TRPA1 Antagonist 1 is a methylene phosphate prodrug which converts to its active parent drug, a TRPA1 antagonist with an IC50 of 8 nM.
SKF-96365 hydrochloride is a non-selective TRP Channel blocker.
M8-B is a potent transient receptor potential melastatin-8 (TRPM8) antagonist. M8-B blocks cold-induced and TRPM8-agonist-induced activation TRPM8 channels. M8-B decreases deep body temperature (Tb)[1].
ML-SI3 is a TRPML Channel Inhibitor. ML-SI3 blocks TRPML1 and TRPML2 with IC50s of 4.7 µM and 1.7 µM respectively. ML-SI3 prevents lysosomal calcium efflux and blocks downstream TRPML1-mediated induction of autophagy[1][5].
Naltriben is a selective δ2-opioid receptor antagonist and TRPM7 activator. Naltriben enhances glioblastoma cell migration and invasion. Naltriben can be used in research into neurological diseases and cancer[1][2].
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].
TAT-M2NX (tatM2NX) is a TRPM2 inhibitor with specific neuroprotective activity in male mice. TAT-M2NX can be used to study ischemic neuronal damage[1].
DS88790512 is a potent, selective, and orally bioavailable TRPC6 inhibitor with an IC50 of 11 nM.
Amiloride (hydrochloride) is an epithelial sodium channel (ENaC) inhibitor and a competitive inhibitor of Urokinase-type plasminogen activator (uPA).
Umbellulone is an active constituent of the leaves of Umbellularia californica. Umbellulone stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism[1].
TC-I 2014 (compound 5) is a potent Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models[1].
GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3[1][2].
ABT-102 is a potent and highly selective Vanilloid Receptor (TRPV1) receptor antagonist. ABT-102 potently and reversibly increases heat pain thresholds and reduced painfulness of suprathreshold oral/cutaneous heat. ABT-102 reduces nociceptive responses of animals in models of inflammatory, bone cancer, postoperative, and osteoarthritic pain[1][2].
N-Oleoyl valine is a N-acyl valine compound that acts as a TRPV3 receptor antagonist[1].
Beta-Eudesmol is a natural oxygenated sesquiterpene, activates hTRPA1, with an EC50 of 32.5 μM. Beta-Eudesmol increases appetite through TRPA1[1].
Amiloride-15N3 (hydrochloride) is the 15N labeled Amiloride hydrochloride[1]. Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC[2]) and urokinase-type plasminogen activator receptor (uTPA[3]). Amiloride hydrochloride is a blocker of polycystin-2 (PC2;TRPP2[4]) channel.
A potent, selective orally-bioavailable TRPV4 antagonist with IC50 of 320, 420 and 660 nM for mouse, human and rat TRPV4 channels, respectively; >15-fold selectivity for TRPV4 over TRPV1, TRPV3 and TRPM8, and a panel of 54 other common biological targets.
AS1269574 is a potent, orally available GPR119 agonist, with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes[1][2].
Vanilloid receptor antagonist 1 is a potent vanilloid receptor TRPV1 antagonist extracted from patent US8349852B2, compound B8[1].
Moringin is a potent and selective TRPA1 ion channel natural agonist with an EC50 of 3.14 μM. Moringin does not activate or activates very weakly the vanilloids somatosensory channels TRPV1, TRPV2, TRPV3 and TRPV4, and the melastatin cooling receptor TRPM8. Moringin has hypoglycemic, antimicrobial, anti-inflammatory, anticancer and neuroprotection activities[1][2].
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.
Mifamurtide(CGP19835; MTP-PE) is a drug against osteosarcoma.Target: OthersMifamurtide is an immunomodulator with antitumor effects that appear to be mediated via activation of monocytes and macrophages. Mifamurtide is generally well tolerated; adverse events attributed to administration of the drug include chills, fever, headache, nausea, and myalgias. Based on the available data, mifamurtide can be considered for inclusion in treatment protocols for localized osteosarcoma [1]. Mifamurtide has orphan drug status for the treatment of osteosarcoma in the US and EU [2].
RQ-00203078 is a highly selective, potent and orally available TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively), exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1. IC50 value: 5.3 nM (for rat channel), 8.3 nM nM ( for human channel)Target: TRPM8in vitro: RQ-00203078 reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion.in vivo: RQ-00203078 demonstrates excellent in vivo activity in a dose dependent manner with an ED50 value of 0.65 mg/kg in the icilin-induced wet-dog shakes model in rats after oral administration and may become an important pharmacological tool for fully assessing the potential therapeutic use of the targets activated by cold stimulation. RQ-00203078 also attenuates icilin-induced wet dog shakes in rats.
NMDAR/TRPM4-IN-2 free base (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 free base shows neuroprotective activity. NMDAR/TRPM4-IN-2 free base prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 free base protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss[1].
AC1903 is a potent, specific TRPC5 channel inhibitor with IC50 of 14.7 uM; blocks riluzole-activated TRPC5 whole-cell current, but fails to block carbachol (CCh)-induced TRPC4 and OAG-induced TRPC6 currents, even at high micromolar concentrations; pecifically blocks TRPC5 channel activity in glomeruli of proteinuric rats, suppresses severe proteinuria and prevents podocyte loss in a transgenic rat model of FSGS.
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.
VPC01091.4 (VPC4) is a?TRPM7?inhibitor and blocks TRPM7 current at low micromolar concentrations. VPC01091.4 is an efficacious?anti-inflammatory?agent that arrests systemic inflammation in vivo[1].
AMG 333 is a potent and highly selective TRPM8 antagonist with an IC50 of 13 nM.