trpv 2

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

Methyl salicylate (Gaultheria oil) is an organic ester naturally produced by many species of plants, particularly wintergreens. For acute joint and muscular pain, methyl salicylate is used as a rubefacient and analgesic in deep heating liniments.

Camphor (2-Camphanone) is a bicyclic monoterpene ketone found widely in plants, especially CINNAMOMUM CAMPHORA. It is used topically as a skin antipruritic and as an anti-infective agent.

1. trans-Cinnamaldehyde (Phenylacrolein) exhibits excellent anti-inflammatory activities and antidepressant-like effects in stressed mid-aged rats as a COX-2 inhibitor. 2. Cinnamic aldehyde induces apoptosis of CML cells in vitro, down-regulation of the expression and function of BCR-ABL may be one of its most important anti-leukemia mechanisms. 3. Cinnamic aldehyde and cinnamic acid are cardioprotective in a rat model of ischemic myocardial injury, the mechanism is related to anti-oxidative and anti-inflammatory properties.

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.

TRPM8 antagonist WS-3 (Cyclohexanecarboxamide) is an agonist of TRPM8( EC50 : 3.7 μM).

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.

Cardamonin (Cardamomin) is a chalcone isolated from Alpiniae katsumadai. It has anticancer, anti-inflammatory, antimicrobial, antioxidant and anti-diabetic activities. It can inhibit mTOR, NF-κB, Akt, STAT3, Wnt β-catenin and COX-2, inhibit the growth of breast cancer, and can be used to study acute kidney injury and chronic renal fibrosis.

SN 2 is a novel and potent TRPML3 ion channel activator(EC50 of 1.8±0.13 μM).

TRPA1-IN-2 is a potent and orally active TRPA1 inhibitor with an IC50 value of 0.04 µM.TRPA1-IN-2 has anti-inflammatory activity.

M084 (N-Butyl-1H-benzimidazol-2-amine) is a blocker of TRPC4 5 channel, with antidepressant and anxiolytic effects.

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

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.

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.

Ononetin (2',4'-Dihydroxy-2-(4-methoxyphenyl)acetophenone) is a TRPM3 channel blocker(IC50: 0.3 μM).

SB 452533 is an antagonist of the vanilloid receptor 1(pKb: 7.8).

SET 2 is an antagonist of transient receptor potential vanilloid type 2(TRPV2) with an IC50 of 0.46 μM. SET 2 shows selectivity over TRPV1, TRPV3 and TRPV4.

TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator that induces a transient increase in intracellular Ca2+ with an EC50 of 2.37 μM in HEK cells expressing TRPC6 and enhances OAG-induced platelet aggregation.

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.

TRPM4-IN-2 (NBA), also known as NBA, is a highly effective inhibitor of transient receptor potential melastatin 4 (TRPM4). Its inhibitory potency is represented by an IC 50 value of 0.16 μM. This compound serves as a valuable tool in the investigation of prostate cancer and colorectal cancer [1] [2].

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.

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

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

NGD-8243 (N-[4-(trifluoromethyl)phenyl]-7-[3-(trifluoromethyl)pyridin-2-yl]quinazolin-4-amine) is a TRPV1 inhibitor and can be used in studies for prevention and treatment of cardiac hypertrophy.