TRPM8

TRPM8 Related Products (22):

By Type:	Pan (4) Selective (8)
By Effects:	Inhibitors (4) Agonists (5) Antagonists (8) Activators (2) Modulator (1)

Cat. No.	Product Name	Effect	Purity

HY-11062

Icilin	Agonist	99.26%
Icilin (AG-3-5) is a super-agonist of the transient receptor potential M8 (TRPM8) ion channel. Icilin activates TRPM8 in EGTA in a dose-dependent manner (EC₅₀=1.4 μM). Icilin is a "super-cooling agent" . Icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response.

HY-108449

Acoltremon	Agonist	99.13%
Acoltremon (WS-12; AR-15512) is a potent and selective TRPM8 agonist, the menthol derivative, as a cooling agent. Acoltremon shows analgesic effect, and can be used in chronic neuropathic pain research.

HY-18662

RQ-00203078	Antagonist	99.84%
RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC₅₀s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels.

HY-115506

PF-05105679	Antagonist	99.88%
PF-05105679, a chemical probe, is an orally active and selective TRPM8 antagonist with an IC₅₀ of 103 nM. PF-05105679 has the potential for cold-related pain.

HY-19976

RN-1747	Agonist	99.27%
RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 (TRPV4) agonist, with EC₅₀ values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC₅₀ of 4 μM.

HY-179432

Cannabitwinol	Modulator
Cannabitwinol is a selective thermosensitive TRP modulator and NF-κB inhibitor. Cannabitwinol inhibits TNFα-induced NF-κB-driven transcription and TNFα-induced IL-8 release, and exhibits anti-inflammatory and antioxidant activities. Cannabitwinol shows selectivity for cold-activated TRP channels, activating TRPA1 (EC₅₀ = 3.0 μM) and antagonizing TRPM8 (IC₅₀ = 3.9 μM), but has no significant affinity for heat-activated TRP channels such as TRPV1 and TRPV2. Cannabitwinol can be used in research related to inflammatory skin diseases, cold allodynia, and hyperalgesia.

HY-110181

M8-B	Antagonist	99.74%
M8-B is a potent transient receptor potential melastatin-8 (TRPM8) antagonist. M8-B blocks cold-induced and TRPM8-agonist-induced activation TRPM8 channels. M8-B decreases deep body temperature (Tb).

HY-144372

TRPV1 antagonist 3	Antagonist	99.30%
TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC₅₀ of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant.

HY-N7144A

Citronellyl acetate		98.0%
Citronellyl acetate, a monoterpene product of the secondary metabolism of plants, is an orally active antinociceptive agent. Citronellyl acetate modulates TRPV1, TRPM8, ASIC, glutamate receptors, PKC, and PKA-mediated nociception. Citronellyl acetate can be used for the research of acute pain.

HY-N7117

1,4-Cineole	Activator
1,4-Cineole is an oxygenated monoterpene found in eucalyptus oil. 1,4-Cineole is a hTRPM8 and hTRPA1 agonist. 1,4-Cineole can increase intracellular Ca²⁺ concentration. 1,4-Cineole exhibits anti-anxiety and anti-depression effects. 1,4-Cineole can be used for the research of neurological disease, such as depression .

HY-108461

TRPM8-IN-1	Inhibitor	99.44%
TRPM8-IN-1 (example 14) is an inhibitor of transient receptor potential melastatin-8 (TRPM8) channels, IC₅₀<5 μM.

HY-N7117R

1,4-Cineole (Standard)	Activator
1,4-Cineole (Standard) is the analytical standard of 1,4-Cineole (HY-N7117). 1,4-Cineole is an oxygenated monoterpene found in eucalyptus oil. 1,4-Cineole is a hTRPM8 and hTRPA1 agonist. 1,4-Cineole can increase intracellular Ca²⁺ concentration. 1,4-Cineole exhibits anti-anxiety and anti-depression effects. 1,4-Cineole can be used for the research of neurological disease, such as depression .

HY-172774

TRPV1 antagonist 10	Antagonist	98.54%
TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist (IC₅₀ = 33.06 nM), moderate to weak URAT1 (IC₅₀ = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain.

HY-141712

ZA18	Inhibitor
ZA18 is a selective TRPM2 channel inhibitor, with an IC₅₀ value of 6.2 μM. ZA18 can effectively suppress intracellular Ca²⁺ overload triggered by TRPM2 channel activation. ZA18 significantly reduce the mortality of SH-SY5Y cells induced by H2O2. ZA18 can be used for the study of ischemia-reperfusion injury, inflammation, or other neurodegenerative diseases.

HY-W014394

Vanillyl butyl ether	Agonist	99.75%
Vanillyl butyl ether is a major contributor to the characteristic flavor and fragrance of vanilla. Vanillyl butyl ether is one of the eco-friendly and nontoxic substances. Vanillyl butyl ether exhibits mutually inhibitory effects on mammalian TRPV1 and TRPM8 channels. Vanillyl butyl ether shows repellency activity against Tribolium castaneum, T. confusum and L. bostrychophila. Vanillyl butyl ether acts as a mild warming agent, providing a warming sensation and enhancing blood circulation.

HY-168471

AAL-149	Inhibitor
AAL-149 is a FTY720 (HY-12005) analog and TRPM7 inhibitor (IC₅₀ = 1.081 μM) with multimodal anti-inflammatory effects and without targeting S1P receptors. AAL-149 can be utilized in anti-inflammatory research.

HY-177763

TRPM8 receptor agonist-1	Agonist
TRPM8 receptor agonist-1 (Example 81) is a TRPM8 receptor agonist. TRPM8 receptor agonist-1 can trigger the inward flow of calcium, sodium and other ions within the cell, causing the cell membrane to depolarize and triggering an action potential. TRPM8 receptor agonist-1 can activate signals related to the swallowing reflex and can be used for the research of oropharyngeal dysphagia.

HY-174825

TRPM8 antagonist 4	Antagonist
TRPM8 antagonist 4 is a CB2R partial agonist (EC₅₀=54.2 nM, K_i=3.2 μM) and TRPM8 antagonists (IC₅₀=42.3 nM) with high functional selectivity and good physicochemical properties. TRPM8 antagonist 4 has significant anti-inflammatory and analgesic effects and good safety, reduces the mRNA expression of TNF-α, IL-6, and IL-1β.

HY-170302

CMP233	Inhibitor
CMP233 is a potent antagonist of TRPM4, with the IC₅₀ of 0.15 μM. CMP233 plays an important role in neurodegenerative disorders research.

HY-174846

TRPM8 antagonist 4 prodrug	Antagonist
TRPM8 antagonist 4 prodrug (Compound 8b) is an orally active CB₂R agonist (EC₅₀: 51.2 nM) and a weak TRPM8 antagonist. TRPM8 antagonist 4 prodrug is a prodrug of TRPM8 antagonist 4 (HY-174825). TRPM8 antagonist 4 prodrug exhibits anti-inflammatory and analgesic activities and can be used in the research of inflammation-related pain disorders.

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