TRP Channel Modulators

发布于 2025年8月20日更新时间 2025年8月20日

Transient receptor potential (TRP) channels are ion channels embedded in the plasma membrane of many cell types, where they play key roles in sensory transduction, including the detection of pain, temperature, taste, and mechanical pressure.

Among these, TRP vanilloid (TRPV) channels are the most extensively studied. Naturally occurring compounds such as Capsaicin (Aladdin C423851, C107691, C107692, C107693) and Piperine (P107401, P107402)—found in certain plants—activate TRPV channels and are responsible for the hot or spicy sensation associated with some peppers.

TRP canonical (TRPC) channels are commonly expressed in cardiomyocytes and neurons, where they contribute to processes such as cardiac hypertrophy. The amyotrophic lateral sclerosis (ALS) therapeutic Riluzole (R129533, R408717) is known to activate TRPC5 channels, whereas Clemizole (C125175, C423994), a compound that blocks NS4B and histamine receptors, inhibits TRPC5 channels and may influence neurite length.

TRP melastatin-like (TRPM) channels participate in sensory responses to temperature and taste, as well as in cell adhesion mechanisms. Icilin (I303569) activates TRPM8 channels while inhibiting TRPV3 channels, producing a cooling effect.

Other TRP channel subfamilies include TRP ankyrin (TRPA) channels, TRP polycystin (TRPP) channels, and TRP mucolipin (TRPML) channels, each with distinct physiological roles.

Representative Compounds and Targets from Aladdin are listed in the below sheet

TRP-Channels	Product Catalog	Name	Purity	Description
TRPV	A288783	Arvanil	≥98% 50mg/ml in ethanol	TRPV1 activator
TRPV	A129214 A408950	Azelastine HCl	≥98%, 10mM in DMSO	TRPV1 activator
TRPV	C423851 C107691 C107692 C107693	Capsaicin	≥95% , ≥60%, natural, 10mM in DMSO	TRPV activator
TRPV	C102530	Carveol	≥97%	TRPV3 activator
TRPV	G111261 G422764	[6]-Gingerol	≥98% analytical standard , 10mM in DMSO	TRPV1 activator
TRPV	M110428 M110426 M110429 M420855	Methyl salicylate	≥99.5% standard for GC, AR ≥99%, pharmaceutical grade, 10mM in DMSO	TRPV1 activator/blocker
TRPV	N421516 N109019 N432048 N109017 N412785	Neomycin sulfate	10mM in Water, analytical standard, BioReagent, USP, ≥97%	TRPV1 blocker
TRPV	P422761 P110193	Peimine	10mM in DMSO, ≥98% analytical standard	TRPV1 and TRPA1 blocker
TRPV	P671384 P579447 P422213 P110194	Peiminine	≥90%,≥97%,10mM in DMSO, analytical standard ≥98%	TRPV1 and TRPA1 blocker
TRPV	P107401 P107402	Piperine	analytical standard≥98%, ≥97%	TRPV activator
TRPV	H614219	Resiniferatoxin	≥98%	TRPV activator
TRPV	S129681 S407749	Sumatriptan	≥98%,10mM in DMSO	TRPV1 blocker
TRPV	T129491 T407718	Tranilast	≥98%,10mM in DMSO	TRPV2 blocker
TRPC	C423994 C125175	Clemizole	≥98%,10mM in DMSO	TRPC5 blocker
TRPC	F129495 T580273	Flufenamic Acid	≥99%,10mM in DMSO	TRPC3 and TRPM2 blocker
TRPC	T580273	Riluzole	≥98%	TRPC5 activator
TRPM	G107683 G424525	Ginsenoside Rd	≥98% analytical standard,10mM in DMSO	TRPM7 blocker
TRPM	I303569	Icilin	≥96%	TRPM8 activator, TRPV3 blocker
TRPM	P129412	Pregnenolone	≥98%	TRPM3 activator
TRPA	D276523	D,L-1'-Acetoxychavicol acetate	≥98%	TRPA activator
TRPA	E129317 E408574	Etodolac	≥98%,10mM in DMSO	TRPA activator
TRPA	P115736 P422495	Parthenolide	≥98% analytical standard,10mM in DMSO	TRPA activator

References:

1. Kissin I. Anesth Analg. 2008 Jul;107(1):271-81.

2. Bush EW, Hood DB, Papst PJet al. J Biol Chem. 2006 Nov

3;281(44):33487-96. 3. Richter JM, Schaefer M, Hill K. Mol Pharmacol. 2014 Nov;86(5):514- 21.

4. Sherkheli MA, Gisselmann G, Hatt H. ScientificWorldJournal. 2012;2012:982725.

Aladdin: https://www.aladdinsci.com/

Categories: 技术文章

探索主题: TRPV TRPC TRPM TRPA TRPP TRPML TRP Channel Modulators

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