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Nonivamide

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Chemical Structure| 2444-46-4 同义名 : Pelargonic acid vanillylamide;Nonanoic acid vanillylamide;N-Vanillylpelargonamide;N-Vanillylnonanamide;NSC 172795;Vanillyl-N-nonylamide;Pseudocapsaicin
CAS号 : 2444-46-4
货号 : A244101
分子式 : C17H27NO3
纯度 : 98%
分子量 : 293.4
MDL号 : MFCD00017286
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(357.87 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

SC 5% DMSO +30% PEG400+2% tween80 + H2O 2 mg/mL clear

生物活性
描述 Nonivamide is a TRPV1 (transient receptor potential vanilloid 1) agonist. Agonism of the VR1 (TRPV1) receptor by Nonivamide was demonstrated to induce the release of Ca2+ from the endoplasmic reticulum (ER) of human lung cells, producing ER stress and cell death[3]. The TRPV1 agonist nonivamide induced GADD153 expression and caused cytotoxicity in immortalized and primary human bronchial, bronchiolar/alveolar, and microvascular endothelial cells, proportional to TRPV1 mRNA expression[4]. Nonivamide (1 μM) stimulated the Ca(2+) -dependent release of serotonin (272 ± 115%) and dopamine (646 ± 48%) in SH-SY5Y cells compared to nontreated cells (100%) to a similar extent as capsaicin[5]. Nonivamide possessed similar anti-inflammatory potential as capsaicin and t-pellitorine. In U-937 macrophages, the tested compounds exploited an anti-inflammatory effect by inhibiting the EC(Escherichia coli)-LPS induced activation of the MAPK (mitogen-activated protein kinase) pathway. In addition, the TRP (transient receptor protein) channel activation plays a role in the anti-inflammatory capacity of capsaicin and nonivamide[6]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.41mL

0.68mL

0.34mL

17.04mL

3.41mL

1.70mL

34.08mL

6.82mL

3.41mL
参考文献

[1]Gaubitz M, Schiffer T, et al. Efficacy and safety of nicoboxil/nonivamide ointment for the treatment of acute pain in the low back - A randomized, controlled trial. Eur J Pain. 2016 Feb;20(2):263-73.

[2]Zhou J, Yang C, et al. Toxic effects of environment-friendly antifoulant nonivamide on Phaeodactylum tricornutum. Environ Toxicol Chem. 2013 Apr;32(4):802-9.

[3]Thomas KC, Sabnis AS, Johansen ME, Lanza DL, Moos PJ, Yost GS, Reilly CA. Transient receptor potential vanilloid 1 agonists cause endoplasmic reticulum stress and cell death in human lung cells. J Pharmacol Exp Ther. 2007 Jun;321(3):830-8

[4]Thomas KC, Roberts JK, Deering-Rice CE, Romero EG, Dull RO, Lee J, Yost GS, Reilly CA. Contributions of TRPV1, endovanilloids, and endoplasmic reticulum stress in lung cell death in vitro and lung injury. Am J Physiol Lung Cell Mol Physiol. 2012 Jan 1;302(1):L111-9

[5]Rohm B, Holik AK, Somoza MM, Pignitter M, Zaunschirm M, Ley JP, Krammer GE, Somoza V. Nonivamide, a capsaicin analog, increases dopamine and serotonin release in SH-SY5Y cells via a TRPV1-independent pathway. Mol Nutr Food Res. 2013 Nov;57(11):2008-18

[6]Walker J, Ley JP, Schwerzler J, Lieder B, Beltran L, Ziemba PM, Hatt H, Hans J, Widder S, Krammer GE, Somoza V. Nonivamide, a capsaicin analogue, exhibits anti-inflammatory properties in peripheral blood mononuclear cells and U-937 macrophages. Mol Nutr Food Res. 2017 Feb;61(2)