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activation slowing

" in MedChemExpress (MCE) Product Catalog:

23

Inhibitors & Agonists

3

Natural
Products

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0219
    Bicuculline
    Maximum Cited Publications
    23 Publications Verification

    (+)-Bicuculline; d-Bicuculline

    GABA Receptor Neurological Disease
    Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
    Bicuculline
  • HY-16642A

    Cannabinoid Receptor Neurological Disease
    LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
    LY2828360
  • HY-113673

    Potassium Channel Cardiovascular Disease
    A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. A-935142 enhances hERG current in a complex manner by facilitation of activation, reduction of inactivation, and slowing of deactivation, and abbreviates atrial and ventricular repolarization .
    A-935142
  • HY-106844A

    Others Cardiovascular Disease
    (+)-EMD 57033 is a cardiac troponin C (cTnC) activator, is a dominant Ca 2+ sensitizer. (+)-EMD 57033 binds the cardiac/slow skeletal troponin C isoform and exerts myocardial contractile promotion function .
    (+)-EMD 57033
  • HY-108591

    R-L3

    Potassium Channel Cardiovascular Disease
    L-364,373 (R-L3) is a voltage-gated Kv7.1 (KCNQ1)/mink channels activator. L-364,373 activates Iks (slow delayed rectifier potassium current) and shortens action potential duration in guinea pig cardiac myocytes, and suppresses early afterdepolarizations in rabbit ventricular myocytes .
    L-364,373
  • HY-147140

    Furin Inflammation/Immunology
    BOS-318 is a potent, slowly dissociating, highly selective, and cell-permeable furin inhibitor with IC50 value of 1.9 nM. BOS-318 protects ENaC from subsequent activation by neutrophil elastase. BOS-318 can be used for the rsearch for CF lung disease .
    BOS-318
  • HY-126106

    Potassium Channel Others
    (BrMT)2 (compound 2) is a non-peptide snail toxin that slows down the activation of Kv1.1 channels .
    (BrMT)2
  • HY-144812

    Cathepsin Inflammation/Immunology Cancer
    Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen .
    Gü1303
  • HY-N0219R

    GABA Receptor Neurological Disease
    Bicuculline (Standard) is the analytical standard of Bicuculline. This product is intended for research and analytical applications. Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
    Bicuculline (Standard)
  • HY-149933

    Cannabinoid Receptor Neurological Disease
    AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility .
    AM841
  • HY-108588

    Potassium Channel Cardiovascular Disease
    NS5806, a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2 .
    NS5806
  • HY-152949

    Myosin Neurological Disease
    Myosin V-IN-1 (compound 8) is a potent and selective Myosin V inhibitor, with a Ki of 6 μM. Myosin V-IN-1 shows acute inhibition of myosin V. Myosin V-IN-1 slows the actin-activated myosin V ATPase by specifically inhibiting ADP release from the actomyosin complex .
    Myosin V-IN-1
  • HY-120026

    KB015

    Thyroid Hormone Receptor Neurological Disease
    KB130015 (KB015) is an orally active and potent ThRα and ThRβ (Thyroid Hormone Receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 has antiarrhythmic properties. KB130015 markedly slows the kinetics of inactivation of Na + channels. KB130015 opens large-conductance Ca 2+-activated K + channels and relaxes vascular smooth muscle .
    KB130015
  • HY-156420

    Phosphatase Others
    ATUX-1215 is an activator of protein phosphatase 2A (PP2A). ATUX-1215 reduced the phosphorylation of ERK, p38, JNK, and Akt and the secretion of IL-12p70, GM-CSF, and IL1α in BLM-treated animals. ATUX-1215 can slow the progression of lung fibrosis .
    ATUX-1215
  • HY-N0283
    Diacerein
    3 Publications Verification

    Diacerhein; Diacetylrhein

    Interleukin Related Calcium Channel Inflammation/Immunology
    Diacerein (Diacerhein), an orally active anthraquinone, reduces production of IL-1 converting enzyme then inhibits the activation of IL-1β by related downstream signaling. Diacerein is an anti-inflammatory and anti-rheumatic drug. Diacerein can relieve bronchospasm and control airway inflammation in asthmatic mice. Diacerein has the potential for slow acting drug in osteoarthritis (SYSADOA) research .
    Diacerein
  • HY-110162

