| Size | Price | |
|---|---|---|
| 1mg | ||
| Other Sizes |
| Targets |
Superoxide anion (inhibitor of generation) and elastase (inhibitor of release). Aristololactam IIIa targets these two inflammatory mediators, though the exact molecular target is not always specified. It inhibits the respiratory burst in neutrophils and the degranulation process that releases elastase.
|
|---|---|
| ln Vitro |
Aristololactam IIIa exhibits significant inhibitory effects on superoxide anion generation and elastase release with IC50 values of 0.12 ug/mL and 0.20 ug/mL, respectively. Superoxide anion is a reactive oxygen species produced by activated neutrophils during inflammation, and elastase is a protease released from neutrophil granules that can damage tissue. The compound's inhibition of these two key inflammatory mediators suggests a dual anti-inflammatory mechanism.
|
| ln Vivo |
In vivo activity data for Aristololactam IIIa are not detailed in the supplier literature. Based on its in vitro mechanism of action, it has potential applications in animal models of acute and chronic inflammatory diseases where neutrophil activation contributes to pathology, such as acute lung injury (ALI), rheumatoid arthritis, and inflammatory bowel disease. Further in vivo studies are needed to characterize its efficacy, pharmacokinetics, and safety profile.
|
| Enzyme Assay |
For non-cellular assays, the generation of superoxide anion is measured in a cell-free system using xanthine and xanthine oxidase, which produce superoxide. The superoxide is detected by the reduction of cytochrome c (increase in absorbance at 550 nm) or by luminol chemiluminescence. Aristololactam IIIa is added at varying concentrations (0.01-10 ug/mL), and the IC50 for superoxide inhibition is calculated from the dose-response curve. For elastase release, purified elastase is used.
|
| Cell Assay |
Cellular assays utilize isolated human neutrophils or neutrophil-like cell lines (e.g., differentiated HL-60 cells). The cells are pre-incubated with Aristololactam IIIa (0.01-10 ug/mL) for 10-15 minutes. Superoxide anion generation is then stimulated with a phorbol ester (PMA) or a chemotactic peptide (fMLP), and the superoxide is measured by cytochrome c reduction in the culture media. Elastase release is measured in the supernatant following stimulation with cytochalasin B and fMLP, using a chromogenic or fluorogenic elastase substrate. The IC50 values are calculated from dose-response curves.
|
| Animal Protocol |
In vivo efficacy studies could be performed in a mouse model of acute lung injury (ALI), induced by intratracheal instillation of LPS or carrageenan. Aristololactam IIIa would be administered intraperitoneally or intravenously prior to or after the challenge. Bronchoalveolar lavage fluid (BALF) would be collected to measure superoxide anion levels (by luminol chemiluminescence) and elastase activity (by a fluorogenic substrate). The number of neutrophils in the BALF would be counted, and lung tissue would be examined histologically for inflammation.
|
| ADME/Pharmacokinetics |
Aristololactam IIIa has a molecular formula of C16H9NO4 and a molecular weight of 279.25 g/mol. It is a natural product. The compound is typically soluble in DMSO. It is stored as a solid at -20degC, protected from light. Detailed pharmacokinetic parameters (half-life, oral bioavailability, tissue distribution) are not reported in the supplier literature. It is supplied as a lyophilized powder.
|
| Toxicity/Toxicokinetics |
No detailed toxicological data for Aristololactam IIIa are available in the supplier literature. As a natural product, its safety profile is not well-characterized. It is intended for research use only and not for human consumption. Standard safety precautions for handling research chemicals should be followed, including the use of gloves and eye protection. Some aristololactams are known to have nephrotoxic and genotoxic properties, so caution is advised.
|
| References | |
| Additional Infomation |
Aristolochia IIIa has been reported to be found in Aristolochia debilis, Aristolochia kaempferi, and other organisms with available data.
Aristololactam IIIa is a natural product isolated from Aristolochia plants, which have been used in traditional medicine but are also known to contain aristolochic acids, which are nephrotoxic and carcinogenic. This specific lactam is used as a research probe for anti-inflammatory activity. The compound is not an FDA-approved drug. |
| Molecular Formula |
C16H9NO4
|
|---|---|
| Molecular Weight |
279.246964216232
|
| Exact Mass |
279.053
|
| CAS # |
97399-89-8
|
| PubChem CID |
5319620
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
2.8
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
21
|
| Complexity |
469
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1OC2=C(O1)C3=C4C=C(C=CC4=CC5=C3C(=C2)C(=O)N5)O
|
| InChi Key |
XCYLMCOZDQCDRH-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H9NO4/c18-8-2-1-7-3-11-13-10(16(19)17-11)5-12-15(21-6-20-12)14(13)9(7)4-8/h1-5,18H,6H2,(H,17,19)
|
| Chemical Name |
16-hydroxy-3,5-dioxa-10-azapentacyclo[9.7.1.02,6.08,19.013,18]nonadeca-1(18),2(6),7,11(19),12,14,16-heptaen-9-one
|
| 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
|
|---|---|
| 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 | 3.5810 mL | 17.9051 mL | 35.8102 mL | |
| 5 mM | 0.7162 mL | 3.5810 mL | 7.1620 mL | |
| 10 mM | 0.3581 mL | 1.7905 mL | 3.5810 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
