Withanoside IV
Based on 1 Customer Validation
Withanoside IV is an orally active, blood-brain barrier-permeable withanolide derivative. Withanoside IV specifically binds to the Sudlow I site of HSA, induces secondary structural changes in HSA, and forms stable HSA complexes. Withanoside IV inhibits the enzymatic activity of COX-2. Withanoside IV induces axonal regeneration, peripheral nervous system myelination and increased axonal density in spinal cord tissue, reduces reactive gliosis-related changes, and improves hindlimb motor function. Withanoside IV binds to amyloid-β 1-42 to inhibit its aggregation, induces neurite outgrowth and synapse reconstruction, repairs damaged axons and dendrites, enhances mitochondrial biogenesis, exerts neuroprotective effects via the BDNF and SIRT1 signaling pathways, reduces ROS production and neuronal apoptosis, and ameliorates memory deficits. Withanoside IV inhibits the activity of the SARS-CoV-2 main protease. Withanoside IV can be used in research related to spinal cord injury, Alzheimer's disease, and coronavirus disease 2019 (COVID-19).
For research use only. We do not sell to patients.
- Purity: 98.47%
- CAS No.: 362472-81-9
- Formula: C40H62O15
- Molecular Weight:782.91
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from 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
Withanoside IV binds tightly to purified human serum albumin via a static quenching mechanism, with a Ks value of 6.74 × 104 M-1, and specifically locates at Sudlow's drug binding site I (subdomain IIA) on purified human serum albumin[1].
Withanoside IV (100 μM; 6-72 h) potently inhibits the oligomerization and fibrillar aggregation of Aβ (1-42) in a cell-free system[3].
Withanoside IV (10-100 μM; 24-48 h; 9.38 μM; 24 h) exhibits an IC50 of 18.76 μM after 48 h of treatment on human SK-N-SH neuroblastoma cells, and half of this concentration reduces Aβ (1-42)-induced cytotoxicity in the same cell line[3].
Withanoside IV (9.38 μM; 24 h) induces only a minimal level of apoptosis in human SK-N-SH neuroblastoma cells, with a cell viability rate of 94.9%, and reduces apoptotic DNA damage[3].
Withanoside IV (9.38 μM; 24 h) significantly reduces intracellular ROS levels in human SK-N-SH cells exposed to Aβ (1-42)[3].
Withanoside IV (1 μM; 4 days) significantly increases the axonal and dendritic lengths of primary embryonic rat cortical neurons damaged by Aβ(25-35), restoring the axonal length to 897.7 μm and the dendritic length to 188.9 μm[4].
Withanoside IV (1 μM; 7 days) significantly increases the area of synaptophysin-positive synaptic boutons in rat embryonic mature primary cortical neurons damaged by Aβ(25-35), restoring it to 140.3 μm2/μm dendrite[4].
Withanoside IV binds tightly to the active site of SARS-CoV-2 main protease (Mpro), with a docking score of -11.02 kcal/mol[5].
Withanoside IV (1 μM; 72 h) enhances mitochondrial biogenesis and cellular ATP production in primary rat cortical neurons[7].
Withanoside IV (1 μM; 4-72 h) upregulates the expression and release of mature BDNF, and increases the expression of SIRT1 protein in primary rat cortical neurons, exerting neuroprotective effects against Corticosterone (HY-B1618)-induced cell death[7].
Withanoside IV (1 μM; 6 days) significantly promotes neurite outgrowth in human neuroblastoma SH-SY5Y cells[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human SK-N-SH neuroblastoma cells
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Concentration:0, 20, 40, 60, 80, 100 μM (cell viability assay); 9.38 μM (half the IC50, neuroprotection assay)
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Incubation Time:48 h (cell viability assay); 24 h (neuroprotection assay, after 6 h pre-incubation with amyloid-β(1-42))
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Result:Determined the IC50 value against SK-N-SH cells to be 18.76 μM.
Increased neuronal cell viability when cells were pre-treated with amyloid-β(1-42) then treated with half the IC50 concentration, indicating reduced amyloid-β-induced toxicity.
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Cell Line:human SK-N-SH neuroblastoma cells
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Concentration:9.38 μM (half the IC50)
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Incubation Time:24 h
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Result:Resulted in 94.9% live cells, 1.1% dead cells, 3.4% early apoptotic cells, and 0.6% late apoptotic cells, compared to untreated controls with 96.1% live cells.\nDecreased the number of TUNEL-positive apoptotic cells remarkably compared to controls.
Withanoside IV (10 μM/kg; p.o.; daily for 13 consecutive days) significantly enhances spatial memory retention in mice and prevents Aβ(25-35)-induced loss of axons, dendrites, and synapses[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ddY mice (6-week-old, male)[2]
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Dosage:1 mM/kg body weight/day; 10 mM/kg body weight/day
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Administration:p.o.; once daily; day 0 to day 20
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Result:Showed no improvement in locomotor behavior at 1 mmol/kg body weight/day.
Significantly increased BBB locomotion scale scores at all time points compared to vehicle-treated mice at 10 mmol/kg body weight/day.
Increased hindlimb rearing frequency from day 6, with a significant treatment-time interaction relative to vehicle controls at 10 mmol/kg body weight/day.
Increased length of P-NF-H-positive axons in rostral and caudal white matter adjacent to the injury center relative to vehicle at 10 mmol/kg body weight/day.
