TRP Channel

Cat. No.

A39368

CAS No.

2108567-79-7

(rel)-ML-SI3

Synonyms: trans-ML-SI3

(rel)-ML-SI3 is a selective inhibitor of TRPML1 and TRPML3, exhibiting IC50 values of 3.1 μM and 28.5 μM, respectively. In contrast, it acts as a potent activator of TRPML2 with an EC50 of 3.3 μM. This compound is valuable for research into the roles of TRPML channels in cellular processes and potential therapeutic interventions in related pathologies. Its specificity for multiple isoforms contributes to its utility in exploring calcium signaling pathways and lysosomal function.

Cat. No.

A44010

CAS No.

74916-57-7

Aurothiomalate disodium

Aurothiomalate disodium acts as a TRPA1 inhibitor, effectively blocking NF-κB activation and inhibiting iNOS expression. This compound fosters the M2 transformation of macrophages and enhances the expression of TREM-2 and arginase-1. Aurothiomalate disodium is applicable in research concerning liver fibrosis, cirrhosis, and arthritis, providing insights into inflammation and tissue repair mechanisms.

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.

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.

A67969

CAS No.

105431-72-9

Linopirdine

Synonyms: DuP 996

Linopirdine is a selective inhibitor of the M-type potassium current (IM; Kv7; KCNQ channels) with an IC50 of 2.4 μM. This compound exhibits potential as a cognition-enhancing agent by promoting acetylcholine release in rat brain tissue. Linopirdine is primarily utilized in research focused on understanding cognitive function and the modulation of neurotransmitter release. Additionally, its role as a TRPV1 agonist provides further avenues for investigation in neurobiology and pharmacology.

Cat. No.

A68189

CAS No.

875755-39-8

NS8593

NS8593 is a selective inhibitor of small conductance Ca2+-activated K+ channels (SK channels), specifically targeting the SK1-3 subtypes. It exhibits a reversible inhibition of SK3-mediated currents with Ca2+-dependent potency (Kd values of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca2+), while leaving intermediate and large conductance K channels unaffected. Additionally, NS8593 inhibits the TRPM7 channel with an IC50 of 1.6 mM. This compound is valuable for research into central nervous system-related diseases and the physiological roles of SK and TRPM7 channels.

Cat. No.

A68684

CAS No.

2019994-90-0

Trpvicin

Trpvicin is a selective inhibitor of the TRPV3 channel, demonstrating IC50 values of 0.41 μM and 0.22 μM for human TRPV3-WT and the hTRPV3-G573S mutant, respectively. Its mechanism of action involves stabilizing TRPV3 in a closed conformation primarily through VSLD-PD binding, while also engaging alternative binding sites in the G573S mutant to impede channel activity. Trpvicin exhibits minimal off-target effects on other TRP family members, making it a valuable tool for studying inflammation, immunology, and conditions associated with itch and hair loss in mouse models.

Cat. No.

A68686

CAS No.

2776193-88-3

TRPM3-IN-1

TRPM3-IN-1 is a potent inhibitor of the TRPM3 ion channel, exhibiting an IC50 value of less than 1 µM. This compound is valuable for research focused on the modulation of pain mechanisms and inflammatory responses. Its ability to selectively target TRPM3 makes it a promising tool for investigating related biological pathways and potential therapeutic applications.

Cat. No.

A68691

CAS No.

2418594-00-8

(1R,2R)-ML-SI3

Synonyms: (-)-trans-ML-SI3

(1R,2R)-ML-SI3 is a selective inhibitor of the TRPML1, TRPML2, and TRPML3 ion channels, with IC50 values of 1.6 μM, 2.3 μM, and 12.5 μM, respectively. This compound is valuable for investigating the physiological roles of TRPML channels in cellular signaling and ion homeostasis. It is well-suited for research applications related to lysosomal function, calcium signaling, and potential therapeutic strategies targeting lysosomal storage disorders.

Cat. No.

A68694

CAS No.

