“Ligand-gated Ion Channels”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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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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TRPC1/4/5 channels inhibitor
Pico145 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.
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N- and P/Q-type Ca2+ channels agonist
GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.
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Kir7.1 potassium channels blocker
ML418 is a selective, sub-micromolar pore blocker of Kir7.1 potassium channels. The inward rectifier potassium (Kir) channel Kir7.1 (KCNJ13) is a key regulator of melanocortin signaling in the brain, electrolyte homeostasis in the eye, and uterine muscle contractility during pregnancy.
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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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TRPC6 inhibitor
SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected.
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NaV1.3 and NaV1.1 channels 抑制剂
ICA-121431是人NaV1.3和NaV1.1通道的有效和选择性抑制剂(IC50值分别为13和23 nM)。
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KCa2.1 channels activator
GW 542573X是小电导Ca2+激活的K+通道(KCa2)的激活剂。
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Voltage-gated sodium channels 拮抗剂
Proparacaine HCl是一种电压门控钠通道拮抗剂,ED50为3.4 mM。
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nuclear export receptor CRM1 inhibitor
Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.
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HERG activator
RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes.
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Calcium channel proteins inhibitor
Dantrolene sodium is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm. Dantrolene sodium is a skeletal muscle relaxant which acts by blocking muscle contraction beyond the neuromuscular junction.
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Na+ channel blocker
Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na+ channel blocker derived from α-aminoamide, with function of suppressing pain.
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L-type calcium antagonist
Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors.
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TRPC3 inhibitor
Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).
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AMPA receptor positive allosteric modulator
PF-4778574 is a potent AMPA receptor positive allosteric modulator (PAM) that has been shown to enhance cognition in animal models.
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voltage-gated sodium channel Nav1.7 inhibitor
Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration.
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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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P-gp inhibitor
Norverapamil hydrochloride ((??)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
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intracellular Ca2+ handling modulator
Caldaret is an intracellular Ca2+ handling modulator that acts through reverse mode Na+/Ca2+ exchanger inhibition.
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NCX inhibitor
ORM-10962 is a potent, highly selective sodium-calcium exchanger (NCX) inhibitor, with IC50 values of 67 and 55 nM for the reverse and forward mode inhibition, respectively.
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TRPV1 agonist
Zucapsaicin, also known as cis-Capsaicin, is a medication used to treat osteoarthritis of the knee and other neuropathic pain. It is applied three times daily for a maximum of three months. It reduces pain, and improves articular functions.
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SGLT inhibitor
Ertugliflozin pidolate belongs to the class of potent and selective inhibitors of the sodium-dependent glucose cotransporters (SGLT), more specifically the type 2 which is responsible for about 90% of the glucose reabsorption from glomerulus.
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Slows neuronal Na+ channel inactivation
beta-Pompilidotoxin是具有序列H2N-Arg的肽。
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AMPA desensitization 抑制剂
Cyclothiazide是苯并噻二叠氮,可作为AMPA受体的增效剂,正向调节其对谷氨酸的响应(EC50 = 3.8 M)。
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Protein translocation 抑制剂
Brefeldin A阻断ADP-核糖基化因子与高尔基体的结合并抑制GDP-GTP交换。
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