>98%,Standard References

A membrane permeable IP3 receptor antagonist and broad TRP channels (TRPC5, TRPM2) blcoker.

A small molecule positive allosteric modulator of both proton and vanilloid activation of TRPV1 (EC50=21.3 uM).

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.

AMG 333 is a potent and highly selective TRPM8 antagonist with an IC50 of 13 nM.

AMG 517 is a potent and selective TRPV1 antagonist, antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM.

AMG9810 is a potent and selective, competitive vanilloid TRPV1 receptor antagonist (IC50 = 17 nM).

ASP 7663 is a selective TRPA1 activator (EC50 values are ~0.5 μM in human, mouse and rat).

BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.

Clemizole is a H1 histamine receptor antagonist.Recently, researchers have identified that clemizole hydrochloride can inhibit NS4B's RNA binding and hepatitis C virus (HCV) replication.

Clemizole is a H1 histamine receptor antagonist.Recently, researchers have identified that clemizole hydrochloride can inhibit NS4B's RNA binding and hepatitis C virus (HCV) replication.

GSK1016790A is a novel and potent TRPV4 channel agonist.

GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC50 of 2 nM and 40 nM for rTRPV4 and hTRPV4.

HC-067047 is a potent and selective TRPV4 antagonist with IC50 values of 48 ± 6 nM, 133 ± 25 nM, and 17 ± 3 nM, respectively in human, rat, and mouse. Also inhibits the endogenous TRPV4-mediated response to 4α-PDH (IC50 = 22 nM).

Icilin is a synthetic super-agonist of the transient receptor potential M8 (TRPM8) ion channel.

Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.

ML 204 isa blocker of TRPC4 channels (IC50 values are 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively).

Optovin is a reversible photoactive TRPA1 activator.

PAC-14028 is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist.

Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).

RN-1734 is a transient receptor potential vanilloid 4 (TRPV4) antagonist, blocking calcium influx induced by the TRPV4 agonist 4α-phorbol 12,13-didecanoate with IC50 values of 2.3, 5.9, and 3.2 µM for human, mouse, and rat TRPV4, respectively.

RQ-00203078 is a potent TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively).

SB-366791 is a selective and competitive VR1 (TRPV1) antagonist that is commonly used in pain research.

SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.

SKF96365 is blocker of TRP cation channels. Inhibits capacitative Ca2+ entry.

SN 2 is a novel and potent small molecule activator of TRPML3 with EC50 of 1.13 uM.

TRPC6 inhibitor is a potent TRPC6(Transient receptor potential cation channel, subfamily C, member 6) inhibitor.

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

GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.

Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.

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.

GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.

Umbellulone is an active constituent of the leaves of Umbellularia californica. Umbellulone stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism.

Methyl syringate, a chemical marker of asphodel monofloral honey, is an efficient phenolic mediator for bacterial and fungal laccases. Methyl syringate is a TRPA1 agonist..

L-R4W2 is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC50 of 0.1 μM. L-R4W2 may act as a potent analgesic.

L-R4W2 TFA is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC50 of 0.1 μM. L-R4W2 TFA may act as a potent analgesic.

AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 μM.

IA-Alkyne (Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide) is a TRP channel (TRPC) agonist and has the potential for the study of respiratory infection. IA-Alkyne can be used to develop an isotopically tagged probe for quantitative cysteine-reactivity profiling.

CIM0216, a potent and selective agonist of TRPM3, has the ability to open two distinct cation-permeable pores in TRPM3. CIM0216 exhibits selectivity for TRPM3 over TRPM1, TRPM2 and TRPM4-8. CIM0216 acts as a powerful tool for use in investigating the physiological roles of TRPM3, and can be used for neurogenic inflammation research.

TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator. TRPC6-PAM-C20 selectively activates TRPC6 over other TRP channels and also activates TRPA1. TRPC6-PAM-C20 induces transient increase in intracellular Ca2+ in HEK cells expressing TRPC6 (EC50=2.37 μM).

AMG2850 is a potent, orally bioavailable and selective transient receptor potential melastatin 8 (TRPM8) antagonist.

OptoBI-1 is a photochromic TRPC3 agonist, which asts as a photopharmacological tool to control of neuronal firing.

GSK2332255B is a potent, selective TRPC3 and TRPC6 antagonist with IC50s of 5 nM and 4 nM for rat TRPC3 and rat TRPC6. GSK2332255B shows ≥100-fold selectivity for TRPC3/6 over other calcium-permeable channels.

