TRP Channel

Cat. No.

A68861

CAS No.

1366233-41-1

GSK2332255B

GSK2332255B is a highly selective antagonist of TRPC3 and TRPC6 channels, exhibiting IC50 values of 5 nM and 4 nM, respectively, for rat TRPC3 and TRPC6. This compound demonstrates over 100-fold selectivity for TRPC3 and TRPC6 compared to other calcium-permeable channels. GSK2332255B is valuable for research applications investigating the role of TRPC channels in various physiological and pathological processes.

Cat. No.

A68862

CAS No.

2861260-80-0

RhTx

RhTx is a transient receptor potential vanilloid 1 (TRPV1) activator that plays a crucial role in the modulation of pain perception. By enhancing TRPV1 activity, RhTx facilitates research into pain mechanisms and is valuable for studying nociception and the sensory transduction processes involved in inflammatory pain responses. This compound serves as a useful tool in pain research and therapeutic studies targeting TRPV1-related pathways.

Cat. No.

A68863

CAS No.

464152-46-3

BCTP

BCTP is a selective antagonist of the TRPV1 receptor, functioning through inhibition of ion channel activity. It exhibits potent antagonistic effects on human TRPV1 in CHO cells, with an IC50 of 18 nM at low pH conditions. BCTP is valuable for research into mechanisms underlying chronic pain and can aid investigations into pain modulation pathways.

Cat. No.

A68864

CAS No.

810668-53-2

Resolvin D2 methyl ester

Resolvin D2 methyl ester is a methyl ester derivative of the docosahexaenoic acid metabolite Resolvin D2, functioning as a TRP channel inhibitor. It exhibits significant anti-inflammatory and anti-infective properties, effectively modulating leukocyte activity. The compound selectively inhibits neuronal TRPV1 (IC50=0.1 nM) and TRPA1 (IC50=2 nM), making it a valuable tool in sepsis research and related studies on inflammation.

Cat. No.

A68865

CAS No.

939040-79-6

TRPV1 antagonist 9

TRPV1 antagonist 9 is a potent antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel. It effectively inhibits calcium influx in Chinese hamster ovary (CHO) cells expressing TRPV1 receptors, with IC50 values of 0.6 nM for capsaicin and 0.8 nM for acid-induced calcium uptake. This compound has demonstrated the ability to block capsaicin-induced flinch responses and can induce hyperthermia in rat models, making it a valuable tool for exploring nociceptive pathways and pain mechanisms.

Cat. No.

A68866

CAS No.

1481646-76-7

HC-067047 hydrochloride

HC-067047 hydrochloride is a potent and selective antagonist of the Transient Receptor Potential Vanilloid 4 (TRPV4). It effectively inhibits TRPV4 currents in human, rat, and mouse orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively. This compound is valuable for research into TRPV4-related physiological processes and the development of therapeutic strategies targeting this ion channel.

Cat. No.

A68868

CAS No.

60374-41-6

N-Oleoyl valine

N-Oleoyl valine is a N-acyl valine derivative that functions as an antagonist of the TRPV3 receptor. This compound exhibits significant biological activity in modulating thermal and pain sensation, making it valuable for research in pain management and sensory biology. It is used in studies investigating the mechanisms of TRPV3-mediated signaling pathways and potential therapeutic targets in sensory disorders.

Cat. No.

A68869

CAS No.

160498-00-0

Bisandrographolide A

Synonyms: BAA

Bisandrographolide A is a potent TRPV4 channel activator with an EC50 ranging from 790 to 950 nM. This compound has demonstrated anti-inflammatory, immunostimulant, and antihypertensive properties. Additionally, Bisandrographolide A binds to CD81, leading to functional suppression, making it valuable for research applications in inflammation, immune response, and cardiovascular studies.

Cat. No.

A68870

CAS No.

862269-73-6

(Rac)-AMG 628

(Rac)-AMG 628 is a potent TRPV1 antagonist, exhibiting an IC50 of 3.7 nM. This compound is valuable for research in chronic pain mechanisms, providing insights into the role of TRPV1 in nociception and pain modulation. Its efficacy makes it a noteworthy tool for exploring potential therapeutic avenues in pain management.

