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.

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.

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).

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.

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).

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).

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

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.

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.

Resolvin D2 (RvD2) is a potent TRPV1 inhibitor and pro-absorptive mediator with anti-inflammatory, anti-infective and pro-absorptive effects for the study of immune disorders and cancer.

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

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

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

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

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.

(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.

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.

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].

N-[(1S)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-N'-1H-indazol-4-ylurea is a potent TRPV1 antagonist, blocking activation of TRPV1 by capsaicin with the IC50 of 123 nM.

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).

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

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.

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.

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.

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.

Caffeic Acid is an orally bioavailable, hydroxycinnamic acid derivative and polyphenol, with potential anti-oxidant, anti-inflammatory, and antineoplastic activities.

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

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

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.

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.

Adenosine 5'-diphosphoribose sodium (ADP ribose sodium) is a metabolite of nicotinamide adenine nucleotide (NAD+), which is widely present in organisms.Adenosine 5'-diphosphoribose sodium (ADP ribose sodium) is a potent intracellular Ca2+-permeable cation TRPM2 channel activator. Adenosine 5'-diphosphoribose sodium (ADP ribose sodium) is a potent intracellular Ca2+ permeable cation TRPM2 channel activator that also induces autophagy.)

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

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.

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

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.

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

ML-SI3 is an inhibitor of the TRPML family of calcium channels that selectively inhibits TRPML1, TRPML2, and TRPML3. ML-SI3 can be used to study neurodegenerative and cardiovascular diseases.

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.

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

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.

PF-05105679 is a selective TRPM8 antagonist (IC50 = 103 nM). PF-05105679 can be used in research on cold-related pain.

GSK205 is a selective TRPV4 antagonist that blocks Ca(2+) signaling and may be used to reduce inflammation and pain.

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

ICILIN (AG-3-5) is a synthetic TRPM8 ion channel super-agonist.

1. 8-Gingerol has antioxidant activity. 2. 8-Gingerol has antimycobacterial activity. 3. 8-Gingerol could be used as an effective skin-whitening agent. 4. 8-Gingerol shows antipyretic and anti-inflammation characteristics. 5. 8-Gingerol seems to be effect

Asivatrep (PAC14028) is a selective and potent antagonist of transient receptor potential vanilloid subtype 1 (TRPV1) for the study of atopic dermatitis.

Podocarpic acid is a natural product and a novel TRPA1 activator.