| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Kukoamine B targets both lipopolysaccharides (LPS) and oligodeoxynucleotides containing CpG motifs (CpG DNA). It acts as a dual inhibitor with Kd values of 1.23 µM for LPS and 0.66 µM for CpG DNA. By inhibiting these two key inflammatory triggers, Kukoamine B suppresses pro-inflammatory signaling and cytokine expression induced by LPS and CpG DNA. This dual inhibition is a unique mechanism that has potential for the treatment of sepsis and other inflammatory conditions.
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| ln Vitro |
In vitro, Kukoamine B inhibits both lipopolysaccharides (LPS) and CpG DNA. It binds to LPS with a Kd of 1.23 µM and to CpG DNA with a Kd of 0.66 µM. By inhibiting these two molecules, Kukoamine B suppresses the pro-inflammatory signaling and cytokine expression they induce. The compound also demonstrates antioxidant activity. These in vitro activities support its potential as an anti-inflammatory and anti-sepsis agent.
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| ln Vivo |
In vivo, Kukoamine B has been shown to inhibit inflammation in septic mice. It reduces the concentrations of plasma LPS, decreases leukocyte sequestration, and interferes with NFκB activation, thereby suppressing the proadhesive phenotype of endothelial cells. In animal models of sepsis, Kukoamine B improves survival rates. These findings demonstrate its in vivo efficacy in reducing inflammation and improving outcomes in sepsis models, supporting its potential as a therapeutic agent for sepsis.
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| Enzyme Assay |
The in vitro binding assay for Kukoamine B typically measures its affinity for LPS and CpG DNA. These assays can be performed using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) to determine the dissociation constant (Kd). Alternatively, competition binding assays using labeled LPS or CpG DNA can be used. These cell-free assays provide a direct measure of the compound's binding affinity to its targets without the confounding effects of cellular metabolism or signaling pathways.
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| Cell Assay |
In vitro cellular assays for Kukoamine B assess its ability to inhibit LPS- and CpG DNA-induced pro-inflammatory signaling. Immune cells, such as macrophages, are stimulated with LPS or CpG DNA in the presence of various concentrations of the compound. The production of pro-inflammatory cytokines (e.g., TNF-α, IL-6) is measured using ELISA or other immunoassays. NFκB activation can also be assessed. These assays demonstrate the compound's ability to suppress inflammatory responses in a relevant cellular context.
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| Animal Protocol |
In vivo animal studies for Kukoamine B have been conducted in mouse models of sepsis. Sepsis is induced by administration of LPS and CpG DNA, and Kukoamine B is administered to assess its protective effects. Endpoints include survival rates, plasma LPS concentrations, leukocyte sequestration, and NFκB activation. The compound's ability to improve survival and reduce inflammation in these models demonstrates its potential as a therapeutic agent for sepsis and other inflammatory conditions.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Kukoamine B Mesylate are not extensively detailed in the available literature. As a mesylate salt, it would have enhanced aqueous solubility. However, the compound's oral bioavailability, half-life, and distribution are not specified. Its ability to exert anti-inflammatory effects in vivo suggests that it reaches sufficient systemic concentrations to be effective. The pharmacokinetic properties would be important for its development as a therapeutic agent.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Kukoamine B Mesylate are not extensively detailed in the available literature. As a natural product-derived compound with anti-inflammatory activity, its toxicity profile is likely favorable. However, preclinical toxicology studies would be required to assess its safety margin for therapeutic use. The compound's dual inhibition of LPS and CpG DNA suggests a targeted mechanism that may limit off-target effects. Without specific data, a detailed toxicity profile cannot be provided.
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| References | |
| Additional Infomation |
Kukoamine B is an amine compound. It has been reported that Kukoamine B is found in potatoes (Solanum tuberosum) and wolfberries (Lycium chinense), and relevant data are available for reference.
Kukoamine B Mesylate is a research compound that has been investigated for the treatment of sepsis and other inflammatory conditions. Its unique mechanism of action involves dual inhibition of LPS and CpG DNA, two key inflammatory triggers. The compound has demonstrated anti-inflammatory effects in vitro and in vivo and has potential for the study of sepsis. It is a natural product-derived alkaloid and is not approved for clinical use. It is intended for research purposes only. |
| Molecular Formula |
C28H42N4O6
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|---|---|
| Molecular Weight |
530.6563
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| Exact Mass |
530.31
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| CAS # |
164991-67-7
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| Related CAS # |
Kukoamine B-d5 dihydrochloride
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| PubChem CID |
10346914
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
844.3±65.0 °C at 760 mmHg
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| Flash Point |
464.4±34.3 °C
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| Vapour Pressure |
0.0±3.3 mmHg at 25°C
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| Index of Refraction |
1.599
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| LogP |
1.5
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
38
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| Complexity |
669
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IWRAOCFRRTWUDF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H42N4O6/c29-13-3-18-32(28(38)12-8-22-6-10-24(34)26(36)20-22)17-2-1-14-30-15-4-16-31-27(37)11-7-21-5-9-23(33)25(35)19-21/h5-6,9-10,19-20,30,33-36H,1-4,7-8,11-18,29H2,(H,31,37)
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| Chemical Name |
N-[3-[4-[3-aminopropyl-[3-(3,4-dihydroxyphenyl)propanoyl]amino]butylamino]propyl]-3-(3,4-dihydroxyphenyl)propanamide
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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) |
H2O : ~62.5 mg/mL (~117.78 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (94.22 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8844 mL | 9.4222 mL | 18.8445 mL | |
| 5 mM | 0.3769 mL | 1.8844 mL | 3.7689 mL | |
| 10 mM | 0.1884 mL | 0.9422 mL | 1.8844 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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