TRP Channel

Cat. No.

A68726

CAS No.

1400699-64-0

Elismetrep

Synonyms: MT-8554

Elismetrep (MT-8554) is a selective TRPM8 antagonist that inhibits the activity of the transient receptor potential melastatin 8 channel. It is shown to reduce the frequency of vasomotor symptoms and is valuable for research in pain modulation and sensory perception. Elismetrep offers potential applications in the study of disorders related to thermal sensation and nociception.

Cat. No.

A68727

CAS No.

2765294-54-8

TRPV1 antagonist 3

TRPV1 antagonist 3 (Compound 7q) is a highly effective antagonist of the TRPV1 receptor, demonstrating an IC50 of 2.66 nM against capsaicin. This compound exhibits mode-selectivity and is characterized by favorable oral bioavailability (F = 60%) as well as the ability to penetrate the central nervous system. TRPV1 antagonist 3 is valuable for research focused on pain modulation and inflammatory processes.

Cat. No.

A68728

CAS No.

3118-34-1

Hyp9

Hyp9 is a potent agonist specific for the transient receptor potential canonical 6 (TRPC6) channel. This compound facilitates TRPC6 activation, making it a valuable tool for investigating its role in cellular signaling pathways and the pathophysiology of spinal cord injury (SCI). Researchers can utilize Hyp9 to explore therapeutic strategies targeting TRPC6 in models of neuroprotection and regeneration.

Cat. No.

A68729

CAS No.

70351-51-8

Supercinnamaldehyde

Supercinnamaldehyde is a potent activator of the transient receptor potential ankyrin 1 (TRPA1) channel, exhibiting an EC50 value of 0.8 μM. It activates TRPA1 through covalent modification of cysteine residues, making it a valuable tool for studying pain pathways and sensory signaling. Its applications include research into inflammation, nociception, and neurobiology.

Cat. No.

A68730

CAS No.

1669444-50-1

PF-05214030

PF-05214030 is a potent TRPV4 antagonist, exhibiting IC50 values of 4 nM for human TRPV4 and 27 nM for rat TRPV4. This compound effectively counteracts the decrease in bladder capacity induced by intravesical administration of a TRPV4 agonist. PF-05214030 is therefore a valuable tool for investigating the role of TRPV4 in bladder physiology and may hold potential for therapeutic applications in bladder dysfunction research.

Cat. No.

A68731

CAS No.

2070015-10-8

ML204 hydrochloride

ML204 hydrochloride is a selective inhibitor of the TRPC4 and TRPC5 channels, demonstrating a minimum of 19-fold selectivity over the TRPC6 channel. It has no significant effects on other transient receptor potential (TRP) channels or on voltage-gated sodium, potassium, or calcium channels. This compound is valuable for research applications exploring cellular calcium signaling and the physiological roles of TRPC4 and TRPC5 in various biological processes.

Cat. No.

A68732

CAS No.

1933528-96-1

MDR-652

MDR-652 is a targeted agonist of the transient receptor potential vanilloid 1 (TRPV1) channel. This compound displays high specificity with binding affinities (Kis) of 11.4 nM for human TRPV1 and 23.8 nM for rat TRPV1. The effective concentrations (EC50s) are 5.05 nM and 93 nM for hTRPV1 and rTRPV1, respectively. MDR-652 demonstrates significant potential as a topical analgesic, making it a valuable tool in pain research and therapeutic applications.

Cat. No.

A68733

CAS No.

2304549-73-1

GFB-8438

GFB-8438 is a highly selective inhibitor of the transient receptor potential channel TRPC5, exhibiting IC50 values of 0.18 μM for hTRPC5 and 0.29 μM for hTRPC4. This compound demonstrates significant selectivity over TRPC6, other TRP family members, NaV 1.5, and shows minimal activity against the hERG channel. GFB-8438 has been shown to provide protective effects to mouse podocytes from injury induced by protamine sulfate, highlighting its potential for research in renal protection and related pathways.

Cat. No.

A68734

CAS No.

