Aloesone
Based on 1 Customer Validation
Aloesone is an orally active phenolic heptaketide natural product that can cross the blood-brain barrier. Aloesone inhibits LPS-induced oxidative stress, inflammation, M1 polarization and apoptosis in RAW264.7 macrophages by reducing ROS production and NO release, and downregulating the mRNA expression of iNOS, IL-1β and TNF-α. Aloesone also inhibits glutamate-induced neuronal damage and pentylenetetrazol (PTZ)-induced seizures by activating c-SRC.
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- Purity: 99.49%
- CAS No.: 40738-40-7
- 화학식: C13H12O4
- 분자량:232.23
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[2]|
iNOS |
IL-1β |
In Vitro
Aloesone (0.1-1000 μM; 12 h) shows no cytotoxicity in RAW264.7 murine macrophages after 12 h of incubation[1].
Aloesone (0.1-1000 μM; 24 h) is non-toxic to murine hippocampal HT22 cells at concentrations up to 100 μM after 24 h incubation, with reduced viability observed only at 1000 μM[3].
Aloesone (0.1-100 μM; 12 h) activates c-SRC signaling in glutamate-stimulated murine hippocampal HT22 cells after 12 h co-incubation by increasing phosphorylation at Y418 and decreasing phosphorylation at Y529, without changing total c-SRC expression[3].
Aloesone (0.1-100 μM; 2 h pretreatment, followed by 12 h LPS exposure) dose-dependently inhibits LPS-induced oxidative stress in RAW264.7 murine macrophages by reducing ROS production and upregulating Gpx-1 and SOD-1 mRNA expression[1].
Aloesone (0.1-100 μM; 2 h pretreatment, followed by 12 h LPS exposure) inhibits LPS-induced inflammation in RAW264.7 murine macrophages by reducing NO release and downregulating iNOS, IL-1β, and TNF-α mRNA expression[1].
Aloesone (0.1-100 μM; 2 h pretreatment, followed by 12 h LPS exposure) inhibits LPS-induced M1 polarization in RAW264.7 murine macrophages by reducing CD86 surface expression and altering M1-specific cell morphology[1].
Aloesone (0.1-100 μM; 2 h pretreatment, followed by 12 h LPS exposure) dose-dependently inhibits LPS-induced early and late phase apoptosis in RAW264.7 murine macrophages[1].
Aloesone (0.1-100 μM; 12 h) reduces total apoptosis, and at 1 μM specifically reduces early-phase apoptosis, in glutamate-stimulated murine hippocampal HT22 cells after 12 h co-incubation[3].
Aloesone (0.1-100 μM; 2 h pretreatment, followed by 12 h LPS exposure) exerts protective effects in LPS-stimulated RAW264.7 murine macrophages by inhibiting the activation of mTOR, p-mTOR, and HIF-1α, and reducing membrane expression of TLR4[1].
Aloesone (1 μM; 24 h) reduces intracellular ROS levels in glutamate-stimulated murine hippocampal HT22 cells after 24 h co-incubation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:murine macrophage RAW264.7 cells
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Concentration:0.1, 1, 10, 100, 1000 μM
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Incubation Time:12 h
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Result:Did not affect the survival rate of RAW264.7 cells.
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Cell Line:LPS-stimulated murine macrophage RAW264.7 cells
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Concentration:0.1, 1, 10, 100 μM
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Incubation Time:2 h pretreatment
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Result:Prevented LPS-induced early phase apoptosis in a dose-dependent manner.
Reduced LPS-induced late phase apoptosis.
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Cell Line:LPS-stimulated murine macrophage RAW264.7 cells
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Concentration:0.1, 1, 10, 100 μM
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Incubation Time:2 h pretreatment
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Result:Significantly repressed LPS-induced activation of mTOR, p-mTOR, and HIF-1α.
Decreased LPS-induced membrane expression of TLR4.
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Cell Line:murine hippocampal HT22 cells
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Concentration:0.1, 1, 10, 100, 1000 μM
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Incubation Time:24 h
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Result:Did not affect cell viability at 0.1, 1, 10, and 100 μM after 24 h.
Reduced cell viability at 1000 μM after 24 h.
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Cell Line:glutamate-stimulated murine hippocampal HT22 cells
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Concentration:0.1, 1, 10, 100 μM
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Incubation Time:12 h
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Result:Reduced chromatin condensation and nuclear shrinkage.
Decreased total apoptosis rate.
Reduced early-phase apoptosis at 1 μM, with no effect on late-phase apoptosis.
