| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Stachydrine hydrochloride targets multiple pathways including NF-κB, Akt, and ERK. It inhibits the NF-κB signaling pathway. The compound inhibits proliferation and induces apoptosis of breast cancer cells via inhibition of Akt and ERK pathways. It promotes IL-12 and IL-6 protein expression and modulates T-bet, RORγt, GATA-3, and Foxp3 mRNA expression. Stachydrine hydrochloride has anti-cardiac hypertrophy activity. It acts as a compatible solute and helps maintain cell turgor during water deficit.
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| ln Vitro |
Stacchydrine hydrochloride (50 μM, 200 μM, 500 μM, and 1000 μM) was found to strongly suppress the cytoplasmic p-IκB (ser32) protein and the nucleus-based NF-κB (p65) protein (level P<0.05)[1]. Stachydrine hydrochloride may trigger a cell life cycle, as evidenced by the considerable increase in the frequency of the G1 phase of the cell cycle in both investigated cell lines at high concentrations (500 μM and 1000 μM) of stachydrine [2].
In vitro, Stachydrine hydrochloride inhibits proliferation and induces apoptosis of breast cancer cells via inhibition of Akt and ERK pathways. The compound inhibits the NF-κB signaling pathway. It promotes the protein expression of IL-12 and IL-6, as well as the mRNA expression of T-bet and RORγt, while inhibiting GATA-3 and Foxp3. Stachydrine hydrochloride has been shown to be a potent anti-metastatic agent that can markedly inhibit the malignancy and invasive capacity of malignant cancer cells. The compound is a potentially useful alkaloid for activity screening. |
| ln Vivo |
In vivo, Stachydrine hydrochloride is the major active constituent of Motherwort and is a potential therapy for cardiovascular diseases. It has anti-cardiac hypertrophy activity. The compound plays a role in osmoprotection and stress tolerance in plants. Further in vivo studies have evaluated its cardiovascular protective effects. The compound is typically administered orally in preclinical studies. Its effects on immune modulation have also been investigated.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Stachydrine hydrochloride involve measuring NF-κB pathway inhibition. NF-κB activation is assessed by measuring nuclear translocation or DNA binding activity. Akt and ERK pathway inhibition is assessed by phosphorylation studies. The compound’s effects on cytokine expression are measured by ELISA. Assays are performed in appropriate buffer systems with positive controls (e.g., known pathway inhibitors). IC50 values are calculated from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for Stachydrine hydrochloride are conducted in various cell lines including breast cancer cells and immune cells. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations (e.g., up to 1000 μM). Cell viability is assessed by MTT or CCK-8 assays. Apoptosis is evaluated by Annexin V/PI staining and caspase activity assays. Cytokine levels are measured by ELISA. Pathway protein phosphorylation is analyzed by Western blot. Experiments are performed in triplicate with appropriate controls.
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| Animal Protocol |
In vivo animal studies for Stachydrine hydrochloride are conducted in rodent models of cardiovascular disease. For cardiac hypertrophy studies, animals with induced cardiac hypertrophy are treated with the compound. For cancer studies, tumor-bearing mice may be used. For immunomodulation studies, animal models of immune challenge are employed. Stachydrine hydrochloride is administered orally or via injection. Animals are monitored for clinical signs. Heart and other tissues are collected for histopathological and biomarker analysis.
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| ADME/Pharmacokinetics |
Stachydrine hydrochloride (MW 185.65 g/mol, C7H13NO2·HCl) is a small molecule alkaloid with high water solubility. The compound is the major active constituent of Leonurus artemisia (Motherwort). It is orally bioavailable. Stachydrine hydrochloride is metabolized by hepatic enzymes. The compound is distributed to tissues including heart, as evidenced by its cardioprotective effects. Pharmacokinetic parameters such as Cmax, Tmax, and half-life have been characterized in preclinical studies. The compound shows stability under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Stachydrine hydrochloride is generally well-tolerated in preclinical studies. The compound is a natural alkaloid derived from Motherwort, a plant used in traditional medicine. Its cardiovascular protective effects have been demonstrated with acceptable safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
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| References | |
| Additional Infomation |
Stachydrine hydrochloride is the major active constituent of Leonurus artemisia (Motherwort), a potential therapy for cardiovascular diseases. It inhibits the NF-κB signaling pathway and has anti-cardiac hypertrophy activity. The compound inhibits proliferation and induces apoptosis of breast cancer cells via inhibition of Akt and ERK pathways. It promotes IL-12 and IL-6 expression and modulates T-bet, RORγt, GATA-3, and Foxp3. Stachydrine hydrochloride is a potent anti-metastatic agent. All applications are limited to non-human research use.
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| Molecular Formula |
C7H15CLNO2
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| Molecular Weight |
180.6525
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| Exact Mass |
179.071
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| CAS # |
4136-37-2
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| Related CAS # |
Stachydrine;471-87-4
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| PubChem CID |
17751044
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| Appearance |
White to off-white solid powder
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| Melting Point |
225ºC
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
11
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| Complexity |
148
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[N+]1(CCC[C@H]1C(=O)[O-])C.Cl
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| InChi Key |
DUNMULOWUUIQIL-RGMNGODLSA-N
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| InChi Code |
InChI=1S/C7H13NO2.ClH/c1-8(2)5-3-4-6(8)7(9)10;/h6H,3-5H2,1-2H3;1H/t6-;/m0./s1
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| Chemical Name |
(2S)-1,1-dimethylpyrrolidin-1-ium-2-carboxylate;hydrochloride
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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) |
H2O : ~100 mg/mL (~556.67 mM)
DMSO : ~100 mg/mL (~556.67 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (16.70 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 30.0 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: ≥ 3 mg/mL (16.70 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 30.0 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: ≥ 3 mg/mL (16.70 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 (556.67 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 | 5.5356 mL | 27.6778 mL | 55.3557 mL | |
| 5 mM | 1.1071 mL | 5.5356 mL | 11.0711 mL | |
| 10 mM | 0.5536 mL | 2.7678 mL | 5.5356 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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