2413739-88-3

Evifacotrep

Evifacotrep is a potent antagonist of the transient receptor potential channel 5 (TRPC5) with an IC50 of ≤50 nM. This compound effectively inhibits TRPC5/TRPC4 activity, making it a valuable tool for investigating neurological diseases. Its selective mechanism of action allows for detailed study of TRPC channel involvement in various pathophysiological processes.

Cat. No.

A68735

CAS No.

2763378-71-6

JW-65

JW-65 is a selective inhibitor of the TRPC3 channel, targeting its role in various cellular processes. This compound exhibits significant biological activity that can be leveraged in studies of neurological and cardiovascular diseases. JW-65 is useful for investigating the mechanisms of TRPC3 in pathophysiological conditions and may provide insights into potential therapeutic applications.

Cat. No.

A68736

CAS No.

528583-91-7

17(R)-Resolvin D1

Synonyms: 17(R)-RvD1; AT-RvD1

17(R)-Resolvin D1 is a TRPV3 inhibitor known for its potent anti-inflammatory properties. This aspirin-triggered epimer of Resolvin D1 exhibits significant biological activity by specifically inhibiting TRPV3 with an IC50 of 398 nM. It has demonstrated peripheral anti-nociceptive efficacy, making it a valuable tool for research applications focused on inflammation and pain management.

Cat. No.

A68737

CAS No.

2776151-36-9

L687

L687 is a potent activator of the TRPC3, TRPC6, and TRPC7 channels, facilitating the cellular uptake of oligonucleotides. Its ability to modulate calcium influx makes it a valuable tool for studying TRP channel function and its role in various physiological processes. L687 has potential applications in molecular biology, particularly in gene delivery and therapeutic research involving nucleic acid-based strategies.

Cat. No.

A68738

CAS No.

667427-75-0

TRPC6-PAM-C20

TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) targeting TRPC6 channels. This compound significantly enhances channel activation at low basal concentrations of diacylglycerol (DAG), facilitating increases in intracellular calcium ([Ca2+]i) levels in TRPC6-expressing HEK293 cells with an EC50 of 2.37 μM. TRPC6-PAM-C20 serves as an essential reagent for researchers investigating TRPC6-dependent signaling pathways and calcium dynamics.

Cat. No.

A68739

CAS No.

205687-01-0

Capsiate

Capsiate is a TRPV1 agonist derived from a non-pungent variety of CH-19 sweet red pepper. This compound exhibits potent biological activity by activating the transient receptor potential vanilloid 1 (TRPV1) channel, which is involved in the modulation of pain and inflammation pathways. Capsiate is utilized in research applications focused on pain management, metabolic studies, and the exploration of sensory receptor functions.

Cat. No.

A68740

CAS No.

1803003-68-0

RN-9893

RN-9893 is a potent and selective antagonist of the TRPV4 receptor, exhibiting IC50 values of 320 nM, 420 nM, and 660 nM for mouse, human, and rat channels, respectively. This compound is valuable for research applications involving the modulation of TRPV4-mediated physiological processes. Its selective inhibition can aid in studies related to pain sensation, inflammation, and other TRPV4-associated diseases.

Cat. No.

A68741

CAS No.

915972-17-7

Afidopyropen

Synonyms: ME-5343

Afidopyropen is an insecticide that targets sucking insects, including whiteflies, aphids, and leafhoppers. It operates by influencing the Nanchung (Nan) and Inactive (Iav) genes in these insects, thereby affecting the TRPV channel. Due to its degradability, Afidopyropen is suitable for use on a variety of crops, making it a valuable tool in agricultural research and pest management.

Cat. No.

A68742

CAS No.

103560-62-9

(E)-4-Oxo-2-nonenal

Synonyms: 4-ONE

(E)-4-Oxo-2-nonenal is a potent agonist of the transient receptor potential ankyrin 1 (TRPA1) channel, identified as a significant product of lipid hydroperoxide decomposition. This compound plays a crucial role in mediating oxidative stress responses and has been implicated in various pathological conditions. It is useful in research applications exploring TRPA1-related signaling pathways and the impact of oxidative stress on cellular functions.

