TRP Channel

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.

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.

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.

A68752

CAS No.

15533-81-0

ELP-004

ELP-004 is a selective TRPC channel inhibitor that targets TRPC-mediated calcium entry. It effectively inhibits osteoclast differentiation and activity, suppressing the translocation of NFATc1 in inflammatory osteoclastogenesis. Additionally, ELP-004 demonstrates a protective effect against bone erosion in mouse models of rheumatoid arthritis, making it a valuable tool for studying osteoclast biology and potential therapeutic strategies in bone degenerative diseases.

Cat. No.

A68768

CAS No.

3046390-54-6

TRPV4-IN-5

TRPV4-IN-5 is a selective TRPV4 inhibitor with an IC50 value of 0.46 μM. This compound exhibits significant efficacy in reducing acute lung injury symptoms induced by lipopolysaccharide in murine models. TRPV4-IN-5 is valuable for research into the modulation of TRPV4-associated pathways and potential therapeutic applications in lung inflammatory conditions.

Cat. No.

A68769

CAS No.

35482-50-9

Cannabidiorcol

Synonyms: O-1821; CBD-C1

Cannabidiorcol (CBDO) is an inhibitor of transient receptor potential (TRP) channels. This compound, structurally related to cannabidiol with a shortened pentyl side chain, exhibits anti-inflammatory properties while displaying low affinity for cannabinoid receptors. Research applications include investigations into its potential role in modulating inflammation and exploring its effects on tumorigenesis at elevated concentrations.

Cat. No.

A68776

CAS No.

1819366-84-1

TRPV6-IN-1

TRPV6-IN-1 is a potent and selective inhibitor of the transient receptor potential cation channel subfamily V member 6 (TRPV6). It exhibits significant anti-proliferative effects, making it a valuable tool for cancer research. This compound can be utilized in studies investigating the role of TRPV6 in tumor growth and progression, aiding in the development of potential therapeutic strategies.

Cat. No.

A68777

CAS No.

187947-37-1

N-Arachidonoylserotonin

Synonyms: Arachidonyl serotonin; AA-5-HT

N-Arachidonoylserotonin is a potent fatty acid amide hydrolase (FAAH) inhibitor, exhibiting an IC50 value ranging from 1 to 12 µM. Additionally, it serves as an antagonist of transient receptor potential vanilloid-type 1 (TRPV1) channels, with an IC50 of 70 to 100 nM. Due to its dual action, N-Arachidonoylserotonin demonstrates significant analgesic properties in rodent models, making it a valuable tool for research in pain mechanisms and therapeutic interventions.

Cat. No.

A68793

CAS No.

177258-60-5

AAL-149

AAL-149 is a selective inhibitor of the TRPM7 ion channel, exhibiting an IC50 value of 1.081 μM. This compound demonstrates multimodal anti-inflammatory effects while avoiding interaction with sphingosine-1-phosphate (S1P) receptors. AAL-149 is a valuable tool for researchers investigating the role of TRPM7 in inflammation and related biological pathways.

Cat. No.

A68801

CAS No.

2833727-43-6

TRPM2-IN-1

TRPM2-IN-1 is a selective inhibitor of the TRPM2 ion channel, which plays a critical role in calcium influx and cellular signaling. This compound has demonstrated significant neuroprotective effects and exhibits antistroke activity, making it a valuable tool in the study of ischemic stroke and related neurological disorders. Its capacity to modulate TRPM2 activity provides insight into potential therapeutic strategies for neurodegenerative conditions.

Cat. No.

A68802

CAS No.

3027529-88-7

HZS60

HZS60 is a selective TRP channel inhibitor that demonstrates significant neuroprotective effects against cerebral ischemia. It effectively mitigates primary neuronal damage induced by NMDA and oxygen-glucose deprivation/reoxygenation. Additionally, HZS60 exhibits favorable pharmacokinetic properties and can reduce injury associated with cerebral ischemia-reperfusion. This compound serves as a promising candidate for research applications targeting ischemic stroke.

Cat. No.

A68806

CAS No.

87657-67-8

TRPV1-IN-3

TRPV1-IN-3 is a selective inhibitor of the transient receptor potential vanilloid 1 (TRPV1) channel, demonstrating significant antifibrotic activity in vitro with an IC50 of 0.51 μM. Its mechanism involves the modulation of fibrosis markers such as collagen I and α-SMA through inhibition of the TGF-β/Smads and MAPK signaling pathways. Research applications include studying idiopathic pulmonary fibrosis, where TRPV1-IN-3 has been shown to reduce collagen deposition in lung tissue, enhance alveolar structure, and increase survival rates in Bleomycin-induced pulmonary fibrosis models.

Cat. No.

A68807

CAS No.

2308595-83-5

TRPC6-IN-2

TRPC6-IN-2 is a selective inhibitor of TRPC6 channels. This compound effectively inhibits TRPC6 protein activity, making it a valuable tool for studying calcium signaling pathways. TRPC6-IN-2 can be utilized in various research applications, including investigations into cardiovascular and neurological disorders where TRPC6 plays a critical role in cellular function.

Cat. No.

A68810

CAS No.

2387893-55-0

TRPC3/6-IN-2

TRPC3/6-IN-2 is a potent inhibitor targeting the TRPC3 and TRPC6 channels, exhibiting IC50 values of 16 nM and 29.8 nM for TRPC3 and TRPC6, respectively. This compound is valuable for investigating the physiological and pathological roles of TRPC channels in various cellular processes. It can be utilized in research focused on cardiovascular function, neuronal signaling, and other conditions associated with TRPC dysregulation.

