| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 500mg |
|
||
| Other Sizes |
| ln Vitro |
The proliferative activity of PC-3 cells is inhibited by pinenepine (100-140 μg/mL; 24 hours)]. Lung and prostate cancer cells migrate less when exposed to penerepine (110 μg/mL for 24 hours) [2]. GLI1 expression is inhibited in PC-3 cells by pinenepine (100–130 μg/mL; 0–24 hours) [2].
|
|---|---|
| ln Vivo |
In lipopolysaccharide-induced septic shock, pirenzepine treatment (intraperitoneal injection; 0.3 mg/kg; once) has demonstrated positive results [3].
|
| Cell Assay |
Cell proliferation assay [2]
Cell Types: PC-3 Cell Tested Concentrations: 100-140 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited PC-3 cell proliferation in a concentration-dependent manner. Cell migration experiment [2] Cell Types: PC-3 and A549 cells Tested Concentrations: 110 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited the migration of PC-3 and A549 cell lines (P=0.014). Western Blot Analysis [2] Cell Types: PC-3 cells Tested Concentrations: 110 μg/mL Incubation Duration: 0-24 hrs (hours) Experimental Results: Inhibition of the expression of GLI1 and PTCH1. RT-PCR[2] Cell Types: PC-3 cells Tested Concentrations: 100-130 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: GLI1 mRNA expression was inhibited in PC-3 cells. PTCH1 mRNA levels were increased but did not reach statistical significance. SHH mRNA expression levels did not change. |
| Animal Protocol |
Animal/Disease Models: Experimental endotoxemia male C57BL/6 mice [3]
Doses: 0.3 mg/kg Route of Administration: intraperitoneal (ip) injection; 0.3 mg/kg; one-time Experimental Results:improve the survival rate of septic shock caused by LPS. Alleviates LPS-induced lung and liver damage. diminished SOCS3 expression at the mRNA level. |
| References |
|
| Additional Infomation |
Pirenzepine is a pyridobenzodiazepine. It has anti-ulcer, antimuscarinic, and antispasmodic effects. It is an antimuscarinic drug that inhibits gastric acid secretion at low doses without affecting gastrointestinal motility, salivation, central nervous system, cardiovascular, ocular, or urinary system function. It promotes the healing of duodenal ulcers and, due to its cytoprotective effects, helps prevent recurrence. It can also enhance the efficacy of other anti-ulcer drugs (such as cimetidine and ranitidine). Patients generally tolerate it well. Patients generally tolerate it well. Drug Indications For the treatment of peptic ulcers, gastric ulcers, and duodenal ulcers. Mechanism of Action Pirenzepine is a muscarinic receptor antagonist that binds to muscarinic acetylcholine receptors. Muscarinic acetylcholine receptors mediate various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphatidylinositol, and regulation of potassium channels through the action of G proteins. Pharmacodynamics Pirenzepine belongs to a class of drugs called antispasmodics/anticholinergics. These drugs are used to relieve spasms or cramps in the stomach, intestines, and bladder. Pirenzepine is used to treat duodenal ulcers, gastric ulcers, or intestinal disorders. It can be used in combination with antacids or other medications to treat peptic ulcers. It can also be used to prevent nausea, vomiting, and motion sickness.
|
| Molecular Formula |
C19H21N5O2
|
|---|---|
| Molecular Weight |
351.41
|
| Exact Mass |
351.169
|
| Elemental Analysis |
C, 64.94; H, 6.02; N, 19.93; O, 9.11
|
| CAS # |
28797-61-7
|
| Related CAS # |
Pirenzepine dihydrochloride;29868-97-1;Pirenzepine-d8 dihydrochloride;Pirenzepine-d8
|
| PubChem CID |
4848
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
541.7±50.0 °C at 760 mmHg
|
| Melting Point |
226 - 230ºC
|
| Flash Point |
281.4±30.1 °C
|
| Vapour Pressure |
0.0±1.4 mmHg at 25°C
|
| Index of Refraction |
1.615
|
| LogP |
-0.08
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
26
|
| Complexity |
534
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN1CCN(CC(N2C3=CC=CC=C3C(NC4=C2N=CC=C4)=O)=O)CC1
|
| InChi Key |
RMHMFHUVIITRHF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H21N5O2/c1-22-9-11-23(12-10-22)13-17(25)24-16-7-3-2-5-14(16)19(26)21-15-6-4-8-20-18(15)24/h2-8H,9-13H2,1H3,(H,21,26)
|
| Chemical Name |
6H-Pyrido(2,3-b)(1,4)benzodiazepin-6-one, 5,11-dihydro-11-((4-methyl-1-piperazinyl)acetyl)-
|
| Synonyms |
Pirenzepine free base; Pirenzepin;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~284.6 mM; with ultrasonication and warming by heating to 60°C)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (14.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (50.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (14.23 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (50.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8457 mL | 14.2284 mL | 28.4568 mL | |
| 5 mM | 0.5691 mL | 2.8457 mL | 5.6914 mL | |
| 10 mM | 0.2846 mL | 1.4228 mL | 2.8457 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
