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Results for "

high exposure

" in MedChemExpress (MCE) Product Catalog:

18

Inhibitors & Agonists

2

Biochemical Assay Reagents

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15043

    Bradykinin Receptor Inflammation/Immunology Endocrinology
    ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse .
    ELN-441958
  • HY-156618

    ABSK011

    FGFR Cancer
    Irpagratinib (ABSK011) is an orally active inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinase, targeting to FGFR4 (IC50<10 nM). Irpagratinib inhibits the auto-phosphorylation of FGFR4 and blocks signal transduction from FGFR4 to downstream pathway activation. Irpagratinib exhibits high exposure in PK study in mouse, rat and dog, and also shows antineoplastic/anti-tumor activity in subcutaneous xenograft tumor models .
    Irpagratinib
  • HY-130609A

    γ-secretase Neurological Disease
    Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease .
    Aβ42-IN-1 free base
  • HY-157455

    Androgen Receptor Cancer
    AR antagonist 5 (compound 30a) is a selective androgen receptor (AR) antagonist with an IC50 value of 134.8 nM. AR antagonist 5 has favorable pharmacokinetic properties and shows a high skin exposure and low plasma exposure [1.
    AR antagonist 5
  • HY-163087

    Others Neurological Disease Metabolic Disease
    PT-91 is an agonist of GPR27. PT-91 exhibits high metabolic stability and brain exposure in mice .
    PT-91
  • HY-130609

    γ-secretase Neurological Disease
    Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50 value of 0.091 µM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
    Aβ42-IN-1
  • HY-14375

    NAMPT Cancer
    CB 300919 is a quinazoline-based antitumour agent with high activity in the CH1 human ovarian tumour xenograft. CB 300919 has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft .
    CB 300919
  • HY-156593

    ROCK Cancer
    ROCK-IN-9 (Compound T345) is a ROCK inhibitor. ROCK-IN-9 shows cytotoxicity in HepG2 cell, with an IC50 of 40.8 μM. ROCK-IN-9 has good pharmacokinetic properties in mice, and shows high in vivo exposure and oral bioavailability at lower doses .
    ROCK-IN-9
  • HY-125920

    Biochemical Assay Reagents Others
    Lauroylsarcosine sodium is a surfactant commonly used in personal care and cosmetics such as shampoos, facial cleansers and toothpaste. It works by lowering the surface tension of water, allowing it to better penetrate and clean surfaces. Lauroylsarcosine sodium is considered safe for cosmetic use and is approved for use in several countries. However, it can cause skin irritation in high concentrations or with prolonged exposure.
    Lauroylsarcosine sodium
  • HY-155992

    Sigma Receptor Neurological Disease
    WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (Ki: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .
    WLB-89462
  • HY-143439

    Estrogen Receptor/ERR Cancer
    LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity .
    LX-039
  • HY-12570

    Casein Kinase Wnt Cancer
    CK2-IN-9 is a potent and selective inhibitor of CK2 kinase with an IC50 of 3 nM. CK2-IN-9 reduces Wnt reporter activity with an IC50 of 75 nM. CK2-IN-9 has low exposure (AUC=0.36 μM/h) and high clearance (CL=65 mL/min/kg) properties in rat .
    CK2-IN-9
  • HY-138879B

    (1S,5R)-CP-601927

    nAChR Neurological Disease
    CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS .
    CP-601932
  • HY-157053

    Others Cancer
    [Ru(dppn)2phen](PF6)2 (compound 4) is a polypyridylruthenium compound used in photodynamic therapy (PDT). [Ru(dppn)2phen](PF6)2 is normally nontoxic under dark conditions and induces mitochondrial respiratory damage upon light exposure. [Ru(dppn)2phen](PF6)2 exhibits high levels of singlet oxygen quantum yield and phototoxicity against cancer cells .
    [Ru(dppn)2phen](PF6)2
  • HY-147720

    γ-secretase Neurological Disease
    5-{8-[(3,4'- difluoro [1,1'- biphenyl]-4-yl) methoxy] - 2-methylimidazo [1,2-a] pyridin-3-yl}-n-methylpyridin-2-formamide (1o) showed high potency in vitro and brain exposure, inducing brain a β 42 levels were significantly reduced and showed undetectable inhibition of cytochrome P450 enzymes. In addition, compound 1o showed excellent anti cognitive deficit effect in AD model mice.
    γ-Secretase modulator 11
  • HY-147859

    Amyloid-β Neurological Disease
    BChE-IN-8 (compound 20) is an orally active, potent and BBB-penetrated BChE (butyrylcholinesterase) inhibitor, with IC50 values of 0.15 nM (eqBChE, equine serum BChE) and 45.2 nM (hBChE), respectively. High stability of BChE-IN-8 contributes to significantly improved blood concentration and tissue exposure. BChE-IN-8 can exert neuro-protecting and cognition improving properties through multiple modulations, including cholinergic system, Aβ aggregation, neuropeptide levels. BChE-IN-8 can be used for Alzheimer's disease (AD) research .
    BChE-IN-8
  • HY-12545

    PbTx-3

    Sodium Channel Inflammation/Immunology
    Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na + channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain) . Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na + channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation .
    Brevetoxin-3
  • HY-W099594

    Benzyldimethyldodecylammonium bromide

    Biochemical Assay Reagents Others
    N-Benzyl-N, N-dimethyldodecan-1-aminium bromide, also known as Benzalkonium Chloride (BAC), is a quaternary ammonium compound widely used as an antimicrobial and surfactant in various industries. BAC is commonly used as a disinfectant and antiseptic in a variety of products including hand sanitizers, disinfectant wipes and eye drops. Its ability to kill bacteria, viruses and fungi makes it an effective tool in preventing the spread of infection. BAC is also used as a preservative and disinfectant in the food industry. It is added to food packaging and processing equipment to prevent the growth of microorganisms and increase the shelf life of foods. Additionally, BACs are found in many household products such as cleaning solutions, fabric softeners and personal care products. Its surfactant properties allow it to be used to reduce surface tension and increase the effectiveness of cleaning agents. Although BAC has many uses, ingestion or exposure to high concentrations of BAC can cause skin irritation and other adverse effects.
    Benzalkonium bromide

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