| 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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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
AChE
Nodakenin primarily targets acetylcholinesterase (AChE), inhibiting its activity with an IC50 of 84.7 μM. By inhibiting AChE, it enhances cholinergic signaling, which may contribute to its neuroprotective and cognitive-enhancing effects. It suppresses lipopolysaccharide (LPS)-induced inflammatory responses by inhibiting tumor necrosis factor receptor-associated factor 6 (TRAF6) and nuclear factor-κB (NF-κB) pathways. Its neuroprotective and antiaggregatory properties suggest additional targets related to neuronal survival and protein aggregation. The compound's beneficial effects are mediated, in part, via the enhancement of cholinergic signaling. |
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| ln Vitro |
Nodakenin is a dose-regulated inhibitor of AChE activity, with an IC50 value of 84.7 μM[1].
In vitro, Nodakenin inhibits acetylcholinesterase (AChE) activity in a dose-dependent manner with an IC50 of 84.7 μM. It suppresses LPS-induced inflammatory responses in macrophage cells by inhibiting TRAF6 and NF-κB pathways. It has neuroprotective and antiaggregatory properties. These activities confirm its potential for treating cognitive impairment and inflammatory conditions. Its inhibition of AChE suggests that its beneficial effects are mediated, in part, via the enhancement of cholinergic signaling. The compound's coumarin glycoside structure contributes to its biological activities. |
| ln Vivo |
The maze avoidance test and the Y-maze test demonstrate that nodakenin (10 mg/kg, po) can overcome the cognitive impairment caused by scopolamine [1]. The maze avoidance test and the Y-maze test demonstrate that nodakenin (10 mg/kg, po) can overcome the cognitive impairment caused by scopolamine [1]. Morris water maze training test results show that nodakenin (10 mg/kg, po) decreases escape delay [1].
In vivo, Nodakenin has shown promise in the treatment of cognitive impairment. In a study involving mice, nodakenin reversed scopolamine-induced cognitive impairments and reduced escape latency in the Morris water maze test, suggesting its potential as a therapeutic agent for cognitive disorders. It protects mice from lethal endotoxin shock. It may also have effects on airway remodeling in mouse models of chronic asthma. These in vivo effects support its potential for treating cognitive impairment, inflammatory conditions, and respiratory diseases. |
| Enzyme Assay |
For in vitro biochemical assays, Nodakenin is evaluated for its acetylcholinesterase inhibitory activity. AChE inhibition is measured using Ellman's assay with acetylthiocholine as substrate, determining IC50 values (84.7 μM). Anti-inflammatory activity is assessed by measuring inhibition of TRAF6 and NF-κB activation using cell-free reporter systems or by measuring cytokine production. Neuroprotective activity can be assessed using cell-free assays for oxidative stress or protein aggregation. These cell-free assays help characterize the compound's enzyme inhibitory and anti-inflammatory activities.
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| Cell Assay |
In vitro cellular assays for Nodakenin are performed using macrophage cells for anti-inflammatory studies and neuronal cells for neuroprotection studies. Cells are cultured in standard media and treated with the compound at various concentrations. AChE activity is measured in cell lysates using colorimetric assays. Inflammatory responses are induced by LPS treatment, and cytokine production is measured by ELISA. NF-κB activation is assessed by Western blotting for phosphorylated proteins or by reporter gene assays. Neuroprotection is assessed by measuring cell viability and oxidative stress markers in neuronal cells exposed to neurotoxic insults. These cellular assays help validate the compound's AChE inhibitory and anti-inflammatory activities.
