TRP Channel Inhibitor

Isosakuranetin is a flavanone flavonoid which can be found in the fruit of Citrus bergamia. Isosakuranetin is a TRPM3 blocker.

SAR7334 is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC₅₀ of 7.9 nM.

TRPV2-selective blocker 1 is a TRPV2-selective blocker that inhibits calcium influx and ionic currents. TRPV2-selective blocker 1 exhibits an IC₅₀ of 6.3 μM against rat TRPV2, and shows no activity against TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 attenuates macrophage phagocytosis, LPS-induced macrophage migration, and calcium microdomains generated by peripheral TRPV2. TRPV2-selective blocker 1 is non-cytotoxic and can be used to investigate the function of TRPV2 during immune processes.

TRPM4-IN-2 (NBA) is a potent transient receptor potential melastatin 4 (TRPM4) inhibitor with an IC₅₀ value of 0.16 μM. TRPM4-IN-2 can be used for researching prostate cancer and colorectal cancer.

ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca²⁺ channels.

GSK2798745 is a potent, selective, and orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC₅₀s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 can be used in cardiac and respiratory diseases research.

BD-1063 dihydrochloride is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 dihydrochloride exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 dihydrochloride also significantly reduces excessive ethanol self-administration behavior. BD-1063 dihydrochloride is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence.

TRPM4-IN-1 (CBA) is a potent and selective inhibitor of the cation channel TRPM4, with an IC₅₀ of 1.5 μM. TRPM4-IN-1 can be used for the research of cardiac diseases and prostate cancer.

Apecotrep (TRPC6-IN-3) (compound 17) is a potent, orally active transient receptor potential C6 ion channel (TRPC6) inhibitor. Apecotrep modulates not only intracellular calcium concentration, but also membrane potential by modulating the flux of cations including calcium and sodium ions. Apecotrep can be used in research of respiratory system.

AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model.

Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis.

Trpvicin is a potent and subtype-selective TRPV3 inhibitor with IC₅₀s of 0.41 and 0.22 μM for hTRPV3-WT and hTRPV3-G573S mutant, respectively. Trpvicin exhibits minimal effects on other TRP family members (such as TRPV1/2/4/5/6, TRPA1 and TRPM8). Trpvicin inhibits the TRPV3 channel by stabilizing it in a closed state via VSLD-PD binding. Trpvicin accesses additional binding sites inside the central cavity of the G573S mutant to remodel symmetry and block the channel. Trpvicin inhibits itch and hair loss in mouse models. Trpvicin can be used for study of inflammation and immunology.

Tivanisiran sodium (SYL1001 sodium) is a small interfering RNA (siRNA) targeting TRPV1 . Tivanisiran sodium induces the degradation of TRPV1 mRNA, thereby inhibiting protein synthesis. Tivanisiran sodium alleviates ocular discomfort and pain, and improves ocular hyperemia and tear quality. Tivanisiran sodium is applicable to research related to dry eye disease.

Clemizole hydrochloride is an orally active, blood-brain barrier permeable TRPC5 inhibitor, with an IC₅₀ value of 1.05-1.34 μM against mouse TRPC5. Clemizole hydrochloride blocks TRPC1:TRPC5, TRPC3, TRPC4, TRPC6, TRPC7, hERG, hKCNQ1/hKCNE1 and hKv1.5 channels, and activates TRPA1; it modulates 5HT-2B and HTR2A receptors; it inhibits HCV RNA replication, CrtN enzymatic activity, oxidative stress, neuroinflammation, cell apoptosis and bacterial virulence; it maintains blood-brain barrier (BBB) integrity; it enhances DNA repair capacity; it improves cell viability; and it alters cardiac electrophysiological properties. Clemizole hydrochloride can be used in the research of Dravet syndrome, hepatitis C virus infection, Staphylococcus aureus skin infection, Cisplatin (HY-17394)-induced nephrotoxicity, STXBP1-related diseases, traumatic brain injury and xeroderma pigmentosum type C.

Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca²⁺ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC₅₀ of 0.72 μM (IC₅₀ of 13.08 μM for store operated Ca²⁺ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels.

Resolvin D2 is a metabolite of docosahexaenoic acid (DHA), with anti-inflammatory, anti-infective activities. Resolvin D2 is a potent regulator of leukocytes and controls microbial sepsis. Resolvin D2 is a remarkably potent inhibitor of TRPV1 (IC₅₀ = 0.1 nM) and TRPA1 (IC₅₀ = 2 nM) in primary sensory neurons.

VPC01091.4 (VPC4) is a TRPM7 inhibitor and blocks TRPM7 current at low micromolar concentrations. VPC01091.4 can penetrate the blood-brain barrier. VPC01091.4 is an efficacious anti-inflammatory agent that arrests systemic inflammation in vivo.

(rel)-ML-SI3 is one of the active ingredients of ML-SI3 (HY-139426) (another component is (cis)-ML-SI3) that targets three isoforms of TRPML. (rel)-ML-SI3 is an inhibitor of TRPML1 and TRPML3 (IC₅₀=3.1 μM/28.5 μM), and a potent activator of TRPML2 (EC₅₀=3.3 μM).

BTD is a selective transient receptor potential canonical 5 (TRPC5) activator. BTD can be used for the research of neurological disease.

Amiloride (hydrochloride) (Standard) is the analytical standard of Amiloride (hydrochloride). This product is intended for research and analytical applications. Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride is a blocker of polycystin-2 (PC2; TRPP2) channel.