| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
NO Synthase (indirect inhibition of NO production).
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|---|---|
| ln Vitro |
Schiarisanrin A inhibits NO production in LPS‑stimulated BV‑2 mouse microglial cells with an IC50 of 9.6 microM, about 1.5‑fold more potent than Kadsulignan H, demonstrating concentration‑dependent suppression of nitrite accumulation without significant cytotoxicity at active concentrations.
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| ln Vivo |
No in vivo activity data available. For similar NO inhibitors, typical in vivo models include LPS‑induced endotoxemia in mice (e.g., 5 mg/kg LPS i.p.) with test compound administered prior to LPS challenge; serum NOx levels and pro‑inflammatory cytokines (TNF‑alpha, IL‑1beta, IL‑6) are measured 4‑6 hours post‑challenge.
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| Enzyme Assay |
Not available. Generic protocol: Recombinant murine iNOS (0.1‑0.5 units) is incubated with 10 microM L‑arginine, 1 mM NADPH, and varying concentrations of test compound in assay buffer (50 mM Tris‑HCl, pH 7.4, 10 microM FAD, 10 microM FMN). After 30‑60 min at 37degC, NO production is quantified by Griess reaction or by measuring conversion of [3H]‑arginine to [3H]‑citrulline.
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| Cell Assay |
BV-2 mouse microglial cells (5×10⁴/well in 96‑well plates) were cultured overnight, then stimulated with LPS (1 microg/mL) and treated with Schiarisanrin A at 0‑100 microM for 24‑48 h. Supernatant nitrite levels were determined by Griess assay (OD 540 nm). Cell viability was assessed by MTT assay to ensure that observed NO inhibition was not due to cytotoxicity.
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| Animal Protocol |
No published animal data for Schiarisanrin A. A generic protocol: Female C57BL/6 mice (6‑8 weeks) receive LPS (10 mg/kg, i.p.) to induce systemic inflammation. Test compound is administered orally or intraperitoneally 1‑2 h before LPS challenge. Blood is collected via cardiac puncture 4‑6 h later; serum is separated for nitrite/nitrate measurement using Griess reagent kit.
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| ADME/Pharmacokinetics |
No PK data reported. A generic PK study for small molecule NO inhibitors: Male SD rats (n=3 per time point) receive single intravenous (2‑5 mg/kg) or oral (10‑20 mg/kg) dose. Blood samples (0.1‑0.2 mL) are collected at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 12, and 24 h post‑dose. Plasma concentrations are analyzed by LC‑MS/MS, and PK parameters (t1/2, Cmax, Tmax, AUC, CL, Vd, F%) are calculated by non‑compartmental analysis.
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| Toxicity/Toxicokinetics |
No toxicity data reported. Generic subchronic toxicity protocol: Rats receive daily oral doses (10, 30, 100 mg/kg) for 28 days, with monitoring of body weight, food consumption, hematology (CBC), serum chemistry (ALT, AST, BUN, creatinine), and histopathology of major organs (liver, kidney, heart, lung, spleen).
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| References | |
| Additional Infomation |
According to reports, KadsulignanJ has records and relevant data in Kadsura.
Schiarisanrin A is a natural product research tool for studying NO‑mediated inflammation in microglial cells. Its potency (IC50 9.6 microM) suggests potential anti‑inflammatory applications, but no clinical development or regulatory approvals exist. The compound is structurally characterized by a dibenzocyclooctadiene skeleton typical of Schisandra lignans. |
| Molecular Formula |
C27H32O8
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|---|---|
| Molecular Weight |
484.54
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| Exact Mass |
483.202
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| CAS # |
130252-41-4
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| PubChem CID |
145709656
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.179
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
35
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| Complexity |
940
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| Defined Atom Stereocenter Count |
5
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| SMILES |
O1C2=C3C(=CC4C(C(C)C(C)CC5=CC(=C(C([C@]5(C1)C=42)=O)OC)OC)OC(C(C)CC)=O)OCO3
|
| InChi Key |
JHTGXHCLRHKLER-ZPNZURAVSA-N
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| InChi Code |
InChI=1S/C27H32O8/c1-7-13(2)26(29)35-21-15(4)14(3)8-16-9-18(30-5)23(31-6)25(28)27(16)11-32-24-20(27)17(21)10-19-22(24)34-12-33-19/h9-10,13-15,21H,7-8,11-12H2,1-6H3/t13-,14+,15+,21+,27-/m0/s1
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| Chemical Name |
[(1S,12R,13R,14R)-18,19-dimethoxy-13,14-dimethyl-20-oxo-3,6,8-trioxapentacyclo[9.9.1.01,16.04,21.05,9]henicosa-4(21),5(9),10,16,18-pentaen-12-yl] (2S)-2-methylbutanoate
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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 | 2.0638 mL | 10.3191 mL | 20.6381 mL | |
| 5 mM | 0.4128 mL | 2.0638 mL | 4.1276 mL | |
| 10 mM | 0.2064 mL | 1.0319 mL | 2.0638 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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