规格: | 1mg | 产品价格: | 640 |
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规格: | 5mg | 产品价格: | 2870 |
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规格: | 10mg | 产品价格: | 5090 |
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规格: | 25mg | 产品价格: | 11140 |
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Catalog Number GC15580
Molecular Formula C28H46N2O2
Relative Molecular Mass 442.7
CAS Registry Number 67964-87-8
Formulation A solid
Purity ≥98%
Storage Store at -20°C
SMILES O=C(NCCC1=CNC2=CC=C(O)C=C12)CCCCCCCCCCCCCCCCC
产品描述
Stearoyl Serotonin is a TRPV1 antagonist with IC50 value of 0.76 μM for human TRPV1 [1]. The transient receptor potential vanilloid-type 1 (TRPV1) channel is a nonselective cation channel that may be activated by a variety of exogenous and endogenous physical and chemical stimuli. TRPV1 is decreased in the injured nerve fibers but increased in those proximal to the site damage. TRPV1 is a potential new target for the development of analgesic and anti-inflammatory drugs [1].Stearoyl Serotonin is a hybrid molecule patterned after arachidonoyl serotonin. Arachidonoyl serotonin is a dual antagonist of TRPV1 and fatty acid amide hydrolase (FAAH) with IC50 values of 0.27 and 8 μM, respectively. Arachidonoyl serotonin was highly effective against both acute and chronic peripheral pain [1][2]. In TRPV1 and FAAH assays, Stearoyl Serotonin inhibited anandamide hydrolysis mediated by FAAH and capsaicin-induced intracellular Ca2+ elevation in HEK293 cells overexpressing the human recombinant TRPV1 receptor with IC50 values of > 50 μM and 0.76 μM, respectively. However, the effects of replacing the arachidonoyl portion with the saturated 18-carbon stearoyl moiety had not been studied [1].References:[1]. Ortar G, Cascio MG, De Petrocellis L, et al. New N-arachidonoylserotonin analogues with potential "dual" mechanism of action against pain. J Med Chem. 2007 Dec 27;50(26):6554-69.[2]. Maione S, De Petrocellis L, de Novellis V, et al. Analgesic actions of N-arachidonoyl-serotonin, a fatty acid amide hydrolase inhibitor with antagonistic activity at vanilloid TRPV1 receptors. Br J Pharmacol. 2007 Mar;150(6):766-81.
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