TRP Channel Inhibitor

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

TRPC3/6-IN-1 is a potent selectivity blocker of the canonical transient receptor channels (TRPC3/6), has block potency for hTRPC3 and hTRPC6 with IC₅₀ values of 1260 nM and 500 nM, respectively. TRPC3/6-IN-1 can be used for the research of chronic models of heart failure.

TAT-EE3 is a neuroprotective peptide which can uncouple TRPM2-NMDARs interaction. TAT-EE3 inhibits TRPM2-induced enhancement of NMDAR surface expression and current amplitude.TAT-EE3 protects neurons against ischemic injury in vitro and in vivo. TAT-EE3can be used for the study of ischemic stroke.

TRPV4-IN-5 (Compound 1f) is a potent TRPV4 inhibitor (IC₅₀ = 0.46 μM). TRPV4-IN-5 significantly alleviates the symptoms of acute lung injury induced by lipopolysaccharide (HY-D1056) in mice.

TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC₅₀ of 4.66 μM.

CMP233 is a potent antagonist of TRPM4, with the IC₅₀ of 0.15 μM. CMP233 plays an important role in neurodegenerative disorders research.

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.

ZA18 is a selective TRPM2 channel inhibitor, with an IC₅₀ value of 6.2 μM. ZA18 can effectively suppress intracellular Ca²⁺ overload triggered by TRPM2 channel activation. ZA18 significantly reduce the mortality of SH-SY5Y cells induced by H2O2. ZA18 can be used for the study of ischemia-reperfusion injury, inflammation, or other neurodegenerative diseases.

FP802 is an orally active potent TwinF interface inhibitor that disrupts and detoxifies the NMDAR/TRPM4 death complex. FP802 exerts powerful neuroprotective effects in the 5xFAD mouse model of Alzheimer’s disease (AD) by preventing cognitive decline, preserving neuronal structural integrity, reducing amyloid-β plaque formation, and mitigating mitochondrial pathology. FP802 stops loss of motor neurons, reduces serum neurofilament light chain (NfL) levels, improves motor performance, and extends life in a mouse model of amyotrophic lateral sclerosis (ALS). FP802 can be used for AD and ALS research.

TRPV6-IN-1 is a potent and selective TRPV6 inhibitor. TRPV6-IN-1 has anti-proliferative effect and can be used for the research of cancer.

Clemizole-d₄ is the deuterated-labeled Clemizole (HY-30234). Clemizole is an orally active, blood-brain barrier permeable TRPC5 inhibitor, with an IC₅₀ value of 1.05-1.34 μM against mouse TRPC5. Clemizole 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 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.

8-Br-ADPR disodium (8-Bromoadenosine-5'-O-diphosphoribose) is a TRPM2 inhibitor and ADPR signaling pathway antagonist. 8-Br-ADPR disodium inhibits glucagon-mediated nuclear calcium signaling and downstream CaMKII/CREB phosphorylation by blocking ADPR-induced TRPM2 activation. 8-Br-ADPR disodium significantly reduces gluconeogenic gene expression and blood glucose levels in diabetic models. 8-Br-ADPR disodium 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 disodium is widely used in studies related to diseases such as diabetes, melanoma and lymphoma.

TRPA1 Antagonist 1 is a methylene phosphate proagent which converts to its active parent agent, a TRPA1 antagonist with an IC₅₀ of 8 nM.

DS88790512 is a potent, selective, and orally bioavailable TRPC6 inhibitor with an IC₅₀ of 11 nM.

Primidone-d₅ is the deuterium labeled Primidone. Primidone is the orally active inhibitor for TRPM3 (IC₅₀ = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for GABA receptor. Primidone can be used as the analgesic and anticonvulsant agent.

ZA10 is a selective TRPM2 channel inhibitor, with an IC₅₀ value of 8.1 μM. ZA10 can effectively suppress intracellular Ca²⁺ overload triggered by TRPM2 channel activation. ZA10 significantly reduce the mortality of SH-SY5Y cells induced by H2O2. ZA10 can be used for the study of ischemia-reperfusion injury, inflammation, or other neurodegenerative diseases.

FAAH/TRPV1 blocker-1 (compound 2R) is a dual FAAH/TRPV1 blocker, with IC₅₀ of 0.12 and 94.9 μM, respectively. FAAH/TRPV1 blocker-1 plays an important role in analgesic and anti-inflammatory research.

AAL-149 is a FTY720 (HY-12005) analog and TRPM7 inhibitor (IC₅₀ = 1.081 μM) with multimodal anti-inflammatory effects and without targeting S1P receptors. AAL-149 can be utilized in anti-inflammatory research.

3-Chlorobenzoic acid (Standard) is the analytical standard of 3-Chlorobenzoic acid. This product is intended for research and analytical applications. (±)-Eriodictyol ((±)-Huazhongilexone; Dihydroluteolin) is an orally active TRPV1 receptor antagonist (IC₅₀=44-47 nM, rTRPV1) with antioxidant and anti-inflammatory activities. (±)-Eriodictyol effectively inhibits lipid peroxidation and the release of proinflammatory cytokines by specifically antagonizing the TRPV1 receptor and activating the Nrf2 signaling pathway. (±)-Eriodictyol reduces the levels of ICAM-1, VEGF, eNOS and TNF-α in the retina and maintains the integrity of the blood-retinal barrier. (±)-Eriodictyol alleviates oxidative stress-induced apoptosis and hyperalgesia, enhances the activity and cytotoxicity of immune cells (such as B lymphocytes, NK cells and macrophages), and increases the levels of antioxidant enzymes simultaneously. (±)-Eriodictyol can be used in the research of diabetic retinopathy, acute lung injury and various pain-related diseases.

AMG-8562 is a selective, orally active transient receptor potential vanilloid 1 (TRPV1) modulator that inhibits the activation of rat TRPV1 by Capsaicin (HY-10448), Anandamide (HY-10863) and N-arachidonyldopamine (HY-110018), with IC₅₀ values of 1.75, 9.29 and 3.87 nM, respectively. AMG-8562 blocks capsaicin-induced activation, potentiates pH5-induced activation and has no effect on heat-induced activation of rat TRPV1, whereas it completely blocks capsaicin- and heat-induced activation and partially blocks pH5-induced activation of human TRPV1. AMG-8562 can be used in studies of TRPV1 activation patterns, hyperalgesia and pain-related research.