6'''-Feruloylspinosin
Based on 1 Customer Validation
6'''-Feruloylspinosin is an orally active RORα activator that crosses the blood-brain barrier, with a Kd of 0.308 μM, and is found in natural sources. 6'''-Feruloylspinosin modulates AMPK and mTOR phosphorylation. 6'''-Feruloylspinosin promotes autophagy through the AMPK/mTOR signaling pathway, inhibits GSK3β phosphorylation at Tyr216, and activates the PGC-1α/Nrf2/HO-1 pathway. 6'''-Feruloylspinosin regulates neurotransmitter levels, enhances mRNA expression of GABAA α1, α5, and GABAB R1 receptor subunits, increases brain 5-HT and GABA, restores melatonin levels, and ameliorates anxiety-like behaviors. 6'''-Feruloylspinosin regulates oxidative stress homeostasis, inhibits mitochondrial dysfunction, decreases MDA while increasing GSH. 6'''-Feruloylspinosin can be used for research on Alzheimer's disease, acute myocardial infarction, heart failure with insomnia, and insomnia.
For research use only. We do not sell to patients.
- Purity : 99.65%
- CAS No.: 77690-92-7
- Formula: C38H40O18
- Molecular Weight:784.71
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Storage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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RORα 0.308 μM (Kd) |
AMPK |
mTOR |
GSK3β |
PGC-1α |
Nrf2 |
HO-1 |
GABA |
5-HT |
MDA |
GSH |
In Vitro
6'''-Feruloylspinosin (1-40 μM) dose-dependently protects SH-SY5Y cells against Aβ1-42-induced cytotoxicity[1].
6'''-Feruloylspinosin (10 μM) enhances autophagy in SH-SY5Y cells, thereby exerting a protective effect against Aβ1-42-induced damage[1].
6'''-Feruloylspinosin (5-20 μM) attenuates Aβ1-42-induced mitochondrial dysfunction in SH-SY5Y cells, including improving MMP, reducing ROS, restoring ATP levels, and normalizing the expression of mitochondrial marker proteins[1].
6'''-Feruloylspinosin (10 μM) activates the AMPK pathway and inhibits the mTOR pathway in SH-SY5Y cells to regulate autophagy and protect against Aβ1-42-induced damage[1].
6'''-Feruloylspinosin directly binds to recombinant RORα with a Kd of 3.08 × 10-7 M[3].
6'''-Feruloylspinosin (10 μM; 6 h) stabilizes RORα in cardiomyocytes[3].
6'''-Feruloylspinosin (5-20 μM; 48 h) attenuates Ang II-induced hypertrophy and restores RORα expression in neonatal rat cardiomyocytes[3].
6'''-Feruloylspinosin (32-128 µM; 24 h) enhances the mRNA expression of GABAA α1, GABAA α5, and GABAB R1 in cultured rat hippocampal neurons in a dose-dependent manner[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Cultured rat hippocampal neurons
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Concentration:32 µM; 64 µM; 128 µM
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Incubation Time:24 h
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Result:Enhanced the mRNA expression of GABAA α1, GABAA α5, and GABAB R1 in cultured rat hippocampal neurons in a dose-dependent manner.
Parmacokinetics
| Species | Dose | Route | Cmax | T1/2 | AUC0-t | AUC0-∞ | MRT0-∞ |
|---|---|---|---|---|---|---|---|
| Rat[4] | 5 mg/kg | i.v. | 4060.58 ng/mL | 2.25 h | 2669.5 ng·h/mL | 2803.31 ng·h/mL | 0.98 h |
In Vivo
6'''-Feruloylspinosin (8 mg/kg/day; i.g.; daily; 28 days) activates RORα to mitigate pressure overload-induced heart failure with comorbid insomnia by improving cardiac function, reducing hypertrophy, and normalising sleep behaviours and neurochemical imbalances[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar albino rats (male, 8-10 weeks, 250-300 g, AMI induced by LAD occlusion for 30 min followed by 1 h reperfusion)[2]
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Dosage:5 mg/kg
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Administration:i.p.; single dose; 30 min before surgery
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Result:Reduced serum cTnI levels from 662.0 to 429.2 pg/mL.
Reduced serum LDH activity from 61286 to 48270 U/mL.
Reduced apoptotic myocardial cells from 55.3% to 38.1%.
Increased LC3B-II levels and decreased p62 levels.
