| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
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| Targets |
Spinasterol targets the transient receptor potential vanilloid 1 (TRPV1) receptor, a non-selective cation channel that is activated by capsaicin, heat, and protons and is involved in pain sensation and inflammation. By acting as a selective antagonist at TRPV1, spinasterol blocks TRPV1-mediated signaling, thereby exerting antinociceptive and anti-inflammatory effects. The compound also exhibits antioxidant activity by scavenging reactive oxygen species. Spinasterol's antidepressant effects may be mediated through modulation of TRPV1 signaling or other pathways.
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| ln Vitro |
In vitro, spinasterol acts as a selective antagonist at the TRPV1 receptor. It exhibits anti-inflammatory, antioxidant, and antinociceptive activities. The compound has been shown to have antibacterial activity. Its ability to inhibit TRPV1-mediated signaling has been demonstrated in cell-based assays measuring calcium influx or other downstream signaling events. Spinasterol's antioxidant activity can be assessed using cell-free assays such as DPPH radical scavenging or ABTS assays.
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| ln Vivo |
In vivo, spinasterol has demonstrated anticonvulsant activity in mice at doses of 0.001-1 mg/kg administered intraperitoneally, without affecting neuromuscular strength, impairing motor coordination, or changing body temperature. The compound also exhibits anti-inflammatory, antidepressant, antioxidant, and antinociceptive effects. Spinasterol has been studied for its potential cholesterol-lowering effects, as it may inhibit cholesterol absorption in the intestine. These activities support its potential for treating various conditions including pain, inflammation, and neurological disorders.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for spinasterol are radioligand binding assays using membrane preparations from cells expressing recombinant human TRPV1 receptors. The compound's binding affinity is determined by its ability to displace a labeled TRPV1 ligand such as [3H]resiniferatoxin or [3H]capsaicin. Functional assays such as calcium flux assays are used to measure the compound's antagonist activity at TRPV1. The IC50 for inhibition of capsaicin-induced calcium influx is determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for spinasterol are performed using cell lines expressing recombinant TRPV1 receptors or primary sensory neurons. Cells are loaded with a calcium-sensitive fluorescent dye and treated with varying concentrations of spinasterol. Calcium influx is elicited by application of capsaicin or other TRPV1 agonists, and intracellular calcium levels are measured using a fluorometric plate reader. The compound's ability to inhibit TRPV1-mediated calcium influx is assessed. Cell viability is evaluated using MTT assays to ensure that the observed effects are not due to cytotoxicity.
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| Animal Protocol |
In vivo animal experiments for spinasterol have been conducted in mouse models. To assess anticonvulsant activity, mice are administered spinasterol at doses of 0.001-1 mg/kg via intraperitoneal injection, and seizure threshold is measured using models such as the maximal electroshock test or pentylenetetrazol-induced seizure test. Neuromuscular strength, motor coordination, and body temperature are also assessed to evaluate potential side effects. The compound's anti-inflammatory and antinociceptive effects can be evaluated in models of pain and inflammation.
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| ADME/Pharmacokinetics |
Spinasterol has a molecular weight of 412.70 g/mol and a molecular formula of C29H48O. The compound is a white powder that is soluble in organic solvents. It is blood-brain barrier-permeable and orally active. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have not been extensively reported. As a plant-derived phytosterol, spinasterol is expected to have moderate oral bioavailability and may undergo extensive metabolism in the liver.
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| Toxicity/Toxicokinetics |
Spinasterol has been evaluated in preclinical studies and has been reported to be well-tolerated at effective doses. In anticonvulsant studies in mice, spinasterol did not affect neuromuscular strength, impair motor coordination, or change body temperature at active doses, suggesting a favorable safety profile. No significant toxicity has been reported in the available literature. However, comprehensive toxicology studies would be necessary to fully assess the compound's safety for clinical development.
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| References |
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| Additional Infomation |
α-Spinasterol is a steroidal compound derived from the hydrogenation of stigmasterane. It has been reported to exist in tea (Camellia sinensis), Rhodiola rosea (Erythrophleum fordii), and other organisms with relevant data. See also: Leaf (part) of Hibiscus trifoliata (Menyanthes trifoliata).
Spinasterol is a plant-derived phytosterol that acts as a selective antagonist for the TRPV1 receptor. It is blood-brain barrier-permeable and orally active. Spinasterol exhibits anti-inflammatory, antidepressant, antioxidant, antinociceptive, and anticonvulsant effects. It has been studied for its potential cholesterol-lowering effects and has antibacterial activity. Spinasterol is a research compound with potential applications in pain, inflammation, and neurological disorders. |
| Molecular Formula |
C29H48O
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|---|---|
| Molecular Weight |
412.702
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| Exact Mass |
412.37
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| CAS # |
481-18-5
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| PubChem CID |
5281331
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| Appearance |
White to off-white solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
500.0±44.0 °C at 760 mmHg
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| Melting Point |
168-169°
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| Flash Point |
219.1±20.7 °C
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| Vapour Pressure |
0.0±2.9 mmHg at 25°C
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| Index of Refraction |
1.531
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| LogP |
10.13
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
674
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CC[C@H](/C=C/[C@@H](C)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3C2=CC[C@@H]4[C@@]3(CC[C@@H](C4)O)C)C)C(C)C
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| InChi Key |
JZVFJDZBLUFKCA-FXIAWGAOSA-N
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| InChi Code |
InChI=1S/C29H48O/c1-7-21(19(2)3)9-8-20(4)25-12-13-26-24-11-10-22-18-23(30)14-16-28(22,5)27(24)15-17-29(25,26)6/h8-9,11,19-23,25-27,30H,7,10,12-18H2,1-6H3/b9-8+/t20-,21-,22+,23+,25-,26+,27+,28+,29-/m1/s1
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| Chemical Name |
(3S,5S,9R,10S,13R,14R,17R)-17-[(E,2R,5S)-5-ethyl-6-methylhept-3-en-2-yl]-10,13-dimethyl-2,3,4,5,6,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol
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| Synonyms |
Bessisterol; alpha-Spinasterin; Spinasterol
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4231 mL | 12.1153 mL | 24.2307 mL | |
| 5 mM | 0.4846 mL | 2.4231 mL | 4.8461 mL | |
| 10 mM | 0.2423 mL | 1.2115 mL | 2.4231 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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