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Results for "

HEK+cells

" in MedChemExpress (MCE) Product Catalog:

21

Inhibitors & Agonists

4

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-19608
    GSK1016790A
    35+ Cited Publications

    		 TRP Channel Calcium Channel Cardiovascular Disease Metabolic Disease
    GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca 2+ influx and elevate intracellular Ca 2+ in HEK cells .
    GSK1016790A
  • HY-B1167
    Ajmaline

    Cardiorythmine; (+)-Ajmaline

    		 Sodium Channel Cardiovascular Disease
    Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC50 of 1 μM in HEK cells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia .
    Ajmaline
  • HY-15039
    SSR240612

    		Bradykinin Receptor Metabolic Disease Inflammation/Immunology Endocrinology
    SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
    SSR240612
  • HY-N125722
    Venturicidin A

    Aabomycin A1

    		 ATP Synthase Antibiotic Infection
    Venturicidin A (Aabomycin A1), from actinomycetes, is a membrane-active natural product inhibitor of ATP synthase. Venturicidin A potentiates the aminoglycoside antibiotic gentamicin against multidrug-resistant clinical isolates of Staphylococcus, Enterococcus, and Pseudomonas aeruginosa. Venturicidin A shows noticeable toxicity toward human embryonic-kidney (HEK)cells with an IC50 of 31 μg/mL.
    Venturicidin A
  • HY-134988
    EDP-305

    		FXR Phosphatase Cytochrome P450 Inflammation/Immunology
    EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research .
    EDP-305
  • HY-135783
    AT 1001
    1 Publications Verification

    		 nAChR Neurological Disease Metabolic Disease Inflammation/Immunology
    AT 1001 is an orally effective α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) antagonist with a Ki value of 2.64 nM. AT 1001 reversibly blocks Epibatidine (HY-101078)-induced inward currents in HEK cells transfected with α3β4 nAChR. AT 1001 dose-dependently blocks nicotine self-administration behavior in rats, alleviates gluten-induced gastrointestinal symptoms, blocks tight junction toxin-induced immune responses, and reduces the incidence of type 1 diabetes in rats. AT 1001 can be used in the research of nicotine addiction and celiac disease .
    AT 1001
  • HY-171347
    gamma-secretase modulator 6

    		γ-secretase Amyloid-β Neurological Disease
    gamma-secretase modulator 6 (Example 50) is a gamma-secretase modulator. gamma-secretase modulator 6 inhibits Aβ42 secretion in HEK cell line stably expressing APP (Aβ amyloid precursor protein) (pIC50: 8.1). gamma-secretase modulator 6 can be used for research of Alzheimer's disease .
    gamma-secretase modulator 6
  • HY-148939
    MPX-004

    		iGluR Neurological Disease
    MPX-004 is a potent GluN2A antagonist. MPX-004 inhibits GluN2A-containing NMDA receptors expressed in HEK cells with an IC50 of 79 nM. MPX-004 has no inhibitory effect on GluN2B or GluN2D receptor-mediated responses. MPX-004 has the potential for neuropsychiatric and developmental disorders research .
    MPX-004
  • HY-114962
    S-22153

    		Melatonin Receptor Neurological Disease
    S-22153 is a potent melatonin receptor antagonist with EC50 values of 19 nM, 4.6 nM for hMT1 and hMT2 melatonin receptor, respectively. S-22153 has Ki values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT1, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT2. S-22153 is a specific ligand of MT1 and MT2 melatonin receptors subtypes .
    S-22153
  • HY-143312D
    (R)-V-0219 hydrochloride

    		GLP Receptor Metabolic Disease
    (R)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R .
    (R)-V-0219 hydrochloride
  • HY-143312E
    (S)-V-0219 hydrochloride

    		GLP Receptor Metabolic Disease
    (S)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 hydrochloride is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice .
    (S)-V-0219 hydrochloride
  • HY-168758
    Delta3,5-cholestadien-7-one

