TRP Channel

Cat. No.

A65984

CAS No.

238074-03-8

Hyperforin dicyclohexylammonium salt

Synonyms: Hyperforin DCHA

Hyperforin dicyclohexylammonium salt is a selective activator of transient receptor potential canonical 6 (TRPC6) channels. By modulating Ca2+ flux, this compound influences a variety of biological processes and exhibits notable pharmacological activities, including anti-depression, anti-tumor, anti-dementia, and anti-diabetic effects. Additionally, Hyperforin dicyclohexylammonium salt has been shown to enhance the secretion of IL-17α from γδ T cells and demonstrates efficacy in improving psoriasis-like symptoms in the Imiquimod-induced mouse model. This compound serves as a valuable tool in research focused on calcium signaling and related therapeutic applications.

Cat. No.

A66070

CAS No.

581809-67-8

A-425619

A-425619 is a selective antagonist of the transient receptor potential type V1 (TRPV1), exhibiting oral bioactivity. It effectively inhibits capsaicin- and N-arachidonoyl-dopamine (NADA)-induced calcium influx in both dorsal root ganglia and trigeminal ganglia. A-425619 demonstrates efficacy in alleviating pathophysiological pain linked to inflammation and tissue injury in preclinical models. This compound is valuable for researching pain mechanisms associated with inflammatory conditions.

Cat. No.

A66205

CAS No.

372-97-4

Farnesyl pyrophosphate

Synonyms: Farnesyl diphosphate

Farnesyl pyrophosphate is an agonist of the TRPM2 channel, initiating calcium influx and promoting cell death. As a vital intermediate in the mevalonate pathway, it plays a crucial role in cholesterol and ubiquinone synthesis, as well as protein farnesylation and geranylgeranyl pyrophosphate synthesis. Farnesyl pyrophosphate is utilized in research focused on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, and the study of inflammation and autoimmune disorders.

Cat. No.

A66366

CAS No.

895550-58-0

Farnesyl pyrophosphate-d6

Synonyms: Farnesyl diphosphate-d6

Farnesyl pyrophosphate-d6 is a deuterium-labeled stable isotope derivative of farnesyl pyrophosphate, an important metabolic intermediate in the mevalonate pathway. It acts as an agonist for TRP channel TRPM2, facilitating calcium influx and promoting cell death. Farnesyl pyrophosphate plays a crucial role in cholesterol and ubiquinone synthesis, as well as in protein farnesylation and geranylgeranyl pyrophosphate synthesis. This reagent is utilized in research exploring cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune disorders.

Cat. No.

A67969

CAS No.

105431-72-9

Linopirdine

Synonyms: DuP 996

Linopirdine is a selective inhibitor of the M-type potassium current (IM; Kv7; KCNQ channels) with an IC50 of 2.4 μM. This compound exhibits potential as a cognition-enhancing agent by promoting acetylcholine release in rat brain tissue. Linopirdine is primarily utilized in research focused on understanding cognitive function and the modulation of neurotransmitter release. Additionally, its role as a TRPV1 agonist provides further avenues for investigation in neurobiology and pharmacology.

Cat. No.

A68071

CAS No.

1119503-63-7

JNc-440

JNc-440 is a TRPV4-KCa2.3 interaction enhancer with significant potential as an antihypertensive agent. This compound promotes the interaction between the transient receptor potential vanilloid 4 (TRPV4) and the calcium-activated potassium channel 3 (KCa2.3) in endothelial cells, resulting in enhanced vasodilation. Furthermore, JNc-440 demonstrates effective antihypertensive properties in murine models, making it a valuable tool for cardiovascular research.

Cat. No.

A68189

CAS No.

875755-39-8

NS8593

NS8593 is a selective inhibitor of small conductance Ca2+-activated K+ channels (SK channels), specifically targeting the SK1-3 subtypes. It exhibits a reversible inhibition of SK3-mediated currents with Ca2+-dependent potency (Kd values of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca2+), while leaving intermediate and large conductance K channels unaffected. Additionally, NS8593 inhibits the TRPM7 channel with an IC50 of 1.6 mM. This compound is valuable for research into central nervous system-related diseases and the physiological roles of SK and TRPM7 channels.

Cat. No.

A68469

CAS No.

