Pirenzepine dihydrochloride|29868-97-1|(LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride)-陌孚医药/Medlife

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Pirenzepine dihydrochloride (Synonyms: LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride)

目录号: PL06860 纯度: ≥99%

CAS No. :29868-97-1

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中文名称	Pirenzepine dihydrochloride
中文别名	盐酸哌仑西平;5,11-二氢-11-[(4-甲基-1-哌嗪基)乙酰]-6H-吡啶并[2,3-b][1,4]苯并二氮卓-6-酮二盐酸盐;哌仑西平盐酸盐一水 EP标准品;哌伦西平;5,11-二氢-11-[(4-甲基-1-哌嗪基)乙酰基]-6H-吡啶并[2,3-b][1,4]苯并二氮杂卓-6-酮二盐酸盐
英文名称	Pirenzepine dihydrochloride
英文别名	Pirenzepine hydrochloride;5,11-Dihydro-11-[(4-methylpiperazin-1-yl)acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one dihydrochloride;Pirenzepine dihydrochloride;Pirenzepine, Dihydro;Pirenzepine dihydrochloride monohydrate;5,11-Dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one dihydrochloride;Tabe;Pirenzepine HCl;Gastrozepin;Bisvanil;Pirenzepine 2HCl;Maghen;Leblon;Pirenzepinehydrochloride;LS 519 dihydrochloride;Pirenzepine (dihydrochloride);LS 519 cl2;LS 519Cl2;Pirenzepine hydrochloride [USAN:JAN];10YM403FLS;LS519;AK162585;5,11-Dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one Dihydrochloride
Cas No.	29868-97-1
分子式	C₁₉H₂₃Cl₂N₅O₂
分子量	424.32
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	Pirenzepine (LS 519) dihydrochloride 是一种选择性的 M1 mAChR (毒蕈碱乙酰胆碱受体) 拮抗剂。Pirenzepine dihydrochloride 可减少胃酸分泌并减少肌肉痉挛，可用于消化性溃疡的研究。Pirenzepine dihydrochloride 具有对癌细胞的抗增殖活性。
生物活性	Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells.
性状	Solid
IC50 & Target[1][2]	mAChR1
体外研究(In Vitro)	Pirenzepine (100-140 μg/mL; 24 h) inhibits PC-3 cell proliferation activity. Pirenzepine (110 μg/mL; 24 h) inhibits prostate and lung cancer cell migration. Pirenzepine (100-130 μg/mL; 0-24 h) inhibits the expression of GLI1 in PC-3 cells. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)	Pirenzepine (intraperitoneal injection; 0.3?mg/kg; once) treatment shows beneficial effects in lipopolysaccharide-induced septic shock. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Carmine AA, et al. Pirenzepine. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in peptic ulcer disease and other allied diseases. Drugs. 1985 Aug;30(2):85-126. [2]. Yin QQ, et al. Muscarinic acetylcholine receptor M1 mediates prostate cancer cell migration and invasion through hedgehog signaling. Asian J Androl. 2018 Nov-Dec;20(6):608-614.

溶解度数据	In Vitro: H₂O : 75 mg/mL (176.75 mM; Need ultrasonic)DMSO : 25 mg/mL (58.92 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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