    		GABA Receptor Neurological Disease
    Delta3,5-cholestadien-7-one is an oxysterol and a negative allosteric modulator of GABAA receptors. Delta3,5-cholestadien-7-one reduces GABA-induced currents in HEK cells expressing α1β1γ2 or α4β3γ2 subunit-containing GABAA receptors with IC50 values of 1.5 and 1 µM, respectively. Delta3,5-cholestadien-7-one reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons .
    Delta3,5-cholestadien-7-one
  • HY-119282
    AZD6538

    		mGluR Neurological Disease
    AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG (HY-12598A)-stimulated intracellular Ca2+ release in HEK cells expressing rat or human mGluR5, with IC50 values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain .
    AZD6538
  • HY-172999
    Nav1.8-IN-19

    		Sodium Channel Neurological Disease
    Nav1.8-IN-19 (Compound 122) is a Nav1.8 inhibitor with an IC50 of 0.44 nM in HEK cells. Nav1.8-IN-19 can be used for the study of pain .
    Nav1.8-IN-19
  • HY-157503
    Photosensitizer-3

    		Photosensitizer Cancer
    Photosensitizer-3 is a photosensitizer that exhibits powerful selective killing effects on transfected HEK cells and affibody-targeted A431 cancer cells when exposed to near-infrared light excitation .
    Photosensitizer-3
  • HY-B1167R
    Ajmaline (Standard)

    Cardiorythmine (Standard); (+)-Ajmaline (Standard)

    		 Reference Standards Sodium Channel Cardiovascular Disease
    Ajmaline (Standard) is the analytical standard of Ajmaline. This product is intended for research and analytical applications. Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC50 of 1 μM in HEK cells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia .
    Ajmaline (Standard)
  • HY-143312B
    (R)-V-0219

    		GLP Receptor Metabolic Disease
    (R)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R .
    (R)-V-0219
  • HY-168720
    Apoptosis inducer 32

    		Apoptosis Cancer
    Apoptosis inducer 32 (Compound 7g) is an apoptosis inducer with a KD of 42 μM, showing anti-tumor activity. Apoptosis inducer 32 caused significant cellular morphological changes in MDA-MB-231 cells, including membrane bubbling, nuclear fragmentation, and apoptotic body formation. The IC50 of Apoptosis inducer 32 in MCF-7, MDA-MB-231, and HEK cells is 4.77, 6.56 and 337.8 μM respectively .
    Apoptosis inducer 32
  • HY-143312C
    (S)-V-0219

    		GLP Receptor Metabolic Disease
    (S)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice .
    (S)-V-0219
  • HY-B1167A
    Ajmaline hydrochloride

    Cardiorythmine hydrochloride; (+)-Ajmaline hydrochloride

    		 Others Cardiovascular Disease
    Ajmaline hydrochloride is a Class Ia antiarrhythmic agent. It inhibits HERG potassium channels with IC50s of 1.0 μmol/l and 42.3 μmol/l in HEK cells and moth spider oocytes respectively. The inhibitory effect of Ajmaline hydrochloride is rapid, reversible, and positive frequency dependent. It acts primarily on the open state of the HERG channel and may also be combined with the inactivated state. The inhibitory effect of ajmaline hydrochloride is dependent on aromatic residues in the S6 domain, and the sensitivity is significantly reduced in the inactivation-deficient HERG S620T channel. It can also slightly affect the activation voltage of HERG channels. Ajmaline hydrochloride's inhibitory effect on HERG channels may contribute to both its potent antiarrhythmic effects and its potential proarrhythmic risk.
    Ajmaline hydrochloride
  • HY-176778A
    (rac)-BDM88951

    		Aminopeptidase Inflammation/Immunology Cancer
    (rac)-BDM88951 is the racemate of BDM88951 (HY-176778). BDM88951 (Compound 4 d) is a selective ERAP2 inhibitor with an IC50 of 19 nM. BDM88951 significantly inhibits antigen presentation in HEK cells. BDM88951 can be used for research on autoimmune diseases and cancer .
    (rac)-BDM88951

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