| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
NO Synthase (indirect inhibition of NO production).
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|---|---|
| ln Vitro |
Kadsulignan H inhibits NO production in LPS-stimulated BV-2 mouse microglial cells with an IC50 of 14.1 microM, suggesting its potential as an anti‑neuroinflammatory agent by reducing excessive NO release.
|
| ln Vivo |
No in vivo activity data available for Kadsulignan H. In general, lignans with NO inhibitory activity may be evaluated in murine models of inflammation or neuroinflammation (e.g., LPS‑induced systemic inflammation) with measurement of plasma NOx levels.
|
| Enzyme Assay |
Not available. Generic procedure: Recombinant NOS enzyme incubated with L‑arginine, NADPH, and test compound; NO production measured via Griess reaction or fluorometric method. Inhibition calculated by comparing NO formation in test vs. control wells.
|
| Cell Assay |
BV-2 mouse microglial cells were seeded in 96‑well plates, stimulated with LPS (1 microg/mL) and treated with Kadsulignan H at varying concentrations (e.g., 0‑100 microM). After 24‑48 h, culture supernatants were collected and nitrite (NO metabolite) was measured using the Griess assay. Cell viability assessed by MTT or CCK‑8 to exclude cytotoxicity.
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| Animal Protocol |
No published animal experiments are available for Kadsulignan H. A generic protocol for NO inhibitors: Female BALB/c mice (6‑8 weeks) are injected with LPS (5 mg/kg, i.p.) to induce systemic inflammation. Test compound is administered (e.g., 10‑50 mg/kg, i.p. or p.o.) 1 h before LPS challenge. Blood is collected 4‑6 h later, and serum nitrite/nitrate levels are measured.
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| ADME/Pharmacokinetics |
No pharmacokinetic data reported for Kadsulignan H. For similar lignans, PK studies in rats typically involve intravenous and oral administration (e.g., 5‑20 mg/kg), with blood collected at serial time points. Plasma concentrations are analyzed by LC‑MS/MS to determine parameters such as t1/2, Cmax, Tmax, AUC, and oral bioavailability.
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| Toxicity/Toxicokinetics |
No toxicity data reported. A generic acute toxicity study: mice receive single escalating doses (e.g., 100‑1000 mg/kg, i.p. or p.o.) and are observed for 14 days for mortality, body weight changes, and clinical signs. Gross necropsy is performed at study termination.
|
| References | |
| Additional Infomation |
According to reports, Kadsulignan H has been discovered in Kadsura, and there is relevant data.
This natural lignan is primarily a research biochemical tool for studying NO‑mediated inflammation, with no clinical development or approved therapeutic use reported. Its mechanism involves inhibition of NO production in microglia, potentially via downregulation of iNOS expression rather than direct enzyme inhibition. |
| Molecular Formula |
C26H30O8
|
|---|---|
| Molecular Weight |
470.51
|
| Exact Mass |
470.194
|
| CAS # |
144049-91-2
|
| PubChem CID |
145709337
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
4.119
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
34
|
| Complexity |
909
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
O1C2=C3C(=CC4C(C(C)C(C)CC5=CC(=C(C([C@]5(C1)C=42)=O)OC)OC)OC(CCC)=O)OCO3
|
| InChi Key |
KYPYUTUECVZWHD-WGUADZDVSA-N
|
| InChi Code |
InChI=1S/C26H30O8/c1-6-7-19(27)34-21-14(3)13(2)8-15-9-17(29-4)23(30-5)25(28)26(15)11-31-24-20(26)16(21)10-18-22(24)33-12-32-18/h9-10,13-14,21H,6-8,11-12H2,1-5H3/t13-,14-,21-,26+/m1/s1
|
| 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] butanoate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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 | 2.1254 mL | 10.6268 mL | 21.2535 mL | |
| 5 mM | 0.4251 mL | 2.1254 mL | 4.2507 mL | |
| 10 mM | 0.2125 mL | 1.0627 mL | 2.1254 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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