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Results for "

TREK-1

" in MedChemExpress (MCE) Product Catalog:

22

Inhibitors & Agonists

3

Peptides

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-149538
    TWIK-1/TREK-1-IN-3

    		Potassium Channel Neurological Disease
    TWIK-1/TREK-1-IN-3 (compound 2h) is an inhibitor of TWIK-related potassium channel (Potassium Channel) TREK-1. TREK-1 contains a two-pore domain potassium (K2p) channel that dimerizes into TREK-1 homodimer and TWIK-1/TREK-1 heterodimer, and is an important antidepressant target. TWIK-1/TREK-1-IN-3 targets TREK-1 homodimer and TWIK-1/TREK-1 heterodimer with IC50s of 9.74 μM and 16.5 μM, respectively, and has antidepressant-like effects [1].
    TWIK-<em>1</em>/<em>TREK-1</em>-IN-3
  • HY-134559
    TKIM

    		Potassium Channel Neurological Disease
    TKIM is a TREK-1 channel inhibitor with an IC50 of 2.96 μM. TKIM binds to the pocket of the intermediate (IM) state of TREK-1 [1].
    TKIM
  • HY-149536
    TWIK-1/TREK-1-IN-1

    		Potassium Channel Neurological Disease
    TWIK-1/TREK-1-IN-1 (compound 2a) is an inhibitor of the TWIK-related potassium channel (Potassium Channel) TREK-1. TREK-1 contains a two-pore domain potassium (K2p) channel that dimerizes into TREK-1 homodimer and TWIK-1/TREK-1 heterodimer, and is an important antidepressant target. TWIK-1/TREK-1-IN-3 targets TREK-1 homodimer and TWIK-1/TREK-1 heterodimer with IC50s of 9.36 μM and 14.6 μM, respectively, and has antidepressant-like effects [1].
    TWIK-<em>1</em>/<em>TREK-1</em>-IN-<em>1</em>
  • HY-149537
    TWIK-1/TREK-1-IN-2

    		Potassium Channel Neurological Disease
    TWIK-1/TREK-1-IN-2 (Compound 2g) is a TWIK-1/TREK-1 inhibitor. TWIK-1/TREK-1-IN-2 inhibits TREK-1 homodimer and TWIK-1/TREK-1 heterodimer with IC50s of 10.13 μM and 15.5 μM. TWIK-1/TREK-1-IN-2 is an antidepressant [1].
    TWIK-<em>1</em>/<em>TREK-1</em>-IN-2
  • HY-P3581
    PE 22-28

    		Potassium Channel Neurological Disease
    PE 22-28 is a TREK-1 inhibitor with IC50 value of 0.12 nM. PE 22-28 also is a 7 amino-acid peptide that is used as a core sequence for preparing analogs by chemical modifications and also by substitution of amino-acids. PE 22-28 can be used for the research of depression [1].
    PE 22-28
  • HY-P1422
    Spadin

    		Potassium Channel 5-HT Receptor Neurological Disease
    Spadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC50 value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research [1] .
    Spadin
  • HY-P1422A
    Spadin TFA
    1 Publications Verification

    		 Potassium Channel 5-HT Receptor Neurological Disease
    Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC50 value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research [1] .
    Spadin TFA
  • HY-104005
    ML335

    		Potassium Channel Neurological Disease
    ML335 is a selective activator of both TREK-1 and TREK-2.
    ML335
  • HY-W013712
    GI-530159

    		Potassium Channel Neurological Disease
    GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect [1].
    GI-530159
  • HY-B0563A
    Ropivacaine hydrochloride monohydrate
    4 Publications Verification

    		 Sodium Channel Potassium Channel Cardiovascular Disease Neurological Disease
    Ropivacaine hydrochloride monohydrate is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese [1] . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for regional anesthesia and neuropathic pain management in vivo [1].
    Ropivacaine hydrochloride monohydrate
  • HY-B0563B
    Ropivacaine hydrochloride
    4 Publications Verification

