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Capsiconiate (Synonyms: Coniferyl (E)-8-methyl-6-nonenoate)

Catalog No.GC12636

TRPV1 agonist

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Capsiconiate Chemical Structure

Cas No.: 946572-73-2

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Sample solution is provided at 25 µL, 10mM.

Description of Capsiconiate

EC50: 3.2 μM for TRPV1

Capsiconiate is a TRPV1 agonist.

The capsaicin receptor, also termed as transient receptor potential vanilloid type 1 (TRPV1), is an non-selective cation, calcium permeable channel. The activation of TRPV1 has been reported to contribute to the various physiological activities of capsaicin.

In vitro: Capsiconiate was isolated from the fruits of the pepper, Capsicum baccatum L. var. praetermissum. The agonist activity of the capsiconiate for TRPV1 was evaluated by conducting an analysis of the intracellular calcium concentrations in TRPV1-expressing HEK293 cells. The EC50 value of capsiconiate was determined to be 3.2 microM. However, the activity was weaker than that of capsaicinor capsiate. It was found that capsiconiate had no pungency, and therefore, the low activity could be explained on the basis of the structure-activity relationship. The instability capsiconiate in aqueous solvents might also be responsible for its low activity. Even though the agonist activity for TRPV1 was lower than that of capsaicin, its activity was comparable with that of other naturally occurring compounds such as gingerol, piperine, and capsaicinol [1].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Kobata, K. ,Tate, H.,Iwasaki, Y., et al. Isolation of coniferyl esters from Capsicum baccatum L., and their enzymatic preparation and agonist activity for TRPV1. Phytochemistry 69(5), 1179-1184 (2008).

Chemical Properties of Capsiconiate

Cas No. 946572-73-2 SDF
Synonyms Coniferyl (E)-8-methyl-6-nonenoate
Chemical Name 8-methyl-6E-nonenoic acid 3-(4-hydroxy-3-methoxyphenyl)-2E-propen-1-yl ester
Canonical SMILES COC1=C(O)C=CC(/C=C/COC(CCCC/C=C/C(C)C)=O)=C1
Formula C20H28O4 M.Wt 332.4
Solubility ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Capsiconiate

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1 mg 5 mg 10 mg
1 mM 3.0084 mL 15.0421 mL 30.0842 mL
5 mM 0.6017 mL 3.0084 mL 6.0168 mL
10 mM 0.3008 mL 1.5042 mL 3.0084 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Average Rating: 5 ★★★★★ (Based on Reviews and 2 reference(s) in Google Scholar.)

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