| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg |
| Targets |
Hydroxy-α-sanshool targets TRPA1 (transient receptor potential ankyrin 1) and TRPV1 (TRP vanilloid 1) receptors. It acts as a covalent agonist of TRPA1 and a non-covalent agonist of TRPV1. The EC50 values for TRPA1 and TRPV1 activation are 69 and 1.1 µM, respectively. It also has antiobesity and hypolipidemic activities.
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| ln Vitro |
In cultured DRG neurons, hydroxy-α-sanshool (0-10 mM; 20 s) generates inward currents [2]. In cultured DRG neurons, hydroxy-α-sanshool (1 mM; 0-1 min) raises intracellular Ca2+ [2].
In vitro, Hydroxy-α-sanshool is a TRPA1 and TRPV1 agonist with EC50s of 69 and 1.1 µM, respectively. It is a covalent agonist of TRPA1 and a non-covalent agonist of TRPV1. It has analgesic properties. Quantitative IC50 values for its effects on other targets are not detailed in the publicly available sources. |
| ln Vivo |
In both wild-type and TRPV1-deficient mice, hydroxy-α-sanshool (intradermal injection; 4 mg per mouse; once) causes paw-licking reactions [2]. One can clearly observe a clear aversion to 1 mM hydroxy-α-sanshool in WT mice, but in TRPV1 KO mice, this aversion is nearly gone (P<0.001) [1].
In vivo, Hydroxy-α-sanshool exerts antiobesity and hypolipidemic activities in high-fat diet (HFD) rats by reducing liver oxidative stress. It could be considered as a potential candidate drug to cure or prevent obesity and hyperlipidemia. It also has analgesic properties. Detailed dose-response and pharmacokinetic data in animal models are limited. |
| Enzyme Assay |
For cell-free assays, the activity of Hydroxy-α-sanshool at TRPA1 and TRPV1 receptors can be studied using calcium flux assays with membrane preparations or liposomes containing the receptors. The compound is added to the preparations, and calcium influx is measured using fluorescent calcium indicators. EC50 values are calculated from concentration-response curves.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Dorsal Root Ganglion (DRG) Neuron Tested Concentrations: 0-10 mM Incubation Duration: 20 seconds Experimental Results: Induced small but strong inward current in DRG neurons with EC50 of 66.2 μM. Cell viability assay[2] Cell Types: Dorsal Root Ganglion (DRG) Neuronal Tested Concentrations: 1 mM Incubation Duration: 0-1 min Experimental Results: Resulted in intracellular Ca2+ in the majority of DRG neurons tested (98 out of 100) Increase. For in vitro cellular assays, the TRPA1 and TRPV1 agonistic activity of Hydroxy-α-sanshool is assessed in cells expressing these receptors. Cells are loaded with a calcium-sensitive fluorescent dye and treated with various concentrations of the compound. Calcium influx is measured using a fluorometric imaging plate reader (FLIPR). EC50 values are calculated from concentration-response curves. |
| Animal Protocol |
Animal/Disease Models: wild-type and TRPV1-deficient mice [2]
Doses: 4 mg per mouse Route of Administration: intradermal injection; 4 mg per mouse; Experimental Results: TRPV1-deficient mice had diminished paw licking responses (160 times , P < 0.05). Wild-type mice demonstrated paw licking responses (average 284.8 times) within 20 minutes. For in vivo studies, Hydroxy-α-sanshool could be administered orally in animal models of obesity and hyperlipidemia. Endpoints include body weight, adipose tissue mass, serum lipid levels, and markers of oxidative stress. Its analgesic effects could be evaluated in pain models. |
| ADME/Pharmacokinetics |
Hydroxy-α-sanshool (CAS 83883-10-7) has a molecular formula of C16H25NO2 and a molecular weight of 263.38 g/mol. IUPAC name: (2E,6Z,8E,10Z)-N-(2-hydroxy-2-methylpropyl)dodeca-2,6,8,10-tetraenamide. Appearance: typically a powder or oil. Solubility: DMSO and other organic solvents. Storage: typical for natural products (desiccated, protected from light, -20°C). Purity: typically >98% for research use.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a natural alkylamide from Szechuan pepper, it is generally considered to have low toxicity at moderate doses, but standard toxicological studies would be required for drug development.
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| References | |
| Additional Infomation |
Hydroxy-α-sanshinol is a fatty amide. It has been reported to be found in plants of the genus Zanthoxylum (such as Zanthoxylum schinifolium, Zanthoxylum bungeanum, and Zanthoxylum piperitum), and relevant data are available for reference.
Hydroxy-α-sanshool is a research-grade compound and is not approved for therapeutic use. It serves primarily as a pharmacological tool for studying TRPA1 and TRPV1 receptor function, pain mechanisms, and metabolic disorders. Its mechanism of action involves agonism of TRPA1 and TRPV1 receptors. It is a natural product from Szechuan pepper. No clinical trials have been reported. |
| Molecular Formula |
C16H25NO2
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|---|---|
| Molecular Weight |
263.3752
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| Exact Mass |
263.189
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| CAS # |
83883-10-7
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| PubChem CID |
10084135
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| Appearance |
White to yellow viscous liquid
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| Density |
0.973 g/cm3
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| Boiling Point |
471.5±45.0℃ at 760 mmHg
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| LogP |
3.289
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
19
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| Complexity |
363
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(=O)(NCC(O)(C)C)/C=C/CC/C=C\C=C\C=C\C
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| InChi Key |
LHFKHAVGGJJQFF-UEOYEZOQSA-N
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| InChi Code |
InChI=1S/C16H25NO2/c1-4-5-6-7-8-9-10-11-12-13-15(18)17-14-16(2,3)19/h4-9,12-13,19H,10-11,14H2,1-3H3,(H,17,18)/b5-4+,7-6+,9-8-,13-12+
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| Chemical Name |
(2E,6Z,8E,10E)-N-(2-hydroxy-2-methylpropyl)dodeca-2,6,8,10-tetraenamide
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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 (~379.68 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (9.49 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (9.49 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 ultrasonication. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7968 mL | 18.9840 mL | 37.9680 mL | |
| 5 mM | 0.7594 mL | 3.7968 mL | 7.5936 mL | |
| 10 mM | 0.3797 mL | 1.8984 mL | 3.7968 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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