    		 Sodium Channel Potassium Channel Cardiovascular Disease Neurological Disease Cancer
    Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese [1] . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain management in vivo [1].
    Ropivacaine hydrochloride
  • HY-B0563
    Ropivacaine
    4 Publications Verification

    		 Sodium Channel Potassium Channel Cardiovascular Disease Neurological Disease
    Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese [1] . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is used for the research of neuropathic pain management [1].
    Ropivacaine
  • HY-B1500
    2,2,2-Trichloroethanol

    2,2,2-Trichloroethanol, the active form of Chloral hydrate, is an agonist for the nonclassical K2P channels TREK-1 (KCNK2) and TRAAK (KCNK4) [1].
    2,2,2-Trichloroethanol
  • HY-B0563BS
    Ropivacaine-d7 hydrochloride

    		Isotope-Labeled Compounds Neurological Disease
    Ropivacaine-d7 hydrochloride is a deuterium labeled Ropivacaine (hydrochloride) (HY-B0563B) [1]. Ropivacaine hydrochloride is a potent?sodium channel?blocker and blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain?management in vivo .
    Ropivacaine-d7 hydrochloride
  • HY-108596
    BL-1249

    		Potassium Channel Inflammation/Immunology
    BL-1249 is a nonsteroidal anti-inflammatory agent (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM) [1] .
    BL-1249
  • HY-137563
    A2793

    		Potassium Channel Neurological Disease
    A2793 is an efficient dual TWIK-related acid-sensitive K + channel (TASK)-1/TRESK inhibitor, with an IC50 of 6.8 μM for mTRESK. A2764 is more selective for TRESK, and it only moderately influences TREK-1 and TALK-1 [1].
    A2793
  • HY-120348
    ML67-33

    		Potassium Channel Cardiovascular Disease Neurological Disease
    ML67-33 is a selective activator of temperature- and mechano-sensitive K2P channels. ML67-33 rapidly and reversibly affects K2P2.1 (TREK-1) with EC50s of 36.3 μM and 9.7 μM in cell-free and HEK293 cells, respectively [1].
    ML67-33
  • HY-B0563S1
    Ropivacaine-d7

    		Isotope-Labeled Compounds Sodium Channel Potassium Channel Cardiovascular Disease Neurological Disease
    Ropivacaine-d7 is deuterium labeled Ropivacaine. Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese[1][2]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane[3]. Ropivacaine is used for the research of neuropathic pain management[1].
    Ropivacaine-d7
  • HY-135809
    A2764 dihydrochloride

    		Potassium Channel Neurological Disease
    A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K + channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception [1].
    A2764 dihydrochloride
  • HY-103371
    DCPIB
    5 Publications Verification

    		 Chloride Channel Potassium Channel Neurological Disease
    DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB voltage-dependently activates potassium channels TREK1 and TRAAK, and inhibits TRESK, TASK1 and TASK3 (IC50s: 0.14, 0.95, 50.72 μM, respectively). DCPIB is also a selective blocker of swelling-induced chloride current (ICl,swell), with an IC50 of 4.1 μM. DCPIB is a useful tool for investigating structure-function studies of K2P channels [1] .
    DCPIB
  • HY-B0563C
    Ropivacaine mesylate
    4 Publications Verification

    		 Sodium Channel Potassium Channel Cardiovascular Disease Neurological Disease
    Ropivacaine mesylate is a long-acting amide local anaesthetic agent for a spinal block and effectively blocks neuropathic pain. Ropivacaine blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibressup>[1] . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane .
    Ropivacaine mesylate
  • HY-104027
    ML402

    		Potassium Channel Neurological Disease
    ML402, a thiophene-carboxamide, is a selective K2P2.1(TREK-1) and K2P10.1(TREK-2) activator. ML402 is inactive against K2P4.1(TRAAK) [1].
    ML402

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