Pirenzepine dihydrochloride LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride|cas:29868-97-1|西域试剂

Pirenzepine dihydrochloride LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride,99.89%

产品编号：Bellancom-17037| CAS NO：29868-97-1| 分子式：C₁₉H₂₃Cl₂N₅O₂| 分子量：424.32

Pirenzepine dihydrochloride (LS519) 是一种选择性 M1 型毒蕈碱受体拮抗剂。

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-17037		￥500.00	杭州北京（现货）
Bellancom-17037		￥880.00	杭州北京（现货）

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Pirenzepine dihydrochloride LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride

产品介绍

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.

体外研究

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.

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

Cell Proliferation Assay

Cell Line:	PC-3 cells
Concentration:	100-140 μg/mL
Incubation Time:	24 hours
Result:	Inhibited PC-3 cell proliferation in a concentration-dependent manner.

Cell Migration Assay

Cell Line:	PC-3 and A549 cells
Concentration:	110 μg/mL
Incubation Time:	24 hours
Result:	Inhibited the migration of PC-3 and A549 cell lines (P=0.014).

Cell Migration Assay

Cell Line:	PC-3 cells
Concentration:	110 μg/mL
Incubation Time:	0-24 hours
Result:	Inhibited the expression of GLI1 and PTCH1.

RT-PCR

Cell Line:	PC-3 cells
Concentration:	100-130 μg/mL
Incubation Time:	24 hours
Result:	Suppressed GLI1 mRNA expression in PC-3 cells. Increased PTCH1 mRNA level but not reach statistical significance. Showed no SHH mRNA expression level change.

体内研究
(In Vivo)

Pirenzepine (intraperitoneal injection; 0.3 mg/kg; once) treatment shows beneficial effects in lipopolysaccharide-induced septic shock.

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

Animal Model:	Male C57BL/6 mice with experimental endotoxemia
Dosage:	0.3 mg/kg
Administration:	Intraperitoneal injection; 0.3 mg/kg; once
Result:	Improved survival rate of LPS-induced septic shock. Relieved LPS-induced pulmonary and hepatic injury. Reduced the expression of SOCS3 at mRNA level.

体内研究

Pirenzepine (intraperitoneal injection; 0.3 mg/kg; once) treatment shows beneficial effects in lipopolysaccharide-induced septic shock.

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

Animal Model:	Male C57BL/6 mice with experimental endotoxemia
Dosage:	0.3 mg/kg
Administration:	Intraperitoneal injection; 0.3 mg/kg; once
Result:	Improved survival rate of LPS-induced septic shock. Relieved LPS-induced pulmonary and hepatic injury. Reduced the expression of SOCS3 at mRNA level.

体内研究

Pirenzepine (intraperitoneal injection; 0.3 mg/kg; once) treatment shows beneficial effects in lipopolysaccharide-induced septic shock.

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

Animal Model:	Male C57BL/6 mice with experimental endotoxemia
Dosage:	0.3 mg/kg
Administration:	Intraperitoneal injection; 0.3 mg/kg; once
Result:	Improved survival rate of LPS-induced septic shock. Relieved LPS-induced pulmonary and hepatic injury. Reduced the expression of SOCS3 at mRNA level.

性状

Solid

溶解性数据

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

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3567 mL	11.7836 mL	23.5671 mL
5 mM	0.4713 mL	2.3567 mL	4.7134 mL
10 mM	0.2357 mL	1.1784 mL	2.3567 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 (sealed storage, away from moisture)。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

. 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. [Content Brief]

. 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. [Content Brief]

. Yabuki Y, et al. The T-type calcium channel enhancer SAK3 inhibits neuronal death following transient brain ischemia via nicotinic acetylcholine receptor stimulation. Neurochem Int. 2017 Sep;108:272-281. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

个人防护装备	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
危险品运输编码	NONH for all modes of transport
WGK德国	2
RTECS号	UU7883000

1. 物质的识别

产品名：	Pirenzepine dihydrochloride
CAS号：	29868-97-1
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	Pirenzepine dihydrochloride
别名：	LS519
分子式：	C19H21N5O2.2HCl
分子量：	424.33

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。

10. 生态资料

一般注意事项：

无可用资料。

11. 废弃处置

按照所在国家，省份，县市和地方的法规处置。

12. 运输信息

正确的运输名称：	无
非危险品运输：	这种物质被视为非危险品运输。

13. 法规信息

尚未有针对此产品作出的化学安全性评估。

14. 其他信息

[1]. Del Tacca M, et al. A selective antimuscarinic agent: pirenzepine. Review of its pharmacologic and clinical properties. Minerva Dietol Gastroenterol. 1989 Jul-Sep;35(3):175-89.

[2]. Ojewole JA, et al. Effects of pirenzepine (Gastrozepin) on skeletal muscle contractility. Methods Find Exp Clin Pharmacol. 1983 Nov;5(9):619-23.

[3]. Caulfield MP, et al. Central administration of the muscarinic receptor subtype-selective antagonist pirenzepine selectively impairs passiveavoidance learning in the mouse. J Pharm Pharmacol. 1983 Feb;35(2):131-2.

[4]. Hirschowitz BI, et al. Effects of pirenzepine and atropine on vagal and cholinergic gastric secretion and gastrin release and on heart rate in the dog. J Pharmacol Exp Ther. 1983 May;225(2):263-8.

Pirenzepine dihydrochloride LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride,99.89%

Pirenzepine dihydrochloride LS 519; Pirenzepin dihydrochloride; Gastrozepin dihydrochloride

化学品安全说明书(MSDS)

质检证书(COA)

1. 物质的识别

2. 合成/成分数据

3. 急救措施

4. 消防措施

5. 泄漏应急处理

6. 处理和储存

7. 接触控制和个人防护

8. 稳定性和反应活性

9. 毒性资料

10. 生态资料

11. 废弃处置

12. 运输信息

13. 法规信息

14. 其他信息

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