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Pathways Recommended: Membrane Transporter/Ion Channel
Results for "

TRPC channels

" in MedChemExpress (MCE) Product Catalog:

34

Inhibitors & Agonists

2

Peptides

5

Natural
Products

1

Isotope-Labeled Compounds

1

Click Chemistry

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-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
    PPZ2

    		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-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-136190
    TRPC6-PAM-C20

    		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-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-132813
    Evifacotrep

    		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-125942
    SKF-96365

    		CRAC Channel TRP Channel Na+/Ca2+ Exchanger Calcium Channel CaMK Akt Apoptosis Autophagy Neurological Disease Cancer
    SKF-96365 is a blocker of calcium store-operated calcium influx (SOCE) and transient receptor potential channels (TRPC). SKF-96365 reduces the increase in intracellular calcium concentration by blocking TRPC channels and SOCE. SKF-96365 enhances the reverse operation of Na⁺/Ca²⁺ exchanger (NCX) (Ca²⁺ influx) in glioblastoma, leading to intracellular calcium overload and cytotoxicity. SKF-96365 inhibits the CaMKIIγ/AKT pathway and simultaneously induces apoptosis and cell protective autophagy in colorectal cancer cells. SKF-96365 can be used in calcium signaling and cancer research .
    SKF-96365
  • HY-W707161
    4-Methyl-2-(1-piperidinyl)-quinoline-d10

    		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
    OptoDArG

    		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
    TRPC4/5-IN-3

    		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-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-121519
    GSK2332255B

    		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-146155
    TRPC4/5-IN-1

    		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-147357
    TRPC3/6-IN-1

    		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-162090
    TRPC antagonist 1

    		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
    M084 hydrochloride

    		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-148129
    Apecotrep

    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-W641445
    ELP-004

    		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-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-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-133168R
    Englerin A (Standard)

    		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-116330A
    Hyperforin dicyclohexylammonium salt
    2 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-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-133012
    GFB-8438

    		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-30234
    Clemizole

    		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-116330
    Hyperforin

    		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-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-116330AR
    Hyperforin dicyclohexylammonium salt (Standard)

    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-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-B0700
    Rosiglitazone sodium

    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-14600
    Rosiglitazone maleate
    Maximum Cited Publications
    143 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-136205
    IA-Alkyne
    2 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-14600R
    Rosiglitazone maleate (Standard)

    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)

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