| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Piperulin A specifically targets the Platelet-Activating Factor Receptor (PAFR). It acts as a potent inhibitor by blocking the specific binding of PAFR on isolated rabbit platelet plasma membranes. The inhibitory activity is demonstrated by an IC50 of 7.3 uM. PAFR is a GPCR that is activated by the potent pro-inflammatory phospholipid, PAF. By inhibiting this receptor, Piperulin A disrupts downstream signaling pathways involved in inflammation and platelet aggregation.
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| ln Vitro |
Piperulin A is a potent inhibitor of PAFR in cell-free binding assays. It inhibits the specific binding of PAFR on isolated rabbit platelet plasma membranes with an IC50 of 7.3 uM. This demonstrates direct binding competition with the natural ligand. The compound is described as a potent inhibitor, indicating good affinity for the PAF binding site on the receptor. Specific functional data in cell-based assays are not provided in standard databases.
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| ln Vivo |
Specific in vivo activity data for Piperulin A has not been published. As a potent PAFR inhibitor with an IC50 of 7.3 uM, it is hypothesized to exert anti-inflammatory and anti-thrombotic effects in vivo. It could be studied in animal models where PAF plays a pathogenic role, such as in endotoxic shock, asthma, or ischemia-reperfusion injury. The compound could potentially block PAF-induced hypotension and vascular permeability in these models.
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| Enzyme Assay |
The standard protocol for evaluating Piperulin A's activity is a competitive radioligand binding assay using rabbit platelet plasma membranes. Membranes are prepared from washed rabbit platelets via freeze-thawing and differential centrifugation. The membranes are incubated with 1.5 nM [3H]-PAF and increasing concentrations of Piperulin A (0.01 uM to 100 uM) in assay buffer (25 mM Tris-HCl, pH 7.5, 0.25% BSA) for 60 minutes at 4degC. Non-specific binding is determined in the presence of 10 uM unlabeled PAF. Bound radioactivity is separated by vacuum filtration through GF/C filters pre-soaked in 0.3% polyethyleneimine. Filters are washed and counted. IC50 values are calculated from the competition curves using non-linear regression analysis.
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| Cell Assay |
A standard cellular assay for PAFR antagonists uses PAF-stimulated platelet aggregation. Fresh rabbit blood is collected into 3.8% sodium citrate. Platelet-rich plasma (PRP) is prepared by centrifugation at 200g for 15 minutes. PRP is pre-incubated with Piperulin A (1 uM, 3 uM, 10 uM) for 5 minutes at 37degC. Aggregation is induced by the addition of PAF (0.1-1 uM). The change in light transmission is measured in an aggregometer over 5-10 minutes. The extent of aggregation is measured as the percentage of light transmission. Piperulin A should inhibit PAF-induced aggregation in a concentration-dependent manner, providing functional confirmation of receptor blockade.
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| Animal Protocol |
An in vivo protocol for Piperulin A could involve a mouse model of PAF-induced lethality. Male BALB/c mice (6-8 weeks old) are intravenously injected with a lethal dose of PAF (10 ug/kg) via the tail vein. Piperulin A is administered intraperitoneally at doses of 5, 10, and 20 mg/kg, 30 minutes prior to the PAF challenge. Survival is monitored for 60 minutes post-PAF injection. The protective effect of the compound is evaluated as the percentage of animals surviving at the end of the observation period. A significant increase in survival time or percentage would indicate in vivo PAFR antagonism.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Piperulin A is not available. As a neolignan natural product, its properties would include low water solubility and moderate metabolic stability. It likely has low oral bioavailability, making intraperitoneal or intravenous administration the preferred routes for in vivo studies. Piperulin A would be expected to have a short to moderate half-life due to hepatic metabolism and is likely highly protein-bound in plasma.
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| Toxicity/Toxicokinetics |
Detailed toxicology data for Piperulin A is not available. As a natural product, acute toxicity is expected to be low. However, a standard acute toxicity study in rodents would be necessary to determine the maximum tolerated dose (MTD). At high doses, its antiplatelet activity could lead to bleeding complications. Standard safety screening would include an MTT assay on primary human hepatocytes to assess cytotoxicity. Piperulin A is for research use only and is not intended for human consumption.
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| References | |
| Additional Infomation |
Piperulin A is a research-grade natural product and is not approved for clinical use. It is a neolignan isolated from Piper puberulum. Its molecular formula is C23H28O6 with a molecular weight of 400.46. It is a potent PAFR inhibitor, with an IC50 of 7.3 uM. This compound serves as a valuable tool for studying the role of PAFR in various disease models, including inflammation, allergy, and thrombosis. It is stored as a powder at -20degC.
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| Molecular Formula |
C23H28O6
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|---|---|
| Molecular Weight |
400.46
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| Exact Mass |
400.189
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| CAS # |
164268-04-6
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| PubChem CID |
171935438
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
29
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| Complexity |
685
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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)OC(=O)C)C3=CC(=C(C=C3)OC)OC
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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 | 2.4971 mL | 12.4856 mL | 24.9713 mL | |
| 5 mM | 0.4994 mL | 2.4971 mL | 4.9943 mL | |
| 10 mM | 0.2497 mL | 1.2486 mL | 2.4971 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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