TRP/TRPV Channel

D-GsMTx4 TFA, a selective spider venom peptide, is a TRPC1/6 and Piezo2 inhibitor that inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families, blocks cation-selective stretch-activated channels (SACs), and attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglia reactivity. toxicity and microglia reactivity.D-GsMTx4 TFA prevented myocardial infarction in a mouse model of ischemia/reperfusion and can be used to characterize the role of excitatory MSCs in normal physiology and pathology.

Trovafloxacin is a broad-spectrum fluoroquinolone antibiotic that inhibits the activity of DNA gyrase and topoisomerase IV, enzymes involved in DNA replication. It also acts as an effective and specific inhibitor of the pannexin 1 channel (PANX1, IC50 = 4 μM).

Capsaicin ((E)-Capsaicin) is a natural product extracted from Capsicum annuum, and is a TRPV1 agonist (EC50=0.29 μM). Capsaicin has antitumor, anti-inflammatory, antioxidant and neuroprotective activities.

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

Vanilloid receptor antagonist 1 (4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile) is a potent vanilloid receptor TRPV1 antagonist.

Clemizole, an H1 histamine receptor antagonist, inhibits NS4B's RNA binding and hepatitis C virus (HCV) replication.

(Z)-Capsaicin (Zucapsaicin) is a medication used to treat osteoarthritis of the knee and Others neuropathic pain.(Z)-Capsaicin is a synthetic cis isomer of natural capsaicin that has shown therapeutic efficacy in pain accompanying osteoarthritis of the knee.

Vocacapsaicin hydrochloride (CA-008 hydrochloride) is a non-opioid TRPV1 agonist, a raw material for capsaicin, and is used for pain relief.

Elismetrep (MT-8554) is an orally available TRPM8 inhibitor with potential analgesic activity for the study of vasomotor symptoms in postmenopausal women.

ASP7663 is a TRPA1 Receptor Agonist and exhibiting an abdominal analgesic effect in vivo.

AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat TRPV1, respectively).

Hydroxy-α-sanshool is an alkyl amide isolated from the pepper. It acts as a TRPA1 covalent and TRPV1 non-covalent agonist (EC50s: 69 and 1.1 μM).

GSK2193874 was identified as a selective, orally active TRPV4 blocker.

BI-749327 is a high selectivity and orally bioavailable antagonist of TRPC6 (IC50s: 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6).

Pico145 (HC-608) is a remarkable inhibitor of TRPC1 4 5 channels, specifically inhibiting ( )-englerin A-activated TRPC4 TRPC5 channels with IC50s of 0.349 and 1.3 nM in cells, while showing no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, or TRPM8.

Capsazepine is an antagonist of TRPV1 receptor ( IC50 : 562 nM). Capsazepine blocks the painful sensation of heat caused by capsaicin (the active ingredient of chilli pepper) which activates the TRPV1 ion channel. It is therefore considered to be a capsaicin antagonist.

A 967079 is a potent, selective, and bioavailable inhibitor of the TRPA1 channel, with IC50 values of 67 and 289 nM for the human and rat isoforms, respectively.

Fingolimod hydrochloride (FTY720) , a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).

Diphenyleneiodonium chloride (DPI)(DPI) is an irreversible inhibitor of iNOS and eNOS (IC50 values of 50 nM and 0.3 μM, respectively),and displays broad-spectrum bactericidal activity.

HC-067047 is a potent and selective TRPV4 antagonist that also inhibits the endogenous TRPV4-mediated response to 4α-PDH.

ML-SA1 (Mucolipin synthetic agonist 1) is 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[1].

SKF-96365 hydrochloride (SKF96365) , a SOCE inhibitor, exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal Y cells. SKF-96365 hydrochloride can induce cytoprotective autophagy to delay apoptosis by preventing the release of cytochrome c (cyt c) from the mitochondria into the cytoplasm. Mechanistically, SKF-96365 hydrochloride treatment inhibited the calcium calmodulin-dependent protein kinase IIγ (CaMKIIγ) AKT signaling cascade in vitro and in vivo. Overexpression of CaMKIIγ or AKT abolished the effects of SKF-96365 on Y cells, suggesting a critical role of the CaMKIIγ AKT signaling pathway in SFK-96365-induced biological effects. SKF-96365 hydrochloride inhibited hERG current in a concentration-dependent manner.

2-Aminoethyl diphenylborinate (2-APB) is a chemical compound that inhibits IP3 receptors and TRP channels, though it activates TRPV1, TRPV2, and TRPV3 at higher concentrations.

Pinokalant (LOE-908) is a novel non-selective cation channel inhibitor.Pinokalant significantly reduces cortical infarct volume in in vivo experiments, improves the metabolic and electrophysiological status of the ischemic penumbra region, and reduces the size of the lesion on magnetic resonance images in the acute phase after middle cerebral artery occlusion in rats.Pinokalant is a potential SARS-CoV-2 protease inhibitor for the study of stroke.

GSK1016790A (GSK101) (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34 nM in choroid plexus epithelial cells.

Probenecid (Benemid) is a benzoic acid derivative with antihyperuricemic property.