Showed a relative increase in density of P-NF-H-positive axons in rostral and caudal gray matter adjacent to the injury center compared to vehicle at 10 mmol/kg body weight/day.
Eliminated the P-NF-H-positive cluster of dead neurons/crushed axons at the lesion center (present in vehicle-treated mice) at 10 mmol/kg body weight/day.
Markedly increased PMP-22-positive peripheral nervous system myelin level in the lesion center and proximal areas relative to vehicle at 10 mmol/kg body weight/day.
Left loss of CNS myelin (MBP expression) and reactive gliosis (GFAP expression) unchanged compared to vehicle at 10 mmol/kg body weight/day.
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Animal Model:ddY (male, 6-weeks old)[4]
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Dosage:10 μM/kg
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Administration:p.o.; daily; 13 days
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Result:Showed a significantly higher number of platform crossings (6.7) compared to vehicle-treated Aβ(25-35)-injected mice (3.3).
Prevented the reduction of phosphorylated NF-H-positive axonal areas, MAP2-positive dendritic areas, and synaptophysin-positive synaptic areas in the parietal cortex, temporal cortex, and hippocampal CA1/CA3 regions induced by Aβ(25-35).
Chemical Information
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CAS No. 362472-81-9
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Appearance Solid
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Molecular Weight 782.91
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Formula C40H62O15
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Color off-white
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SMILES
C[C@]1(CC2)[C@](CC[C@]1([H])[C@@H]([C@@](OC3=O)([H])CC(C)=C3CO)C)([H])[C@@](CC=C4C[C@H]5O[C@@H]([C@@H]([C@H]6O)O)O[C@@H]([C@H]6O)CO[C@@H]([C@@H]([C@H]7O)O)O[C@@H]([C@H]7O)CO)([H])[C@@]2([H])[C@]4([C@H](C5)O)C
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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, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 50 mg/mL (63.86 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 (protect from 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 (protect from 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)
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.
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 (protect from 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 (284 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]. Dubey S, et al. Elucidating the active interaction mechanism of phytochemicals withanolide and withanoside derivatives with human serum albumin. PLoS One. 2018;13(11):e0200053. Published 2018 Nov 7. [Content Brief]
[2]. Nakayama N, et al. Withanoside IV improves hindlimb function by facilitating axonal growth and increase in peripheral nervous system myelin level after spinal cord injury. Neurosci Res. 2007;58(2):176-182. [Content Brief]
[3]. Dubey S, et al. Improving the inhibition of β-amyloid aggregation by withanolide and withanoside derivatives. Int J Biol Macromol. 2021;173:56-65. [Content Brief]
[4]. Kuboyama T, et al. Withanoside IV and its active metabolite, sominone, attenuate Abeta(25-35)-induced neurodegeneration. Eur J Neurosci. 2006;23(6):1417-1426. [Content Brief]
[5]. Choe J, et al. The Efficacy of Traditional Medicinal Plants in Modulating the Main Protease of SARS-CoV-2 and Cytokine Storm. Chem Biodivers. 2022;19(11):e202200655. [Content Brief]
[6]. Tohda C, et al. Yakugaku Zasshi. 2008;128(8):1159-1167. [Content Brief]
[7]. Fanibunda SE, et al. Withania somnifera Regulates Mitochondrial Biogenesis and Energetics in Rat Cortical Neurons: Role of BDNF and SIRT1. Mol Neurobiol. 2025;62(8):10277-10295. [Content Brief]
[8]. Zhao J, et al. Withanolide derivatives from the roots of Withania somnifera and their neurite outgrowth activities. Chem Pharm Bull (Tokyo). 2002;50(6):760-765. [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 (protect from 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 | 1.2773 mL | 6.3864 mL | 12.7729 mL | 31.9322 mL |
| 5 mM | 0.2555 mL | 1.2773 mL | 2.5546 mL | 6.3864 mL | |
| 10 mM | 0.1277 mL | 0.6386 mL | 1.2773 mL | 3.1932 mL | |
| 15 mM | 0.0852 mL | 0.4258 mL | 0.8515 mL | 2.1288 mL | |
| 20 mM | 0.0639 mL | 0.3193 mL | 0.6386 mL | 1.5966 mL | |
| 25 mM | 0.0511 mL | 0.2555 mL | 0.5109 mL | 1.2773 mL | |
| 30 mM | 0.0426 mL | 0.2129 mL | 0.4258 mL | 1.0644 mL | |
| 40 mM | 0.0319 mL | 0.1597 mL | 0.3193 mL | 0.7983 mL | |
| 50 mM | 0.0255 mL | 0.1277 mL | 0.2555 mL | 0.6386 mL | |
| 60 mM | 0.0213 mL | 0.1064 mL | 0.2129 mL | 0.5322 mL |
Withanoside IV Related Classifications
HY-N8693 Related Classifications
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- Withanoside IV
- 362472-81-9
- COX
- Amyloid-β
- Sirtuin
- Reactive Oxygen Species (ROS)
- Apoptosis
- SARS-CoV
- SARS-CoV-2 main protease
- withanolide derivative
- spinal cord injury
- Alzheimer's disease
- coronavirus disease 2019 (COVID-19)
- K-N-SH neuroblastoma cells
- primary embryonic rat cortical neurons
- primary rat cortical neurons
- ddY mice
- Inhibitor
- inhibitor
- inhibit