Cat. No.

A68813

CAS No.

738603-63-9

TRPC5-IN-5

TRPC5-IN-5 is a selective inhibitor of the Transient Receptor Potential Canonical 5 (TRPC5), with an IC50 value of 1.28 μM. This compound exhibits promising biological activity, making it valuable for research focused on neurological and renal diseases. Its ability to modulate TRPC5 activity provides insights into potential therapeutic strategies for disorders associated with these systems.

Cat. No.

A68815

CAS No.

3032263-08-1

TRPC4/5-IN-1

TRPC4/5-IN-1 is a selective inhibitor of the transient receptor potential channel 4 and 5 (TRPC4/5), exhibiting IC50 values of 2.06 μM and 0.54 μM, respectively. This compound demonstrates significant biological activity in modulating TRPC channel-mediated calcium influx, making it useful for investigations into proteinuric kidney diseases and skin inflammatory conditions. Its targeted inhibition offers potential insights into the underlying mechanisms of these pathologies and may aid in the development of novel therapeutic strategies.

Cat. No.

A68819

CAS No.

616884-66-3

OMDM-5

OMDM-5 is a selective anandamide cellular uptake (ACU) inhibitor, exhibiting a Ki of 4.8 μM. In addition, OMDM-5 demonstrates potent activity as a vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM. This compound also shows weak activity as a cannabinoid receptor type 1 (CB1) ligand, with a Ki of 4.9 μM. Its properties make OMDM-5 useful for studies involving pain modulation and endocannabinoid signaling pathways.

Cat. No.

A68820

CAS No.

3053390-98-7

TRPC4/5-IN-3

TRPC4/5-IN-3 is a potent inhibitor of the transient receptor potential canonical channels 4 and 5, exhibiting IC50 values of 3.6 nM and 5.5 nM, respectively. This compound shows additional hERG channel inhibition with an IC50 of 6.5 µM, along with favorable metabolic stability in liver microsomes from humans, rats, and mice. TRPC4/5-IN-3 demonstrates significant antidepressant and anxiolytic effects in murine models and possesses excellent pharmacokinetic properties, highlighted by an oral bioavailability of 87%. This reagent is valuable for research involving TRPC channel modulation and related therapeutic pathways.

Cat. No.

A68823

CAS No.

1366234-01-6

TRPC3/6-IN-3

TRPC3/6-IN-3 is a selective inhibitor of TRPC3 and TRPC6 channels, primarily targeting the regulation of calcium influx in cells. This compound exhibits significant biological activity in modulating vascular smooth muscle contraction and endothelial function, making it relevant for cardiovascular disease research. TRPC3/6-IN-3 offers a valuable tool for elucidating the roles of these channels in various pathophysiological conditions, contributing to the understanding of cardiovascular mechanisms.

Cat. No.

A68826

CAS No.

652967-47-0

BTB 06061

BTB 06061 is a selective inhibitor of the TRPM7 ion channel, known for its involvement in cellular magnesium homeostasis and signaling. This compound exhibits significant biological activity in modulating TRPM7-mediated pathways, making it a valuable tool for investigating ischemic diseases and related conditions. Its application in research can enhance the understanding of TRPM7's role in cellular processes and disease mechanisms.

Cat. No.

A68829

CAS No.

59259-77-7

8-Br-ADPR

Synonyms: 8-Bromoadenosine-5'-O-diphosphoribose

8-Br-ADPR (8-Bromoadenosine-5'-O-diphosphoribose) is a TRPM2 inhibitor that antagonizes the ADPR signaling pathway. This compound inhibits glucagon-mediated nuclear calcium signaling and downstream signaling through CaMKII/CREB phosphorylation by preventing ADPR-induced activation of TRPM2. In diabetic models, 8-Br-ADPR effectively decreases gluconeogenic gene expression and lowers blood glucose levels. Additionally, it inhibits ADPR-mediated calcium signaling in NK cells, affecting immune synapse formation, granzyme B release, and cytolytic activity against melanoma cells. 8-Br-ADPR is useful in research on diabetes, melanoma, and lymphoma.

Cat. No.

A68830

CAS No.

2696407-32-4

ZA18

ZA18 is a selective inhibitor of the TRPM2 channel, characterized by an IC50 value of 6.2 μM. This compound effectively mitigates intracellular calcium overload caused by TRPM2 activation and significantly decreases the mortality of SH-SY5Y cells subjected to H2O2-induced stress. ZA18 is suitable for investigating mechanisms underlying ischemia-reperfusion injury, inflammation, and various neurodegenerative diseases.

Cat. No.

A68831

CAS No.

2758126-11-1

TRPC5-IN-3

TRPC5-IN-3 is a selective inhibitor of the Transient Receptor Potential Cation Channel 5 (TRPC5), exhibiting an IC50 value of 10.75 nM. This compound has demonstrated significant potential in modulating calcium influx in cells and is useful for studying TRPC5-related physiological processes and pathologies. Its applications include investigating the role of TRPC5 in neurobiology, renal function, and various disease states.

Cat. No.

A68842

CAS No.

2304552-99-4

TRPC5-IN-2

TRPC5-IN-2 is a selective inhibitor of the transient receptor potential cation channel 5 (TRPC5), known for its role in calcium ion influx and various physiological processes. This compound has demonstrated significant inhibitory activity against TRPC5, making it valuable for research into calcium signaling and its implications in neurological disorders, cardiovascular diseases, and gene regulation. TRPC5-IN-2 is essential for studies aimed at elucidating the functional roles of TRPC5 and exploring potential therapeutic interventions.