Cat. No.

A68743

CAS No.

2126166-03-6

TAT-M2NX

TAT-M2NX is a selective inhibitor of the human TRPM2 channel, playing a crucial role in modulating calcium influx induced by hydrogen peroxide. This compound demonstrates neuroprotective effects in models of ischemic stroke, preserving hippocampal long-term potentiation and improving memory function following traumatic brain injury. Additionally, TAT-M2NX reduces infarct volume after middle cerebral artery occlusion, although its effects have not been observed in female mice. This reagent is valuable for research applications related to traumatic brain injury and ischemic stroke.

Cat. No.

A68744

CAS No.

2265215-18-5

TRPC5-IN-1

TRPC5-IN-1 is a selective TRPC5 inhibitor that demonstrates 50.5% inhibition of TRPC5 at a concentration of 3 μM. This compound is valuable for studying the role of TRPC5 in chronic kidney disease (CKD) and may facilitate research aimed at understanding the underlying mechanisms of renal pathophysiology. Its specificity makes it a useful tool in investigating potential therapeutic interventions targeting TRPC5-related pathways.

Cat. No.

A68745

CAS No.

1507344-37-7

Cryosim-3

Cryosim-3 is a selective agonist of the TRPM8 receptor, known for its role in thermosensation and chemosensation. This compound enhances tear secretion and alleviates ocular discomfort in various animal models, making it valuable for research in ocular therapeutics and sensory biology. Its application may extend to understanding the modulation of pain and inflammation through TRP channel pathways.

Cat. No.

A68746

CAS No.

1803003-65-7

RN-1665

RN-1665 is an orally active TRPV4 inhibitor, demonstrating high selectivity for other related TRP receptors, including TRPV1, TRPV3, and TRPM8. This compound serves as an effective probe for screening TRPV4 interactions, exhibiting IC50 values of 0.26 μM and 0.39 μM for human TRPV4 and rat TRPV4, respectively. RN-1665 is valuable for research applications focused on pain pathways, sensory physiology, and potential therapeutic interventions targeting TRPV4-mediated processes.

Cat. No.

A68747

CAS No.

119959-65-8

N-Arachidonoyl Taurine

N-Arachidonoyl Taurine is a selective activator of the transient receptor potential vanilloid channels TRPV1 and TRPV4, exhibiting EC50 values of 28 μM and 21 μM, respectively. This compound is pivotal in studies investigating pain perception, thermoregulation, and various neurophysiological processes. Its unique properties make it a valuable tool for researching TRPV-mediated signaling pathways and their implications in sensory biology.

Cat. No.

A68748

CAS No.

1889218-34-1

LY3526318

LY3526318 is a selective antagonist of the TRPA1 ion channel, with an IC50 of 5-6 μM. This compound effectively inhibits TRPA1-mediated pain signal transduction, demonstrating notable analgesic activity. LY3526318 is primarily utilized in research focused on chronic pain conditions, including diabetic peripheral neuropathy, chronic low back pain, and osteoarthritis-related pain.

Cat. No.

A68749

CAS No.

2415206-22-1

TRPA1-IN-2

TRPA1-IN-2 is a potent inhibitor of the transient receptor potential ankyrin 1 (TRPA1) channel, exhibiting an IC50 of 0.04 µM. This compound demonstrates significant anti-inflammatory properties, making it a valuable tool for research into pain pathways and inflammatory diseases. Its oral bioavailability further enhances its utility in preclinical studies aimed at targeting TRPA1-related conditions.

Cat. No.

A68750

CAS No.

459429-39-1

SB 452533

SB 452533 is a potent and selective antagonist of the TRPV1 ion channel. It demonstrates a pKb of 7.8, indicating strong binding affinity and inhibitory activity. This compound is primarily utilized in research applications related to pain modulation and inflammation, offering insights into the role of TRPV1 in nociception and sensory neurons. SB 452533 is an essential tool for studying pain pathways and developing potential analgesic therapies.