decreased plasma glucose levels (6.670.35 mmol/L, 6.770.34 mmol/L vs. 8.27 0.38 mmol/L), and the plasma glucose levels of the two groups were even neared to that of the normal control group (6.07±0.35 mmol/L). Resulted in a decrease in triglycerides and total cholesterol levels (51.8% and 43.0%, respectively) and an elevation in HDL-C level (increase of 32.4%).

Animal Model:	Five groups of 12-wk-old rats (10/group).
Dosage:	5-50 mg/kg.
Administration:	Intraperitoneal injection in 18:00 every day.
Result:	Plasma glucose was decreased significantly by 27.3%, 34.5% and 61.5%, respectively.

Animal Model:	Male C57BL/6 J mice, weighing 22-26 g (10 weeks old; PSL mice).
Dosage:	25, 50, or 100 mg/kg.
Administration:	IP 1 h before assessment of thermal hyperalgesia and mechanical allodynia.
Result:	Remarkably prolonged thermal latency (surgery×treatment interaction, F_1,24=15.7, p<0.001; surgery×treatment×hours interaction, F_5,120=3.0, p<0.05) and increased mechanical threshold (surgery×treatment interaction, F_1,24=18.4, p<0.001; surgery× treatment×hours interaction, F_5,120=2.6, p<0.05) for 4 h after administration of piromelatine to PSL mice.

分子式

C₁₇H₁₆N₂O₄

分子量

312.32

CAS号

946846-83-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 250 mg/mL (800.46 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2018 mL	16.0092 mL	32.0184 mL
5 mM	0.6404 mL	3.2018 mL	6.4037 mL
10 mM	0.3202 mL	1.6009 mL	3.2018 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 (protect from light)。-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 (6.66 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.66 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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (6.66 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.66 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。