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

Pirenzepine (dihydrochloride)  (Synonyms: LS 519; Pirenzepin (dihydrochloride); Gastrozepin (dihydrochloride); ピレンゼピン二塩酸塩)

製品番号: HY-17037 純度: 99.84%
COA 取扱説明書 Technical Support

Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist, with poor penetration of the blood-brain barrier. 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Pirenzepine dihydrochloride

Pirenzepine (dihydrochloride) 構造式

CAS 番号 : 29868-97-1

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 44 在庫あり
Solution
10 mM * 1 mL in Water USD 44 在庫あり
Solid
100 mg $40 在庫あり
500 mg $90 在庫あり
1 g $162 在庫あり
5 g   お問い合わせ  
10 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Other Forms of Pirenzepine dihydrochloride:

Pirenzepine (dihydrochloride) 関連抗体

Top Publications Citing Use of Products

mAChR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist, with poor penetration of the blood-brain barrier. 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

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
2.1 x 10-2 3
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 1
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 1
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 1
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 1
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 1
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]
体外実験

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

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

Pirenzepine (dihydrochloride) 関連抗体

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.
体内実験

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

MedChemExpress (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.
臨床実験
分子量

424.32

分子式

C19H23Cl2N5O2
CAS 番号
Appearance

Solid

Color

White to yellow

SMILES

O=C1NC2=CC=CN=C2N(C(CN3CCN(C)CC3)=O)C4=CC=CC=C14.[H]Cl.[H]Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

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

H2O : 50 mg/mL (117.84 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
純度とドキュメンテーション

純度: 99.84%

COA (256 KB) HNMR (137 KB) RP-HPLC (168 KB) LCMS (104 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
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
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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Pirenzepine dihydrochloride Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pirenzepine29868-97-1LS 519PirenzepinGastrozepinLS519LS-519mAChRMuscarinic acetylcholine receptorpeptic ulcersanti-proliferative activityPC-3A549Inhibitorinhibitorinhibit

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

  

カスタマ需要量 *

お名前 *

 

タイトル

メールアドレス *

 

電話番号 *

デパートメント

 

組纖名 *

市区町村

都道府県

国或いは地域 *

      

必ず会社名を記載ください。個人への返信は行いません。

備考

バルクお問い合わせ

Inquiry Information

製品名:
Pirenzepine dihydrochloride
製品番号:
HY-17037
数量:
MCE 日本正規代理店:

カスタマーレビュー

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

製品名

  

Lot #

お名前 *

 

メールアドレス *

電話番号 *

 

部門 *

組纖名 *

 

国或いは地域 *

備考

Request for HNMR Report

We have received your request and will respond to you as soon as possible.