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  2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. Pirenzepine dihydrochloride

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

目錄號(hào): HY-17037 純度: 99.89%
COA 產(chǎn)品使用指南 技術(shù)支持

Pirenzepine (LS 519) dihydrochloride 是一種選擇性的 M1 mAChR (毒蕈堿乙酰膽堿受體) 拮抗劑。Pirenzepine dihydrochloride 可減少胃酸分泌并減少肌肉痙攣，可用于消化性潰瘍的研究。Pirenzepine dihydrochloride 具有對(duì)癌細(xì)胞的抗增殖活性。

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Pirenzepine dihydrochloride Chemical Structure

Pirenzepine dihydrochloride Chemical Structure

CAS No. : 29868-97-1

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規(guī)格 價(jià)格 是否有貨 數(shù)量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥550
In-stock
100 mg ￥500
In-stock
500 mg ￥880
In-stock
1 g ￥1600
In-stock
5 g   詢價(jià)  
10 g   詢價(jià)  

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Customer Review

Other Forms of Pirenzepine dihydrochloride:

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)

查看 mAChR 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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[1][2].

IC50 & Target

mAChR1

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
2.1 x 10-2 μM
Compound: Pirenzepine
Displacement of [3H]pirenzepine from human recombinant M1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [3H]pirenzepine from human recombinant M1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
CHO IC50
246.8 nM
Compound: pirenzepine
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells
[PMID: 9986705]
CHO IC50
28.2 nM
Compound: pirenzepine
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M1 using membranes from transfected CHO cells
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M1 using membranes from transfected CHO cells
[PMID: 9986705]
CHO IC50
340.6 nM
Compound: pirenzepine
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells
[PMID: 9986705]
CHO IC50
955.6 nM
Compound: pirenzepine
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells
[PMID: 9986705]
CHO IC50
968.2 nM
Compound: pirenzepine
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M2 using membranes from transfected CHO cells
Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M2 using membranes from transfected CHO cells
[PMID: 9986705]
體外研究
(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].

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

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.
體內(nèi)研究
(In Vivo)

Pirenzepine (intraperitoneal injection; 0.3?mg/kg; once) treatment shows beneficial effects in lipopolysaccharide-induced septic shock[3].

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

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

Formula

C19H23Cl2N5O2
CAS 號(hào)
性狀

固體

顏色

White to yellow

中文名稱

二鹽酸哌侖西平
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)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)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

H2O 中的溶解度 : 50 mg/mL (117.84 mM; 超聲助溶)

DMSO 中的溶解度 : 25 mg/mL (58.92 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

掃碼獲得
動(dòng)物溶解方案

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
純度 & 產(chǎn)品資料

純度: 99.89%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.3567 mL 11.7836 mL 23.5671 mL 58.9178 mL
5 mM 0.4713 mL 2.3567 mL 4.7134 mL 11.7836 mL
10 mM 0.2357 mL 1.1784 mL 2.3567 mL 5.8918 mL
15 mM 0.1571 mL 0.7856 mL 1.5711 mL 3.9279 mL
20 mM 0.1178 mL 0.5892 mL 1.1784 mL 2.9459 mL
25 mM 0.0943 mL 0.4713 mL 0.9427 mL 2.3567 mL
30 mM 0.0786 mL 0.3928 mL 0.7856 mL 1.9639 mL
40 mM 0.0589 mL 0.2946 mL 0.5892 mL 1.4729 mL
50 mM 0.0471 mL 0.2357 mL 0.4713 mL 1.1784 mL
H2O 60 mM 0.0393 mL 0.1964 mL 0.3928 mL 0.9820 mL
80 mM 0.0295 mL 0.1473 mL 0.2946 mL 0.7365 mL
100 mM 0.0236 mL 0.1178 mL 0.2357 mL 0.5892 mL

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

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產(chǎn)品名稱：
Pirenzepine dihydrochloride
目錄號(hào)：
HY-17037
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