| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Kukoamine A targets trypanothione reductase, an enzyme essential for redox balance in trypanosomatid parasites, with a Ki of 1.8 µM. It also targets pathways involved in inflammation, oxidative stress, and cancer cell proliferation. Its hypotensive activity suggests it may also affect vascular function.
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| ln Vitro |
In vitro, Kukoamine A is a potent inhibitor of trypanothione reductase with a Ki of 1.8 µM. It exhibits anti-inflammatory, antioxidant, anti-diabetic, and anti-cancer activities. It also has hypotensive activity. These diverse activities suggest it may modulate multiple signaling pathways, including those involved in oxidative stress, inflammation, and cell proliferation.
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| ln Vivo |
In vivo, Kukoamine A has been shown to have hypotensive (blood pressure lowering) activity. Its anti-inflammatory and antioxidant properties suggest potential in vivo efficacy in models of inflammation and oxidative stress. Its anti-cancer activity may translate to efficacy in tumor models. Further in vivo studies are needed to fully characterize its therapeutic potential.
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| Enzyme Assay |
In vitro enzyme inhibition assays for Kukoamine A are conducted using purified trypanothione reductase. Enzyme activity is measured by monitoring the reduction of trypanothione disulfide or by using chromogenic substrates. The compound is incubated with the enzyme and substrate at varying concentrations, and Ki values are calculated from dose-response curves using appropriate kinetic models.
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| Cell Assay |
Cellular assays for Kukoamine A are performed using various cell lines to study its anti-inflammatory, antioxidant, and anti-cancer activities. Cells are treated with compound concentrations ranging from 0.1 to 100 µM for 24-72 hours. Inflammatory cytokine production (TNF-α, IL-6) is measured by ELISA. ROS levels are measured using fluorescent probes such as DCFH-DA. Cell viability and proliferation are assessed using MTT or CCK-8 assays.
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| Animal Protocol |
In vivo animal studies for Kukoamine A would typically utilize rodent models of hypertension, inflammation, cancer, or diabetes. The compound is administered orally or intraperitoneally. Blood pressure is measured using tail-cuff or telemetry methods. Inflammatory markers are measured in serum or tissues. Tumor growth is monitored in xenograft models.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Kukoamine A are not well characterized. The compound has a molecular weight of 530.66 and a molecular formula of C₂₈H₄₂N₄O₆. As a natural product-derived compound, it is expected to have moderate oral bioavailability. Standard PK studies in rodents would be required to determine half-life, bioavailability, and tissue distribution.
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| Toxicity/Toxicokinetics |
Toxicological data for Kukoamine A are limited. As a natural product-derived compound, it may have a moderate safety profile. No significant acute toxicity has been reported. The compound is designated for research use only.
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| References | |
| Additional Infomation |
Kukoamine A is an amine substance.
Kukoamine A is a natural spermine analogue from Lycium barbarum that inhibits trypanothione reductase (Ki = 1.8 µM). It has anti-inflammatory, antioxidant, anti-diabetic, anti-cancer, and hypotensive activities. It has a molecular weight of 530.66 and formula C₂₈H₄₂N₄O₆. It is not clinically approved. |
| Molecular Formula |
C28H42N4O6
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|---|---|
| Molecular Weight |
530.6563
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| Exact Mass |
530.31
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| CAS # |
75288-96-9
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| Related CAS # |
Kukoamine A-d8 dihydrochloride
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| PubChem CID |
5318865
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
872.1±65.0 °C at 760 mmHg
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| Flash Point |
481.2±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.588
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| LogP |
-0.17
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
19
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| Heavy Atom Count |
38
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| Complexity |
601
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IOLDDENZPBFBHV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H42N4O6/c33-23-9-5-21(19-25(23)35)7-11-27(37)31-17-3-15-29-13-1-2-14-30-16-4-18-32-28(38)12-8-22-6-10-24(34)26(36)20-22/h5-6,9-10,19-20,29-30,33-36H,1-4,7-8,11-18H2,(H,31,37)(H,32,38)
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| Chemical Name |
3-(3,4-dihydroxyphenyl)-N-[3-[4-[3-[3-(3,4-dihydroxyphenyl)propanoylamino]propylamino]butylamino]propyl]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 : ~125 mg/mL (~235.56 mM)
DMSO : ~100 mg/mL (~188.44 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (188.44 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| 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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