TRP Channel Inhibitor

ZQMT-10 is an orally active and potent antagonist of TRPA1, with the K_d of 1.04 μM. ZQMT-10 plays an important role in cancer research.

BTB 06061 is a TRPM7 inhibitor and can be used for study of ischemic disease.

17(R)-Resolvin D1-d₅ (17(R)-RvD1-d₅) is deuterium labeled 17(R)-Resolvin D1. 17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells. 17R-Resolvin D1 specificially inhibits TRPV3 with an IC₅₀ of 398 nM and exhibits peripheral anti-nociceptive efficacy.

NS8593 is an SK channel (small conductance Ca²⁺-activated K+ channels) inhibitor. NS8593 reversibly inhibited recombinant SK3-mediated currents (human SK3 and rat SK3). NS8593 inhibits all the SK1-3 subtypes Ca²⁺-dependently (K_d = 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca²⁺). NS8593 does not affect the Ca²⁺-activated K channels of intermediate and large conductance (hlk and hBK channels, respectively). NS8593 can also inhibit TRPM7 (melastatin-related TRP cation channel 7) (IC₅₀ = 1.6 mM). NS8593 can be used for the study of central nervous system (CNS) related diseases.

8-Br-ADPR (8-Bromoadenosine-5'-O-diphosphoribose) is a TRPM2 inhibitor and ADPR signaling pathway antagonist. 8-Br-ADPR inhibits glucagon-mediated nuclear calcium signaling and downstream CaMKII/CREB phosphorylation by blocking ADPR-induced TRPM2 activation. 8-Br-ADPR significantly reduces gluconeogenic gene expression and blood glucose levels in diabetic models. 8-Br-ADPR effectively blocks ADPR-mediated calcium signal transduction in NK cells, inhibits immune synapse formation, granzyme B release and cytolytic activity against melanoma cells. 8-Br-ADPR is widely used in studies related to diseases such as diabetes, melanoma and lymphoma.

TRPC5-IN-3 is a potent TRPC5 inhibitor with IC₅₀ of 10.75 nM (WO2022001767A1, L001).

TRPC5-IN-2 is a potent TRPC5 inhibitor (WO2019055966A2，Compound IO).

TRPA1-IN-5 is a TRPA1 inhibitor with inhibitory activity against TRPA1. TRPA1-IN-5 has pharmacokinetic and pharmacodynamic activities.

N-oleoyl-glutamine is a PM20D1-regulated N-acyl amino acids (NAAs). N-oleoyl-glutamine is a transient receptor potential (TRP) antagonist.

TRPM5 agonist-1 is an orally active TRPM5 agonist with a pEC₅₀ of 8.1. TRPM5 agonist-1 shows excellent selectivity (> 100-fold) versus related cation channels (TRPM8, TRPV1, TRPV4, TRPA1, TRPM4). TRPM5 agonist-1 exhibits locally acting stimulatory effect on gastrointestinal transit in mice. TRPM5 agonist-1 can be used for research on promoting gastric motility.

TRPV4/TRPA1-IN-1 is a TRPV4/TRPA1 inhibitor that suppresses TRPV4/TRPA1-mediated calcium influx. TRPV4/TRPA1-IN-1 alleviates pain behaviors in a mouse trigeminal stimulation pain model and inhibits inflammation and pain-related behaviors in a mouse acute pancreatitis model. TRPV4/TRPA1-IN-1 can be used in research on acute pancreatitis.

TRPM2-IN-2 is a potent and selective TRPM2 inhibitor (IC₅₀ = 0.66 μM) with minimal activity against TRPM8 and TRPV1 (IC₅₀ >10 μM). TRPM2-IN-2 exhibits robust neuroprotective effects in both in vitro oxygen-glucose deprivation/reperfusion (OGD/R) model and in vivo transient middle cerebral artery occlusion (tMCAO) mouse model. TRPM2-IN-2 can be used for ischemic stroke research.

hTRPA1-IN-1 (19), a norsesterterpenoid that can be isolated from the Marine Sponge Diacarnus spinipoculum, is an inhibitor of transient receptor potential Ankyrin 1 (TRPA1), with an IC₅₀ of 2 μM.

TRPA1-IN-4 (12) is a TRPA1 inhibitor, with an IC₅₀ of 45 nM. TRPA1-IN-4 (12) can be used in the pain research.

Alginate oligosaccharides (AOS) are orally effective linear oligosaccharides with anti-inflammatory, antioxidant and antimicrobial activities. Alginate oligosaccharides inhibit the activation of NLRP3 inflammasome and NF-κB, promote nuclear translocation of Nrf2 and phosphorylation of AMPK, and reduce the enhanced functional level of TRPV1. Alginate oligosaccharides improve oxidative stress, ROS production, mitochondrial bioenergetic dysfunction and gait impairment. Alginate oligosaccharides inhibit the release of neuropeptides; alter the structure and viscoelasticity of mucin matrix; disrupt bacterial and fungal biofilms; regulate gut microbiota; and exert anti-apoptotic effects.

Murpanicin (murraxocin) is a coumarin that is a thermosensitive transient receptor potential vanilloid 2 (TRPV2) channel inhibitor. Murpanicin has significant anti-inflammatory and insecticidal effects.

TRPC3-IN-1 is a human transient receptor potential canonical 3 (hTRPC3) inhibitor with an IC₅₀ of 0.09 μM. TRPC3-IN-1 inhibits hTRPC3-mediated currents. TRPC3-IN-1 is applicable to research related to diseases such as epilepsy.

A 80426 is an orally active serotonin (5-HT uptake) inhibitor (IC₅₀ = 13 nM; K_i = 3.8 nM) and α₂-Adrenoceptor receptor antagonist (K_i = 2 nM). A 80426 shows weak antagonistic effect to dopamine D₁ receptor (K_i = 744 nM) and D₂ receptor (K_i = 52 nM). A 80426 upregulates the expression and activity of TRPV1, activates the NF-κB and PI3K pathways, and reduces the levels of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. A 80426 can be used in research related to inflammatory pain and depression.

TRPM4-IN-4 (Compound 118) is a selective TRPM4 inhibitor with an IC₅₀ value of 0.339 μM against hTRPM4. TRPM4-IN-4 inhibits hTRPM4 and mTRPM4. TRPM4-IN-4 can be used for the research of colorectal cancer.

TRPC5-IN-4 is potent and safe TRPC inhibitor with IC₅₀ value of 14.07 nM and 65 nM for TRPC5 and TRPC4, respectively. TRPC5-IN-4 shows no damage on the cellular component of liver and kidney. TRPC5-IN-4 can be used for the research of chronic kidney disease (CKD).