Methyl kakuol shows agonistic activity against TRPA1 with an EC50 of 0.27 µM.

ML-SA1, as 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. ML-SA1 induces autophagy. ML-SA1 can be used for the research of broad-spectrum antiviral.

Capsiate, as a capsaicin analogue extracted from a non-pungent cultivar of CH-19 sweet red pepper, is an orally active agonist of TRPV1.

Dihydrocapsiate, as a compound of capsinoid family, is an orally active TRPV1 agonist. Dihydrocapsiate can be used for the research of metabolism disease.

9-Phenanthrol (9-Hydroxyphenanthrene, Phenanthren-9-o, 9-Phenanthrenol) is a selective TRPM4 inhibitor with an IC50 in the range of 0.02 μM, without effects on TRPM5.

Vocacapsaicin (CA-008), a prodrug of Capsaicin, is a first-in-class non-opioid TRPV1 agonist. Vocacapsaicin can provide meaningful and long-lasting pain relief.

Evifacotrep, a short transient receptor potential channel 5 (TRPC5) antagonist (WO2020061162, compound 100), can be used for the research of neurological diseases.

SB 452533 is a potent and selective TRPV1 antagonist with the pKb of 7.8.

Tivanisiran (SYL1001) is a siRNA used for the study of dry eye disease. Tivanisiran was designed to silence transient receptor potential vanilloid 1 (TRPV1).

ML-SI3 is a potent TRPML channel inhibitor with IC50s of 4.7 µM and 1.7 µM for TRPML1 and TRPML2, respectively.

4-(Phenyldiazenyl)benzoic acid is a photosensitive and photoswitchable TRPA1 agonist that can be used as pharmacological tools for study of pain signaling.

TRPA1 Antagonist 3 is a photoswitchable TRPA1 agonist that enables optical control of the TRPA1 channel.

TRPM8 antagonist 3 is a novel TRPM8 blocker with an IC50 value of 11 nM.

Oleoyl Serotonin is a TRPV1 antagonist with IC50 value of 2.57 μM for human TRPV1.

TRPA1-IN-1 is a potent, selective, and orally bioavailable TRPA1 small molecule antagonist.

TRPV4 antagonist 3 is a TRPV4 antagonist (pIC50 = 8.4).

Motugivatrep is the potent antagonist of transient receptor potential type 1 (TRPV1). Motugivatrep has a wide range of usefulness in treating drugs, urine tabletops, and respiratory diseases (extracted from patent WO2007010383A1).

The compound inhibits TRPC proteins, and more specifically inhibits the TRPC6 protein.

TRPC5-IN-1 (Compound 6j) is a selective TRPC5 inhibitor with 50.5 % Inhibition for TRPC5 at 3 μM. TRPC5-IN-1 can be used for the research of chronic kidney disease (CKD).

N-Oleoyldopamine (OLDA) is a product of condensation of oleic acid and dopamine (DA) and an endogenous TRPV1 selective agonist. N-Oleoyldopamine (OLDA) can crosses the blood-brain barrier. N-oleoyl-dopamine protects the heart against ischemia-reperfusion injury via activation of TRPV1.

TRPC5 modulator-1 (Compound 9) is a TRPC5 modulator with an IC50 of <1 nM for the research of neuropsychiatry disorders.

TRPC5-IN-2 is a potent TRPC5 inhibitor (WO2019055966A2, Compound IO).

(1R,2R)-ML-SI3 is a potent inhibitor of both TRPML1 and TRPML2 (IC50 values of 1.6 and 2.3 μM) and a weak inhibitor (IC50 12.5 μM) of TRPML3.

TRPC5-IN-3 is a potent TRPC5 inhibitor with IC50 of 10.75 nM (WO2022001767A1, L001).

GSK 2833503A (GSK2833503A, GSK503A) is a potent, and selective inhibitor of TRPC3/6 channels with IC50 of 4 nM/5 nM, respectively.