2765255-93-2

JNJ-28583113

JNJ-28583113 is a potent TRPM2 inhibitor that exhibits permeability across the blood-brain barrier. By inhibiting TRPM2, JNJ-28583113 effectively blocks the phosphorylation of GSK3α and β subunits, offering protective effects against oxidative stress-induced cell death. Additionally, it reduces cytokine release from microglia in response to pro-inflammatory stimuli, making it a valuable tool for research in neuroinflammation and oxidative stress pathways.

Cat. No.

A68700

CAS No.

2242724-49-6

TRPV2-selective blocker 1

TRPV2-selective blocker 1 is a selective inhibitor of the transient receptor potential vanilloid 2 (TRPV2) channel, exhibiting an IC50 of 6.3 μM. This compound selectively targets TRPV2 without affecting TRPV1, TRPV3, or TRPV4 channels. Its primary biological activities include blocking TRPV2-mediated Ca2+ influx in macrophages and inhibiting macrophage phagocytosis, making it a valuable tool for research on immune responses and cellular signaling pathways involving TRPV2.

Cat. No.

A68702

CAS No.

667411-04-3

TRPM4-IN-2

Synonyms: NBA

TRPM4-IN-2 is a potent inhibitor of the transient receptor potential melastatin 4 (TRPM4) channel, exhibiting an IC50 value of 0.16 µM. This compound is particularly relevant in the study of prostate and colorectal cancers, providing valuable insights into TRPM4's role in tumor biology and potential therapeutic pathways. Its ability to modulate TRPM4 activity makes it a useful tool in cancer research and drug development.

Cat. No.

A68705

CAS No.

810668-37-2

Resolvin D2

Synonyms: RvD2

Resolvin D2 is a potent TRPV1 and TRPA1 inhibitor with a primary mechanism targeting these transient receptor potential channels in primary sensory neurons. As a metabolite of docosahexaenoic acid (DHA), it exhibits significant anti-inflammatory and anti-infective properties, effectively regulating leukocyte function and controlling microbial sepsis. This compound's high potency and specificity make it a valuable tool in research focused on pain modulation and inflammatory responses.

Cat. No.

A68706

CAS No.

351424-20-9

TRPM4-IN-1

Synonyms: CBA

TRPM4-IN-1 is a selective inhibitor of the TRPM4 ion channel, exhibiting an IC50 value of 1.5 μM. This compound is primarily utilized in studies related to cardiac diseases and prostate cancer, facilitating insights into the role of TRPM4 in these conditions. Its potency makes it a valuable tool for investigating the modulation of calcium signaling pathways in various biological contexts.

Cat. No.

A68714

CAS No.

55224-94-7

AP-18

AP-18 is a selective inhibitor of the transient receptor potential ankyrin 1 (TRPA1), effectively blocking TRPA1 activation by 50 µM cinnamaldehyde with IC50 values of 3.1 µM for human and 4.5 µM for mouse TRPA1. This compound demonstrates significant analgesic properties, as it reverses complete Freund's adjuvant-induced mechanical hyperalgesia in murine models. Additionally, AP-18 significantly reduces AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 µM, making it a valuable tool for research into pain mechanisms and TRPA1-related pathways.

Cat. No.

A68715

CAS No.

945604-76-2

VPC01091.4

Synonyms: VPC4

VPC01091.4 is a potent TRPM7 inhibitor that effectively blocks TRPM7 current at low micromolar concentrations. This compound is capable of crossing the blood-brain barrier, making it suitable for neurological studies. Additionally, VPC01091.4 demonstrates significant anti-inflammatory properties, halting systemic inflammation in vivo, and can be utilized in research focused on inflammation and neuronal signaling pathways.

Cat. No.

A68716

CAS No.

1432051-63-2

TRPV3 antagonist 74a

TRPV3 antagonist 74a is a selective and potent inhibitor of the transient receptor potential vanilloid 3 (TRPV3) channel. Exhibiting minimal activity against a broad range of other ion channels, this compound serves as a valuable tool for investigating the role of TRPV3 in various biological processes. Its specific antagonistic properties make TRPV3 antagonist 74a particularly useful in research focusing on neuropathic pain and related disorders.

