| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Kadsurenin B specifically targets the Platelet-Activating Factor (PAF) receptor (PAFR). It acts as an antagonist, blocking the binding of the endogenous pro-inflammatory mediator PAF to its receptor. PAF is involved in numerous pathological processes, including inflammation, thrombosis, and neurodegeneration. By inhibiting this receptor, Kadsurenin B downregulates PAF-mediated signaling cascades.
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| ln Vitro |
In vitro, Kadsurenin B acts as a PAF antagonist. It has a wide range of pharmacological research potential, including antibacterial, anti-inflammatory, neuroprotective, antioxidant, antiplatelet aggregation, and cytotoxic effects. These diverse activities are primarily attributed to its ability to block the PAF receptor, which is a key upstream mediator of many inflammatory and thrombotic pathways. Specific IC50 values for its antagonistic activity are not provided.
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| ln Vivo |
Specific in vivo activity data for Kadsurenin B has not been published. Given its in vitro PAF antagonism, it is hypothesized to exhibit neuroprotective activity in vivo. This could be demonstrated in models of cerebral ischemia-reperfusion injury or traumatic brain injury, where PAF is known to contribute to neuronal damage. Its anti-inflammatory and antioxidant properties also suggest potential in models of chronic inflammatory diseases.
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| Enzyme Assay |
The protocol for assessing PAF antagonism by Kadsurenin B would involve a competitive binding assay using rabbit platelet membranes. Platelets are isolated from fresh rabbit blood, and membranes are prepared via homogenization and differential centrifugation. The membranes (100 ug protein) are incubated with [3H]-PAF (1 nM) and varying concentrations of Kadsurenin B (1 nM to 100 uM) in Tris-HCl buffer containing 0.25% BSA (pH 7.5) for 60 minutes at 4degC. Non-specific binding is determined in the presence of 10 uM unlabeled PAF. Bound radioactivity is collected on GF/C filters and measured. IC50 values are calculated from displacement curves.
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| Cell Assay |
For an in vitro cell-based assay, primary rat microglial cells are isolated from neonatal rat pups. Cells are seeded in 96-well plates and cultured for 7 days. Microglia are pre-treated with Kadsurenin B (1, 5, 10 uM) for 1 hour, then stimulated with lipopolysaccharide (LPS, 100 ng/mL) to induce neuroinflammation. After 24 hours, cell culture supernatants are collected. Nitric oxide (NO) production is measured using the Griess reagent, and pro-inflammatory cytokines (TNF-alpha, IL-1beta, IL-6) are quantified by ELISA. The neuroprotective activity of Kadsurenin B is evaluated by its ability to reduce LPS-induced inflammation in these cells.
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| Animal Protocol |
An in vivo protocol for studying neuroprotection would involve a transient middle cerebral artery occlusion (tMCAO) model in rats. Male Sprague-Dawley rats (250-300g) undergo 90 minutes of MCAO followed by 24 hours of reperfusion. Kadsurenin B is administered intraperitoneally at doses of 5, 10, and 20 mg/kg, given 30 minutes before the onset of ischemia and then immediately after reperfusion. Neurological deficit scores are assessed at 24 hours post-ischemia. Rats are then euthanized, and the brains are harvested. Infarct volume is measured using TTC (2,3,5-triphenyltetrazolium chloride) staining. Neuroprotective activity would be indicated by reduced infarct volume and improved neurological scores.
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| ADME/Pharmacokinetics |
Specific PK data for Kadsurenin B is not available. As a natural lignan, it is likely to have low water solubility and variable oral bioavailability. For in vivo studies, it is typically formulated with vehicles such as DMSO, PEG400, or Tween-80, and administered intraperitoneally or intravenously. Its metabolic stability would be influenced by CYP450-mediated oxidation and conjugation reactions.
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| Toxicity/Toxicokinetics |
Detailed toxicology data for Kadsurenin B is not available. As a natural product with multiple proposed activities, its safety profile would need to be established. Standard acute toxicity studies in mice would be required to determine the LD50. The wide range of biological activities suggests potential for off-target effects at high doses. However, as a PAF antagonist, it is not expected to have overt cytotoxicity at low micromolar concentrations.
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| References | |
| Additional Infomation |
Kadsurenin B is a research-grade natural product and is not approved for clinical use. Its molecular formula is C20H22O5 with a molecular weight of 342.39. It is a lignan naturally found in plants such as Piper kadsura. The compound shows potential for antibacterial, anti-inflammatory, neuroprotective, antioxidant, antiplatelet aggregation, cytotoxic, and antiparasitic research. Its value lies in its broad-spectrum activity and its role as a tool to study PAF receptor biology. It is provided as a powder stored at -20degC.
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| Molecular Formula |
C20H22O5
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|---|---|
| Molecular Weight |
342.385686397552
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| Exact Mass |
342.147
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| CAS # |
145701-13-9
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| PubChem CID |
102481771
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| Appearance |
Typically exists as solid at room temperature
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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 |
4
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| Heavy Atom Count |
25
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| Complexity |
599
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[C@@H]1[C@H]([C@H]2C([C@@]1(C=C(C2=O)CC=C)OC)O)C3=CC4=C(C=C3)OCO4
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9206 mL | 14.6032 mL | 29.2065 mL | |
| 5 mM | 0.5841 mL | 2.9206 mL | 5.8413 mL | |
| 10 mM | 0.2921 mL | 1.4603 mL | 2.9206 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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