| Size | Price | Stock | Qty |
|---|---|---|---|
| 1g |
|
||
| 2g | |||
| Other Sizes |
| Targets |
Ligustrazine hydrochloride targets phosphodiesterase (PDE) and modulates calcium ion mobility. It also targets the TRAF6/c-JUN/NFκB signaling pathway in keratinocytes. It has inhibitory effects on phosphodiesterase, which is associated with heart disease and cardioprotective effects.
|
|---|---|
| ln Vitro |
In vitro, Ligustrazine hydrochloride displayed protective effects against injured ECV304 cells. It significantly increases NOS and NO formation compared to the model group. It inhibits the TRAF6/c-JUN/NFκB signaling pathway in keratinocytes, regulating psoriasis-like inflammation. It has antioxidant and anti-inflammatory activities.
|
| ln Vivo |
In vivo, Ligustrazine hydrochloride is used in China for the treatment of heart diseases. It improves microcirculation, inhibits platelet aggregation, and provides antioxidant activity. It protects vascular endothelium during cardiopulmonary bypass and reduces excessive activation of coagulation and inflammation.
|
| Enzyme Assay |
In vitro assays for Ligustrazine hydrochloride are conducted to evaluate its effects on phosphodiesterase activity and calcium ion mobility. Phosphodiesterase activity is measured using colorimetric or fluorometric assays. Calcium mobilization is assessed using fluorescent calcium indicators such as Fluo-4 AM. NOS activity and NO production are measured by Griess reaction.
|
| Cell Assay |
Cellular assays for Ligustrazine hydrochloride are performed using ECV304 cells (endothelial cells) and keratinocytes. Cells are treated with compound concentrations ranging from 0.1 to 100 µM. Cell viability is assessed using MTT or CCK-8 assays. NOS activity is measured, and NO production is assessed by Griess reaction. NFκB signaling is evaluated by Western blotting or immunofluorescence.
|
| Animal Protocol |
In vivo animal studies for Ligustrazine hydrochloride are conducted in rodent models of cardiovascular disease, psoriasis, or ischemia-reperfusion injury. The compound is administered orally or intraperitoneally. Endpoints include infarct size, platelet aggregation, microcirculation, inflammatory markers, and histopathological evaluation.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Ligustrazine hydrochloride are not well characterized. The compound has a molecular weight of 172.66 and a molecular formula of C8H12N2·HCl. As a small molecule, it is expected to be well absorbed and distributed. Standard PK studies in rodents would be required.
|
| Toxicity/Toxicokinetics |
Toxicological data for Ligustrazine hydrochloride are limited. It is generally well-tolerated at therapeutic doses. No significant acute toxicity has been reported.
|
| References |
|
| Additional Infomation |
Ligusticum hydrochloride belongs to the pyrazine class of compounds.
Ligustrazine hydrochloride (tetramethylpyrazine) is a natural product from Rhizoma Chuanxiong used in China for heart diseases. It is a vasodilatory and antiplatelet agent that inhibits phosphodiesterase and modulates calcium mobility. It has antioxidant and anti-inflammatory activities. It has a molecular weight of 172.66 and formula C8H12N2·HCl. It is not an FDA-approved drug. |
| Molecular Formula |
C₈H₁₂N₂
|
|---|---|
| Molecular Weight |
136.19
|
| Exact Mass |
172.076
|
| CAS # |
76494-51-4
|
| Related CAS # |
Ligustrazine;1124-11-4; tetramethylpyrazine phosphate; 848645-86-3; LigustrazinePhosphate; 105256-26-6;
|
| PubChem CID |
156709
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
192.7ºC at 760mmHg
|
| Flash Point |
71.6ºC
|
| LogP |
2.512
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
11
|
| Complexity |
87.8
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
RQKFOGXUTRDQPB-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C8H12N2.ClH/c1-5-6(2)10-8(4)7(3)9-5;/h1-4H3;1H
|
| Chemical Name |
2,3,5,6-tetramethylpyrazine;hydrochloride
|
| Synonyms |
Chuanxiongzine hydrochloride; Ligustrazine (hydrochloride); orb1304805; orb3140801; Chuanxiongzine HCl; Tetramethylpyrazine
|
| 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 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL
H2O : ~100 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (Infinity 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 25.0 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: ≥ 2.5 mg/mL (Infinity 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 25.0 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: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (Infinity mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 7.3427 mL | 36.7134 mL | 73.4268 mL | |
| 5 mM | 1.4685 mL | 7.3427 mL | 14.6854 mL | |
| 10 mM | 0.7343 mL | 3.6713 mL | 7.3427 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