Decreased GSK3β phosphorylation at Tyr216 and enhanced PGC-1α, Nrf2, and HO-1 expressions.
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Animal Model:C57BL/6 mice (male, 6-8 weeks old, 22-24 g, TAC surgery plus CUMS and PCPA administration)[3]
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Dosage:2 mg/kg/day; 4 mg/kg/day; 8 mg/kg/day
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Administration:i.g.; daily; 28 days
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Result:Improved left ventricular ejection fraction, left ventricular fractional shortening, and stroke volume.
Attenuated increased interventricular septal thickness diastole, left ventricular mass, left ventricular volume diastole, and relative wall thickness.
Ameliorated disrupted myofilament organisation, cytoplasmic vacuolisation, inflammatory cell infiltration, and reduced collagen fibre accumulation.
Decreased elevated serum levels of NT-proBNP and cardiac troponin-T.
Reduced the cross-sectional area of cardiomyocytes and decreased both HW/TL and HW/BW ratios.
Suppressed the mRNA expression of hypertrophy markers ANP, BNP, and MYH7.
Restored normal locomotor activity and significantly increased centre distance and duration time.
Normalised the prolonged sleep latency and enhanced sleep duration.
Significantly reduced immobility time.
Elevated cerebral levels of 5-HT and GABA.
Attenuated neuronal degeneration, reduced CD68+ macrophage infiltration, decreased the levels of inflammatory cytokines IL-1β and TNF-α, and restored tight junction integrity by enhancing ZO-1 and occludin expression.
Significantly up-regulated RORα expression in heart and brain tissues and restored melatonin levels in brain tissue.
Chemical Information
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CAS No. 77690-92-7
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Appearance Solid
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Molecular Weight 784.71
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Formula C38H40O18
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Color Off-white to yellow
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SMILES
O[C@@H]1[C@H]([C@H](C(C(O)=C(C2=O)C(OC(C3=CC=C(O)C=C3)=C2)=C4)=C4OC)O[C@H](CO)[C@H]1O)O[C@]([C@@H]([C@@H](O)[C@@H]5O)O)([H])O[C@@H]5COC(/C=C/C6=CC(OC)=C(O)C=C6)=O
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (127.44 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (299 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Liu J, et al. 6‴-Feruloylspinosin alleviates Aβ-induced toxicity by modulating relevant neurotransmitter and the AMPK/mTOR signaling pathway. Free radical biology & medicine. 2025 Feb 01;227:434-445. [Content Brief]
[2]. Gu M, et al. Spinosin and 6'''‑Feruloylspinosin protect the heart against acute myocardial ischemia and reperfusion in rats. Molecular medicine reports. 2019 Nov;20(5):4253-4261. [Content Brief]
[4]. Qiao L, et al. A HPLC-MS/MS method for determination of 6'''-feruloylspinosin in rat plasma and tissues: Pharmacokinetics and tissue distribution study. Journal of pharmaceutical and biomedical analysis. 2016 Mar 20;121:77-83. [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 (sealed storage, away from moisture and light). 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 | 1.2744 mL | 6.3718 mL | 12.7436 mL | 31.8589 mL |
| 5 mM | 0.2549 mL | 1.2744 mL | 2.5487 mL | 6.3718 mL | |
| 10 mM | 0.1274 mL | 0.6372 mL | 1.2744 mL | 3.1859 mL | |
| 15 mM | 0.0850 mL | 0.4248 mL | 0.8496 mL | 2.1239 mL | |
| 20 mM | 0.0637 mL | 0.3186 mL | 0.6372 mL | 1.5929 mL | |
| 25 mM | 0.0510 mL | 0.2549 mL | 0.5097 mL | 1.2744 mL | |
| 30 mM | 0.0425 mL | 0.2124 mL | 0.4248 mL | 1.0620 mL | |
| 40 mM | 0.0319 mL | 0.1593 mL | 0.3186 mL | 0.7965 mL | |
| 50 mM | 0.0255 mL | 0.1274 mL | 0.2549 mL | 0.6372 mL | |
| 60 mM | 0.0212 mL | 0.1062 mL | 0.2124 mL | 0.5310 mL | |
| 80 mM | 0.0159 mL | 0.0796 mL | 0.1593 mL | 0.3982 mL | |
| 100 mM | 0.0127 mL | 0.0637 mL | 0.1274 mL | 0.3186 mL |
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