| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg | |||
| 25mg |
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| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Alnustone is a potent inhibitor of the Thyroid Adenoma Associated (THADA) function, which reverses THADA-induced β-cell dysfunction and ameliorates hyperglycemia in obese mice. It significantly decreases fed blood glucose and improves glucose tolerance in mice. The compound also inhibits inflammatory mediators like NF-κB, COX-2, and iNOS. The NF-κB signaling pathway is a plausible target for alnustone's anti-inflammatory effects. Additionally, alnustone has been shown to promote megakaryocyte differentiation and platelet production via the interleukin-17A/interleukin-17A receptor/Src/RAC1/MEK/ERK signaling pathway.
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| ln Vitro |
In vitro, alnustone demonstrates antitumor potential by suppressing cancer cell proliferation and inducing apoptosis. It promotes the differentiation and maturation of megakaryocytes in vitro. Alnustone has been shown to inhibit the growth of microorganisms, with an exceptionally low MIC of 1.25 μg/mL against H. pylori. It displays anti-emetic and anti-inflammatory activities. The compound has inhibitory effects against infectious diseases such as malaria. It has been shown to inhibit inflammatory mediators like NF-κB, COX-2, and iNOS, thereby reducing oxidative stress and tissue damage.
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| ln Vivo |
In vivo, alnustone exerts significant anti-inflammatory activity in the carrageenin-induced hind paw edema model in rats, reducing edema by 44.0% at 100 mg/kg i.p. It significantly decreases fed blood glucose and improves glucose tolerance in obese mice. Alnustone restores platelet production in thrombocytopenic mice and zebrafish. It has anti-inflammatory and antiemetic effects. The compound exhibits anti-hyperglycemic, anti-inflammatory, antihepatotoxic and antiemetic activities in vivo.
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| Enzyme Assay |
For non-cellular enzyme/receptor binding assays, standard radioligand binding assays can be employed to assess the compound's affinity for its target, THADA. Competitive binding experiments using labeled ligands and varying concentrations of alnustone are performed to determine the inhibition constant (Ki). Given its inhibition of COX-2 and iNOS, enzyme activity assays using purified COX-2 or iNOS proteins can be conducted to measure direct inhibition. Fluorescent or colorimetric substrate-based assays are commonly used to determine IC50 values.
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| Cell Assay |
For in vitro cell-based assays, cancer cell lines are cultured and treated with various concentrations of alnustone. Cell proliferation is assessed using MTT or similar viability assays. Apoptosis can be evaluated through flow cytometry using Annexin V/PI staining or by assessing caspase activity. For megakaryocyte differentiation studies, cells are treated with alnustone and differentiation markers are assessed. For antimicrobial assays, broth microdilution methods are used to determine minimum inhibitory concentrations (MIC).
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| Animal Protocol |
For in vivo anti-inflammatory evaluation, the carrageenin-induced hind paw edema model in rats is used. Edema is induced by injecting carrageenin into the hind paw. Alnustone is administered orally or intraperitoneally (e.g., 100 mg/kg i.p.), and paw volume is measured plethysmographically at various time points to assess the reduction in edema. For hyperglycemia studies, alnustone is administered to obese mice and fed blood glucose levels and glucose tolerance are measured. For thrombocytopenia models, alnustone is administered to mice or zebrafish and platelet production is assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of alnustone include solubility in DMSO (52 mg/mL, 198.2 mM). It is also soluble in DMSO at 2 mg/mL for clear solution. The compound is a powder that should be stored desiccated at 2-8°C. It is hygroscopic. For in vivo formulation, it can be suspended in CMC-Na solution at 5 mg/mL. The molecular weight is 262.35. Alnustone (Standard) is available as a high-purity analytical standard (≥98% by HPLC).
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| Toxicity/Toxicokinetics |
Toxicological data for alnustone is limited. However, as a natural product, its safety profile is generally considered favorable. It has been shown to reduce oxidative stress and tissue damage, suggesting potential protective effects. No significant toxicity has been reported in preclinical studies at the doses used for efficacy evaluation (e.g., 100 mg/kg i.p.). The compound exhibits antihepatotoxic activities, indicating potential liver-protective effects.
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| References | |
| Additional Infomation |
Alnustone is a diarylheptane compound. It has been reported to exist in turmeric, Hainan turmeric, and other organisms with relevant data.
Alnustone ((4E,6E)-1,7-Diphenyl-4,6-heptadien-3-one) is a natural product with diverse pharmacological activities. It has anti-inflammatory, antihepatotoxic and antiemetic properties. Its potential in treating type-2 diabetes by targeting THADA is an area of active research. It has been shown to inhibit inflammatory mediators like NF-κB, COX-2, and iNOS. It also demonstrates antitumor potential by suppressing cancer cell proliferation and inducing apoptosis. Alnustone promotes megakaryocyte differentiation and platelet production via the IL-17A/IL-17RA/Src/RAC1/MEK/ERK signaling pathway. |
| Molecular Formula |
C19H18O
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|---|---|
| Molecular Weight |
262.35
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| Exact Mass |
262.135
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| CAS # |
33457-62-4
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| PubChem CID |
5317598
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| Appearance |
White to yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
442.9±34.0 °C at 760 mmHg
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| Melting Point |
60.5-61℃
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| Flash Point |
170.9±24.9 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.604
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| LogP |
4.16
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
20
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| Complexity |
328
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)CCC(=O)/C=C/C=C/C2=CC=CC=C2
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| InChi Key |
OWMJDOUOHDOUFG-FNCQTZNRSA-N
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| InChi Code |
InChI=1S/C19H18O/c20-19(16-15-18-11-5-2-6-12-18)14-8-7-13-17-9-3-1-4-10-17/h1-14H,15-16H2/b13-7+,14-8+
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| Chemical Name |
(4E,6E)-1,7-diphenylhepta-4,6-dien-3-one
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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 (~381.17 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (9.53 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8117 mL | 19.0585 mL | 38.1170 mL | |
| 5 mM | 0.7623 mL | 3.8117 mL | 7.6234 mL | |
| 10 mM | 0.3812 mL | 1.9059 mL | 3.8117 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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