Piromelatine|946846-83-9|(Neu-P11)-陌孚医药/Medlife

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Piromelatine (Synonyms: Neu-P11)

目录号: PL07082 纯度: ≥99%

CAS No. :946846-83-9

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中文名称	Piromelatine
中文别名	N-[2-(5-methoxy-1H-indol-3-yl)ethyl]-4-oxopyran-2-carboxamide
英文名称	Piromelatine
英文别名	N-[2-(5-Methoxy-1H-indol-3-yl)ethyl]-4-oxo-4H-pyran-2-carboxamide;Neu-P 11;Piromelatine;N-(2-(5-Methoxy-1H-indol-3-yl)ethyl)-4-oxo-4H-pyran-2-carboxamide;S3UN2146K9;4H-Pyran-2-carboxamide, N-(2-(5-methoxy-1H-indol-3-yl)ethyl)-4-oxo-;4H-Pyran-2-carboxamide, N-[2-(5-methoxy-1H-indol-3-yl)ethyl]-4-oxo-;Piromelatine [INN];DB12288;SB19819;Q18388725;N-[2-(5-methoxy-1H-indol-3-yl)ethyl]-4-oxopyran-2-carboxamide;Neu-P11;N-[2-(5-Methoxy-1H-indol-3-yl)ethyl]-4-oxo-4H-pyran-2-carboxamide (ACI)
Cas No.	946846-83-9
分子式	C₁₇H₁₆N₂O₄
分子量	312.32
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情

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。

生物活性

Piromelatine (Neu-P11) is a melatonin MT 1 /MT 2 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.

性状

Solid

IC50 & Target[1][2]

5-HT1A Receptor 5-HT1D Receptor

体内研究(In Vivo)

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.
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

4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

ClinicalTrial

参考文献

[1]. Meihua She, et al. Piromelatine, a Novel Melatonin Receptor Agonist, Stabilizes Metabolic Profiles and Ameliorates Insulin Resistance in Chronic Sleep Restricted Rats. Eur J Pharmacol. 2014 Mar 15;727:60-5.
[2]. L Huang, et al. Blood Pressure Reducing Effects of Piromelatine and Melatonin in Spontaneously Hypertensive Rats. Eur Rev Med Pharmacol Sci. 2013 Sep;17(18):2449-56.

溶解度数据	In Vitro: DMSO : 250 mg/mL (800.46 mM; Need ultrasonic)配制储备液

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Data Sheet

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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