3035547-78-2

ErSO-TFPy

Synonyms: TEQ103; Sera2

ErSO-TFPy is a selective activator of the TRPM4 ion channel, designed for studying its effects on calcium and sodium ion homeostasis in cells. This compound exhibits low nanomolar cytotoxicity specifically towards ERα+ breast cancer cells, leading to dysregulation of calcium balance and triggering an anticipatory unfolded protein response. The resultant cellular stress induces immune cell-independent necrotic cell death. ErSO-TFPy is a valuable tool for investigating the mechanisms underlying estrogen receptor alpha positive breast cancer.

Cat. No.

A68684

CAS No.

2019994-90-0

Trpvicin

Trpvicin is a selective inhibitor of the TRPV3 channel, demonstrating IC50 values of 0.41 μM and 0.22 μM for human TRPV3-WT and the hTRPV3-G573S mutant, respectively. Its mechanism of action involves stabilizing TRPV3 in a closed conformation primarily through VSLD-PD binding, while also engaging alternative binding sites in the G573S mutant to impede channel activity. Trpvicin exhibits minimal off-target effects on other TRP family members, making it a valuable tool for studying inflammation, immunology, and conditions associated with itch and hair loss in mouse models.

Cat. No.

A68685

CAS No.

1644134-60-0

ADM 12

ADM 12 is a selective antagonist of the transient receptor potential ankyrin 1 (TRPA1) channel. It effectively inhibits nitroglycerin-induced trigeminal hyperalgesia in animal models, leading to decreased expression of pain-related genes such as c-Fos and TRPA1, as well as neuropeptides including CGRP and substance P. This compound holds potential for research applications in the fields of migraine and neuropathic pain.

Cat. No.

A68686

CAS No.

2776193-88-3

TRPM3-IN-1

TRPM3-IN-1 is a potent inhibitor of the TRPM3 ion channel, exhibiting an IC50 value of less than 1 µM. This compound is valuable for research focused on the modulation of pain mechanisms and inflammatory responses. Its ability to selectively target TRPM3 makes it a promising tool for investigating related biological pathways and potential therapeutic applications.

Cat. No.

A68687

CAS No.

2418670-70-7

ML-SA5

ML-SA5 is a potent agonist of the TRPML1 cation channel, effectively activating the endosomal TRPML1 current in DMD myocytes with an EC50 of 285 nM. This compound demonstrates significant anticancer activity by inhibiting tumor growth, making it valuable for research applications aimed at exploring TRPML1 functions and their implications in cancer biology and muscle disorders.

Cat. No.

A68688

CAS No.

930800-38-7

IA-Alkyne

Synonyms: Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide

IA-Alkyne is a TRPC channel (TRPC) agonist that facilitates the investigation of respiratory infections through enhanced channel activity. This compound serves as a versatile chemical probe for quantitative profiling of cysteine reactivity, enabling isotopic tagging. Additionally, IA-Alkyne features an alkyne functional group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool for click chemistry applications in various biological research studies.

Cat. No.

A68689

CAS No.

1031496-06-6

CIM0216

CIM0216 is a selective agonist of the TRPM3 ion channel, demonstrating potent stimulation specifically for this target over other TRPM family members such as TRPM1, TRPM2, and TRPM4-8. It activates TRPM3-dependent pathways to induce pain and facilitate the release of neuropeptides from sensory nerve terminals in vitro. This compound serves as an important research tool for investigating the physiological roles of TRPM3 and has applications in the study of neurogenic inflammation.

Cat. No.

A68690

CAS No.

2361241-23-6

BI-749327

BI-749327 is a potent and highly selective antagonist of the TRPC6 channel, exhibiting IC50 values of 13 nM for mouse TRPC6, 19 nM for human TRPC6, and 15 nM for guinea pig TRPC6. This compound demonstrates an 85-fold selectivity for mouse TRPC6 over TRPC3 and a 42-fold selectivity over TRPC7. Due to its oral bioavailability and inhibition of TRPC6, BI-749327 is suitable for research applications involving ion channel modulation and the investigation of associated physiological and pathological processes.

Cat. No.

A68691

CAS No.

2418594-00-8

(1R,2R)-ML-SI3

Synonyms: (-)-trans-ML-SI3

(1R,2R)-ML-SI3 is a selective inhibitor of the TRPML1, TRPML2, and TRPML3 ion channels, with IC50 values of 1.6 μM, 2.3 μM, and 12.5 μM, respectively. This compound is valuable for investigating the physiological roles of TRPML channels in cellular signaling and ion homeostasis. It is well-suited for research applications related to lysosomal function, calcium signaling, and potential therapeutic strategies targeting lysosomal storage disorders.

