“Ligand-gated Ion Channels”的搜索结果
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Kv3.1/Kv3.2/Kv3.3 channels modulator
Kv3 modulator 3 (Compound 4) is a selective modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 channels extracted from patent WO2017098254A1, compound 4, has analgesic activity for use in the prophylaxis o or treatment of pain.
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Kv3 channels modulator
Kv3 modulator 2 (formula (I)) is a potent Kv3 channels modulator extracted from patent WO2018109484A1, compound formula (I) , has analgesic activity and is used in the prophylaxis or treatment of related disorders.
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progesterone receptor modulator
Ulipristal (acetate) is a novel selective progesterone receptor modulator (SPRM) for the treatment of benign gynecological conditions such as uterine myoma.
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APP expression modulator
ARN2966 is a potent post-transcriptional modulator of APP expression; reduces expression of APP with resultant lower production of Aβ.
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mAChR M5 negative allosteric modulator
(Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration.
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mGluR5 positive allosteric modulator
(R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC50 of 168 nM for potentiation .
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α7 nAChR-positive allosteric modulator
CCMI is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs.
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GABA(A) receptor modulator
NS11394 is a potent and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing receptors.
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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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Small utrophin's translation modulator
Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .
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selective estrogen receptor modulator (SERM)
Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.
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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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HBV capsid assembly modulator
GLP-26 is a HBV capsid assembly modulators (CAM), inhibits HBV DNA replication in Hep AD38 system (IC50=3 nM), and reduces cccDNA by >90% at 1 μM. GLP-26 disrupts the encapsidation of pre-genomic RNA, causes nucleocapsid disassembly and reduces cccDNA pools.
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gp130 modulator
RCGD423 is a gp130 modulator, which prevents articular cartilage degeneration and promotes repair.
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Ryanodine receptor modulator
Ryanodine is a cell permeant ryanodine receptor modulator. Ryanodine can either stimulate or inhibit Ryanodine-mediated Ca2+ release depending on its concentrations. Poisonous diterpenoid found in Ryania speciosa.
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Thyrotropin receptor modulator
D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro.
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CRBN modulator
TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation.
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γ-secretase modulator
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively.
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PANK modulator
PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.
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selective Estrogen receptor modulator
Lasofoxifene tartrate is a third-generation selective estrogen receptor modulator.
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PUN30119, also known as Imidazole ketone erastin (IKE), is a potent, metabolically stable inhibitor of system xc- and inducer of ferroptosis potentially suitable for in vivo applications.
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NAD+ Modulator
KL1333 is an orally available, small organic molecule that reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation. KL-1333 Improves Energy Metabolism and Mitochondrial Dysfunction in MELAS Fibroblasts.
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gap-junction modulator
Tonabersat (SB-220453)是一种新颖的苯并吡喃衍生物,是一种gap-junction调节剂。
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