1. Search Result

Search Result

Results for "PIGS Inhibitors" in MCE Product Catalog:

27

Inhibitors & Agonists

1

Peptides

4

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-100254
    TAK-024

    P2Y Receptor Cardiovascular Disease
    TAK-024 is a platelet inhibitor with IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively.
  • HY-101408
    Docosatrienoic Acid

    cis-13,16,19-docosatrienoic acid; (13Z,16Z,19Z)-13,16,19-Docosatrienoic acid

    Endogenous Metabolite Cardiovascular Disease
    Docosatrienoic acid is a rare ω-3 fatty acid; inhibits LTB4 binding to pig neutrophil membranes with an Ki of 5 μM.
  • HY-19102
    NSP-805

    Phosphodiesterase (PDE) Cardiovascular Disease
    NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3), and a cardiotonic agent with vasodilator properties.
  • HY-50723
    3-Methylxanthine

    Endogenous Metabolite Others
    3-Methylxanthine, a xanthine derivative, is a cyclic guanosine monophosphate (GMP) inhibitor, with an IC50 of 920 μM on guinea-pig isolated trachealis muscle.
  • HY-101749
    WAY127093B racemate

    Phosphodiesterase (PDE) Inflammation/Immunology
    WAY127093B racemate is the racemate of WAY127093B. WAY127093B is an orally active phosphodiesterase IV inhibitor in guinea pigs and rats.
  • HY-15754
    CGP37157

    Na+/Ca2+ Exchanger Cancer Neurological Disease
    CGP37157 is a potent, selective inhibitor of Na +/Ca 2+ exchanger, inhibiting the Na +-induced Ca 2+-release from guinea-pig heart mitochondria, with an IC50 of 0.8 μM.
  • HY-13283
    MF63

    PGE synthase Inflammation/Immunology
    MF63 is a selective mPGES-1 inhibitor with an IC50 of 0.9 nM and 1.3 nM for pig mPGES-1 and human mPGES-1 enzyme, respectively.
  • HY-12887
    Piclamilast

    RP 73401; RPR 73401

    Phosphodiesterase (PDE) Cancer Inflammation/Immunology
    Piclamilast (RP 73401) is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively.
  • HY-18600A
    Azimilide Dihydrochloride

    NE-10064 Dihydrochloride

    Potassium Channel Cardiovascular Disease
    Azimilide Dihydrochloride (NE-10064 Dihydrochloride) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
  • HY-18600
    Azimilide

    NE-10064

    Potassium Channel Cardiovascular Disease
    Azimilide(NE-10064) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
  • HY-50202
    Etomoxir

    (R)-(+)-Etomoxir

    Apoptosis Cancer Metabolic Disease
    Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
  • HY-50202A
    Etomoxir sodium salt

    (R)-(+)-Etomoxir sodium salt

    Apoptosis Metabolic Disease Cancer
    Etomoxir sodium salt ((R)-(+)-Etomoxir sodium salt) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
  • HY-100164
    SDZ-MKS 492

    MKS 492

    Phosphodiesterase (PDE) Inflammation/Immunology
    SDZ-MKS 492 (MKS 492) is a selective inhibitor of cyclic GMP-inhibited phosphodiesterase (type III PDE). SDZ-MKS 492 inhibits antigen- or platelet activating factor (PAF)-induced bronchoconstriction and allergic reactions in guinea pigs and rats.
  • HY-B1404
    Nylidrin hydrochloride

    Buphenine hydrochloride

    Others Inflammation/Immunology
    Nylidrin hydrochloride was an effective inhibitor of IgE-mediated release of histamine from passively sensitized rat peritoneal mast cells and human basophils, and of IgG1-mediated release of histamine from passively sensitized guinea pig lung slices.
  • HY-116042
    FSCPX

    Adenosine Receptor Cardiovascular Disease
    FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modify the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium.
  • HY-P3057
    [D-Trp11]-Neurotensin

    Neurotensin Receptor Neurological Disease
    [D-Trp11]-Neurotensin, an analogue of Neurotensin (NT), is a selective antagonist of NT in perfused rat hearts but behaves as a full agonist in guinea pig atria and rat stomach strips. [D-Trp11]-Neurotensin can inhibit NT-induced hypotension.
  • HY-N2106
    Dehydroevodiamine

    NF-κB COX PGE synthase NO Synthase Inflammation/Immunology
    Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.
  • HY-134004
    Pentoxyverine

    Carbetapentane

    Sigma Receptor Neurological Disease
    Pentoxyverine (Carbetapentane) is a sigma-1 receptor agonist, with a Ki of 75 nM on guinea-pig brain membranes. Pentoxyverine is a centrally-acting cough suppressant with antimuscarinic and anticonvulsant properties. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.
  • HY-13402A
    Varespladib sodium

    LY315920 sodium

    Phospholipase Inflammation/Immunology
    Varespladib sodium (LY315920 sodium) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib sodium exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively.
  • HY-13402
    Varespladib

    LY315920

    Phospholipase Inflammation/Immunology
    Varespladib (LY315920) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively.
  • HY-N1860
    3-O-Methylquercetin

    Phosphodiesterase (PDE) Inflammation/Immunology
    3-O-Methylquercetin (3-MQ), a main constituent of Rhamnus nakaharai, inhibits total cAMP and cGMP-phosphodiesterase (PDE) of guinea pig trachealis. 3-O-Methylquercetin (3-MQ) exhibits IC50 values of 31.9 μM, 86.9 μM, 18.6 μM and 1.6 μM for PDE1, PDE5, PDE2 and PDE4, respectively.
  • HY-100001
    SKF-96365 hydrochloride

    TRP Channel CRAC Channel Potassium Channel Autophagy Apoptosis Cancer Cardiovascular Disease
    SKF-96365 hydrochloride is a potent TRP channel blocker and a store-operated Ca 2+ entry (SOCE) inhibitor. SKF-96365 hydrochloride significantly inhibits hERG, hKCNQ1/hKCNE1, hKir2.1 and hKv4.3 current, and significantly prolongs the QTc interval in isolated guinea pig hearts. SKF-96365 hydrochloride exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal cancer cells.
  • HY-101676
    RG-12525

    NID 525

    Leukotriene Receptor PPAR Cytochrome P450 Metabolic Disease
    RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.
  • HY-121495
    BKI-1369

    Parasite Infection
    BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves.
  • HY-13438
    AZD3839 free base

    Beta-secretase Cancer
    AZD3839 free base is a potent and selective orally active, brain-permeable BACE1 inhibitor (Ki=26 nM). AZD3839 free base shows 14 and >1000-fold selectivity against BACE2 and cathepsin D, respectively. AZD3839 free base exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. AZD3839 free base can be used for the research of Alzheimer's disease.
  • HY-101044
    PPADS tetrasodium

    P2X Receptor Na+/Ca2+ Exchanger Neurological Disease
    PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca²⁺exchanger in guinea pig airway smooth muscle.
  • HY-108511A
    PB28

    Sigma Receptor Apoptosis SARS-CoV Cancer Infection
    PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.