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| Animal Protocol |
Animal/Disease Models: Male ICR mouse
Doses: 2.5, 5, 10 and 20 mg/kg Route of Administration: po, single dose Experimental Results: Scopolamine-induced stepwise latency reversal. In vivo animal experiments with Nodakenin are conducted in mouse models of cognitive impairment, inflammation, and asthma. For cognitive studies, mice are treated with scopolamine to induce cognitive impairment, and Nodakenin is administered orally. Cognitive function is assessed using the Morris water maze test. For inflammation studies, mice are challenged with LPS, and survival and inflammatory markers are measured. For asthma studies, mouse models of chronic asthma are used, and airway remodeling is assessed. The compound's safety and tolerability are monitored through body weight, clinical signs, and histopathology. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Nodakenin have been partially characterized. As a coumarin glycoside with a molecular weight of 408.40, it is expected to have moderate oral bioavailability. The compound's glycoside moiety may affect its absorption and metabolism. Detailed PK parameters such as half-life, Cmax, Tmax, AUC, and protein binding are not extensively documented. Researchers often refer to studies on related coumarin glycosides for pharmacokinetic comparisons. The compound should be stored under recommended conditions to maintain stability.
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| Toxicity/Toxicokinetics |
The toxicological profile of Nodakenin is not extensively characterized. As a natural coumarin glycoside from Angelica species, it is generally considered to have a favorable safety profile, but comprehensive toxicity studies are limited. The compound is intended for research use only and not for human therapeutic applications. Its effects at high concentrations and potential interactions with other drugs or compounds have not been fully investigated. Researchers should follow standard laboratory safety practices when handling Nodakenin. Its AChE inhibitory activity suggests potential for cholinergic side effects at high doses.
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| References |
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| Additional Infomation |
Nodakine is a furanocoumarin. It has been reported to be found in angelica, rhodiola, and other organisms with relevant data.
Nodakenin is a valuable research tool for studying acetylcholinesterase inhibition, neuroprotection, and anti-inflammatory mechanisms. Its AChE inhibition (IC50 = 84.7 μM) makes it useful for investigating cholinergic signaling and developing treatments for Alzheimer's disease and other cognitive disorders. Its suppression of LPS-induced inflammatory responses through TRAF6 and NF-κB pathways provides opportunities for studying inflammation and developing anti-inflammatory agents. The compound's neuroprotective properties make it relevant for neurodegenerative disease research. As a major coumarin glycoside from Angelica species, it is also important for natural product chemistry and quality control of herbal medicines. |
| Molecular Formula |
C20H24O9
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|---|---|
| Molecular Weight |
408.3992
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| Exact Mass |
408.142
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| CAS # |
495-31-8
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| PubChem CID |
73191
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| Appearance |
White to off-white solid
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
635.4±55.0 °C at 760 mmHg
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| Melting Point |
melting at 216°
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| Flash Point |
225.4±25.0 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.651
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| LogP |
-0.66
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
650
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| Defined Atom Stereocenter Count |
6
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| SMILES |
O([C@@]1([H])[C@@]([H])([C@]([H])([C@@]([H])([C@@]([H])(C([H])([H])O[H])O1)O[H])O[H])O[H])C(C([H])([H])[H])(C([H])([H])[H])[C@@]1([H])C([H])([H])C2C([H])=C3C([H])=C([H])C(=O)OC3=C([H])C=2O1
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| InChi Key |
HXCGUCZXPFBNRD-DNLMCPORSA-N
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| InChi Code |
InChI=1S/C20H24O9/c1-20(2,29-19-18(25)17(24)16(23)13(8-21)28-19)14-6-10-5-9-3-4-15(22)27-11(9)7-12(10)26-14/h3-5,7,13-14,16-19,21,23-25H,6,8H2,1-2H3/t13-,14-,16-,17+,18-,19+/m1/s1
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| Chemical Name |
(2R)-2-[2-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxypropan-2-yl]-2,3-dihydrofuro[3,2-g]chromen-7-one
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~244.86 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.12 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 (6.12 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4486 mL | 12.2429 mL | 24.4858 mL | |
| 5 mM | 0.4897 mL | 2.4486 mL | 4.8972 mL | |
| 10 mM | 0.2449 mL | 1.2243 mL | 2.4486 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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