TRP Channel

Cat. No.

A46206

CAS No.

120298-73-9

pTH-Related Protein (1-40) (human, mouse, rat)

pTH-Related Protein (1-40) is an activator of the parathyroid hormone receptor (PTHR) and protein kinase C isoforms α and β. This peptide enhances calcium uptake in rat intestinal cells by stimulating the PTHR1 receptor, leading to the upregulation of critical calcium transport proteins, including TRPV6, CaBP-D9k, NCX1, and PMCA1. Its biological activity makes it a valuable tool for research focused on calcium signaling and endocrine regulation in both human and animal models.

Cat. No.

A46307

CAS No.

1848224-71-4

Tivanisiran

Synonyms: SYL1001

Tivanisiran is a small interfering RNA (siRNA) targeting the transient receptor potential vanilloid 1 (TRPV1) mRNA. It is primarily used in research focused on dry eye disease, facilitating the study of TRPV1's role in ocular inflammatory responses. By silencing TRPV1 expression, Tivanisiran enables the investigation of therapeutic strategies aimed at alleviating symptoms associated with dry eye disorders.

Cat. No.

A47892

CAS No.

23795-03-1

Probenecid sodium

Probenecid sodium is the sodium salt form of Probenecid, functioning as a selective agonist for the transient receptor potential vanilloid 2 (TRPV2) channel. This compound has been shown to activate TRPV2, contributing to various physiological responses. Additionally, Probenecid sodium inhibits the pannexin 1 channel, making it valuable for studying cellular communication and inflammation processes. Its utility in research extends to investigating the role of TRPV2 in pain sensation and other biological pathways.

Cat. No.

A48618

CAS No.

1189657-87-1

Probenecid-d14

Probenecid-d14 is a deuterated form of Probenecid, which serves as a selective agonist of the transient receptor potential vanilloid 2 (TRPV2) channels. This stable isotope enables precise tracking and quantification in metabolic studies. Additionally, Probenecid-d14 is recognized for its inhibitory effects on pannexin 1 channels, making it a valuable tool for investigating cellular signaling pathways and receptor interactions in various biological research applications.

Cat. No.

A50556

CAS No.

2119598-24-0

BRD-4592

BRD-4592 is an allosteric inhibitor of Mycobacterium tuberculosis tryptophan synthase (TrpAB), specifically targeting the α-β-subunit interface. It demonstrates potent inhibitory activity, with an IC50 of 70.9 nM for the α-subunit and 22.6 nM for the β-subunit. This compound is valuable for research applications aimed at elucidating the role of tryptophan metabolism in tuberculosis and exploring novel therapeutic strategies against Mycobacterium tuberculosis.

Cat. No.

A50640

CAS No.

27536-56-7

4α-Phorbol 12,13-didecanoate

Synonyms: 4αPDD

4α-Phorbol 12,13-didecanoate is a potent agonist of the transient receptor potential vanilloid 4 (TRPV4). It facilitates calcium ion influx and induces ATP release, thereby serving a role as an osmoreceptor. In animal studies, 4α-Phorbol 12,13-didecanoate has been shown to inhibit water intake and elevate maximal micturition pressure in rats. This compound is valuable for research into inflammation, infection, and the biological mechanisms underlying conditions such as chikungunya virus (CHIKV).

Cat. No.

A50686

CAS No.

332382-54-4

ML-SA1

ML-SA1 is a selective agonist of TRPML channels, promoting lysosomal acidification and enhancing protease activity, which leads to the inhibition of Dengue virus 2 (DENV2) and Zika virus (ZIKV). The compound exhibits IC50 values of 8.3 μM for DENV2 RNA and 52.99 μM for ZIKV RNA. Additionally, ML-SA1 stimulates autophagy, making it a valuable tool for research into broad-spectrum antiviral strategies.

Cat. No.

A52217

CAS No.

891016-02-7

ML-SI3

Synonyms: ML-SI3 (cis/trans mix)

ML-SI3 is a modulator targeting TRPML1 and TRPML2 channels, exhibiting inhibitory activity with IC50 values of 4.7 μM and 1.7 μM, respectively. This compound effectively inhibits lysosomal calcium efflux and impairs TRPML1-mediated autophagy pathways. Additionally, the components of ML-SI3 serve as activators for TRPML2, with EC50 values of 3.3 μM and 9.4 μM, making it a valuable tool for studying TRPML channel dynamics and their roles in cellular processes.

Cat. No.

A53640

CAS No.