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Cell Line:glutamate-stimulated murine hippocampal HT22 cells
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Concentration:0.1, 1, 10, 100 μM
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Incubation Time:12 h
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Result:Increased fluorescence intensity of phosphorylated c-SRC at Y418.
Decreased fluorescence intensity of phosphorylated c-SRC at Y529.
Did not alter total c-SRC protein levels.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | AUC0-t | AUC0-∞ | T1/2 | MRT0-t | CLz | Vz | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[2] | 1.0 mg/kg | i.v. | 193.4 ng/mL | 0.083 h | 86.08 ng/mL·h | 94.78 ng/mL·h | 1.78 h | 0.71 h | 10.72 mL/h/kg | 26.42 L/kg | / |
| Rat[2] | 10 mg/kg | p.o. | 53.63 ng/mL | 0.083 h | 68.44 ng/mL·h | 119.35 ng/mL·h | 3.07 h | 1.59 h | 96.58 L/h/kg | 433.95 L/kg | 12.59 % |
In Vivo
Aloesone (50 mg/kg; p.o.; administered 30 min prior to each PTZ injection; for 26 consecutive days) suppresses PTZ-induced chronic seizures in rats by reducing seizure scores, prolonging seizure latency, and enhancing c-SRC activation via decreasing Y529 phosphorylation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 250 g, pentylenetetrazol-induced acute seizure model)[3]
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Dosage:50, 100 mg/kg
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Administration:p.o.; single dose
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Result:Prolonged the seizure latent period to 777.60 s, reduced seizure scores to 2.6, and increased survival rate to 80.0%.
Increased phosphorylation of c-SRC at Y418 and decreased phosphorylation at Y529 in the hippocampus.
Reduced seizure scores but did not significantly prolong latent period or improve survival rate, and increased phosphorylation of c-SRC at Y529.
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Animal Model:Sprague-Dawley (male, 250 g, pentylenetetrazol-induced chronic seizure model)[3]
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Dosage:50 mg/kg
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Administration:p.o.; administered 30 minutes prior to each PTZ injection; 26 days
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Result:Did not affect rat body weights over 26 days.
Reduced seizure scores and increased seizure latent period on days 19 and 21 compared to PTZ-only rats.
Decreased phosphorylation of c-SRC at Y529 in the hippocampus.
Chemical Information
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CAS No. 40738-40-7
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Appearance Solid
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분자량 232.23
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화학식 C13H12O4
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Color Off-white to light yellow
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SMILES
O=C1C=C(CC(C)=O)OC2=CC(O)=CC(C)=C12
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Structure Classification
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Initial Source
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (430.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (291 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Wang Y, et al. Multiple Beneficial Effects of Aloesone from on LPS-Induced RAW264.7 Cells, Including the Inhibition of Oxidative Stress, Inflammation, M1 Polarization, and Apoptosis. Molecules (Basel, Switzerland). 2023 Feb 08;28(4):1617. [Content Brief]
[4]. Reza Nazifi SM, et al. Antioxidant properties of Aloe vera components: a DFT theoretical evaluation. Free Radic Res. 2019 Aug;53(8):922-931. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.3061 mL | 21.5304 mL | 43.0608 mL | 107.6519 mL |
| 5 mM | 0.8612 mL | 4.3061 mL | 8.6122 mL | 21.5304 mL | |
| 10 mM | 0.4306 mL | 2.1530 mL | 4.3061 mL | 10.7652 mL | |
| 15 mM | 0.2871 mL | 1.4354 mL | 2.8707 mL | 7.1768 mL | |
| 20 mM | 0.2153 mL | 1.0765 mL | 2.1530 mL | 5.3826 mL | |
| 25 mM | 0.1722 mL | 0.8612 mL | 1.7224 mL | 4.3061 mL | |
| 30 mM | 0.1435 mL | 0.7177 mL | 1.4354 mL | 3.5884 mL | |
| 40 mM | 0.1077 mL | 0.5383 mL | 1.0765 mL | 2.6913 mL | |
| 50 mM | 0.0861 mL | 0.4306 mL | 0.8612 mL | 2.1530 mL | |
| 60 mM | 0.0718 mL | 0.3588 mL | 0.7177 mL | 1.7942 mL | |
| 80 mM | 0.0538 mL | 0.2691 mL | 0.5383 mL | 1.3456 mL | |
| 100 mM | 0.0431 mL | 0.2153 mL | 0.4306 mL | 1.0765 mL |
Aloesone Related Classifications
HY-N8559 Related Classifications
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