AM237 is a selective TRPC5 channel activator that potently activated homomeric TRPC5:C5 channels (EC50=15–20 nM in Ca2+i assays).AM237 did not activate TRPC4:C4, TRPC4-C1, TRPC5-C1, TRPC1:C5, and TRPC1:C4 channels, or native TRPC1:C4 channels in A498 cells, but potently inhibited EA‐dependent activation of these channels with IC50 values ranging from 0.9 to 7 nM.AM237 (300 nM) did not activate or inhibit TRPC3, TRPC6, TRPV4, or TRPM2 channels.AM237 potentiated TRPC5:C5 channels activation by sphingosine‐1‐phosphate but suppressed activation evoked by (−)‐englerin A (EA).AM237 concentration‐dependently suppressed further activation of Ca2+ influx mediated by EA with IC50 of 13 nM, potentiated TRPC5:C5 activation by S1P.Pico145 is a competitive antagonist of AM237‐mediated TRPC5:C5 activation.

CDD-1102 (CDD1102) is a potent, selective second bromodomain (BD2) of BRDT and BRD4 inhibitor with IC50 of 7 and 25 nM, >1,000-fold and 300-fold selectivity over BRDT-BD1 and BRD4-BD1.

GDC-0334 (GDC0334) is a highly potent, selective, orally bioavailable TRPA1 antagonist with IC50 of 1.7 nM in cell-based assays.GDC-0334 demonstrated potent TRPA1 inhibition in several species, including human (IC50=1.7 nM), cynomolgus (IC50=3.6 nM), mouse (IC50=2.7 nM), guinea pig (IC50=11.1 nM), and dog (IC50=102 nM).GDC-0334 displays good selectivity against human TRPV1, TRPM8, and TRPC6 (all IC50s>10 uM).GDC-0334 also inhibits calcium flux in human primary cells, HASMCs and HLFs, treated with the TRPA1 agonist AITC.GDC-0334 suppresses AITC-induced edema in vivo in rat (1-10 mg/kg), reduces OVA-induced asthma model in rats and guinea pigs and guinea pig model of cough.GDC-0334 is a potent inhibitor of AITC-induced dermal blood flow (DBF) in vivo in rats and guinea pigs, reduces AITC-induced perfusion and nocifensive behavior in rats and itch and pain scores in humans.

GSK205 derivative 16-8 is a specific small molecule dual-inhibitor of TRPV4 and TRPA1 with IC50 of 0.45 and 0.41 uM, respectively; displays no inhibitory potency toward TRPV1, TRPV2 and TRPV3; effectively attenuates formalin-evoked trigeminal irritant pain in model of acute pancreatitis.

GSK3395879 (GSK-3395879) is a novel potent, selective, orally bioavailable antagonist of TRPV4 with IC50 of 1 nM (hTRPV4); exhibits little or no activity against a broad panel of TRP channels (IC50 > 10µM for TRPA1, TRPV1, TRPM2, TRPM4, TRPM8, TRPC3, TRPC4, TRPC5, TRPC6); demonstrates the ability to inhibit TRPV4-mediated pulmonary edema in an in vivo rat model.

GSK3527497 (GSK-3527497) is a potent, selective TRPV4 inhibitor with IC50 of 12 nM (hTRPV4).GSK3527497 is a pre-clinical candidate for treatment of diseases resulting from TRPV4 activation.

JNJ-28583113 (JNJ28583113) a potent, selective, brain penetrant TRPM2 antagonist with IC50 of 126 nM (hTRPM2).JNJ-28583113 shows similar potency against species chimpanzee and rat TRPM2 with IC50 of 100 and 25 nM, respectively.JNJ-28583113 shows no significant (IC50>10 uM) reactivity towards PARP or PARG and a panel for multiple known kinases GPCRs and ion channels, nine other TRP channels with exception of TRPM5 (IC50<1 uM).Blocking TRPM2 via JNJ-28583113 caused phosphorylation of GSK3α and β subunits in cell assays.JNJ-28583113 also protected cells from oxidative stress induced cell death as well as morphological changes induced by non-cytotoxic concentrations of H2O2。JNJ-28583113 blunted cytokine release in response to pro-inflammatory stimuli in microglia.JNJ-28583113 was brain penetrant but not suitable for systemic dosing as it was rapidly metabolized in vivo, but the in-vitro pharmacology of JNJ-28583113 is the best in class.

JW-65 (JW65) is a selective, potent,CNS-permeable TRPC3 inhibitor improved stability compared to Pyr3.JW-65 shows similar potency and selectivity on TRPC3 channels, but is metabolically much more stable than its precursor, demonstrated by its much longer half-life (>4 h) in mouse, rat, and human liver microsomes when compared to Pyr3.JW-65-treated mice showed substantially decreased susceptibility to PTZ-induced seizures in a dose-dependent manner.