2082631-84-1

Ricorfotide vedotin

Synonyms: CBP-1008; LDC 10B

Ricorfotide vedotin is a dual-ligand peptide-drug conjugate that primarily targets Folate receptor α (FRα) while also binding to TRPV6. It exhibits high-affinity binding to FRα and low-affinity interaction with TRPV6, demonstrating notable antitumor activity. This reagent is applicable in advanced solid tumor research, including studies focused on colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma, and follicular dendritic cell sarcoma.

Cat. No.

A58196

CAS No.

136-69-6

Protokylol hydrochloride

Synonyms: Caytine hydrochloride; JB-251 hydrochloride

Protokylol hydrochloride serves as a potent agonist of the β2-adrenergic receptor. This compound demonstrates significant bronchodilator activity, making it valuable in research related to respiratory function and pulmonary pharmacology. Additionally, it interacts with the TRPV1 receptor, further expanding its potential applications in studying pain pathways and sensory responses.

Cat. No.

A58520

CAS No.

136-70-9

Protokylol

Synonyms: Caytine; JB-251

Protokylol is a TRPV1 agonist that exerts its biological activity through the activation of transient receptor potential vanilloid 1 channels. Its primary application includes functioning as a bronchodilator, which supports airway relaxation and dilation. Research utilizing Protokylol can facilitate investigations into pain modulation, sensory signaling, and respiratory physiology.

Cat. No.

A59188

CAS No.

199875-69-9

N-Arachidonyldopamine

N-Arachidonyldopamine is a selective agonist of the CB1 and TRPV1 receptors, exhibiting a Ki value of 250 nM for the CB1 receptor and an EC50 of approximately 50 nM for TRPV1. This compound plays a significant role in modulating pain and inflammatory responses, making it a valuable tool for research investigating endocannabinoid signaling pathways and their implications in various physiological processes.

Cat. No.

A59193

CAS No.

157182-49-5

(R)-Methanandamide

Synonyms: AM-356

(R)-Methanandamide is a potent CB1 receptor agonist, exhibiting a Ki value of 20 nM. This compound serves as an analytical tool for studying cannabinoid signaling pathways and the endocannabinoid system. Additionally, (R)-Methanandamide can activate vanilloid (TRPV1) receptors, highlighting its potential applications in pain research and modulation of inflammatory processes in cellular assays.

Cat. No.

A59235

CAS No.

616884-67-4

OMDM-6

OMDM-6 is a hybrid agonist targeting vanilloid receptor type 1 (VR1, TRPV1) with an EC50 of 75 nM and cannabinoid receptor type 1 (CB1) with a Ki of 3.2 μM. This compound also inhibits the cellular uptake of anandamide, demonstrating a Ki of 7.0 μM. Due to its dual mechanism of action, OMDM-6 is valuable for research applications exploring pain modulation and the endocannabinoid system.

Cat. No.

A59259

CAS No.

2772693-05-5

CB2 receptor antagonist 1

CB2 receptor antagonist 1 is a selective competitive antagonist of the cannabinoid receptor CB2, exhibiting strong potency. This hexyl resorcinol derivative not only effectively inhibits CB2 receptor activity but also demonstrates significant antinociceptive properties. Additionally, it has been observed to activate both cannabinoid and TRPV1 receptors, making it a valuable tool for research in pain modulation and cannabinoid signaling pathways.

Cat. No.

A59317

CAS No.

2772949-38-7

CB1/2 agonist 4

CB1/2 agonist 4 serves as a full agonist for the CB1 receptor and a partial agonist for the CB2 receptor, exhibiting EC50 values of 15.09 nM and 1.16 nM, respectively. It demonstrates high affinity for human CB1 and CB2 receptors, with Ki values of 1.1 nM and 4.2 nM. This compound displays notable antinociceptive activity and effectively activates both cannabinoid and TRPV1 receptors, featuring IC50 and EC50 values of 0.8 μM and 0.12 μM, respectively. CB1/2 agonist 4 is valuable for studies exploring cannabinoid receptor functions and their implications in pain modulation.

Cat. No.

A59352

CAS No.

316139-50-1

PQM-244

PQM-244 is a multi-target modulator that primarily interacts with TRPV1 and cannabinoid receptors CB1 and CB2. It exhibits noteworthy peripheral antinociceptive properties, effectively addressing both neurogenic and inflammatory pain. Additionally, PQM-244 demonstrates antioxidant activity with an IC50 of 14.15 µM for radical scavenging of DPPH. This compound is suitable for research applications related to chronic pain and inflammatory conditions, including diabetes, atherosclerosis, and Alzheimer's disease.

