| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Oxysophocarpine targets multiple inflammatory and signaling pathways. It attenuates inflammatory pain by suppressing the phosphorylation of extracellular signal-regulated kinase 1/2 (ERK1/2), cyclooxygenase-2 (COX-2), and reducing levels of prostaglandin E2 (PGE2), tumor necrosis factor α (TNF-α), interleukin-1 beta (IL-1β), and interleukin-6 (IL-6). It inhibits the growth and metastasis of OSCC by targeting the Nrf2/HO-1 axis. It also compromises miR-155 activity by attenuating MAPK and NF-κB pathways. Targets include ERK, COX, PGE, TNF-α, IL receptors, Caspase, GABA receptor, Bcl-2/Bax, and P450 enzymes.
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| ln Vitro |
In vitro, oral squamous cell carcinoma (OSCC) cells of SCC-9 and SCC-15 exhibit reduced migration and swelling when exposed to oxysophocarpine (5 μM) as an inhibitor of swelling.
In vitro, Oxysophocarpine (5 μM) inhibits proliferation and reduces migration and invasion of SCC-9 and SCC-15 oral squamous cell carcinoma cells. It protects neonatal rat primary cultured hippocampal neurons injured by oxygen-glucose deprivation and reperfusion (OGD/RP) at concentrations of 1, 2, and 5 μmol/L. The IC50 of Oxysophocarpine for neuroprotection was found to be 100 μmol/L. Treatment with Oxysophocarpine attenuated neuronal injury in a dose-dependent manner. These activities confirm its neuroprotective and anticancer potential in cell-based models. |
| ln Vivo |
In vivo, Oxysophocarpine induces anti-nociception and increases the expression of GABAA1 receptors in mice. It has been shown to decrease the level of serum transaminase, improve lipid metabolism, and reduce synthesis of inflammatory cytokines TNF-α, TGF-β1, and IL-6 while activating the protective adipocytokine adiponectin, suggesting potential as a drug for colonic inflammation and NASH. In OSCC models, it retards tumor growth and metastasis by targeting the Nrf2/HO-1 axis. These in vivo effects support its therapeutic potential in inflammatory and cancerous conditions.
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| Enzyme Assay |
For in vitro enzyme/receptor binding assays (cell-free), Oxysophocarpine can be evaluated using a variety of purified enzymes and receptors. Kinase inhibition assays can be performed to measure its effect on ERK1/2 phosphorylation using recombinant proteins and specific substrates. COX-2 enzyme activity can be assessed using colorimetric or fluorometric assays that measure prostaglandin production. Receptor binding assays, such as those for GABA receptors, can be conducted using radioligand competition binding with membrane preparations. IC50 values for enzyme inhibition or receptor binding are determined from dose-response curves. These cell-free systems help elucidate the compound's direct molecular targets without cellular interference.
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| Cell Assay |
In vitro cellular assays for Oxysophocarpine typically employ cancer cell lines such as SCC-9 and SCC-15 (OSCC) or primary neuronal cultures. Cells are cultured in appropriate media and treated with the compound at varying concentrations (e.g., 1-5 μM for neuroprotection, or higher for cancer studies). Cell viability is assessed using MTT or CCK-8 assays. Apoptosis is evaluated through flow cytometry using Annexin V/PI staining. Cell migration and invasion are measured using Transwell or wound-healing assays. For neuroprotection studies, neurons are subjected to oxygen-glucose deprivation and reperfusion (OGD/RP), and cell injury is measured by LDH release. Western blotting is performed to detect expression changes in Nrf2, HO-1, MAPK, and NF-κB pathway proteins.
