trpm8

TRPM8 antagonist 3 is a blocker of TRPM8 (IC50 = 11 nM).

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.

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

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

2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R and TRP channels. 2-Aminoethyl diphenylborinate also inhibits store-operated Ca2+ (SOC) channels and activates certain TRP channels (V1, V2, and V3). 2-Aminoethyl diphenylborinate also inhibits vasospasm. 2-Aminoethyl diphenylborinate can be used in research on calcium biology, cell signaling, oncology, and neurobiology.

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

1,4-Cineole (Isocineole) is a natural, oxygenated monoterpene. 1,4-Cineole can activate both human TRPM8 and human TRPA1.

RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 agonist (EC50: hTRPV4 of 0.77 μM, mTRPV4 of 4.0 μM, and rTRPV4 of 4.1 μM) and also acts as an antagonist for TRPM8 (IC50: 4 μM).

AMG2850 is a potent, orally bioavailable, and selective antagonist of transient receptor potential melastatin 8 [TRPM8].

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

TC-I 2014 shows antiallodynic properties in pain models. TC-I 2014 is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 antagonist (IC50: 0.8 nM, 3.0 nM, and 4.4 nM for canine, human and rat channels respectively).

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

AMTB hydrochloride (AMTB HCl) is a novel TRPM8 channel blocker and is effective for pain and urinary diseases. AMTB can act on the bladder afferent pathway to attenuate the bladder micturition reflex and nociceptive reflex responses in the rat.

RQ-00203078 is a highly selective, potent, and orally available TRPM8 antagonist.

FEMA-4809, a highly potent TRPM8 receptor activator, TRPM8 is the ion channel responsible for the cool perception, which is triggered either by temperatures below 25 °C or by ligands such as (-)-menthol. FEMA-4809 is used as a cooling agent.

beta-Eudesmol (Beta-Selinenol) is a noncompetitive antagonist of nicotinic acetylcholine receptors (nAChRs). It is a sesquiterpene that has been found in a variety of plants, including Cannabis, and has diverse biological activities.

AMG 333 is TRPM8 antagonist with an IC50 of 13 nM,a Clinical Candidate for the Treatment of Migraine.

M8-B Hydrochloride is a selective transient receptor potential melastatin-8 (TRPM8) channel antagonist.

TC-I2000 is an TRPM8 channel blocker. Inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells with IC50 of 53 nM.

TRPM8 antagonist 4 prodrug (Compound 8b) is an orally active CB2R agonist (EC50: 51.2 nM) and a weak TRPM8 antagonist. It acts as a prodrug of TRPM8 antagonist 4, exhibiting anti-inflammatory and analgesic properties. TRPM8 antagonist 4 prodrug is applicable in studies of inflammation-related pain disorders.

TRPM8 antagonist 4 is a compound with high functional selectivity and favorable physicochemical properties, serving as a CB2R partial agonist (EC50=54.2 μM, Ki=3.2 μM) and a TRPM8 (IC50=42.3 nM) antagonist. It possesses notable anti-inflammatory and analgesic effects, demonstrating good safety by reducing the mRNA expression of TNF-α, IL-6, and IL-1β.

TRPM8 antagonist WS-3 (Standard) is the standard substance of TRPM8 antagonist WS-3, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. TRPM8 antagonist WS-3 (Cyclohexanecarboxamide) is an agonist of TRPM8( EC50 : 3.7 μM).

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].

AMG8788 is a selective, potent and orally active TRPM8 antagonist (IC50: 63.2 nM).