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high exposure

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29

Inhibitors & Agonists

3

Biochemical Assay Reagents

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1

Isotope-Labeled Compounds

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15043
    ELN-441958

    		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
    Irpagratinib

    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-163087
    PT-91

    		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-155992
    WLB-89462

    		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-125920
    Lauroylsarcosine sodium

    		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-130609A
    Aβ42-IN-1 free base

    		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
    AR antagonist 5

    		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-130609
    Aβ42-IN-1

    		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-W653780
    Dimethyl phosphorothioate

    DMTP; O,O-Dimethyl phosphorothionate

    		 Endogenous Metabolite Others
    Dimethyl phosphorothioate (DMTP; O,O-Dimethyl phosphorothionate) is a metabolite of organophosphate pesticides. Dimethyl phosphorothioate can be used as a biomonitoring indicator for assessing pesticide exposure levels of organophosphate pesticides and identifying high-risk groups .
    Dimethyl phosphorothioate
  • HY-156593
    ROCK-IN-9

    		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-143439
    LX-039

    		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-114652
    AalphaC

    2-Amino-α-carboline; AαC

    		 Endogenous Metabolite Cancer
    AalphaC (AαC) is a potential carcinogen with carcinogenic activity. AalphaC is an important biomarker in tobacco smoke and is associated with tobacco smoke exposure. Urinary concentrations of AalphaC are significantly higher in dedicated smokers than in non-smokers, indicating its importance in monitoring tobacco exposure. AalphaC levels increase significantly with increasing serum nicotine levels, indicating its close relationship with tobacco use. In addition, consuming high-temperature cooked beef significantly increases the amount of AalphaC in urine, while consuming vegetables is associated with a decrease in AalphaC concentrations. Smoking half a pack of cigarettes is associated with a significant increase in the amount of AalphaC, which further confirms the biological activity of AalphaC and its association with dietary habits .
    AalphaC
  • HY-12570
    CK2-IN-9

    		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-105110
    SCH 39304

    SM-8668

    		 Fungal Infection
    SM-8668 is an effective orally active antifungal agent, with median effective doses (ED50) of 0.18, 3.7, and 5.9 mg/kg for systemic candidiasis, aspergillosis, and cryptococcosis in mice, respectively. Pharmacokinetic studies in mice and rats indicate that SM-8668 has a long half-life and a high total exposure. SM-8668 can be used in anti-infective research .
    SCH 39304
  • HY-125920R
    Lauroylsarcosine sodium (Standard)

    		Biochemical Assay Reagents Others
    Lauroylsarcosine (sodium) (Standard) is the analytical standard of Lauroylsarcosine (sodium). This product is intended for research and analytical applications. 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 (Standard)
  • HY-112142A
    (Rac)-AB-423

    DVR-23

    		 HBV Inflammation/Immunology
    (Rac)-AB-423 (DVR-23) is an anti-HBV candidate compound with promising anti-HBV activity. (Rac)-AB-423 showed no induction of CYP1A2, CYP3A4, or CYP2B6 enzyme activity at high concentrations. (Rac)-AB-423 exhibited desirable pharmacokinetic properties, enabling good systemic exposure and high oral bioavailability. (Rac)-AB-423 achieved more than 2 log viral load reduction in the hydrodynamic injection (HDI) HBV mouse model .
    (Rac)-AB-423
  • HY-162940
    MerTK/Axl-IN-1

    		TAM Receptor Inflammation/Immunology Cancer
    MerTK/Axl-IN-1 (Compound A-910) is a potent and selective dual MerTK/Axl inhibitor, with IC50s of 4.2 and 8.8 nM in Ba/F3, and 0.2 and 0.9 nM in HTRF. MerTK/Axl-IN-1 results in pMerTK inhibition in vivo. MerTK/Axl-IN-1 has long half-life, high oral exposure and bioavailability .
    MerTK/Axl-IN-1
  • HY-169310
    ATM Inhibitor-11

    		ATM/ATR Cancer
    ATM Inhibitor-11 (Compound 1) is an inhibitor for ATM with an IC50 of 0.32 nM. ATM Inhibitor-11 inhibits the KAP1 phosphorylation with an IC50 of 0.97 nM. ATM Inhibitor-11 exhibits high exposure in the brain, heart and plasma of ICR mouse. ATM Inhibitor-11 exhibits anti-tumor efficacy in NCI-H441 xenograft mouse model .
    ATM Inhibitor-11
  • HY-14375
    CB 300919

    		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 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    CB 300919
  • HY-W700491
    AalphaC-15N3

    2-Amino-α-carboline-15N3; AαC-15N3

    		 Isotope-Labeled Compounds Endogenous Metabolite Cancer
    AalphaC- 15N3 (2-Amino-α-carboline- 15N3) is 15N labeled AalphaC. AalphaC (AαC) is a potential carcinogen with carcinogenic activity. AalphaC is an important biomarker in tobacco smoke and is associated with tobacco smoke exposure. Urinary concentrations of AalphaC are significantly higher in dedicated smokers than in non-smokers, indicating its importance in monitoring tobacco exposure. AalphaC levels increase significantly with increasing serum nicotine levels, indicating its close relationship with tobacco use. In addition, consuming high-temperature cooked beef significantly increases the amount of AalphaC in urine, while consuming vegetables is associated with a decrease in AalphaC concentrations. Smoking half a pack of cigarettes is associated with a significant increase in the amount of AalphaC, which further confirms the biological activity of AalphaC and its association with dietary habits .
    AalphaC-15N3
  • HY-138879B
    CP-601932

    (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
    [Ru(dppn)2phen](PF6)2

    		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-162944
    NA-Ir

    		Ferroptosis Mitochondrial Metabolism STING Autophagy Cancer
    NA-Ir is a Ferroptosis inducer. NA-Ir targets mitochondrial DNA (mtDNA) and activates the cGAS-STING pathway to induce ferritinophagy (Autophagy), while also generating reactive oxygen species (ROS) through photodynamic therapy (PDT), depleting glutathione (GSH), and downregulating glutathione peroxidase 4 (GPX4), thereby triggering lipid peroxidation and Ferroptosis. NA-Ir exhibits higher anticancer activity under light exposure and selectively inhibits cancer cells with high H2S levels .
    NA-Ir
  • HY-147720
    γ-Secretase modulator 11

    		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
    BChE-IN-8

    		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
    Brevetoxin-3

    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-169308
    EGFR-IN-132

    		EGFR Cancer
    EGFR-IN-132 (Compound 23) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC50 of 1.6, 0.025, 0.019, 0.022, and 0.029 nM. EGFR-IN-132 exhibits good pharmacokinetics characteristics with high oral exposure .
    EGFR-IN-132
  • HY-169309
    EGFR-IN-133

    		EGFR Cancer
    EGFR-IN-133 (Compound 24) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC50 of 0.1, 0.044, 0.036, 0.04, and 0.054 nM. EGFR-IN-133 exhibits good pharmacokinetics characteristics with high oral exposure .
    EGFR-IN-133
  • HY-W099594
    Benzalkonium bromide

    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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