TRP Channel Activator

TRP Channel Activators (82):

Cat. No.	Product Name	Effect	Purity

HY-W009724

2-Aminoethyl diphenylborinate	Activator	98.86%
2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of Inositol triphosphate receptor (IP3R). 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca²⁺ (SOC) channel and activates some TRP channels (V1, V2 and V3). Additionally, 2-Aminoethyl diphenylborinate has inhibitory effects on vasospasm. At high concentrations, it exhibits specific anti-inflammatory and antioxidant effects in neural tissue.

HY-100965

Diphenyleneiodonium chloride	Activator	99.85%
Diphenyleneiodonium chloride is a NADPH oxidase (NOX) inhibitor and also functions as a TRPA1 activator with an EC₅₀ of 1 to 3 μM. Diphenyleneiodonium chloride selectively inhibits intracellular reactive oxygen species.

HY-10863

Anandamide	Activator	≥99.0%
Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis.

HY-109061

Lazertinib	Activator	99.87%
Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.

HY-75161

(-)-Menthol	Activator	99.79%
(-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca²⁺-permeable nonselective cation channel, to increase [Ca²⁺]_i. Antitumor activity.

HY-100973A

Adenosine 5′-diphosphoribose sodium	Activator	99.47%
Adenosine 5′-diphosphoribose sodium (ADP ribose sodium) is a nicotinamide adenine nucleotide (NAD⁺) metabolite. Adenosine 5′-diphosphoribose sodium is the most potent and primary intracellular Ca²⁺-permeable cation TRPM2 channel activator. Adenosine 5′-diphosphoribose sodium also can enhance autophagy.

HY-B0151

Pregnenolone	Activator	99.85%
Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

HY-100973

Adenosine 5′-diphosphoribose	Activator	98.21%
Adenosine 5′-diphosphoribose (ADP ribose) is a nicotinamide adenine nucleotide (NAD⁺) metabolite. Adenosine 5′-diphosphoribose is the most potent and primary intracellular Ca²⁺-permeable cation TRPM2 channel activator. Adenosine 5′-diphosphoribose also can enhance autophagy.

HY-14307

Necrocide 1	Activator	99.55%
Necrocide 1, a necrosis by sodium overload (NECSO) inducer, is a selective transient receptor potential melastatin 4 (TRPM4) agonist with an EC₅₀ of 306.3 nM for human TRPM4. Necrocide 1 triggers TRPM4-dependent necrotic cell death through the induction of sodium influx. Necrocide 1 induces hallmarks of immunogenic cell death incurring calreticulin (CALR) exposure, ATP secretion and high mobility group box 1 (HMGB1) release. Necrocide 1 can be used for the study of breast and prostate cancer.

HY-116330A

Hyperforin dicyclohexylammonium salt	Activator	99.48%
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca²⁺ levels by activating Ca²⁺-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model.

HY-110189

Pregnenolone monosulfate sodium	Activator	99.96%
Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

HY-107436

LE135	Activator	99.0%
LE135 is a potent RAR antagonist that binds selectively to RARα (K_i of 1.4 μM) and RARβ (K_i of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC₅₀s of 2.5 μM and 20 μM, respectively.

HY-133168

Englerin A	Activator	99.50%
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC₅₀s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca²⁺ influx and Ca²⁺ cell overload.

HY-P5381

gp91 ds-tat	Activator	99.00%
gp91 ds-tat, a biological active peptide, is a NADPH oxidase 2 (Nox2) inhibitor. gp91 ds-tat blocks NADPH oxidase-dependent superoxide production. gp91 ds-tat ameliorates high glucose-induced increase in total ROS, LPOs and iron levels. gp91 ds-tat inhibits homocysteine (Hcy)-induced activation of NLRP3 inflammasomes and restores Hcy-inhibited lysosomal TRPML1 channel activity. gp91 ds-tat improves cerebrovascular and cognitive function in APP/PS1 mice. gp91 ds-tat can be used for the study of Alzheimer’s disease (AD), glomerular inflammation and cardiovascular disease.

HY-131648

1-Oleoyl-2-acetyl-sn-glycerol	Activator	99.90%
1-Oleoyl-2-acetyl-sn-glycerol is a cell-permeable analog of diacylglycerol (DAG) and can activate Protein kinase C (PKC). 1-Oleoyl-2-acetyl-sn-glycerol can activate the TRPC channels-mediated specific Ca²⁺ influx. 1-Oleoyl-2-acetyl-sn-glycerol can stimulate superoxide-generation from human neutrophils. 1-Oleoyl-2-acetyl-sn-glycerol stimulates the formation of phosphatidylinositol 4-phosphate in intact human platelets. 1-Oleoyl-2-acetyl-sn-glycerol can stimulate ascites tumor cell proliferation.

HY-135013

Umbellulone	Activator	99.83%
Umbellulone is an active constituent of the leaves of Umbellularia californica. Umbellulone stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism.

HY-101302

Naltriben mesylate	Activator	99.65%
Naltriben mesylate is a potent δ2-opioid receptor antagonist and a TRPM7 activator. Naltriben mesylate shows K_i values of 0.013 nM, 19 nM and 152 nM for δ, μ and κ receptors, respectively. Naltriben mesylate enhances glioblastoma cell migration and invasion. Naltriben mesylate can be used in research into neurological diseases and cancer.

HY-N0447

8-Gingerol	Activator	99.82%
8-Gingerol can be found in the rhizome of ginger (Z. officinale) and has oral bioactivity. It activates TRPV1, with an EC₅₀ value of 5.0 µM. 8-Gingerol inhibits COX-2 and also suppresses the growth of H. pylori in vitro. Additionally, 8-Gingerol exhibits anticancer, antioxidant, and anti-inflammatory properties by inhibiting the epidermal growth factor receptor (EGFR) and modulating its downstream STAT3/ERK pathway to suppress the proliferation, migration, and invasion of colorectal cancer cells. 8-Gingerol also exerts immunosuppressive effects by inhibiting oxidative stress, inducing cell cycle arrest, promoting apoptosis, and regulating autophagy. Furthermore, 8-Gingerol has cardioprotective effects. 8-Gingerol is promising for research in the fields of cancer, infection, immunosuppression, and cardiovascular diseases.

HY-B1739

Pregnenolone monosulfate	Activator	99.96%
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication. Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

HY-16696

SN 2	Activator	99.93%
SN 2 is a potent activator of TRPML3 ion channel with an EC₅₀ of 1.8 μM. SN 2 also acts as a potent inhibitor of Dengue virus 2 (DENV2) and Zika virus (ZIKV).

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