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Pathways Recommended: Membrane Transporter/Ion Channel
Results for "

TRPC channel

" in MedChemExpress (MCE) Product Catalog:

40

Inhibitors & Agonists

2

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5

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1

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100001
    SKF-96365 (hydrochloride)
    25+ Cited Publications

    TRP Channel CRAC Channel Autophagy CaMK Akt Apoptosis Na+/Ca2+ Exchanger Calcium Channel Neurological Disease Inflammation/Immunology Cancer
    SKF-96365 hydrochloride is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 hydrochloride reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 hydrochloride inhibits voltage-gated sodium current (cardiac INa/NaV1.5) and slows myocardial conduction. SKF-96365 hydrochloride inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 hydrochloride induces G2/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 hydrochloride alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 hydrochloride reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 hydrochloride inhibits the growth of colorectal cancer xenografts in nude mice . SKF-96365 hydrochloride is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia .
    SKF-96365 (hydrochloride)
  • HY-133168
    Englerin A
    1 Publications Verification

    TRP Channel Cancer
    Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+ influx and Ca 2+ cell overload .
    Englerin A
  • HY-116330A
    Hyperforin dicyclohexylammonium salt
    3 Publications Verification

    Hyperforin DCHA

    TRP Channel Calcium Channel Neurological Disease Cancer
    Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
    Hyperforin dicyclohexylammonium salt
  • HY-14600
    Rosiglitazone maleate
    Maximum Cited Publications
    175 Publications Verification

    BRL 49653C

    PPAR TRP Channel Autophagy Ferroptosis Metabolic Disease Inflammation/Immunology Cancer
    Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
    Rosiglitazone maleate
  • HY-101507
    Zerencotrep
    10+ Cited Publications

    Pico145; HC-608

    TRP Channel Cancer
    Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (-)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8 .
    Zerencotrep
  • HY-136205
    IA-Alkyne
    4 Publications Verification

    Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide

    TRP Channel Infection Inflammation/Immunology
    IA-Alkyne (Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide) is a TRP channel (TRPC) agonist and has the potential for the study of respiratory infection . IA-Alkyne can be used to develop an isotopically tagged probe for quantitative cysteine-reactivity profiling . IA-Alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    IA-Alkyne
  • HY-12949
    ML204
    5+ Cited Publications

    TRP Channel Neurological Disease
    ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels .
    ML204
  • HY-108465
    Pyr3
    5+ Cited Publications

    TRP Channel Others
    Pyr3 is a selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC50 of 700 nM for TRPC3-mediated Ca 2+ influx.
    Pyr3
  • HY-30234A
    Clemizole hydrochloride
    1 Publications Verification

    Histamine Receptor TRP Channel HCV Protease HCV Inflammation/Immunology Endocrinology Cancer
    Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. Clemizole hydrochloride is an inhibitor of TRPC5 channel. The IC50 of Clemizole hydrochloride for RNA binding by NS4B is 24 nM, whereas its EC50 for viral replication is 8 μM.
    Clemizole hydrochloride
  • HY-P2141
    TRV-120027
    3 Publications Verification

    TRV027

    Angiotensin Receptor Arrestin Cardiovascular Disease
    TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages β-arrestins while blocking G-protein signaling . TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R-β-arrestin-1-TRPC3-PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II-mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment .
    TRV-120027
  • HY-19408
    Pyr10
    3 Publications Verification

    TRP Channel Others
    Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca 2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca 2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels .
    Pyr10
  • HY-W641445

    TRP Channel Inflammation/Immunology
    ELP-004 is a TRPC channel inhibitor and inhibtis TRPC channel-mediated Ca 2+ entry. ELP-004 is an osteoclast inhibitor and inhibits osteoclast differentiation. ELP-004 inhibits basal Ca 2+ and related NFATc1 translocation in inflammatory osteoclastogenesis. ELP-004 reduces bone erosion in a mouse model of rheumatoid arthritis .
    ELP-004
  • HY-133012

    TRP Channel Neurological Disease
    GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model .
    GFB-8438
  • HY-116330

    Calcium Channel TRP Channel Neurological Disease Inflammation/Immunology
    Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels and triggers adipose tissue thermogenesis via the Dlat-AMPK signaling axis to suppress obesity. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
    Hyperforin
  • HY-138668

    TRP Channel Neurological Disease
    JW-65 is a selective TRPC3 channel inhibitor with favorable blood-brain barrier penetration. JW-65 directly binds to human TRPC3 protein and modulates calcium signaling to reduce seizure susceptibility. JW-65 reduces seizure incidence, severity, and duration while prolonging seizure latency in multiple seizure models. JW-65 alleviates Aβ‑induced neuronal damage. JW-65 serves as a valuable tool for research on epilepsy, seizure disorders, and Alzheimer’s disease .
    JW-65
  • HY-132813

