TRP Channel

Cat. No.

A68824

CAS No.

2681273-35-6

TRPV4 antagonist 3

TRPV4 antagonist 3 is a selective antagonist of the TRPV4 ion channel, demonstrating a pIC50 value of 8.4. This compound effectively inhibits TRPV4-mediated calcium influx, making it a valuable tool for investigating the physiological roles of TRPV4 in various biological processes. It has potential applications in pain research, inflammation studies, and the exploration of therapeutic strategies for TRPV4-related disorders.

Cat. No.

A68825

CAS No.

1791309-86-8

ZQMT-10

ZQMT-10 is a potent and orally active antagonist of the transient receptor potential ankyrin 1 (TRPA1), exhibiting a Kd of 1.04 μM. This compound is significant in cancer research, offering insights into the mechanisms of pain and inflammation associated with tumor development. Its selective inhibition of TRPA1 makes it a valuable tool for understanding its role in various physiological and pathological processes.

Cat. No.

A68828

CAS No.

573678-04-3

MK-2295

Synonyms: NGD-8243

MK-2295 (NGD-8243) is a potent TRPV1 antagonist that plays a crucial role in pain modulation. Its primary biological activity is as an analgesic agent, making it a valuable tool for research aimed at understanding and addressing pain mechanisms. MK-2295 is useful in studies exploring the therapeutic potential of TRPV1 inhibition in various pain-related conditions.

Cat. No.

A68832

CAS No.

1984824-54-5

GDC-0334

GDC-0334 is a selective antagonist of the Transient Receptor Potential Ankyrin 1 (TRPA1) channel. It effectively inhibits TRPA1 function in airway smooth muscle and sensory neurons, leading to decreased cough reflex and reduced allergic airway inflammation in preclinical models. This compound is valuable for research focused on TRPA1-mediated conditions, including pain and asthma, facilitating the study of therapeutic interventions targeting these pathways.

Cat. No.

A68834

CAS No.

1008529-42-7

ABT-116

ABT-116 is an orally active antagonist of the transient receptor potential vanilloid type 1 (TRPV1) channel. This compound demonstrates significant analgesic efficacy, making it a valuable tool in pain research. ABT-116 is particularly relevant for studies focusing on neurological diseases and the modulation of pain pathways.

Cat. No.

A68836

CAS No.

1345614-89-2

AS1928370

AS1928370 is a selective antagonist of the TRPV1 ion channel, demonstrating the ability to inhibit ligand-induced activation in vivo. This CNS-penetrant compound is particularly valuable for studying mechanisms underlying neuropathic pain. Its application in research offers insights into pain modulation and potential therapeutic strategies for pain management.

Cat. No.

A68838

CAS No.

878811-00-8

TRPV1 antagonist 5

TRPV1 antagonist 5 is a selective antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel. This compound demonstrates potent inhibitory activity against TRPV1, making it a valuable tool for studies focused on pain signaling and thermoregulation. Research applications include investigating nociceptive pathways and exploring therapeutic potential for inflammatory pain relief.

Cat. No.

A68841

CAS No.

1159996-43-6

AMG8788

AMG8788 is a selective, orally active antagonist of the transient receptor potential melastatin 8 (TRPM8), exhibiting an IC50 of 63.2 nM. This compound demonstrates significant inhibitory activity on TRPM8, making it valuable for studying sensory perception, pain pathways, and thermoregulation. It serves as an important tool for research into conditions associated with TRPM8 modulation, including neuropathic pain and cold sensitivity.

Cat. No.

A68844

CAS No.

1159997-27-9

AMG9678

AMG9678 is a selective, orally active antagonist of the transient receptor potential melastatin 8 (TRPM8) channel, exhibiting a potent inhibitory effect with an IC50 value of 31.2 nM. This compound is utilized in research focused on pain modulation, thermosensation, and neurogenic inflammation, providing insights into the role of TRPM8 in various physiological and pathological processes. Its specificity and potency make it a valuable tool for investigating TRPM8-related biological pathways.

Cat. No.

A68847

CAS No.

951135-00-5

JNJ-38893777

JNJ-38893777 is a selective antagonist of the transient receptor potential vanilloid type 1 (TRPV1) channel. By inhibiting neuronal hyperactivation, JNJ-38893777 effectively reduces inflammatory hyperalgesia, making it a valuable tool for studies focused on migraine headaches, as well as neuropathic and inflammatory pain research. Its oral activity further enhances its potential in pharmacological applications targeting pain modulation.

Cat. No.

A68852

CAS No.

1445753-16-1

DFL23448

DFL23448 is a selective antagonist of the transient receptor potential melastatin-8 (TRPM8) channel. It demonstrates potent inhibition with IC50 values of 10 nM and 21 nM in human embryonic kidney 293 cells stimulated by Cooling Agent 10 or cold exposure. DFL23448 exhibits minimal activity against other transient receptor potential channels, such as TRPV1, TRPA1, and TRPV4, as well as various G protein-coupled receptors. This compound has potential applications in modifying bladder function and alleviating bladder overactivity in in vivo models.

Cat. No.

A68856

CAS No.

1253734-75-6

SAR-115740

SAR-115740 is a TRPV1 antagonist that selectively inhibits the transient receptor potential vanilloid 1 channel. This compound has demonstrated developmental toxicity in H9 cell assays, highlighting its potential impact on cellular differentiation and viability. SAR-115740 is valuable for investigating inflammatory conditions and neurological disorders, contributing to research aimed at understanding pain mechanisms and developing therapeutic strategies.

Cat. No.

A68858

CAS No.

1166398-35-1

GRC-6211

GRC-6211 is a selective antagonist of the TRPV1 receptor, demonstrated to be orally active. This compound exhibits significant anti-inflammatory effects, making it a valuable tool for research applications in pain modulation and inflammatory disease studies.

Cat. No.

A68859

CAS No.

790689-76-8

AZ12099548

AZ12099548 is a selective antagonist of the TRPV1 receptor, which plays a critical role in pain and sensory perception. This compound effectively inhibits calcium mobilization induced by both capsaicin and low pH, making it a valuable tool for research into pain mechanisms and sensory disorders. Its utility in studying TRPV1-related pathways facilitates investigations into potential therapeutic strategies for inflammatory and neuropathic pain conditions.

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.

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.

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.

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.

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.

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.

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.

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.