TRP Channel Inhibitor

DD-161515 is a TRPV1/VR1 inhibitor with an IC₅₀ of 0.7 μM in rats. DD-161515 binds to an allosteric site of TRPV1 distinct from that of capsaicin, blocks channel opening, inhibits receptor-mediated calcium ion influx, reduces the excitability of peripheral sensory nerve fibers, and thereby inhibits nociception induced by heat and transmission of chemically induced pain signals. DD-161515 can be used in studies related to inflammatory pain.

EIPA (Standard) is the analytical standard of EIPA. This product is intended for research and analytical applications. EIPA (L593754) is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also enhances autophagy by inhibiting Na+/H+-exchanger 3 (NHE3). EIPA inhibits macropinocytosis as well. EIPA can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma.

Dyclonine hydrochloride (Standard) (Dyclocaine hydrochloride (Standard)) is the analytical standard of Dyclonine hydrochloride (HY-B0364A). This product is intended for research and analytical applications. 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.

Larixyl acetate (Standard) is the analytical standard of Larixyl acetate. This product is intended for research and analytical applications. Larixyl acetate is a potent and selective TRPC6 inhibitor with IC₅₀ values of 0.58 μM and 6.83 μM against hTRPC6-YFP and hTRPC3-YFP, respectively. Larixyl acetate prevents HPV and is effective in protecting against traumatic brain injury-induced systemic endothelial dysfunction.

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

Resolvin D2 methyl ester is an ester derivative of the DHA (HY-B2167) metabolite Resolvin D2 (HY-121636) with anti-inflammatory and anti-infective activities. Resolvin D2 is a leukocyte modulator and a potent inhibitor of neuronal TRPV1 (IC₅₀=0.1 nM) and TRPA1 (IC₅₀=2 nM). Resolvin D2 can be used in sepsis research.

Clemizole sulfate is an orally active, blood-brain barrier permeable TRPC5 inhibitor, with an IC₅₀ value of 1.05-1.34 μM against mouse TRPC5. Clemizole sulfate 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 sulfate 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.

BD-1063 is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 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 also significantly reduces excessive ethanol self-administration behavior. BD-1063 is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence.

HC-030031 (Standard) is the analytical standard of HC-030031. This product is intended for research and analytical applications. HC-030031 is a potent and selective TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.

Pyr3 (Standard) is the analytical standard of Pyr3 (HY-108465). This product is intended for research and analytical applications. Pyr3 is a selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC₅₀ of 700 nM for TRPC3-mediated Ca2+ influx.

Crotamiton (Standard) is the analytical standard of Crotamiton. This product is intended for research and analytical applications. Crotamiton is a TRPV4 inhibitor. Crotamiton inhibits TRPV4 currents. Crotamiton inhibits TRPV4 selective agonist-induced pruritus-related behaviors in mice. Crotamiton inhibits Histamine- and Chloroquine-induced calcium influx via the H1R/TRPV1, MRGPRA3/TRPA1 pathways, and also suppresses calcium influx in primary mouse dorsal root ganglion neurons. Crotamiton is applicable to research related to pruritus, scabies, and non-scabietic pruritus.

Mesendogen (Standard) is the analytical standard of Mesendogen (HY-103073). This product is intended for research and analytical applications. Mesendogen is a TRPM6 inhibitor. Mesendogen enhances the mesoderm and definitive endoderm (DE) differentiations of human embryonic stem cells (hESCs) and human induced pluripotent stem cells (hiPSCs). Mesendogen can be used for the research of magnesium homeostasis during early embryonic cell development.

Clemizole penicillin is a composite preparation containing two active components, Clemizole (HY-30234) and penicillin, with antihistamine, anti-inflammatory, and bactericidal activities. The Clemizole component of Clemizole penicillin targets the H₁ receptor, CrtN, and TRPC5 calcium channel, while penicillin exerts antibacterial effects. The clemizole contained in Clemizole penicillin acts as a reversible competitive inhibitor of the TRPC5 calcium channel; it also competitively targets the CrtN enzyme of Staphylococcus aureus to block staphyloxanthin biosynthesis. Clemizole penicillin can be used in research on lobar pneumonia and syphilis.

Piromelatine (Standard) is the analytical standard of Piromelatine. This product is intended for research and analytical applications. Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.

M084 hydrochloride is a TRPC4/5 channel blocker, with IC₅₀ values of 10.3 μM and 8.2 μM, respectively. M084 hydrochloride has antidepressant and anxiolytic effects.

Amiloride-¹⁵N₃ (MK-870-¹⁵N₃) is ¹⁵N labeled Amiloride. 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.

EIPA (hydrochloride) (Standard) is the analytical standard of EIPA (hydrochloride). This product is intended for research and analytical applications. EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na+/H+-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma.

AMG-628 is an orally active inhibitor for TRPV1, that inhibits Capsaicin (HY-10448) or acid (pH 5)-induced Ca²⁺ influx into TRPV1- expressing CHO cell with IC₅₀ of 4.9 and 3.1 nM. AMG-628 exhibits analgesic activity in Capsaicin (HY-10448)-induced rat model, and exhibits a half-life of 2.4 h in rats.

Zerencotrep (Standard) is the analytical standard of Zerencotrep (HY-101507). This product is intended for research and analytical applications. Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (-)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.

A-784168 (Standard) is the analytical standard of A-784168 (HY-108460). This product is intended for research and analytical applications. A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration.