“Ligand-gated Ion Channels”的搜索结果
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nucleotide
Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
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CRAC inhibitor
CM-4620 is a calcium-release activated calcium-channel (CRAC) inhibitor, with IC50s of 119, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.
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Nav1.7 inhibitor
PF-05241328 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (Nav1.7), with an IC50 of 31 nM.
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?- opioid receptor agonist
Trimebutine Maleate is a drug with antimuscarinic and weak mu opioid agonist effects. Trimebutine Maleate modulates the calcium and potassium channels, relieves abdominal pain in patients with irritable bowel syndrome.
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Tetracaine is a potent local anesthetic. It alters the function of calcium release channels (ryanodine receptors) that control the release of calcium from intracellular stores.
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Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
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5-HT2 receptors inhibitor
Nefazodone HCl is an inhibitor of 5-HT2 receptors, SERT, NET, and hERG K+ channels used to treat mood disorders. It decreases immobility time in the forced swim test.
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Calcium channel blocker
Efonidipine is a dihydropyridine calcium channel blocker that blocks both T-type and L-type calcium channels. It has also been studied in atherosclerosis and acute renal failure.
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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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Guanosine 5'-triphosphate trisodium salt (5'-GTP trisodium salt) is an activator of signal transduction of G proteins.
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Auranofin is a gold salt classified by the World Health Organization as an antirheumatic agent. It is a gold-thiol complex with anti-inflammatory and immunosuppressive actions.
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Anti-adipogenic, anti-inflammatory, and anti-neoplastic activities
Triphala, an Ayurvedic polyherbal formulation comprising of equiproportional fruit parts of Terminalia chebula, Terminalia bellerica, and Phyllanthus emblica. Triphala inhibits NF-κB activation. Triphala exerts antifungal action. Anti-adipogenic, anti-inflammatory, and anti-neoplastic activities.
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Adenosine deaminase is an enzyme that catalyzes the irreversible deamination of adenosine and 2'-deoxyadenosine to inosine and 2'-deoxyinosine, respectively.
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digest GST-tagged proteins
Thrombin is a trypsin-like allosteric serine protease. Thrombin enables site-specific cleavage of fusion proteins with an accessible Thrombin recognition sequence and can be used to digest GST-tagged proteins.
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unique pigment
Melanin is a unique pigment with myriad functions. It is multifunctional, providing defense against environmental stresses such as ultraviolet (UV) light, oxidizing agents and ionizing radiation.
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FLT3 inhibitor
HM-43239 is a Novel Potent Small Molecule FLT3 Inhibitor, in Acute Myeloid Leukemia (AML) with FMS-like Tyrosine Kinase 3 (FLT3) Mutations
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Cinnamylamine can be used for the preparation of Tranylcypromine, a drug that acts as a nonselective and irreversible inhibitor of the enzyme monoamine oxidase (MAO), and is used as an antidepressant and anxiolytic agent.
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Peptide 401, a potent mast cell degranulating factor from bee venom, suppresses the increased vascular permeability due to intradermal injection of various smooth muscle spasmogens (histamine, and 5-HT).
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DNA G-quadruplexe (G4) ligand
BMVC-8C3O is a DNA G-quadruplexe (G4) ligand which can induce topological conversion of non-parallel to parallel forms in human telomeric DNA G4s.
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TLR4 inhibitor
TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.
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PD-1/PD-L1 interaction inhibitor
BMS-1001 is a potent inhibitor of PD-1/PD-L1 interaction with EC50 of 253 nM.
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Candida albicans filamentation inhibitor
Filastatin is a long-lasting inhibitor of Candida albicans filamentation. Filastatin inhibits adhesion by multiple pathogenic Candida species with an IC50 of ~3 μM in the GFP-based adhesion assay.
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photocrosslinker
DiZPK is a photocrosslinker for identifying direct protein-protein interactions in living prokaryotic and eukaryotic cells.
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near-infrared (NIR) probe
CRANAD-2 is a curcumin-derivatized near-infrared (NIR) probe that meets all the requirements for a NIR contrast agent for the detection of Abeta plaques both in vitro and in vivo.
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positive allosteric modulator (PAM)
CYM2503 is a positive allosteric modulator (PAM) of the GAL2 receptor that potentiates galanin-induced IP1 production in vitro.
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Akt inhibitor
API-1 (NSC 177223) is a potent inhibitor of Akt that induces GSK3-dependent, β-TrCP- and FBXW7-mediated Mcl-1 degradation, resulting in induction of apoptosis.
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DNMT1 inhibitor
SW155246 is a potent and selective DNMT1 (DNA methyltransferase 1) inhibitor with IC50 of 1.2 μM. SW155246 induces re-expression of the tumor suppressor geneRASSF1 in A549 cells.
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HCN4 CLP ligand
BPU-11 is a HCN4 CLP ligand. It acts by modulating channel function and completely abolishing the cAMP-induced shift in V1/2.
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pathway-selective inhibitor of estrogen receptor (ER)
WAY-169916 is a pathway-selective inhibitor of estrogen receptor (ER) that acts by inhibiting NF-kB transcriptional activity.
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depalmitoylase inhibitor
JCP174 is a depalmitoylase inhibitor that enhances Toxoplasma host-cell invasion by targeting TgPPT1.
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inhibitor of deregulated NRF2 transcriptional activity
AEM1 is an inhibitor of deregulated NRF2 transcriptional activity in cancer.
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fluorogenic probe
MSBN is a highly selective fluorogenic probe for thiols, selectively imaging thiols in live cells and specifically label protein thiols with a turn-on signal to determine diverse reversible protein thiol modifications.
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negative control compound
GSK106 is a negative control compound that can be used in binding and functional assays for PAD4 inhibitors.
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antiestrogenic properties
FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus.
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inhibitor of Casein Kinase 1 (CK1)
Epiblastin A is an inhibitor of Casein Kinase 1 (CK1) that engages CK1 isoenzymes in cell lysate and induces efficient conversion of epiblast stem cells (EpiSCs) into embryonic stem cells (cESCs).
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choline kinase α (CHKα) inhibitor
MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis.
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bovine tubulin oxidation inhibitor
Takeda103A is a potent GRK2-dependent bovine tubulin oxidation inhibitor.
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strigolactone (SL) antagonist
Soporidine is a strigolactone (SL) antagonist and inhibitor of germination in their biological assays. It binds AtHTL and specifically interferes with SL signaling.
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antagonist of melanopsin-mediated phototransduction
AA41612 is an antagonist of melanopsin-mediated phototransduction.
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inhibitor of polymerase
ERDRP-0519 is an orally available inhibitor of polymerase that shows efficacy against a lethal morbillivirus infection in a large animal model.
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luciferin analogue
Aka Lumine, a luciferin analogue, is a luciferase substrate emitting red, green, and blue light. The longest emission wavelength of Aka Lumine is recorded at 675 nm, which is within the NIR region.
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proteinase inhibitor
FOY 251, an anti-proteolytic active metabolite Camostate (HY-13512), acts as a proteinase inhibitor. FOY 251 inhibits SARS-CoV-2 infection in cells assay.
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ultra short-acting benzodiazepine
Remimazolam besylate is an ultra short-acting benzodiazepine used in the induction and maintenance of sedation during short (<30 minute) procedures.
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integrin-ligand interactions inhibitor
RGD peptide (GRGDNP) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation.
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peptide antagonist
AUNP-12 (NP-12) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions.
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glutathione-independent inhibitor
iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM.
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epigenetic modifier
L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation.
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