    TRP Channel Neurological Disease
    Evifacotrep, a short transient receptor potential channel 5 and 4 (TRPC5/TRPC4) antagonist (WO2020061162, compound 100), can be used for the research of neurological diseases. Evifacotrep targets to TRPC5/TRPC4 with IC50s ≤50 nM .
    Evifacotrep
  • HY-148129

    TRPC6-IN-3

    TRP Channel Cardiovascular Disease
    Apecotrep (TRPC6-IN-3) (compound 17) is a potent, orally active transient receptor potential C6 ion channel (TRPC6) inhibitor. Apecotrep modulates not only intracellular calcium concentration, but also membrane potential by modulating the flux of cations including calcium and sodium ions. Apecotrep can be used in research of respiratory system .
    Apecotrep
  • HY-30234
    Clemizole
    1 Publications Verification

    Histamine Receptor TRP Channel HCV Protease HCV Inflammation/Immunology Endocrinology Cancer
    Clemizole is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. Clemizole is an inhibitor of TRPC5 channel. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM.
    Clemizole
  • HY-131648
    1-Oleoyl-2-acetyl-sn-glycerol
    1 Publications Verification

    Drug Derivative PKC TRP Channel Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
    1-Oleoyl-2-acetyl-sn-glycerol is a cell-permeable analog of diacylglycerol (DAG) and can activate Protein kinase C (PKC). 1-Oleoyl-2-acetyl-sn-glycerol can activate the TRPC channels-mediated specific Ca 2+ influx. 1-Oleoyl-2-acetyl-sn-glycerol can stimulate superoxide-generation from human neutrophils. 1-Oleoyl-2-acetyl-sn-glycerol stimulates the formation of phosphatidylinositol 4-phosphate in intact human platelets. 1-Oleoyl-2-acetyl-sn-glycerol can stimulate ascites tumor cell proliferation .
    1-Oleoyl-2-acetyl-sn-glycerol
  • HY-136190

    TRP Channel Neurological Disease
    TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) of TRPC6 channels. TRPC6-PAM-C20 is a potent enhancer of channel activation, enabling low basal concentrations of DAG to induce activation of the ion channel. TRPC6-PAM-C20 induces increases in intracellular Ca 2+ concentrations ([Ca 2+]i) in TRPC6-expressing HEK293 cells with an EC50 of 2.37 μM. TRPC6-PAM-C20 can be used as a valuable tool to selectively exaggerate TRPC6-dependent signals .
    TRPC6-PAM-C20
  • HY-125942
    SKF-96365
    25+ Cited Publications

    CRAC Channel TRP Channel CaMK Akt Apoptosis Autophagy Na+/Ca2+ Exchanger Calcium Channel Neurological Disease Inflammation/Immunology Cancer
    SKF-96365 is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 inhibits voltage-gated sodium current (cardiac INa/NaV1.5) and slows myocardial conduction. SKF-96365 inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 induces G2/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 inhibits the growth of colorectal cancer xenografts in nude mice . SKF-96365 is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia .
    SKF-96365
  • HY-12949A
    ML204 hydrochloride
    5+ Cited Publications

    TRP Channel Neurological Disease
    ML204 hydrochloride is a novel, potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels .
    ML204 hydrochloride
  • HY-111527

    Calcium Channel Neurological Disease
    PPZ2 is a diacylglycerol (DAG)-activated TRPC3/TRPC6/TRPC7 channel activator with activity in promoting neuronal development and survival. PPZ2 activates recombinant TRPC3/TRPC6/TRPC7 channels in a dose-dependent manner without affecting other TRPC channels. PPZ2 elicits cation currents and calcium ion (Ca(2+)) influx in cultured central neurons. PPZ2 is able to induce BDNF-like neurite outgrowth and neuroprotection, an effect that disappears after TRPC3/TRPC6/TRPC7 knockdown or inhibition. PPZ2 also increases the activation of the calcium-dependent transcription factor cAMP response element binding protein. The effects of PPZ2 suggest that calcium signaling mediated by activation of DAG-activated TRPC channels plays an important role in its neurotrophic effects .
    PPZ2
  • HY-101547
    TRPC6-IN-1
    1 Publications Verification

    TRP Channel Cancer
    TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM.
    TRPC6-IN-1
  • HY-P2141A
    TRV-120027 TFA
    3 Publications Verification

    Angiotensin Receptor Arrestin Cardiovascular Disease
    TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ?-arrestins while blocking G-protein signaling . TRV120027?TFA induces?acute?catecholamine?secretion?through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the?acute decompensated heart failure (ADHF) treatment .
    TRV-120027 TFA
  • HY-121519

