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Pirenzepine dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pirenzepine dihydrochloride图片
CAS NO:29868-97-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
100mg电议
500mg电议
1 g电议
5 g电议

产品名称
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 selectiveM1mAChR(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 tocancercells[1][2].

IC50& Target

mAChR1

 

体外研究
(In Vitro)

Pirenzepine (100-140 μg/mL; 24 h) inhibits PC-3 cell proliferation activity[2].
Pirenzepine (110 μg/mL; 24 h) inhibits prostate and lung cancer cell migration[2].
Pirenzepine (100-130 μg/mL; 0-24 h) inhibits the expression of GLI1 in PC-3 cells[2].

Cell Proliferation Assay[2]

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[2]

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[2]

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

RT-PCR[2]

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[3].

Animal Model:Male C57BL/6 mice with experimental endotoxemia[3]
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.
分子量

424.32

性状

Solid

Formula

C19H23Cl2N5O2

CAS 号

29868-97-1

中文名称

二盐酸哌仑西平

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)

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 mg5 mg10 mg
1 mM2.3567 mL11.7836 mL23.5671 mL
5 mM0.4713 mL2.3567 mL4.7134 mL
10 mM0.2357 mL1.1784 mL2.3567 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。