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

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).

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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

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

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

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

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

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.

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.

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).

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

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.

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).

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

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

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

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.

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

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.