Cat. No.

A59617

CAS No.

185145-34-0

Chrysin 6-C-glucoside 8-C-arabinoside

Chrysin 6-C-glucoside 8-C-arabinoside is a potent inhibitor of calcitonin gene-related peptide (CGRP) release and the TRPV1 channel activation. This compound exhibits significant biological activity relevant to nociceptive signaling pathways, making it a valuable tool for anti-migraine research. Its mechanism of action offers insights into potential therapeutic strategies for migraine and related pain disorders.

Cat. No.

A59923

CAS No.

136181-87-8

N-Palmitoyl dopamine

Synonyms: PALDA

N-Palmitoyl dopamine is a long-chain fatty acid dopamide that interacts with endovaniloids, exhibiting 'entourage' effects on N-arachidonoyl-dopamine (NADA) and anandamide. This compound is not active on the TRPV1 receptor, highlighting its selective profile. N-Palmitoyl dopamine is valuable for research applications focused on cannabinoid and pain signaling pathways, particularly in studies examining the interplay between fatty acid derivatives and endocannabinoid activity.

Cat. No.

A61648

CAS No.

4049-38-1

(±)-Eriodictyol ((±)-Huazhongilexone, Dihydroluteolin)

Synonyms: (±)-Huazhongilexone; Dihydroluteolin

(±)-Eriodictyol is a potent TRPV1 receptor antagonist, exhibiting an IC50 value of 44-47 nM in rTRPV1 assays. This compound demonstrates significant antioxidant and anti-inflammatory properties, effectively inhibiting lipid peroxidation and reducing the release of proinflammatory cytokines. By modulating the Nrf2 signaling pathway, (±)-Eriodictyol helps maintain the integrity of the blood-retinal barrier and can alleviate oxidative stress-induced apoptosis and hyperalgesia. It has potential applications in the research of diabetic retinopathy, acute lung injury, and various pain-related conditions, while also enhancing immune cell activity and promoting antioxidant enzyme levels.

Cat. No.

A62324

CAS No.

122517-78-6

Naltriben mesylate

Naltriben mesylate is a potent antagonist of the δ2-opioid receptor and an activator of TRPM7 channels. It demonstrates high affinity, with Ki values of 0.013 nM for the δ receptor, alongside 19 nM and 152 nM for μ and κ receptors, respectively. Research indicates that Naltriben mesylate enhances glioblastoma cell migration and invasion, making it a valuable tool for studies related to neurological diseases and cancer biology.

Cat. No.

A62558

CAS No.

3084843-71-7

TRPV1 antagonist 11

TRPV1 Antagonist 11 is a potent antagonist of the TRPV1 receptor, exhibiting an IC50 of 29.3 nM. Additionally, it serves as a μ-opioid receptor (MOR) agonist with a Ki value of 60.3 nM. This compound demonstrates significant analgesic properties by antagonizing TRPV1, thereby reducing pain signaling, and activating MOR, which enhances the pain-relief effect. TRPV1 Antagonist 11 has been shown to provide a robust, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice, making it a valuable tool for pain research.

Cat. No.

A62615

CAS No.

111555-58-9

Naltriben

Naltriben is a selective antagonist of the δ2-opioid receptor and an activator of TRPM7 channels. It has been shown to enhance migration and invasion of glioblastoma cells, making it a valuable tool for studying tumor biology. This compound is suited for research into neurological disorders and cancer mechanisms, providing insights into therapeutic approaches targeting these areas.

Cat. No.

A62766

CAS No.

60786-59-6

(Thr4,Gly7)-Oxytocin

(Thr4,Gly7)-Oxytocin is a specific agonist of the oxytocin receptor (OT receptor). This analogue enhances neuronal excitability in subicular neurons through the activation of TRPV1 channels and the inhibition of K+ channels. Its unique properties make it valuable for research applications involving neurobiology and the study of oxytocin-related pathways.

Cat. No.

A65982

CAS No.

116057-57-9

Farnesyl pyrophosphate ammonium

Synonyms: Farnesyl diphosphate ammonium

Farnesyl pyrophosphate ammonium is an agonist of the TRPM2 channel, facilitating calcium influx and promoting cell death. It serves as a crucial intermediate in the mevalonate pathway, with significant roles in cholesterol and ubiquinone synthesis, as well as protein farnesylation. This compound is utilized in research focusing on cerebral ischemia, neurodegenerative diseases, pancreatic cancer, inflammation, and autoimmune disorders.