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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
44 Results for "
K(2P)
" in MedChemExpress (MCE) Product Catalog:
Products (44)
44 Results for "K(2P)" in MCE Product Catalog:
12
12 Publications Verification
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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 [2].
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8 Cited Publications
Cat. No.: HY-B0563
CAS No.: 84057-95-4
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Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese [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 . Ropivacaine is used for the research of neuropathic pain management .
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8 Cited Publications
Cat. No.: HY-B0563B
CAS No.: 98717-15-8
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Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese [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 . Ropivacaine is widely used for neuropathic pain management in vivo .
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8 Cited Publications
Cat. No.: HY-B0563A
CAS No.: 132112-35-7
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Ropivacaine hydrochloride monohydrate is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese [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 . Ropivacaine is widely used for regional anesthesia and neuropathic pain management in vivo .
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8 Cited Publications
Cat. No.: HY-B0563C
CAS No.: 854056-07-8
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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 [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 .
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1
1 Cited Publications
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ML402, a thiophene-carboxamide, is a selective K2P2.1(TREK-1) and K2P10.1(TREK-2) activator. ML402 is inactive against K2P4.1(TRAAK) .
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Doxapram (hydrochloride) is a ventilatory stimulant. Doxapram (hydrochloride) inhibits TASK Tandem Pore (K2P) potassium channel function. Doxapram (hydrochloride) inhibits TASK-1 and TASK-3 with an EC50 values of 410 and 37 nM, respectively. Doxapram (hydrochloride) inhibits TASK-1/TASK-3 heterodimeric channel function with an EC50 value of 9 μM. Doxapram (hydrochloride) can be studied in research on apnea in preterm infants [2].
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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) [2].
Cat. No.: HY-B0563S1
CAS No.: 684647-62-9
Cat. No.: HY-W011235
CAS No.: 57226-68-3
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Norfluoxetine hydrochloride is the active metabolite of the antidepressant Fluoxetine (HY-B0102); it is also a TREK-2 K2P potassium channel inhibitor. Norfluoxetine hydrochloride exhibits neuroimmunological activity, induces apoptosis in primary microglial cells, and inhibits the release of pro-inflammatory factors. Norfluoxetine hydrochloride inhibits high-threshold voltage-gated Ca 2+ currents in neurons with an EC50 of 20.4 μM. Norfluoxetine hydrochloride can be used in research related to depression, ischemic stroke, and epilepsy [2] .
Cat. No.: HY-135556
CAS No.: 83891-03-6
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PK-THPP is a potent and brain-penetrant TWIK-related acid-sensitive K + ion channel (K2P9.1 or TASK-3) blocker with IC50s of 35 nM and 300 nM for TASK-3 and TASK-1, respectively. PK-THPP shows no or less activity against other K + channels. PK-THPP is an effective breathing stimulant and can be used for the study of breathing disorders [2].
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NPBA, a potassium K2P channel TASK-3 (KCNK9) agonist, is a tandem pore domain weak inward rectifying K + channel (TWIK2) channel blocker. NPBA suppresses NLRP3 inflammasome activation in macrophages .
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RU-TRAAK-2 is a completely reversible TRAAK (TWIK-related arachidonic acid-stimulated K + channel) inhibitor. RU-TRAAK-2 exerts no activity for non-K2P channels (Kv1.2, Slo1 and GIRK2) . RU-TRAAK-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-172182
CAS No.: 2230296-66-7
Synonyms: VU6011887
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ONO-2920632 is an orally active and central nervous system (CNS)-penetrant TREK activator, with EC50 values of 0.3 µM and 2.8 μM for TREK-1 and TREK-2, respectively. ONO-2920632 exhibits selectivity for other K2P channels (>91-fold selective versus TASK1, TASK2, TASK3, TRAAK, and TWIK2; 31-fold selective versus TRESK). ONO-2920632 possesses analgesic effects and can be used in research on pain, migraine, and neurological disorders.
Synonyms: S20951
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A1899 is a potent and highly selective blocker of the K2P channel TASK-1. A1899 has IC50 values of 35.1 nM and 7 nM for TASK-1 channels expressed in oocytes and CHO cells, respectively. A1899 is also an IKur blocker that can be used for the research of cardiovascular diseases [2].
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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 .
Cat. No.: HY-W011235S
CAS No.: 1188265-34-0
Cat. No.: HY-135556AS
CAS No.: 1185132-92-6
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