Dihydrocapsaicin (CCRIS1589) is isolated from Capsicum fruit. Capsaicin is the primary active component of the heat and pain-eliciting lipid soluble fraction of the Capsicum pepper. Like capsaicin, dihydrocapsaicin is an irritant. Capsaicin is found in natural hot pepper extracts along with a number of impurities, including dihydrocapsaicin and several lesser impurities. Separation by HPLC is required in order to obtain pure dihydrocapsaicin. Dihydrocapsaicin represents about 10% of the compound present in commercial preparations purporting to be pure capsaicin, but it has about the same pungency as capsaicin. VR1 (vanilloid receptor 1) is a heat activated calcium ion channel which functions as a part of the normal nociceptive pain pathway. Capsaicin elicits a sensation of burning pain by activation of VR1 on small, non-myelinated polymodal C-type nociceptive nerve fibers. The potency of dihydrocapsaicin at VR1 appears equivalent to capsaicin. Antioxidant. Reduces oxidation of serum lipids. Mutagenic. Dihydrocapsaicin is an activator of VR1.

N-Oleoyl Glutamine (Oleoyl-L-glutamine) is an N-acyl amino acid involved in the regulation of PM20D1 and antagonizes TRPV1 of the transient receptor potential (TRP) calcium channel.

EIPA (L593754) is a TRPP3 channel inhibitor (IC50=10.5 μM) and an inhibitor of Na+ H+ exchange (NHE). EIPA inhibits megacytosis, promotes autophagy, and can be used in inflammation and tumor studies.

ABT 102 (CHEMBL398338) is a selective antagonist of transient receptor potential vanilloid 1 (TRPV1) receptor.

AC1903 is a specific inhibitor of TRPC5 channel, and has been shown to suppress severe proteinuria and prevent podocyte loss.

MDR-652 is a highly specific and efficacious agonist of nonpungent transient receptor potential vanilloid 1 (TRPV1), with Ki values of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1, respectively, and EC50s of 5.05 nM and 93 nM for hTRPV1 and rTRPV1, respectively. MDR-652 is a potent topical analgesic.

Capsiate is an orally active TRPV1 agonist, a non-irritating capsaicin analog that acts as an antiallergic agent with anti-inflammatory, antioxidant, hypoglycemic, and inhibitory angiogenic activity.

IA-Alkyne (Iodoacetamide-alkyne) is a TRP channel (TRPC) agonist. IA-Alkyne can be used to develop an isotopically tagged probe for quantitative cysteine-reactivity profiling. It also has the potential for the study of respiratory infection.

Imperatorin (8-Isopentenyloxypsoralene) is a modulator of p38, ERK pathway. Imperatorin increases BMP-2 expression (mRNA) and increases bone density volume and mineralization in vivo.

9-Phenanthrol is inhibitor of the transient receptor potential melastatin 4 (TRPM) channel, a Ca2+ -activated non-selective cation channel.

TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.

CIM0216 is a synthetic TRPM3 activator whose potency and apparent affinity greatly exceeds that of the canonical TRPM3 agonist.

PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel, eliciting TrpA1-mediated nocifensive behavior in mouse, with EC50 values of 97 nM and 23 nM for [rTrpA1] and [hTrpA1], respectively.

Linoleoyl Ethanolamide is an endocannabinoid agent. It acts by binding to TRPV1 increasing ERK phosphorylation and AP-1 dependent transcription in CB-receptor in an independent manner.

AM404 is an endocannabinoid reuptake inhibitor, a TRPV(1) activator, a paracetamol metabolite, with neuroprotective and anticancer activity that blocks anandamide transport. AM404 inhibits NFAT and NF-kappaB signaling pathways and impairs migration and invasiveness of neuroblastoma cells, preventing prostaglandin synthesis in activated microglia by inhibiting COX activity.

D-3263 hydrochloride (D3263 HCl salt) is enteric-coated, orally bioavailable transient receptor potential melatonin member 8 (TRPM8) agonist.

Piromelatine is an agonist of melatonin MT1 MT2 receptors, 5-HT1A and 5-HT1D, and an antagonist of 5-HT2B.Piromelatine has antinociceptive activity with inhibitory effects on P2X3, TRPV1, and Nav1.7 channels, and can be used in studies of sleep-promoting, pain-relieving, anti-neurodegenerative, and antidepressant diseases. diseases, and can be used to improve memory deficits associated with chronic mild stress-induced lack of pleasure in rats.

LASSBio-1135 is an orally effective antagonist of TRPV1 and inhibitor of TNF-α production.

α-Spinasterol is a transient receptor potential vanilloid 1 (TRPV1) antagonist, has anti-inflammatory, antidepressant, antioxidant and antinociceptive effects. α-Spinasterol inhibits COX-1 andCOX-2 activities with IC50 values of 16.17 μM and 7.76 μM, respectively.

Mesendogen is an inhibitor of TRPM6. Mesendogen alters magnesium homeostasis, promotes mesoderm and definitive endoderm differentiation.

WS-12 is a potent TRPM8 agonist that acts as a cooling agent (EC50 : 193 nM)

TRPM4-IN-1 (4-chloro-2-(2-(2-chlorophenoxy)acetamido)benzoic acid) is a potent and selective inhibitor of TRPM4 with an IC50 of 1.5 μM.