| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Liensinine Diperchlorate targets the autophagy pathway, specifically late-stage autophagy/mitophagy, by blocking autophagosome-lysosome fusion. This inhibition prevents the completion of the autophagic process, leading to the accumulation of autophagosomes and impaired cellular recycling. The compound's effects on autophagy contribute to its diverse biological activities, including anti-arrhythmia, anti-hypertension, and anti-pulmonary fibrosis. The compound also induces relaxation of vascular smooth muscle, suggesting additional targets involved in vascular tone regulation.
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| ln Vitro |
In vitro studies have demonstrated that liensinine diperchlorate inhibits late-stage autophagy/mitophagy by blocking autophagosome-lysosome fusion. The compound exhibits a wide range of biological activities, including anti-arrhythmia, anti-hypertension, anti-pulmonary fibrosis, and relaxation of vascular smooth muscle. The compound's effects on autophagy have been characterized in cell-based assays measuring autophagosome accumulation, LC3-II levels, and autophagosome-lysosome fusion. Its vasorelaxant effects have been demonstrated in isolated vascular smooth muscle preparations. The compound's diverse in vitro activities make it a valuable tool for studying the role of autophagy in various physiological and pathophysiological processes.
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| ln Vivo |
In vivo studies have demonstrated that liensinine diperchlorate exhibits anti-arrhythmia, anti-hypertension, and anti-pulmonary fibrosis activities. The compound induces relaxation of vascular smooth muscle in vivo. Its effects on autophagy have been studied in vivo, though specific details are not extensively documented. The compound is derived from the seed embryo of Nelumbo nucifera Gaertn., a plant used in traditional medicine. Its in vivo activities are consistent with its mechanism of action as an inhibitor of late-stage autophagy and as a vasorelaxant. The compound's pharmacological profile supports its potential therapeutic applications in cardiovascular and pulmonary diseases.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for liensinine diperchlorate typically involves studying its effects on autophagy-related proteins and pathways. Cells are treated with liensinine diperchlorate (typically 1-100 uM) for 4-24 hours, and autophagosome formation is assessed by measuring LC3-II levels by Western blotting. Autophagosome-lysosome fusion is assessed by co-localization of autophagosomal markers (LC3) with lysosomal markers (LAMP1 or LysoTracker) using immunofluorescence microscopy. The compound's effects on autophagy flux are assessed using tandem fluorescent-tagged LC3 (GFP-RFP-LC3) reporters, where the ratio of GFP to RFP fluorescence indicates autophagosome maturation. For vascular studies, the compound's effects on calcium channels and smooth muscle contraction are assessed using isolated tissue preparations.
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| Cell Assay |
In vitro cellular assays for liensinine diperchlorate are conducted using various cell lines including cancer cells, cardiomyocytes, vascular smooth muscle cells, and fibroblasts. Cells are seeded in 96-well or 6-well plates and treated with varying concentrations of liensinine diperchlorate (typically 0.1-100 uM) for 4-72 hours. Autophagy is assessed by measuring LC3-II levels, p62 degradation, and autophagosome-lysosome fusion using fluorescence microscopy. Cell viability is monitored using MTT or similar assays. For anti-fibrosis studies, fibroblasts are treated with TGF-beta to induce fibrosis, and the compound's effects on collagen production and alpha-SMA expression are measured. For cardiovascular studies, cardiomyocyte contractility and calcium handling are assessed.
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| Animal Protocol |
In vivo animal studies for liensinine diperchlorate typically involve administration to rodent models of arrhythmia, hypertension, or pulmonary fibrosis. The compound is administered by intravenous injection or oral gavage at doses ranging from 0.1-50 mg/kg. For arrhythmia studies, arrhythmias are induced by drugs such as ouabain or by ischemia-reperfusion, and the compound's anti-arrhythmic effects are assessed by ECG monitoring. For hypertension studies, blood pressure is measured in spontaneously hypertensive rats or angiotensin II-infused mice. For pulmonary fibrosis studies, fibrosis is induced by bleomycin administration, and the compound's effects on lung fibrosis are assessed by histological examination and measurement of collagen content. At study termination, tissues are harvested for histological and biochemical analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of liensinine diperchlorate are not extensively documented. The compound has a molecular weight of 811.67 and a molecular formula of C37H42N2O6·2(HClO4). As an isoquinoline alkaloid salt, it is expected to have good aqueous solubility. The compound is derived from a natural source and is available for research purposes only. Detailed ADME parameters such as half-life, bioavailability, and plasma protein binding are not extensively documented in the available literature. The compound should be stored under appropriate conditions as recommended by the supplier.
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| Toxicity/Toxicokinetics |
The toxicological profile of liensinine diperchlorate is characteristic of an isoquinoline alkaloid. As an inhibitor of late-stage autophagy, the compound may have effects on cellular homeostasis and viability. The compound is for research use only and is not intended for human therapeutic use. Standard safety precautions should be followed when handling the compound in a laboratory setting. No specific LD50 values or detailed toxicity profiles have been reported. The compound's diverse biological activities suggest that it should be handled with appropriate care.
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| References | |
| Additional Infomation |
Liensinine Diperchlorate (CAS 5088-90-4) is a major isoquinoline alkaloid found in the seed embryo of Nelumbo nucifera Gaertn. (lotus). It is also known as liensinine diperchlorate. The compound exhibits a wide range of biological activities, including anti-arrhythmia, anti-hypertension, anti-pulmonary fibrosis, and relaxation of vascular smooth muscle. It inhibits late-stage autophagy/mitophagy by blocking autophagosome-lysosome fusion. The compound is derived from a natural source and has potential applications in cardiovascular and pulmonary disease research. It is available for research purposes only with purity ≥98%.
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| Molecular Formula |
C37H44CL2N2O14
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| Molecular Weight |
811.6563
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| Exact Mass |
710.26
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| CAS # |
5088-90-4
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| Related CAS # |
Liensinine;2586-96-1;Liensinine perchlorate;2385-63-9
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| PubChem CID |
102004400
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
55
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| Complexity |
1030
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN1CCC2=CC(=C(C=C2[C@H]1CC3=CC=C(C=C3)O)OC4=C(C=CC(=C4)CC5C6=CC(=C(C=C6CCN5C)OC)OC)O)OC.OCl(=O)(=O)=O.OCl(=O)(=O)=O
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| InChi Key |
BGUPXKYVHOSZPY-JEAINSHJSA-N
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| InChi Code |
InChI=1S/C37H42N2O6.2ClHO4/c1-38-14-13-26-20-35(43-4)37(22-29(26)30(38)16-23-6-9-27(40)10-7-23)45-33-18-24(8-11-32(33)41)17-31-28-21-36(44-5)34(42-3)19-25(28)12-15-39(31)2;2*2-1(3,4)5/h6-11,18-22,30-31,40-41H,12-17H2,1-5H3;2*(H,2,3,4,5)/t30-,31?;;/m1../s1
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| Chemical Name |
4-[(6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinolin-1-yl)methyl]-2-[[(1R)-1-[(4-hydroxyphenyl)methyl]-6-methoxy-2-methyl-3,4-dihydro-1H-isoquinolin-7-yl]oxy]phenol;perchloric acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~77.00 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.08 mg/mL (2.56 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2320 mL | 6.1602 mL | 12.3204 mL | |
| 5 mM | 0.2464 mL | 1.2320 mL | 2.4641 mL | |
| 10 mM | 0.1232 mL | 0.6160 mL | 1.2320 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.
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