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| Animal Protocol |
In vivo animal experiments with Oxysophocarpine are conducted in mouse models. For anti-nociceptive studies, mice are administered the compound and pain responses are measured. For inflammatory conditions, models such as colitis or NASH are used, with endpoints including serum transaminase levels, lipid profiles, and inflammatory cytokines. For cancer studies, OSCC xenograft models are established by subcutaneous injection of cancer cells, followed by compound administration. Tumor volume and weight are monitored. Endpoint analyses include assessment of Nrf2/HO-1 axis activation, proliferation markers, and apoptosis in tumor tissues. Dosing regimens and routes of administration are determined based on the specific model and study objectives.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Oxysophocarpine have been partially characterized. As a quinolizidine alkaloid with a molecular weight of 262.35, it is expected to have moderate oral bioavailability. The compound is soluble in chloroform, dichloromethane, ethyl acetate, DMSO, and acetone. For in vivo studies, it can be formulated in suitable vehicles. Detailed PK parameters such as half-life, Cmax, Tmax, AUC, and protein binding are less extensively documented. Researchers often refer to general alkaloid pharmacokinetic profiles for experimental design. The compound should be stored as a powder at -20°C for up to three years and in solution at -80°C for up to one year.
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| Toxicity/Toxicokinetics |
The toxicological profile of Oxysophocarpine is not extensively characterized in the available literature. As a natural alkaloid, it may have dose-dependent toxicity at high concentrations. The compound is intended for research use only and not for human therapeutic applications. In animal studies, it has been administered at various doses without significant adverse effects reported, but comprehensive toxicity studies including acute, subchronic, and chronic toxicity assessments are limited. Researchers should follow standard laboratory safety practices when handling Oxysophocarpine. The compound's effects at high concentrations and potential interactions with other drugs or compounds have not been fully investigated.
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| References |
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| Additional Infomation |
Matridin-15-one, 13,14-disehydro-,1-oxide has been reported in Sophora alopecuroides, Sophora viciifolia, and other organisms with available data.
Beyond its primary activities, Oxysophocarpine serves as a valuable research tool for studying the interplay between inflammation and cancer, particularly through the Nrf2/HO-1 and MAPK/NF-κB pathways. It is used to investigate neuroprotective mechanisms in models of excitotoxicity and oxidative stress. The compound's ability to modulate inflammatory cytokines makes it relevant for research into inflammatory bowel disease and non-alcoholic steatohepatitis (NASH). Its anti-nociceptive effects are studied in pain research. Oxysophocarpine is also used as a reference standard in analytical chemistry for the quality control of herbal medicines containing Sophora alkaloids. |
| Molecular Formula |
C15H22N2O2
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| Molecular Weight |
262.3474
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| Exact Mass |
262.168
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| Elemental Analysis |
C, 68.67; H, 8.45; N, 10.68; O, 12.20
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| CAS # |
26904-64-3
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| PubChem CID |
24721085
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| Appearance |
White to off-white solid powder
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| LogP |
-0.41
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
19
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| Complexity |
436
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| Defined Atom Stereocenter Count |
5
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| SMILES |
[O-][N@@+]12C([H])([H])C([H])([H])C([H])([H])[C@@]3([H])C([H])([H])N4C(C([H])=C([H])C([H])([H])[C@]4([H])[C@@]([H])(C([H])([H])C([H])([H])C1([H])[H])[C@@]23[H])=O
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| InChi Key |
QMGGMESMCJCABO-JARXUMMXSA-N
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| InChi Code |
InChI=1S/C15H22N2O2/c18-14-7-1-6-13-12-5-3-9-17(19)8-2-4-11(15(12)17)10-16(13)14/h1,7,11-13,15H,2-6,8-10H2/t11-,12+,13+,15-,17+/m0/s1
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| Chemical Name |
(1R,2R,9S,13R,17S)-13-oxido-7-aza-13-azoniatetracyclo[7.7.1.02,7.013,17]heptadec-4-en-6-one
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| Synonyms |
Oxysophocarpine; (+)-Oxysophocarpine; Sophocarpine N-oxide
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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) |
H2O : ~50 mg/mL (~190.59 mM)
DMSO : ~36.67 mg/mL (~139.78 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (10.48 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 27.5 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: ≥ 2.75 mg/mL (10.48 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 27.5 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: ≥ 2.75 mg/mL (10.48 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 | 3.8117 mL | 19.0585 mL | 38.1170 mL | |
| 5 mM | 0.7623 mL | 3.8117 mL | 7.6234 mL | |
| 10 mM | 0.3812 mL | 1.9059 mL | 3.8117 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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