| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Kumujian A targets inflammatory pathways by inhibiting superoxide anion generation and elastase release. Superoxide anion is a reactive oxygen species (ROS) produced by activated inflammatory cells such as neutrophils and macrophages, and it plays a key role in oxidative stress and tissue damage during inflammation. Elastase is a proteolytic enzyme released by neutrophils that contributes to tissue remodeling and inflammation. By inhibiting both superoxide anion generation and elastase release, Kumujian A reduces oxidative stress and inflammatory tissue damage. The compound's anti-inflammatory activity makes it a valuable tool for studying the mechanisms of inflammation and for developing new anti-inflammatory agents.
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| ln Vitro |
Kumujian A inhibits superoxide anion generation with an IC₅₀ of 4.87 μg/mL. It inhibits elastase release with an IC₅₀ of 6.29 μg/mL. These activities demonstrate the compound's potent anti-inflammatory effects, particularly in the context of neutrophil-mediated inflammation. The compound's ability to inhibit both ROS production and proteolytic enzyme release suggests a dual mechanism of action that may be more effective than single-target anti-inflammatory agents. Specific in vitro activity data for other biological targets are not extensively documented.
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| ln Vivo |
In vivo activity data for Kumujian A are limited in the available literature. Based on its potent in vitro inhibition of superoxide anion generation and elastase release, the compound is anticipated to have potential in vivo efficacy in models of acute and chronic inflammation. However, specific animal studies detailing its therapeutic effects, dosing, and pharmacokinetics are not extensively documented. The compound is primarily used as a research tool for studying inflammatory mechanisms.
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| Enzyme Assay |
Non-cellular assays for Kumujian A typically involve measuring its ability to inhibit superoxide anion generation and elastase release in cell-free systems. For superoxide anion inhibition, a cell-free assay using xanthine oxidase and hypoxanthine as a substrate can be employed. The production of superoxide anion is measured by the reduction of cytochrome c or by using a chemiluminescent probe. For elastase inhibition, purified human neutrophil elastase is incubated with a chromogenic or fluorogenic substrate in the presence of varying concentrations of Kumujian A. The cleavage of the substrate is measured, and IC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
In vitro cellular assays for Kumujian A typically use human neutrophils or neutrophil-like cell lines. Cells are stimulated with a potent activator such as N-formylmethionyl-leucyl-phenylalanine (fMLP) or phorbol 12-myristate 13-acetate (PMA) to induce superoxide anion generation and elastase release. Cells are pre-treated with various concentrations of Kumujian A, and superoxide anion production is measured by the reduction of cytochrome c or by using a chemiluminescent probe. Elastase release is measured by incubating the cell supernatant with a chromogenic or fluorogenic substrate. IC₅₀ values are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for Kumujian A are not extensively documented in the available literature. Based on its anti-inflammatory mechanism, typical study designs would involve rodent models of acute inflammation such as carrageenan-induced paw edema or zymosan-induced peritonitis. Kumujian A would be administered orally or intraperitoneally. Efficacy endpoints would include measurement of inflammatory markers in the inflamed tissue, assessment of edema or inflammatory cell infiltration, and analysis of oxidative stress parameters.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Kumujian A are not extensively characterized. As a small molecule with a molecular weight of 240.26 and a LogP of 2.892, it is expected to have moderate lipophilicity and reasonable membrane permeability. The compound is soluble in DMSO at concentrations up to 100 mg/mL. For in vivo administration, it can be formulated in vehicles such as DMSO, Tween-80, and saline. Specific PK parameters such as half-life, bioavailability, and volume of distribution are not documented in the available literature.
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| Toxicity/Toxicokinetics |
Toxicological data for Kumujian A are limited in the available literature. As a naturally occurring β-carboline alkaloid, it is generally considered to have moderate toxicity. β-Carboline alkaloids can have neuroactive properties and may interact with various receptors in the central nervous system. However, comprehensive toxicology studies are not available. The compound may cause skin and eye irritation upon contact. Standard laboratory safety precautions should be observed when handling this compound. It is intended for research use only and not for human consumption.
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| References | |
| Additional Infomation |
It has been reported that ginseng and sophora flavescens contain 1-ethoxycarbonyl-β-carboline, and there is relevant data on this.
Kumujian A is a research-grade natural product intended for laboratory use only and is not approved for clinical use. Its CAS number is 72755-19-2. The primary applications of Kumujian A include studying the mechanisms of inflammation and oxidative stress, investigating the role of superoxide anion and elastase in inflammatory diseases, and exploring the pharmacological potential of β-carboline alkaloids. The compound is isolated from Picrasma quassioides and is also known as 1-Ethoxycarbonyl-β-carboline. Kumujian A is a valuable tool for natural product chemistry and pharmacology research. |
| Molecular Formula |
C14H12N2O2
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|---|---|
| Molecular Weight |
240.25728
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| Exact Mass |
240.09
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| CAS # |
72755-19-2
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| PubChem CID |
11701473
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| Appearance |
Light yellow to orange solid powder
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| Density |
1.308±0.06 g/cm3 (20 ºC 760 Torr)
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| Melting Point |
145-146 ºC
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| LogP |
2.892
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
321
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC(=O)C1=NC=CC2=C1NC3=CC=CC=C23
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| InChi Key |
CFXOOHNXLDSCHT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H12N2O2/c1-2-18-14(17)13-12-10(7-8-15-13)9-5-3-4-6-11(9)16-12/h3-8,16H,2H2,1H3
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| Chemical Name |
ethyl 9H-pyrido[3,4-b]indole-1-carboxylate
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~100 mg/mL (~416.22 mM)
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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 | 4.1622 mL | 20.8108 mL | 41.6216 mL | |
| 5 mM | 0.8324 mL | 4.1622 mL | 8.3243 mL | |
| 10 mM | 0.4162 mL | 2.0811 mL | 4.1622 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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