KPR-5714 (KPR5714) is a novel potent, selective TRPM8 antagonist with IC50 of 25.3 and 22.4 nM against hTRPM8 and rTRPM8, respectively.KPR-5714 dispalys 400-fold against human TRPA1, TRPV1, and TRPV4, and does not show inhibitory effects for ASIC1a, ASIC3, Nav1.3, Nav1.5, Nav1.6, Nav1.7, and Nav1.8 (IC50 values >10 uM).KPR-5714 (i.p.) inhibited the hyperactivity of mechanosensitive C-fibers of bladder afferents and dose-dependently increased the intercontraction interval shortened by intravesical instillation of acetic acid in anesthetized rats.KPR-5714 (orally administered) dose-dependently increased the mean voided volume and decreased voiding frequency without affecting total voided volume in vivo.

ML204 is a potent, selective antagonist of TRPC4 and TRPC5 channels, inhibits TRPC4β-mediated intracellular Ca(2+) rise with IC50 of 0.96 uM, exhibits 19-fold selectivity against TRPC6 channel; blocks TRPC4β currents activated through either μ-opioid receptor stimulation (50 nm DAMGO, IC50=3.55 uM) or intracellular dialysis of GTPγS (IC50=2.85 uM); shows no appreciable block by 10-20 uM for TRPV1, TRPV3, TRPA1, and TRPM8, as well as KCNQ2 and Nav Channels; also inhibits TRPC5 channel currents activated through co-stimulation of Gi/o and Gq/11 signaling by μ-opioid and M3-like muscarinic receptors.

ML2-SA1 is a potent, selective and efficacious activator (agonist) of TRPML2 with EC50 of 1.24 uM and 2.38 uM for human and mouse TRPML2, respectively.ML2-SA1 displays high selectivity for TRPML2 and no significant activity at the related TRPML1 and TRPML3 channels.ML2-SA1 directly stimulates release of the chemokine CCL2 from macrophages, also stimulates macrophage migration, thus mimicking CCL2 function.

RGM8-51 is a β-lactam derivative, potent, selective TRPM8 antagonist with IC50 of 1.06 and 1.74 uM for rat and human TRPM8, respectively.RGM8-51 does not have any ability to activate TRPM8 channels, but produces a concentration-dependent inhibition of menthol activation.RGM8-51 is selective for cold-activated TRPM8 channels, displays no agonist or antagonist profile in cool-activated TRPA1 channels and has negligible activity as TRPV3 and ASIC3 channel antagonists.RGM8-51 (1 µM) inhibited menthol-activated currents in rTRPM8-expressing HEK293 cells.RGM8-51 exhibits in vivo antinociceptive activity in response to cold, in a mouse model of oxaliplatin-induced peripheral neuropathy.RGM8-51 reduces cold, mechanical and heat hypersensitivity in a rat model of neuropathic pain arising after chronic constriction of the sciatic nerve.RGM8-51 exhibits mechanical hypersensitivity-relieving activity, in a mouse model of NTG-induced hyperesthesia.

SH045 (SH-045, Larixyl-6-N-methylcarbamate) is a potent, selective TRPC6 antagonist (blocker) with IC50 of 63 nM.SH045 displays 13-fold subtype selectivity over TRPC3 in stably expressing HEK293 cells.Treatment of isolated perfused lung preparations with SH045 led to a decrease in lung ischemia-reperfusion edema (LIRE), a life-threatening condition associated with TRPC6 that may occur after organ transplantation.

tatM2NX is a novel potent, selective, cell permeable, peptide TRPM2 channel antagonist with IC50 of 396 nM, IC90 of 2 uM (TRPM2 channel currents), prevents ligand binding and TRPM2 activation.tatM2NX interacts with the ADPR binding site on the NUT9-H domain of TRPM2 channel. tatM2NX inhibits TRPM2-mediated dephosphorylation of GSK3β (activation), tatM2NX demonstrated selective neuroprotective effects in a mouse model of focal ischemia (stroke).

ZINC 17988990 is a potent, selective inhibitor of TRPV5 mediated currents, inhibits rbTRPV5/hTRPV5 with IC50 of 106/177 nM, showing marked selectivity for TRPV5 over TRPV6.ZINC 17988990 shows no activity on other TRP channels (TRPV1, TRPV3, TRPV4 and TRPM8) at 1-3 uM, and moderate inhibition on TRPV3 and TRPM8 at >10 uM.ZINC17988990 (10 uM) fully inhibited Ca2+ signals elicited by application of external Ca2+ in HEK293 cells transfected with TRPV5, but had no effect in cells expressing TRPV6.

