Cannabidiorcol (CBDO, CBD-C1, O-1821) is related to cannabidiol, with the pentyl side chain shortened to a methyl group. Cannabidiorcol has low affinity for cannabinoid receptors (CBs) and is an agonist of the transient receptor potential channel (TRP channel), through which it produces antiinflammatory effects, but can also promote tumorigenesis at high concentrations[1][2].
JT010 is a potent agonist of TRPA1 with an EC50 of 0.65 nM.
Pyr10is a novel TRPC3-selective inhibitor, IC50 of Ca2+ influx inhibition by Pyr10 in carbachol-stimulated YFP-TRPC3-transfected HEK293 cells for ROCE and thapsigargin-depleted native RBL-2H3 cells for SOCE is 0.72 uM and 13.08 uM.IC50 value: 0.72 uM (TRPC3-ROCE), 13.08 uM (SOCE) [1]Target: TRPC3in vitro: Pyr10 displays substantial selectivity for TRPC3-mediated responses (18-fold) and the selective block of TRPC3 channels by Pyr10 barely affected mast cell activation.[1]
TRPM8 antagonist 3 is a novel TRPM8 blocker with an IC50 value of 11 nM.
AMG2850 is a potent, orally bioavailable and selective transient receptor potential melastatin 8 (TRPM8) antagonist[1].
JYL 1421 is a TRPV1 receptor antagonist, with an IC50 of 8 nM.
TRPM8 Antagonist is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.
AMG 517 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with an IC50 of 0.5 nM.
PF-04745637 is a potent and selective TRPA1 antagonist with an IC50 of 17 nM for human TRPA1[1].
Optovin is a reversible photoactive TRPA1 activator; stimulates human TRPA1 channels in vitro and enables repeated photoactivation of motor behaviors in wild-type zebrafish (EC50 = 2 μM).IC50 value:Target: in vitro: Optovin is a rhodanine-containing small molecule with no previously annotated biological activity. Whereas DMSO-treated animals do not respond to photic stimuli, optovin-treated animals respond to light with vigorous motor excitation at an EC50 of 2 μM. Optovin-treated animals respond to 387 nm (violet) stimuli, but not to 485 nm (blue), 560 nm (green) or longer wavelengths. optovin strongly activated 33% (35/105) of DRG neurons. optovin acts on a molecular target expressed in mustard oil responsive mammalian DRG sensory neurons; perhaps on TRPA1 itself. TrpA1 is necessary for the optovin response [1].in vivo: Optovin also elicited nociceptive behaviors in adult mice. optovin shows activity on adult animals in vivo, and may be preferable to conventional TRPA1 ligands for achieving high-resolution spatiotemporal control.
WS-3 is an agonist of TRPM8 with an EC50 of 3.7 μM.
GSK2332255B is a potent, selective TRPC3 and TRPC6 antagonist with IC50s of 5 nM and 4 nM for rat TRPC3 and rat TRPC6. GSK2332255B shows ≥100-fold selectivity for TRPC3/6 over other calcium-permeable channels[1].
EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM[1]. EIPA also inhibits Na+/H+-exchanger (NHE)[2] and macropinocytosis[3].
TRPV1 activator-2 (compound 9), a capsaicin head analog, makes specific interactions with channel residues at the lipid-water[1].
Podocarpic acid is a natural product, which has the best all-round positive effect and acts as a novel TRPA1 activator.
TRPV3 antagonist 74a is a potent and selective TRPV3 antagonist. TRPV3 antagonist 74a displays no significant activity against a panel of other ion channels. TRPV3 antagonist 74a can be used for the research of neuropathic pain[1][2].
SKF-96365 hydrochloride is a non-selective TRP Channel blocker.
TRPC6-IN-3 (compound 17) is a potent, orally active transient receptor potential C6 ion channel (TRPC6) inhibitor. TRPC6-IN-3 modulates not only intracellular calcium concentration, but also membrane potential by modulating the flux of cations including calcium and sodium ions. TRPC6-IN-3 can be used in research of respiratory system[1].
TRPM4 inhibitor 5 is a potent and selective inhibitor of TRPM4 with IC50 of 1.5 uM (Na+ influx); selectively inhibits TRPM4 overexpressed in HEK293 cells (IC50=1.8 uM) using classical patch-clamp electrophysiology recordings, shows no significant effect on the TRPM5 current, as well as other TRP family members including TRPM7, TRPM8, TRPV1 and TRPV6.
ML-SA1, as a selective TRPML agonist, inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 value of ML-SA1 against DENV2 RNA and ZIKV RNA is 8.3 μM and 52.99 μM, respectively. ML-SA1 induces autophagy. ML-SA1 can be used for the research of broad-spectrum antiviral[1].
ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.
Caffeic acid is an inhibitor of both TRPV1 ion channel and 5-Lipoxygenase (5-LO).
NMDAR/TRPM4-IN-2 (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 shows neuroprotective activity. NMDAR/TRPM4-IN-2 prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss[1].
TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM.
8-Gingerol, found in the rhizomes of ginger (Z. officinale) with oral bioavailability, activates TRPV1, with an EC50 of 5.0 µM. 8-Gingerol inhibits COX-2, and inhibits the growth of H. pylori in vitro[1][2].
Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.IC50 value: 6.5 nM (Ki, for TRPV1)Target: TRPV1in vitro: Mavatrep exhibits superior pharmacodynamic properties. In a TRPV1 functional assay, using cells expressing recombinant human TRPV1 channels, Mavatrep antagonizes capsaicin-induced Ca2+ influx, with an IC50 value of 4.6 nM. Mavatrep blocks the activation of hTRPV1 channels by Capsaicin (1 μM) and by pH (5.0) in a concentration-dependent fashion, with IC50 values of 23 and 6.8 nM, respectively. in vivo: Mavatrep exhibits superior pharmacodynamic properties in the CFA model of inflammatory pain.