TRP Channel

Cat. No.

A68751

CAS No.

871814-52-7

Libvatrep

Synonyms: SAF312; Vanilloid receptor antagonist 1

Libvatrep is a selective TRPV1 antagonist that inhibits the activity of the transient receptor potential vanilloid 1 channel. It exhibits significant anti-nociceptive effects, making it a valuable tool for research in pain modulation and sensory neuron signaling. This compound is useful in investigations of neurogenic inflammation and the potential treatment of chronic pain 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.

A68753

CAS No.

1206619-37-5

GSK2220691

GSK2220691 is a potent antagonist of the transient receptor potential vanilloid 4 (TRPV4) channel. This compound effectively inhibits pulmonary edema induced by GSK1016790 and reduces HCl-induced increases in key mediators such as vascular endothelial growth factor (VEGF), keratinocyte-derived chemokine (KC; CXCL1), and granulocyte colony-stimulating factor (GCSF). GSK2220691 serves as a valuable tool for investigating TRPV4-related pathways and therapeutic applications in respiratory disorders.

Cat. No.

A68754

CAS No.

1562-93-2

4-(Phenyldiazenyl)benzoic acid

4-(Phenyldiazenyl)benzoic acid is a selective TRP channel agonist that exhibits photosensitivity and photochemical switchability. This compound serves as a valuable pharmacological tool in the investigation of pain signaling pathways, offering researchers the ability to modulate TRPA1 activity through light exposure. Its unique properties make it suitable for studies focusing on nociception and sensory signaling mechanisms.

Cat. No.

A68755

CAS No.

6938-94-9

Diisopropyl adipate

Synonyms: Adipic acid diisopropyl ester

Diisopropyl adipate is a TRPA1 activator that enhances FITC-induced contact hypersensitivity. This compound is utilized extensively as an alternative plasticizer in various formulations, serving not only as a key ingredient in cosmetic products but also as an excipient in pharmaceutical applications. By functioning as an emollient and plasticizer, diisopropyl adipate improves the stability, solubility, and overall processability of drug formulations, while influencing the absorption, distribution, metabolism, and elimination (ADME) characteristics of co-administered drugs.

Cat. No.

A68756

CAS No.

1002100-44-8

Oleoyl serotonin

Oleoyl Serotonin is a TRPV1 antagonist, exhibiting an IC50 value of 2.57 μM for human TRPV1 receptors. This compound is implicated in the modulation of nociceptive pathways, making it a valuable tool for studies related to pain signaling and sensory transduction. Oleoyl Serotonin is suitable for research applications investigating inflammatory pain and potential therapeutic interventions targeting TRPV1.

Cat. No.

A68757

CAS No.

1820968-63-5

MSP-3

MSP-3 is a potent agonist of the TRPV1 receptor, characterized by an EC50 of 0.87 μM. This compound demonstrates significant neuroprotective and antinociceptive properties, making it valuable for research focused on pain modulation and neuroprotection. Its ability to activate TRPV1 makes MSP-3 an important tool for investigating sensory physiology and related therapeutic interventions.

Cat. No.

A68758

CAS No.

2102179-29-1

TRPM8 antagonist 3

TRPM8 Antagonist 3 is a selective antagonist targeting the Transient Receptor Potential Melastatin 8 (TRPM8) channel, exhibiting an IC50 value of 11 nM. This compound effectively inhibits TRPM8-mediated calcium influx, making it useful for studying nociceptive pathways and cold sensitivity. It has potential applications in research related to pain management, sensory biology, and neurobiology.

Cat. No.

A68759

CAS No.

1035-77-4

Estradiol 3-methyl ether

Synonyms: 3-O-Methyl estradiol; 17β-Estradiol 3-methyl ether; 3-Methoxyestradiol

Estradiol 3-methyl ether (EDME) is a potent antagonist of the TRPML1 ion channel and a microtubule depolymerizer. It exhibits remarkable selectivity, with IC50 values of 0.22 μM against TRPML1 and 3.8 μM against TRPML2, while showing no activity towards TRPML3. EDME disrupts cytoplasmic microtubule networks in mammalian cells with an EC50 of 9 μM. This compound operates independently of estrogen receptors to block autophagy, inhibit TFEB nuclear translocation, and reduce migration and invasion in triple-negative breast cancer cells, making it highly relevant for research in cancer biology.

Cat. No.

A68760

CAS No.

848127-67-3

Phenylcapsaicin

Phenylcapsaicin is a TRPV1 receptor activator known for its role in enhancing fat oxidation during aerobic exercise. This compound serves as an analogue of capsaicin, demonstrating similar biological activity. Its research applications are particularly relevant in studies focused on metabolic processes and pain modulation, providing insights into the physiological effects of TRPV1 activation.

Cat. No.

A68761

CAS No.

2673-72-5

D-erythro-Sphingosine hydrochloride

Synonyms: Erythrosphingosine hydrochloride; erythro-C18-Sphingosine hydrochloride; trans-4-Sphingenine hydrochloride

D-erythro-Sphingosine hydrochloride is a specific activator of the TRPM3 ion channel. This compound has been shown to induce dephosphorylation of the retinoblastoma protein, which can play a significant role in cell cycle regulation. D-erythro-Sphingosine hydrochloride is utilized in research focused on exploring TRPM3-related pathways and cellular processes.

