“Ligand-gated Ion Channel”的搜索结果
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M2 ion channel blocker能够抑制和阻断M2离子通道的活性。抗病毒药。
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NMDA ion-channel antagonist
CNS-5161 hydrochloride is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
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muscarinic acetylcholine receptor (mAChR) antagonist
Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
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TRPV4 ion channel blocker
GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively.
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TRPML3 ion channel activator
SN 2 is a novel and potent activator of TRPML3 ion channel with EC50 of 1.8??0.13 μM.
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sodium channel blocker
Sodium Channel inhibitor 2 is a sodium channel blocker extracted from patent WO 2004011439 A2, compound 3c.
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Ca2+ channel agonist/CDK2 inhibitor
Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
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L-type calcium-channel antagonist
Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist with a rapid onset of action designed for intranasal administration, used to treat Paroxysmal Supraventricular Tachycardia (PSVT). Etripamil (MSP-2017) slows atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells.
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N-type calcium channel blocker-1 is an orally active analgesic agent which shows high affinity to functionally block N-type calcium channels with an IC50 of 0.7 μM in the IMR32 assay.
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K+ Channel 抑制剂
K+ Channel inhibitor,Kv1.5(IKur)的二氢吡唑并嘧啶抑制剂的合成基础。
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Sodium Channel 抑制剂
Sodium Channel inhibitor 1 是一种新型的选择性电压门控钠通道,用于疼痛治疗。
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IK1 inhibitor
IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent IK1 (KIR2.x ion-channel-carried inward rectifier current) inhibitor, with IC50 values of 12-15 nM for human and mouse KIR2.x currents.
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Ion channel blocker
Vernakalant hydrochloride是一种研究性混合离子通道阻滞剂,可以以2至5 mg/kg的剂量终止人的急性心房纤颤(AF),并且与现有药物相比,对房颤的选择性更高。在抗心律不齐的治疗中。
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- Joe Z.Zhang, .et al. A Human iPSC Double-Reporter System Enables Purification of Cardiac Lineage Subpopulations with Distinct Function and Drug Response Profiles, Cell Stem Cell, 2019, 24, 1-10
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NMDA receptor ion channel 拮抗剂
ARL-15896是新型的N-甲基-D-天冬氨酸受体离子通道拮抗剂。
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- Robert A. Volkmann, .et al. MPX-004 and MPX-007: New Pharmacological Tools to Study the Physiology of NMDA Receptors Containing the GluN2A Subunit, PLoS One, 2016, 11(2): e0148129 PMID: 26829109
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used to treat hyperkalemia in patients with chronic kidney disease (CKD)
Calcium polystyrene sulfonate is an ion-exchange resin used for reducing blood levels of potassium. Calcium polystyrene sulfonate is used to treat hyperkalemia in patients with chronic kidney disease (CKD).
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NO synthase inhibitor
Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.
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picomolar PDE1 inhibitor
ITI-214 (free base) is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
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PDE1 inhibitor
ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
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CaSR antagonist
NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist.
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FITC-Dextran is a marker consisting of coupling fluorescein-isothiocyanate to dextran. FITC-Dextrans are polysaccharides comprised of varying lengths of branched glucose molecules and can be used to determine solute, ion and protein permeability of the blood-brain barrier (BBB) based on the size of the dextran used.
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Bax channel blocker
Bax channel blocker是Bax介导的线粒体细胞色素C释放的有效抑制剂(IC50 = 0.52μM)。
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Ca2+-activated K+ channel activator
NS19504 is a Ca2+-activated K+ channel (BK channel, KCa1.1 channel) activator (EC50=11.0 ?M) with relaxing effect on bladder smooth muscle spontaneous phasic contractions.
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anion channel inhibitor
Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
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TRPM8 channel blocker
TC-I 2000 is a TRPM8 channel blocker that inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells
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Nav1.8 channel blocker
PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.
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K+ channel opener
Y-27152, a prodrug of the KATP (Kir6) channel opener Y-26763, is a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state.
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potassium channel (non-GIRK1/X) activator
VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 ?M and 5.2 ?M for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.
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CRAC channel inhibitor
Synta66 is an inhibitor of store-operated calcium entry channel Orai, which forms the pore of the CRAC channel, and used for the research of neurological disease.
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Nav1.7 sodium channel inhibitor
Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
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K+ (KATP) channel activator
Y-26763 is a K+ channel opener and active metabolite of Y-27152. Y-26763 is an ATP-sensitive K+ (KATP) channel activator.
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Kv3 potassium channel modulator
AUT1 is a Kv3 potassium channel modulator with pEC50s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5).
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CRAC channel inhibitor
RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM.
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sodium channel blocker
Levobupivacaine hydrochloride is a sodium channel blocker.
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calcium channel antagonist
SM-6586 is a calcium channel antagonist and inhibitor of Na+/H+ and Na+/Ca2+ exchange transport, potentially for the treatment of cerebrovasular diseases and hypertension.
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HCN channel blocker
ZD7288 is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.
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KCNQ2/Q3 potassium channel activator
ICA-069673 is a KCNQ2/Q3 potassium channel activator with an IC50 of 0.69 μM.
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intravenous BKCa-channel blocker
GAL-021 a new intravenous BKCa-channel blocker.
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lipophilic calcium channel blocker
Teludipine is a lipophilic calcium channel blocker.
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TRPP3 channel inhibitor
EIPA (L593754; MH 12-43) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA (L593754; MH 12-43) also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.
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KATP channel activator
P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation.
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KV7 channel blocker
DMP-543 (XR-543) is a KV7 channel blocker, also acts as a potent neurotransmitter release enhancer.
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sAHP channel blocker
UCL 2077 is a selective slow-afterhyperpolarization (sAHP) channel blocker (IC50 = 500 nM in hippocampal neurons in culture), having minimal effects on Ca2+ channels, action potentials, input resistance and the medium after hyperpolarization.
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hERG channel activator
PD-118057 is a human ether-a-go-go-related gene (hERG) channel activator that does not cause hERG blockade.
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calcium channel blocker
Tiapamil hydrochloride is a calcium channel blocker.
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benzazepine calcium channel blocker
SQ-31765 is a benzazepine calcium channel blocker.
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calcium channel blocker
ACT-709478 is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies.
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T-type calcium channel inhibitor
ML218 is a selective T-type calcium channel inhibitor with IC50s of 270 and 310 nM for Cav3.3 and Cav3.2 in electrophysiology assay, respectively.
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Ca2+ channel blocke
MRS1845 is a Ca2+ channel blocker with relative specificity for store-operated calcium entry (SOCE) channels.
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NMDA channel blocker
Lanicemine (AZD6765) is a low-trapping NMDA channel blocker with a binding (Ki) of 0.56-2.1?μM.
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Kv3 voltage-gated potassium channel modulator
Kv3 modulator 1 is a Kv3 voltage-gated potassium channel modulator extracted from patent WO2018020263A1, Compound X. Kv3 modulator 1 can be used to treat inflammatory pain.
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