(E)-4-Oxo-2-nonenal (4-ONE) is one of the major hemolytic decomposition products of lipid hydroperoxides. (E)-4-Oxo-2-nonenal is a major product of the FeII-mediated breakdown of lipid hydroperoxides. (E)-4-Oxo-2-nonenal is a potent transient receptor potential ankyrin 1 (TRPA1) agonist.

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.

FEMA 4809 is a TRPM8 receptor agonist (EC50=0.2 nM) for use as a cooling agent. TRPM8 is the ion channel responsible for the cool perception.

AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 63.2 nM.

AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM.

Pinokalant is a broad-spectrum and non-selectivecation channel inhibitor. Pinokalant significantly reduces cortical infarct volume. Pinokalant o improves the metabolic and electrophysiologic status of the ischemic penumbra. Pinokalant reduces lesion size on magnetic resonance images in the acute phase following middle cerebral artery occlusion in rats. Pinokalant has the potential for the research of stroke. Pinokalant also shows anti-SARS-CoV-2 activity.

BAY-390 is a selective, across species active and brain penetrating TRPA1 inhibitor. BAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC50s of 16, 82, 63 and 35 nM, respectively.

Farnesyl pyrophosphate, a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. Farnesyl pyrophosphate is a TRPM2 (TRP Channel) agonist, activates TRPM2 opening for ion influx. Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis.

Protokylol (Caytine; JB-251) is a beta-adrenergic receptor agonist and TRPV1 agonist. Protokylol is used as a bronchodilator.

AAL-149 is a non-phosphorylatable FTY720 analogue and novel TRPM7 inhibitor, inhibits IM7 in a dose-dependent manner with IC50 of 1.081 uM, shows potent anti-inflammatory effects in vivo.

AMG2504 (AMG 2504) is a selective small molecule TRPA1 inhibitor, inhibits AITC-induced increase in intracellular calcium mediated by TRPA1 in CHO cells with IC50 of 35 nM.

AZ465 (AZ-465) is a potent selective TRPA1 inhibitor, potently inhibitor Zn2+ (100 μM)- and O-chlorobenzylidene malononitrile (CS) (10 nM)-induced TRPA1 activation with IC50 of 85 nM and 20 nM, respectively.

GDC-6599 is a potent, selective transient receptor potential ankyrin 1 (TRPA1) antagonist with IC50 of 5.3 nM (hTRPA1), exhibits TRPA1 cell potency (IC50=20 nM) in the Ca2+ influx assay in CHO cells.

GNE551 is a potent, selective, non-covalent agonist of TRPA1 ion channel with EC50 of 254 nM in Ca2+ influx assays.

JNc-463 is a small-molecule that could increase the TRPV4-eNOS interaction, enhances vasodilation and exert antihypertensive effects in mice.

KS0365 (KS 0365) is a potent and selective activator of transient receptor potential vanilloid 3 (TRPV3) channel with EC50 of 5.08 uM.

Libvatrep (SAF312) is a potent, selective non-competitive inhibitor/antagonist of the transient receptor potential cation channel subfamily V member 1 (TRPV1), shows potential for treatment of ocular surface pain.

M085 (TRPC3/6/7 activator 4o) is a potent and selective TRPC3/6/7 activator with EC50 of 4.66 uM, also activates hTRPC6 with EC50 of 3.8 uM.

SAR7334 (SAR-7334 ) is a highly potent and selective inhibitor of TRPC6 channel, reduces TRPC6-mediated Ca2+ influx with IC50 of 9.5 nM.

Triphenylphosphine oxide (TPPO) is a selective and potent inhibitor of TRPM5 with IC50 of 12 and 30 uM for human and murine TRPM5 heterologously expressed in HEK293 cells.

Trpvicin is a potent and subtype-selective inhibitor of TRPV3 with IC50 of 0.41 and 0.22 uM for hTRPV3-WT and hTRPV3-G573S mutant, respectively.

VPC01091.4 is a non-phosphorylatable FTY720 analogue and novel TRPM7 inhibitor, inhibits IM7 in a dose-dependent manner with IC50 of 0.665 uM.