Pirenzepine dihydrochloride

(Synonyms: LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride)
目录号: PL06860 纯度: ≥99%
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。
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)
详情描述
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。
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
搜索质检报告(COA)

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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