trpv

TRPV antagonist 1 is an antagonist of transient receptor potential vanilloid (TRPV; IC50 < 250 nM).

TRPV4 agonist-1 free base (OUN67600) is an agonist of transient receptor potential vanilloid 4 (TRPV4;EC50 of 60 nM, in the hTRPV4 Ca2+ assay).

TRPV4 agonist-1 is an agonist of TRPV4 (EC50: 60 nM in the hTRPV4 Ca2+ assay).

TRPV3 antagonist 74a (TRPV3 74a) is a specific TRPV3 antagonist for the study of neurological disorders.

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

TRPV1-IN-2 (( R ) -32) is an inhibitor of TRPV1. It provides protective effects in the ED epilepsy model.

TRPV1 CB2 agonist 1 (compound 41) is a dual agonist targeting hTRPV1 and CB2 receptors, with an EC50 value of 26.8 μM for hTRPV1. It is applicable in research related to the nervous system.

TRPV1-IN-3 (compound 14) is a TRPV1 inhibitor utilized in idiopathic pulmonary fibrosis research. It demonstrates antifibrotic activity in vitro (IC50 = 0.51 μM) by inhibiting the TGF-β Smads and MAPK pathways, thereby affecting the expression of fibrosis markers collagen I and α-SMA. In vivo, TRPV1-IN-3 significantly reduces collagen deposition in lung tissue, improves alveolar structure, and increases survival rates in mice with Bleomycin-induced pulmonary fibrosis.

TRPV1 antagonist 3 (Compound 7q) is a highly potent TRPV1 receptor antagonist with an IC50 of 2.66 nM against capsaicin. It exhibits selectivity in its mode of action, is orally bioavailable (60%), and can penetrate the central nervous system [1].

TRPV1 Activator-1 (Compound 8), a capsaicin analog featuring a modified neck structure, specifically interacts with the T551 residue [1].

TRPV1 activator-2 (Compound 9), a capsaicin head analog, engages in targeted interactions with channel residues at the lipid-water interface [1].

TRPV4 antagonist 4, a potent inhibitor of TRPV4 with an IC50 of 22.65 nM, effectively blocks TRPV4 current and demonstrates protective properties against acute lung injury [1].

TRPV2-selective blocker 1 (compound IV2-1) is a selective inhibitor of the TRPV2 channel, with an IC50 value of 6.3 μM, specifically targeting the TRPV2 channel without affecting TRPV1, TRPV3, or TRPV4 channels, and effectively suppresses TRPV2-mediated calcium influx in macrophages, inhibiting their phagocytic activity [1].

TRPV1-Tat, a peptide antagonist targeting transient receptor potential vanilloid 1 (TRPV1), is composed of amino acids 736-745 derived from TRPV1's A-kinase anchor protein (AKAP)-binding domain, combined with the HIV Tat-derived cell-penetrating peptide sequence. At a concentration of 200 µM, TRPV1-Tat effectively inhibits heat or phorbol 12-myristate 13-acetate (PMA014)-induced currents in primary mouse dorsal root ganglia via whole-cell patch-clamp assays. Additionally, when administered at dosages of 10 or 30 µM, it elevates the mechanical pain threshold in the hind paws of rats.

TRPV4-IN-5 (Compound 1f) is an effective TRPV4 inhibitor with an IC50 value of 0.46 μM. It significantly alleviates symptoms of acute lung injury in mice induced by lipopolysaccharide.

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.

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.

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.

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

OMDM-6 is a dual agonist of TRPV1(EC50 = 75 nM) and CB1 (Ki = 3.2 μM). OMDM-6 inhibits anandamide cellular uptake with a Ki of 7.0 μM.

ABT-239 is a novel, highly efficacious non-imidazole class histamine H3 receptor (H3R) antagonist and also acts as a transient receptor potential vanilloid type 1 (TRPV1) antagonist.

JT010 is an effective agonist of TRPA1 (EC50 = 0.65 nM).

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

Oleoyl Serotonin is an antagonist of hTRPV1 with an IC50 of 2.57 μM.