Cat. No.

A68871

CAS No.

111864-49-4

2′-Deoxy-ADPR

2′-Deoxy-ADPR is an agonist of the transient receptor potential melastatin 2 (TRPM2) channel. This compound is involved in calcium signaling within cells, particularly in Jurkat T-lymphocytes, where it plays a critical role in mediating cellular responses. 2′-Deoxy-ADPR is valuable for research investigating the effects of TRPM2 activation in various physiological and pathological processes.

Cat. No.

A68873

CAS No.

1011457-95-6

8-Br-7-CH-ADPR

Synonyms: 8-Bromo-7-deazaadenosine-5'-O-diphosphoribose

8-Br-7-CH-ADPR, a specific TRPM2 antagonist, effectively inhibits TRPM2 activation by binding to the NUDT9 homology domain of the TRPM2 channel. This modulation controls cation influx through the cell membrane, making it a valuable tool for investigating the physiological and pathological roles of TRPM2. Applications include studying cell death, neurodegenerative diseases, myocardial infarction, and diabetes, providing insights into TRPM2's involvement in various biological processes.

Cat. No.

A68874

CAS No.

862269-92-9

(S)-AMG-628

(S)-AMG-628 is a selective TRPV1 antagonist that effectively inhibits capsaicin- and acid-induced calcium influx, demonstrating IC50 values of 7 nM and 5 nM, respectively, in CHO cells. This compound has shown significant efficacy in reducing capsaicin-induced flinching behavior in rats and reversing thermal hypersensitivity in CFA-induced inflammatory pain models. As such, (S)-AMG-628 serves as a valuable tool in research addressing pain mechanisms and potential therapeutic interventions for inflammatory pain conditions.

Cat. No.

A68875

CAS No.

289902-82-5

MSK-195

MSK-195 is a potent agonist of the transient receptor potential vanilloid 1 (TRPV1) channel, demonstrating a potency of 120 nM and an efficacy of 71% in inducing arteriolar responses. This compound is valuable for research applications aimed at understanding pain pathways, neurogenic inflammation, and the physiological role of TRPV1 in various tissues. Its ability to selectively activate TRPV1 makes it a useful tool for dissecting the functions and mechanisms associated with this receptor in preclinical studies.

Cat. No.

A68876

CAS No.

808756-64-1

A778317

A778317 is a potent TRPV1 antagonist, designed to inhibit the activation of TRPV1 receptors. With a pIC50 value of 8.31, it effectively blocks intracellular calcium level changes mediated by TRPV1. This compound has demonstrated the capability to prevent capsaicin and acid-induced activation of natural rat TRPV1 receptors in dorsal root ganglion neurons, making it a valuable tool for research focused on pain mechanisms and sensory nerve function.

Cat. No.

A68877

CAS No.

52661-97-9

Cyclo(-asp-gly)

Cyclo(-asp-gly) is a cyclic dipeptide that functions as a TRPV1 stimulator, enhancing the activity of the transient receptor potential vanilloid 1 ion channel. This compound is utilized in research applications related to pain signaling and sensory perception, making it a valuable tool in studies focused on nociception and the mechanisms of pain modulation. Its role in activating TRPV1 provides insights into potential therapeutic approaches for pain management.

Cat. No.

A68878

CAS No.

289902-64-3

JYL-79

JYL-79 is a potent TRPV1 agonist, exhibiting an IC50 of 3.9 nM. It is primarily used in research focused on neuropathic pain, allowing for the exploration of TRPV1's role in pain pathways and potential therapeutic interventions. This compound provides valuable insights into the mechanisms of pain modulation and serves as a tool for investigating the biology of sensory neurons.

Cat. No.

A68879

CAS No.

311789-03-4

TRPV3 modulator-1

TRPV3 modulator-1 is a selective modulator of the transient receptor potential vanilloid 3 (TRPV3) channel. It exhibits the ability to regulate TRPV3 activity, influencing calcium ion influx in response to thermal and chemical stimuli. This compound has potential applications in research related to pain sensation, skin physiology, and itch, making it a valuable tool for studying TRPV3-mediated signaling pathways.

