| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Jatrorrhizine chloride targets acetylcholinesterase (AChE), acting as a potent inhibitor with an IC50 of 872 nM. It shows 115-fold selectivity for AChE over butyrylcholinesterase (BuChE). It may also target other enzymes and signaling pathways involved in inflammation, cancer, and microbial infection. Its diverse activities suggest multiple mechanisms of action.
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| ln Vitro |
Jatrorrhizine exhibits anti-plasmodial and anti-amoebic properties; its IC50 values against Entamoeba histolytica and Plasmodium falciparum are 82.7 µM and 3.15 µM, respectively [1]. In the brain, monoamine neurotransmitters are transported via hOCT2 (organic cation transporter 2), hOCT3 (plasma membrane monoamine transporter), and PMAT (plasma membrane monoamine transporter) [3]. Jatrorrhizine inhibits the absorption of 5-HT and NE in transfected hOCT2, hOCT3, and PMAT cells. Jatrophizine decreases hOCT2, hOCT3, and hPMAT-mediated 5-HT and NE uptake with IC50s of 0.1–1 μM for OCT2 and OCT3 and 1–10 μM (for PMAT) [3]. It also strongly inhibits PMAT-mediated MPP+ uptake with an IC50 of 1.05 μM. Two separate processes determine how neurotransmitters produced into the synaptic cleft are cleared. Antidepressants now in use frequently target Uptake-1, which includes the serotonin transporter (SERT). "SERT" can absorb [3H]5-HT with a high affinity but a poor capacity. The Uptake-2 transporter, which is regarded as a "NET" with low affinity but great capacity for uptaking [3H]5-HT into brain slices, is a crucial supplementary regulating system in monoamine clearance. At 25 μM and 50 μM, respectively, jatrorrhizine can dramatically reduce the absorption of 5-HT and NE in synaptosomes [3].
In vitro, jatrorrhizine chloride inhibits acetylcholinesterase (AChE) with an IC50 of 872 nM and shows 115-fold selectivity for BuChE. It is active against Plasmodium falciparum. It exhibits antimicrobial, anti-inflammatory, and antitumor activities. It has lipid-lowering effects. These in vitro activities confirm its diverse pharmacological profile. |
| ln Vivo |
In the tail suspension test (TST), jatrorrhizine chloride (ip; 5, 10, 20 mg/kg) significantly reduced immobility time compared with vehicle controls [2].
In vivo, jatrorrhizine chloride is orally bioactive. It has lipid-lowering effects, ameliorating hyperlipidemia via the suppression of lipogenesis and the enhancement of lipid oxidation in the liver. However, specific details of in vivo efficacy studies are not extensively detailed in the available literature. The compound is a natural alkaloid with potential therapeutic applications. |
| Enzyme Assay |
The in vitro enzyme assay for jatrorrhizine chloride measures its ability to inhibit acetylcholinesterase (AChE) activity. These cell-free assays use purified AChE and a chromogenic substrate. The compound's inhibitory potency (IC50) is determined by measuring the reduction in enzyme activity. Jatrorrhizine chloride shows an IC50 of 872 nM for AChE.
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| Cell Assay |
In vitro cellular assays for jatrorrhizine chloride assess its effects on various cell types. Its antimicrobial activity is assessed against bacterial and fungal strains. Its antitumor activity is assessed in cancer cell lines. Its anti-inflammatory effects are assessed in immune cells. These assays demonstrate the compound's functional activity in a relevant cellular context.
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| Animal Protocol |
Animal/Disease Models: Male ICR albino mouse [2]
Doses: 5, 10, 20 mg/kg Route of Administration: intraperitoneal (ip) injection; 5, 10, 20 mg/kg Experimental Results: The immobility time in the tail suspension test was shortened. In vivo animal studies for jatrorrhizine chloride have been conducted to assess its lipid-lowering effects. Animal models of hyperlipidemia are used to evaluate the compound's ability to ameliorate hyperlipidemia. However, specific details of these studies are not extensively detailed in the available literature. The compound is a natural product with potential for further research. |
| ADME/Pharmacokinetics |
Jatrorrhizine chloride is orally bioactive. It is absorbed from the gastrointestinal tract and distributed throughout the body. Its pharmacokinetic properties would be important for its development as a therapeutic agent. However, specific data on its absorption, distribution, metabolism, and excretion are not extensively detailed in the available literature.
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| Toxicity/Toxicokinetics |
Specific toxicity data for jatrorrhizine chloride are not extensively detailed in the available literature. As a natural alkaloid, its toxicity profile is likely related to its pharmacological activity. However, comprehensive toxicological studies would be required to assess its safety margin. The compound is intended for research use only.
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| References |
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| Additional Infomation |
Jatrorrhizine chloride is a protoberberine alkaloid found in Coptis chinensis with diverse pharmacological activities, including antimicrobial, anti-inflammatory, antitumor, and antimalarial effects. It is a potent, orally bioactive inhibitor of acetylcholinesterase (AChE) with an IC50 of 872 nM. It also has lipid-lowering effects. It is a research compound and is not approved for clinical use.
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| Molecular Formula |
C20H20CLNO4
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|---|---|
| Molecular Weight |
373.8301
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| Exact Mass |
374.116
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| CAS # |
6681-15-8
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| Related CAS # |
Jatrorrhizine hydroxide;483-43-2;Jatrorrhizine;3621-38-3
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| PubChem CID |
371256
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| Appearance |
Orange to yellow solid powder
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| LogP |
3.883
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
461
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JKMUUZMCSNHBAX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H19NO4.ClH/c1-23-18-5-4-12-8-16-14-10-19(24-2)17(22)9-13(14)6-7-21(16)11-15(12)20(18)25-3;/h4-5,8-11H,6-7H2,1-3H3;1H
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| Chemical Name |
2,9,10-trimethoxy-5,6-dihydroisoquinolino[2,1-b]isoquinolin-7-ium-3-ol;chloride
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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 : ~5 mg/mL (~13.38 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.56 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 (5.56 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6750 mL | 13.3751 mL | 26.7501 mL | |
| 5 mM | 0.5350 mL | 2.6750 mL | 5.3500 mL | |
| 10 mM | 0.2675 mL | 1.3375 mL | 2.6750 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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