    Potassium Channel Neurological Disease
    QO 58 is a potent modulator of K(v)7 channels. QO-58 increases the current amplitudes, shifts the voltage-dependent activation curve in a more negative direction and slows the deactivation of K(v)7.2/K(v)7.3 currents. QO-58 has the potential for the research of diseases associated with neuronal hyperexcitability .
    QO 58
  • HY-13422
    Zatebradine hydrochloride
    1 Publications Verification

    UL-FS-49; UL-FS-49CL

    HCN Channel Cardiovascular Disease
    Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 μM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 μM, 2.21 μM, 1.90 μM and 1.88 μM, respectively .
    Zatebradine hydrochloride
  • HY-16915
    RPR-260243
    1 Publications Verification

    Potassium Channel Cardiovascular Disease
    RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivation of hERG1 channels. RPR260243-modified HERG currents are inhibited by Dofetilide (IC50=58 nM). RPR260243 displays no activator-like effects on other voltage-dependent ion channels, including the closely related ERG3 K+ channel . RPR-260243 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    RPR-260243
  • HY-117051

    HSP Cancer
    STA-2842 is an inhibitor of heat shock protein HSP90 with potential to inhibit autosomal dominant polycystic kidney disease (ADPKD). ADPKD is caused by inherited mutations in the PKD1 or PKD2 genes that abnormally activate multiple signaling proteins and pathways that regulate cell proliferation. STA-2842 can significantly reduce initial renal cyst formation and kidney growth in mice, and slow disease progression in mice with existing cysts.
    STA-2842
  • HY-126704

    KC-8857

    Potassium Channel Cardiovascular Disease
    Tedisamil (KC-8857) is an antiarrhythmic compound with important biological activities. Tedisamil exhibits a significant slowing effect on heart rate, which is achieved by inhibiting the transient outward potassium current (I(to)) in the atrium. Tedisamil inhibits multiple potassium currents, including IK, K(ATP), and PKA-activated chloride channels, thereby prolonging the cardiac action potential and QT interval, and increasing cardiac reentry. Tedisamil has antiarrhythmic effects on ventricular arrhythmias and atrial flutter in animal models .
    Tedisamil
  • HY-13422A
    Zatebradine
    1 Publications Verification

    UL-FS-49 free base; UL-FS-49CL free base

    HCN Channel Cardiovascular Disease
    Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively .
    Zatebradine
  • HY-162347

    Sodium Channel Neurological Disease
    Nav1.7-IN-13 (compound 3g) is a sodium channel inhibitor that significantly inhibits Veratridine (HY-N6691)-induced neuronal activity. Nav1.7-IN-13 inhibits total Na+ current in DRG neurons in a concentration-dependent manner; slows down the activation of Navs. Nav1.7-IN-13 significantly alleviated mechanical pain behavior in a rat model of nerve injury (SNI) and had analgesic activity .
    Nav1.7-IN-13
  • HY-126720

    Endogenous Metabolite Metabolic Disease
    N-Lignoceroyl Taurine is an arachidonoyl amino acid and taurine conjugate with a fatty acid that can be isolated from bovine brain. N-Lignoceroyl Taurine is one of several novel taurine-conjugated fatty acids discovered during mass spectrometry lipidomic analysis of the brain and spinal cord of wild-type and fatty acid amide hydrolase (FAAH) knockout mice. N-Lignoceroyl Taurine levels were 23-26-fold higher in FAAH -/- mice compared to wild-type mice, suggesting that FAAH utilizes N-Lignoceroyl Taurine as a substrate. However, in vitro experiments with purified FAAH showed that N-Lignoceroyl Taurine was hydrolyzed 2,000-fold slower in FAAH compared to oleoylethanolamide. N-Acyl Taurines with polyunsaturated acyl chains can activate members of the transient receptor potential (TRP) calcium channel family, including TRPV1 and TRPV4.
    N-Lignoceroyl Taurine

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