Cat. No.

A68762

CAS No.

1881277-33-3

Resolvin D2-d5

Synonyms: RvD2-d5

Resolvin D2-d5 is a deuterium-labeled derivative of Resolvin D2, a metabolite of docosahexaenoic acid (DHA). This compound exhibits significant anti-inflammatory and anti-infective properties, primarily by regulating leukocyte activity and modulating responses to microbial sepsis. Additionally, Resolvin D2 serves as a potent inhibitor of TRPV1 and TRPA1 channels in primary sensory neurons, with IC50 values of 0.1 nM and 2 nM, respectively. It is valuable for research applications focusing on inflammatory responses and pain pathways.

Cat. No.

A68763

CAS No.

808756-71-0

ABT-102

ABT-102 is a potent and highly selective antagonist of the Transient Receptor Potential Vanilloid 1 (TRPV1) channel. This compound effectively elevates heat pain thresholds and diminishes the perception of pain in response to suprathreshold heat stimuli. ABT-102 has demonstrated efficacy in reducing nociceptive responses in various animal models, including those simulating inflammatory pain, bone cancer pain, postoperative pain, and osteoarthritis.

Cat. No.

A68764

CAS No.

1374760-95-8

FEMA 4809

FEMA 4809 is a potent agonist of the TRPM8 receptor, with an EC50 of 0.2 nM. This compound is known for its ability to induce a cooling sensation through the activation of the TRPM8 ion channel, which is crucial for thermosensation. It is primarily utilized in research exploring thermal perception and related sensory pathways.

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.

A68770

CAS No.

510-22-5

Voacangine

Voacangine is a selective antagonist of the TRPM8 channel, competitively inhibiting the binding of menthol (IC50=9 μM) and noncompetitively inhibiting icilin (IC50=7 μM). It is known to block capsaicin binding to TRPV1 (IC50=50 μM) while exhibiting agonistic effects on TRPA1 (EC50=8 μM). Voacangine effectively antagonizes chemical agonist-induced activation of TRPM8, with no impact on cold-induced activation, making it a valuable tool for studying sensory signaling pathways. This alkaloid is derived from the root bark of Voacanga africana, providing a natural source for research applications.

Cat. No.

A68771

CAS No.

206350-79-0

L-R4W2

L-R4W2 is a potent antagonist of the vanilloid receptor 1 (VR1, TRPV1), exhibiting an IC50 of 0.1 μM. This compound demonstrates significant analgesic properties, making it a valuable tool in pain management research. L-R4W2 can be utilized to explore mechanisms of pain signaling and the therapeutic potential for treating pain-related disorders.

Cat. No.

A68772

CAS No.

1931116-86-7

Vocacapsaicin

Synonyms: CA-008

Vocacapsaicin is a first-in-class proagent of Capsaicin that targets the TRPV1 receptor as an agonist. This compound is known for its significant and enduring analgesic properties, making it a valuable tool in pain research. It is applicable in studies exploring non-opioid pain relief mechanisms and the modulation of sensory pathways.

Cat. No.

A68773

CAS No.

205687-03-2

Dihydrocapsiate

Dihydrocapsiate is an orally active TRPV1 agonist derived from the capsinoid family. This compound stimulates the TRPV1 receptor, playing a significant role in thermogenesis and energy metabolism. Dihydrocapsiate is valuable for research applications related to metabolic diseases, providing insights into obesity, energy expenditure, and related disorders.

Cat. No.

A68774

CAS No.

1931116-92-5

Vocacapsaicin hydrochloride

Synonyms: CA-008 hydrochloride

Vocacapsaicin hydrochloride is a potent TRPV1 agonist and a proagent of Capsaicin. This compound is primarily utilized in pain research, demonstrating significant and prolonged analgesic effects. Its unique mechanism offers valuable insights into non-opioid pain relief pathways, making it an important reagent for studies focused on pain modulation and sensory signaling.

Cat. No.

A68775

CAS No.

3083086-77-2

TRPA1 agonist-3

TRPA1 Agonist-3 is a selective agonist for the TRPA1 ion channel, displaying EC50 values of 50.05 μM for human TRPA1 and 314.04 μM for mouse TRPA1. This compound does not activate other transient receptor potential channels, including hTRPV1 and hTRPM8. TRPA1 Agonist-3 has demonstrated efficacy in alleviating inflammatory pain in mouse models, operating through a channel desensitization mechanism, making it a valuable tool for studying pain pathways and TRPA1-related pharmacology.

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.

A68778

CAS No.

1026876-55-0

AMG 7905

AMG 7905 is a selective antagonist of the transient receptor potential vanilloid type 1 (TRPV1), known for its role in mediating pain and thermoregulation. This compound effectively inhibits TRPV1 channel activation by capsaicin while enhancing channel activation by protons. AMG 7905 is employed in research focusing on pain modulation, thermogenesis inhibition, and the physiological responses to temperature changes.