Cat. No.

A68881

CAS No.

1992047-63-8

M084 hydrochloride

M084 hydrochloride is a selective inhibitor of the TRPC4 and TRPC5 ion channels, exhibiting IC50 values of 10.3 μM and 8.2 μM, respectively. This compound demonstrates significant antidepressant and anxiolytic effects, making it a valuable tool for studying anxiety and mood disorders. Its ability to modulate calcium influx through TRPC channels positions M084 hydrochloride as an important reagent for research in neurobiology and pharmacology.

Cat. No.

A68882

CAS No.

3026084-12-5

TRPV4 antagonist 5

TRPV4 antagonist 5 is a selective antagonist of the TRPV4 channel, which is involved in various physiological processes including osmoregulation and pain sensation. This compound demonstrates potential in modulating TRPV4-mediated responses and can be utilized in research focusing on inflammation, pain management, and sensory neuronal pathways. Its application may also extend to investigations of cellular calcium signaling and the development of therapeutics targeting TRPV4-related disorders.

Cat. No.

A68883

CAS No.

1459809-09-6

AC4

AC4 is a potent TRPV1 antagonist that acts as a trans antagonist upon voltage activation of the receptor and functions as a cis antagonist in response to capsaicin stimulation. This compound serves as a valuable tool for investigating TRPV1 signaling pathways and the modulation of nociceptive responses. Its unique photoswitchable properties allow for the combined use of an antagonist and an agonist, making it an essential reagent for research in pain mechanisms and sensory biology.

Cat. No.

A68884

CAS No.

862269-93-0

AMG-628

AMG-628 is a potent orally active inhibitor of the transient receptor potential vanilloid 1 (TRPV1). It effectively blocks capsaicin and acid-induced calcium influx in TRPV1-expressing CHO cells, with IC50 values of 4.9 nM and 3.1 nM, respectively. AMG-628 demonstrates significant analgesic effects in capsaicin-induced rat pain models and has a half-life of approximately 2.4 hours in rats, making it a valuable tool for studying pain mechanisms and potential therapeutic applications.

Cat. No.

A68885

CAS No.

736945-96-3

TRPC3/6-IN-1

TRPC3/6-IN-1 is a selective blocker of the canonical transient receptor potential channels TRPC3 and TRPC6, exhibiting IC50 values of 1260 nM and 500 nM, respectively. This compound is instrumental for investigating the role of TRPC3 and TRPC6 in cardiac physiology and pathophysiology, particularly in chronic models of heart failure. Its specific inhibitory action makes it a valuable tool for studying the mechanisms underlying cardiovascular diseases.

Cat. No.

A68886

CAS No.

115075-59-7

Ibuprofen acyl-β-D-glucuronide

Synonyms: Ibuprofen glucuronide

Ibuprofen acyl-β-D-glucuronide is a selective antagonist of the TRPA1 ion channel. This compound effectively reduces the calcium response induced by allyl isothiocyanate (AITC), exhibiting an IC50 value of 60 μM. It is a valuable tool for investigating TRPA1-related pathways and for exploring potential therapeutic applications in pain modulation and sensory signal transduction.

Cat. No.

A68887

CAS No.

92585-24-5

TRPA1-IN-3

TRPA1-IN-3 is a selective inhibitor of the transient receptor potential ankyrin 1 (TRPA1) channel. This compound is primarily utilized in research focused on skin and respiratory tract conditions, where TRPA1 activation is implicated in nociceptive signaling and inflammatory responses. Its inhibitory properties make it valuable for studying pain mechanisms and potential therapeutic interventions in related disorders.

Cat. No.

A68888

CAS No.

1160606-90-5

JNJ-39729209

JNJ-39729209 is a selective antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel, displaying pIC50 values of 7.9 to 8.5 across various species including human, rat, canine, and guinea pig. This compound effectively inhibits capsaicin-induced hypotension and associated hypothermia. Additionally, JNJ-39729209 demonstrates significant anti-inflammatory and analgesic effects in carrageenan and CFA-induced thermal hyperalgesia models in rats, as well as anti-cough activity in guinea pigs, making it a valuable tool for research in pain and inflammatory response.