Cat. No.

A68718

CAS No.

2741956-55-6

BAY-390

BAY-390 is a selective TRPA1 inhibitor that effectively penetrates the blood-brain barrier. It demonstrates potent inhibitory activity with IC50 values of 16 nM for human TRPA1 (hTRPA1) FLIPR, 82 nM for hTRPA1 electrophysiology (Ephys), 63 nM for rat TRPA1 (rTRPA1) FLIPR, and 35 nM for rat dorsal root ganglion (DRG) Ephys. BAY-390 is suitable for investigating the role of TRPA1 in inflammation-related research.

Cat. No.

A68719

CAS No.

2376824-99-4

Nedizantrep

Synonyms: GDC-6599

Nedizantrep is a potent inhibitor of the transient receptor potential ankyrin 1 (TRPA1) channel, demonstrating IC50 values of 5.3 nM in humans and varying efficacy across different species. This compound is utilized in research focused on neuropathic pain and respiratory conditions, including asthma and chronic cough. Its selective action on TRPA1 underscores its potential as a valuable tool for advancing studies aimed at understanding and treating these conditions.

Cat. No.

A68721

CAS No.

2311863-36-0

Apecotrep

Synonyms: TRPC6-IN-3

Apecotrep is a potent inhibitor of the transient receptor potential C6 (TRPC6) ion channel. This orally active compound effectively modulates intracellular calcium levels and influences membrane potential by regulating the flux of calcium and sodium ions. Apecotrep is particularly relevant for research involving the respiratory system, providing insights into the role of TRPC6 in various biological processes.

Cat. No.

A68724

CAS No.

864716-85-8

Mesendogen

Mesendogen is a selective TRPM6 inhibitor that plays a crucial role in the regulation of magnesium homeostasis. It enhances the differentiation of human embryonic stem cells (hESCs) and human induced pluripotent stem cells (hiPSCs) into mesodermal and definitive endoderm lineages. This compound is valuable for research focused on early embryonic development and the role of magnesium in cellular processes.

Cat. No.

A68731

CAS No.

2070015-10-8

ML204 hydrochloride

ML204 hydrochloride is a selective inhibitor of the TRPC4 and TRPC5 channels, demonstrating a minimum of 19-fold selectivity over the TRPC6 channel. It has no significant effects on other transient receptor potential (TRP) channels or on voltage-gated sodium, potassium, or calcium channels. This compound is valuable for research applications exploring cellular calcium signaling and the physiological roles of TRPC4 and TRPC5 in various biological processes.

Cat. No.

A68733

CAS No.

2304549-73-1

GFB-8438

GFB-8438 is a highly selective inhibitor of the transient receptor potential channel TRPC5, exhibiting IC50 values of 0.18 μM for hTRPC5 and 0.29 μM for hTRPC4. This compound demonstrates significant selectivity over TRPC6, other TRP family members, NaV 1.5, and shows minimal activity against the hERG channel. GFB-8438 has been shown to provide protective effects to mouse podocytes from injury induced by protamine sulfate, highlighting its potential for research in renal protection and related pathways.

Cat. No.

A68735

CAS No.

2763378-71-6

JW-65

JW-65 is a selective inhibitor of the TRPC3 channel, targeting its role in various cellular processes. This compound exhibits significant biological activity that can be leveraged in studies of neurological and cardiovascular diseases. JW-65 is useful for investigating the mechanisms of TRPC3 in pathophysiological conditions and may provide insights into potential therapeutic applications.

Cat. No.

A68736

CAS No.

528583-91-7

17(R)-Resolvin D1

Synonyms: 17(R)-RvD1; AT-RvD1

17(R)-Resolvin D1 is a TRPV3 inhibitor known for its potent anti-inflammatory properties. This aspirin-triggered epimer of Resolvin D1 exhibits significant biological activity by specifically inhibiting TRPV3 with an IC50 of 398 nM. It has demonstrated peripheral anti-nociceptive efficacy, making it a valuable tool for research applications focused on inflammation and pain management.