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| Targets |
TRPV1
Capsiate targets the transient receptor potential vanilloid 1 (TRPV1) receptor as an orally active agonist. TRPV1 is a non-selective cation channel involved in pain sensation, inflammation, and thermoregulation. As a non-irritating capsaicin analog, capsiate activates TRPV1 without the pungent effects of capsaicin. The compound also inhibits angiogenesis and vascular permeability through direct inhibition of Src kinase activity. It has anti-inflammatory, antioxidant, hypoglycemic, and anti-angiogenic activities. The compound's mechanism involves both TRPV1 activation and Src kinase inhibition. |
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| ln Vitro |
Capsiate elicits current responses in TRPV1-expressing HEK293 cells[1].
In vitro studies demonstrate that capsiate evokes current responses in HEK293 cells expressing TRPV1. As a capsaicin analogue extracted from a non-pungent cultivar of CH-19 sweet red pepper, it is an orally active agonist of TRPV1. Capsiate inhibits angiogenesis and vascular permeability through direct inhibition of Src kinase activity. The compound exhibits anti-inflammatory, antioxidant, and hypoglycemic activities. It is a valuable research tool for studying TRPV1-mediated pathways without the pungent effects of capsaicin. The compound's non-irritating profile makes it useful for studying TRPV1 biology without the confounding effects of pain or irritation. |
| ln Vivo |
There are no irritancy-related effects of capsiate on the ocular or oral cavity[1]. Mice exposed to capsiate (0.03~0.54 mM; sc) develop nociceptive responses[1].
In vivo studies show that capsiate is orally active and exhibits anti-inflammatory, antioxidant, hypoglycemic, and inhibitory angiogenic activity. As a non-irritating capsaicin analog, it provides the beneficial effects of TRPV1 activation without the pungent effects of capsaicin. Capsiate inhibits angiogenesis and vascular permeability through direct inhibition of Src kinase activity. The compound has been studied for its potential in metabolic disorders (hypoglycemic effects) and vascular diseases (anti-angiogenic effects). It is extracted from CH-19 sweet red pepper and has been evaluated in various preclinical models. Specific animal model studies have reported its oral bioavailability and efficacy. |
| Enzyme Assay |
For TRPV1 receptor binding and activation assays, cells expressing TRPV1 receptors (e.g., HEK293 cells) are cultured and loaded with calcium-sensitive fluorescent dyes. Capsiate is dissolved in DMSO and diluted in assay buffer to varying concentrations. Cells are treated with the compound and calcium flux is measured using fluorescence plate readers. TRPV1 activation is assessed by measuring intracellular calcium increases. For Src kinase activity assays, purified Src kinase or cell lysates are incubated with capsiate and substrates. Kinase activity is measured by appropriate methods (e.g., radioactive or luminescent assays). IC50 or EC50 values are calculated from dose-response curves. Assays are performed in replicate with vehicle controls.
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| Cell Assay |
For in vitro cellular assays, cells expressing TRPV1 receptors (e.g., HEK293 cells) or cell lines of interest are cultured in appropriate media under standard conditions (37°C, 5% CO2). Capsiate is dissolved in DMSO and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. TRPV1 activation is assessed by measuring intracellular calcium flux using fluorescent indicators. For angiogenesis assays, endothelial cells are treated with capsiate and tube formation, migration, or proliferation is assessed. For anti-inflammatory assays, inflammatory cytokine production is measured. Each concentration is tested in replicate wells with vehicle controls and positive controls (e.g., capsaicin).
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| Animal Protocol |
Animal/Disease Models: Male ddY-strain mice (20–24 g)[1]
Doses: 0.5 or 5 mM Route of Administration: Po Experimental Results: Did not cause pungency-related behaviors. For in vivo animal studies, capsiate is typically administered orally (by gavage) in appropriate formulations. Dosing regimens vary by study objective. For hypoglycemic studies, diabetic animals are treated with capsiate and blood glucose levels are monitored. For anti-angiogenic studies, tumor-bearing animals or angiogenesis models are treated with compound and vascular permeability or tumor growth is assessed. For anti-inflammatory studies, animals are subjected to inflammatory stimuli and inflammatory markers are measured. Blood samples may be collected for pharmacokinetic analysis. Body weight and clinical signs are monitored throughout. All procedures follow institutional animal care and use committee guidelines. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of capsiate indicate it is orally active. The compound has a molecular weight of 208.21, formula C11H12O4, and CAS number 205687-01-0. It is a capsaicin analog extracted from CH-19 sweet red pepper. Storage: typically at -20°C for powder; in solvent at -80°C. Solubility: soluble in DMSO, ethanol, and other organic solvents. Specific pharmacokinetic parameters such as half-life, clearance, and bioavailability are not extensively reported in publicly available sources. The compound is a natural product with established oral activity.
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| Toxicity/Toxicokinetics |
According to available safety information, capsiate is intended for research use only and not for human therapeutic applications. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. As a TRPV1 agonist, it may cause mild effects on sensory neurons. No clinical toxicity data are available.
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| References | |
| Additional Infomation |
Capsiate is a carboxylic acid ester formed by the condensation of the carboxyl group of (6E)-8-methylnon-6-enoic acid with the benzyl hydroxyl group of vanillin. It is a non-spicy analog of Capsiate, possessing similar biological activities. Capsiate functions as a plant metabolite, a hypoglycemic agent, an anti-allergic agent, an antioxidant, an angiogenesis inhibitor, an anti-inflammatory agent, and a Capsiate receptor agonist. It is a carboxylic acid ester, a monomethoxybenzene compound, belonging to the phenolic class. Its functions are similar to vanillin. Capsiate has been reported to be found in bees (Apis cerana), and relevant data exists.
Capsiate is an orally active TRPV1 agonist and non-irritating capsaicin analog extracted from CH-19 sweet red pepper. It acts as an antiallergic agent with anti-inflammatory, antioxidant, hypoglycemic, and inhibitory angiogenic activity. Capsiate inhibits angiogenesis and vascular permeability through direct inhibition of Src kinase activity. It evokes current responses in HEK293 cells expressing TRPV1. The compound is for research use only with no clinical development or regulatory approvals reported. |
| Molecular Formula |
C18H26O4
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| Molecular Weight |
306.40
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| Exact Mass |
306.183
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| CAS # |
205687-01-0
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| PubChem CID |
9839519
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| Appearance |
Colorless to light yellow liquid
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| Boiling Point |
421.3±40.0 °C(Predicted)
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| LogP |
4.216
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
22
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| Complexity |
338
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)C=CCCCCC(=O)OCC1=CC(=C(C=C1)O)OC
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| InChi Key |
ZICNYIDDNJYKCP-SOFGYWHQSA-N
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| InChi Code |
InChI=1S/C18H26O4/c1-14(2)8-6-4-5-7-9-18(20)22-13-15-10-11-16(19)17(12-15)21-3/h6,8,10-12,14,19H,4-5,7,9,13H2,1-3H3/b8-6+
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| Chemical Name |
(4-hydroxy-3-methoxyphenyl)methyl (E)-8-methylnon-6-enoate
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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 (326.37 mM)
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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 | 3.2637 mL | 16.3185 mL | 32.6371 mL | |
| 5 mM | 0.6527 mL | 3.2637 mL | 6.5274 mL | |
| 10 mM | 0.3264 mL | 1.6319 mL | 3.2637 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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