    TRP Channel Cardiovascular Disease
    GSK2332255B is a potent, selective TRPC3 and TRPC6 antagonist with IC50s of 5 nM and 4 nM for rat TRPC3 and rat TRPC6. GSK2332255B shows ≥100-fold selectivity for TRPC3/6 over other calcium-permeable channels .
    GSK2332255B
  • HY-147357

    TRP Channel Cardiovascular Disease
    TRPC3/6-IN-1 is a potent selectivity blocker of the canonical transient receptor channels (TRPC3/6), has block potency for hTRPC3 and hTRPC6 with IC50 values of 1260 nM and 500 nM, respectively. TRPC3/6-IN-1 can be used for the research of chronic models of heart failure .
    TRPC3/6-IN-1
  • HY-133168R

    Reference Standards TRP Channel Cancer
    Englerin A (Standard) is the analytical standard of Englerin A. This product is intended for research and analytical applications. Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca2+ influx and Ca2+ cell overload .
    Englerin A (Standard)
  • HY-W707161

    Isotope-Labeled Compounds TRP Channel Neurological Disease
    4-Methyl-2-(1-piperidinyl)-quinoline-d10 is the deuterium labeled ML204 (HY-12949). ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca2+ channels .
    4-Methyl-2-(1-piperidinyl)-quinoline-d10
  • HY-126424

    Fluorescent Dye Others
    OptoDArG is a photoswitchable probe that has the activity to recognize lipid-gated pores by controlling TRPC3 channels and can be used as a tool to study the lipid sensing mechanism of TRPC channels.
    OptoDArG
  • HY-173024

    TRP Channel Neurological Disease
    TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87% .
    TRPC4/5-IN-3
  • HY-146155

    TRP Channel Metabolic Disease Inflammation/Immunology
    TRPC4/5-IN-1 is a potent TRP channel 4/5 (TRPC4/5) inhibitor with IC50s of 2.06 μM and 0.54 μM, respectively. TRPC4/5-IN-1 can be used for proteinuric kidney diseases and skin inflammatory diseases research .
    TRPC4/5-IN-1
  • HY-162090

    TRP Channel Cancer
    TRPC antagonist 1 (compound 15g) is a potent TRP channel (TRPC) antagonist with IC50s of 2.4 μM, 12.2 μM, 7.6 μM, 2.9 μM, and 3.4 μM for TRPC3, TRPC4, TRPC5, TPRC6, and TRPC7, respectively. TRPC antagonist 1 displays noteworthy anti-glioblastoma efficacy in vitro against U87 cell lines .
    TRPC antagonist 1
  • HY-110379

    TRP Channel Neurological Disease
    M084 hydrochloride is a TRPC4/5 channel blocker, with IC50 values of 10.3 μM and 8.2 μM, respectively. M084 hydrochloride has antidepressant and anxiolytic effects .
    M084 hydrochloride
  • HY-116330AR

    Hyperforin DCHA (Standard)

    Reference Standards TRP Channel Calcium Channel Neurological Disease
    Hyperforin dicyclohexylammonium salt (Standard) is the analytical standard of Hyperforin dicyclohexylammonium salt. This product is intended for research and analytical applications. Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
    Hyperforin dicyclohexylammonium salt (Standard)
  • HY-B0700

    BRL 49653 sodium

    PPAR TRP Channel Autophagy Metabolic Disease Inflammation/Immunology
    Rosiglitazone sodium is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone sodium is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
    Rosiglitazone sodium
  • HY-14600R

    BRL 49653C (Standard)

    Reference Standards PPAR TRP Channel Autophagy Ferroptosis Metabolic Disease Inflammation/Immunology Cancer
    Rosiglitazone (maleate) (Standard) is the analytical standard of Rosiglitazone (maleate). This product is intended for research and analytical applications. Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
    Rosiglitazone maleate (Standard)
  • HY-101507R

    Pico145 (Standard); HC-608 (Standard)

    TRP Channel Reference Standards Cancer
    Zerencotrep (Standard) is the analytical standard of Zerencotrep (HY-101507). This product is intended for research and analytical applications. Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (-)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8 .
    Zerencotrep (Standard)
  • HY-179489

    TRP Channel Others
    TRPC3 agonist-1 (compound 4n) is a selective and competitive TRPC3 channel agonist. TRPC3 agonist-1 binds at L2 site of hTRPC3 .
    TRPC3 agonist-1
  • HY-108465R

    Reference Standards TRP Channel Others
    Pyr3 (Standard) is the analytical standard of Pyr3 (HY-108465). This product is intended for research and analytical applications. Pyr3 is a selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC50 of 700 nM for TRPC3-mediated Ca2+ influx.
    Pyr3 (Standard)

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