Cat. No.

A68692

CAS No.

2313525-20-9

SET2

SET2 is a selective antagonist of the TRPV2 channel, with an IC50 value of 0.46 μM. This compound effectively inhibits TRPV2-mediated signaling, thereby suppressing the migration of prostate cancer cells. Additionally, SET2 diminishes lysophosphatidic acid (LPA)-induced increases in cytoplasmic calcium levels, making it useful for research focused on cancer biology and calcium signaling pathways.

Cat. No.

A68693

CAS No.

1263068-83-2

GSK205

GSK205 is a selective antagonist of the Transient Receptor Potential Vanilloid 4 (TRPV4) channel, exhibiting an IC50 of 4.19 μM for TRPV4-mediated calcium influx inhibition. This compound is instrumental in studying TRPV4's role in various physiological and pathological processes, including pain sensation, inflammation, and cellular mechanotransduction. GSK205 is a valuable tool for researchers investigating the therapeutic potential of TRPV4 modulation in various disease models.

Cat. No.

A68694

CAS No.

2765255-93-2

JNJ-28583113

JNJ-28583113 is a potent TRPM2 inhibitor that exhibits permeability across the blood-brain barrier. By inhibiting TRPM2, JNJ-28583113 effectively blocks the phosphorylation of GSK3α and β subunits, offering protective effects against oxidative stress-induced cell death. Additionally, it reduces cytokine release from microglia in response to pro-inflammatory stimuli, making it a valuable tool for research in neuroinflammation and oxidative stress pathways.

Cat. No.

A68695

CAS No.

926023-82-7

AMTB hydrochloride

AMTB hydrochloride is a selective antagonist of the TRPM8 channel, effectively inhibiting icilin-induced TRPM8 activation with a pIC50 of 6.23. This reagent is valuable in the study of overactive bladder conditions and painful bladder syndrome. Additionally, AMTB hydrochloride exhibits non-selective inhibition of voltage-gated sodium channels, providing a broader context for its use in electrophysiological research.

Cat. No.

A68696

CAS No.

924377-85-5

GSK1702934A

GSK1702934A is a selective agonist of the TRPC3 ion channel. It enhances cardiac contractility and plays a role in the modulation of arrhythmogenesis through TRPC3 activation. This compound is valuable for research applications investigating cardiac function and the physiological effects of TRPC3 modulation in various disease models.

Cat. No.

A68697

CAS No.

83883-10-7

Hydroxy-α-sanshool

Hydroxy-α-sanshool is an agonist of the transient receptor potential ankyrin 1 (TRPA1) and TRP vanilloid 1 (TRPV1) channels, exhibiting EC50 values of 69 μM and 1.1 μM, respectively. This compound plays a significant role in pain research by activating these nociceptive pathways, potentially contributing to studies on pain sensation and modulation.

Cat. No.

A68698

CAS No.

1094250-15-3

Englerin A

Englerin A is a selective activator of TRPC4 and TRPC5 channels, exhibiting EC50 values of 11.2 nM and 7.6 nM, respectively. This compound is known to induce cell death in renal carcinoma cells through the mechanism of increased calcium influx and subsequent calcium overload. Englerin A serves as a valuable tool for investigating TRPC channel function and potential therapeutic approaches in cancer research.

Cat. No.

A68699

CAS No.

155877-83-1

LE135

LE135 is a selective antagonist of retinoic acid receptors RARα and RARβ, exhibiting a Ki of 1.4 μM for RARα and a significantly higher affinity of 220 nM for RARβ. This compound demonstrates high specificity for these targets, with minimal interaction with RARγ and RXR isoforms. Additionally, LE135 acts as a potent activator of TRPV1 and TRPA1 receptors, with EC50 values of 2.5 μM and 20 μM, respectively, making it a valuable tool for studying pathways involving these ion channels in various biological contexts.

Cat. No.

A68700

CAS No.

2242724-49-6

TRPV2-selective blocker 1

TRPV2-selective blocker 1 is a selective inhibitor of the transient receptor potential vanilloid 2 (TRPV2) channel, exhibiting an IC50 of 6.3 μM. This compound selectively targets TRPV2 without affecting TRPV1, TRPV3, or TRPV4 channels. Its primary biological activities include blocking TRPV2-mediated Ca2+ influx in macrophages and inhibiting macrophage phagocytosis, making it a valuable tool for research on immune responses and cellular signaling pathways involving TRPV2.