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systemic exposure

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25

Inhibitors & Agonists

1

Isotope-Labeled Compounds

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15234
    Fluticasone furoate

    		Glucocorticoid Receptor Inflammation/Immunology
    Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment .
    Fluticasone furoate
  • HY-B1325
    Cefuroxime axetil

    		Bacterial Antibiotic Infection Inflammation/Immunology
    Cefuroxime axetil is an orally effective broad-spectrum β-lactam antibiotic that targets bacterial penicillin-binding proteins (PBPs, such as PBP3 and PBP1). Cefuroxime axetil inhibits cell wall synthesis, leading to bacterial lysis and death, with a minimum inhibitory concentration (MIC) of 0.12-4 mg/L for non-typeable Haemophilus influenzae (NTHi). Cefuroxime axetil is hydrolyzed by esterase to the active ingredient Cefuroxime (HY-B1256A) after oral absorption. Topical administration of Cefuroxime via bioadhesive nanoparticles (BNPs) can prolong the drug's retention time in the middle ear (≥7 days). Cefuroxime axetil can be used in the study of otitis media (especially NTHi infection). Cefuroxime axetil can achieve precise antibacterial effects through oral or topical nano-delivery systems, reducing systemic exposure and the risk of antibiotic resistance .
    Cefuroxime axetil
  • HY-109163
    Treprostinil palmitil

    INS-1009

    		 Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Treprostinil palmitil is a long-acting inhaled pulmonary vasodilator prodrug of Treprostinil (HY-100441), formulated in a lipid nanoparticle (LNP). Treprostinil palmitil can inhibit pulmonary vascular remodeling induced by Su/Hx challenge in rats. Treprostinil palmitil can induce cough. Treprostinil palmitil demonstrates a sustained presence in the lungs with reduced systemic exposure and prolonged inhibition of hypoxia-induced pulmonary vasoconstriction in vivo. Treprostinil palmitil can be studied in research for pulmonary arterial hypertension and interstitial lung disease .
    Treprostinil palmitil
  • HY-W725179
    VK-2019

    		EBV Cancer
    VK-2019 is an orally bioavailable selective inhibitor of EBNA1. By binding to the protein-DNA interface to interfere with the recruitment and anchoring of the viral DNA replication machinery, VK-2019 effectively blocks the replication and proliferation of EBV in latently infected cells. VK-2019 reduces the copy number and gene expression level of Epstein-Barr virus in tumor cells, decreases the number of EBER-positive cells, and exhibits significant antiviral, immunomodulatory and antiproliferative activities. VK-2019 successfully inhibits tumor growth in EBV-dependent xenograft models. VK-2019 has favorable systemic exposure and acceptable safety profiles, and is widely used in research on advanced nasopharyngeal carcinoma and various EBV-associated cancers .
    VK-2019
  • HY-B1444
    Isoconazole nitrate
    2 Publications Verification

    		 Bacterial Fungal Antibiotic Infection
    Isoconazole nitrate is a broad-spectrum antimicrobial agent with a highly effective antimycotic and gram-positive antibacterial activity, exhibiting a rapid rate of absorption and low systemic exposure potential .
    Isoconazole nitrate
  • HY-157763
    Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1

    		PROTAC-Linker Conjugates for PAC Btk Cancer
    Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 is a cleavable linker-payload conjugate and cereblon-binding BTK bifunctional degrader. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 induces BTK degradation and exerts cytotoxic effects when delivered via CD79b monoclonal antibody. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1, when formulated as a CD79b antibody-drug conjugate, achieves sustained in vivo BTK degradation in tumor-bearing mice with reduced systemic payload exposure. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 can be used for the research of activated b-cell-like diffuse large b-cell lymphoma (ADC linker: (HY-130944); PROTAC: (HY-163295)) .
    Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1
  • HY-156685
    EDI048

    		PI4K Parasite Infection Metabolic Disease Cancer
    EDI048 is an orally active, gut-restricted parasiticidal agent. EDI048 specifically binds to the ATP-binding site of Cryptosporidium phosphatidylinositol 4-kinase (CpPI (4) K), blocks parasite membrane biogenesis, arrests the pathogen at the schizont stage, and thus irreversibly clears the infection. EDI048 is rapidly converted to an inactive carboxylic acid metabolite via hepatic first-pass metabolism, with extremely low systemic exposure, good safety profile, and no cardiotoxicity, genotoxicity or off-target effects. EDI048 is used in studies of intestinal cryptosporidiosis in children .
    EDI048
  • HY-15234S
    Fluticasone furoate-d3

    		Isotope-Labeled Compounds Glucocorticoid Receptor Inflammation/Immunology
    Fluticasone furoate-d3 is deuterium labeled Fluticasone furoate. Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment .
    Fluticasone furoate-d3
  • HY-15234R
    Fluticasone furoate (Standard)

    		Reference Standards Glucocorticoid Receptor Inflammation/Immunology
    Fluticasone furoate (Standard) is the analytical standard of Fluticasone furoate. This product is intended for research and analytical applications. Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment .
    Fluticasone furoate (Standard)
  • HY-174383
    PDE3/4-IN-2

    		Phosphodiesterase (PDE) Inflammation/Immunology
    PDE3/4-IN-2 is a dual PDE3A and PDE4B1 inhibitor, with an IC50 of 0.13 nM against PDE3A and 50 nM against PDE4B1. PDE3/4-IN-2 exhibits higher systemic exposure and longer retention time in lung tissues in ICR mice. PDE3/4-IN-2 can be used in research on respiratory diseases such as asthma and chronic obstructive pulmonary disease, as well as autoimmune inflammation-related studies .
    PDE3/4-IN-2
  • HY-B1444R
    Isoconazole nitrate (Standard)

    		Reference Standards Bacterial Fungal Antibiotic Infection
    Isoconazole (nitrate) (Standard) is the analytical standard of Isoconazole (nitrate). This product is intended for research and analytical applications. Isoconazole nitrate is a broad-spectrum antimicrobial agent with a highly effective antimycotic and gram-positive antibacterial activity, exhibiting a rapid rate of absorption and low systemic exposure potential .
    Isoconazole nitrate (Standard)
  • HY-W762012
    Octachlorodibenzo-p-dioxin

    OCDD

    		 Cytochrome P450 Environmental Pollutants Others
    Octachlorodibenzo-p-dioxin (OCDD) is an environmental contaminant but is not acutely toxic. In rats, Octachlorodibenzo-p-dioxin (50 μg/kg i.v. or 50-5000 μg/kg p.o.) has a systemic elimination half-life of 3-5 months and accumulates and concentrates in the liver and adipose tissue after low-dose, repeated exposure. Repeated administration of octachlorodibenzo-p-dioxin causes increases in 7-ethoxyresorufin-O-deethylase (7-EROD) activity and total cytochrome P-450 levels .
    Octachlorodibenzo-p-dioxin
  • HY-163672
    Glucocorticoid receptor modulator 3

    		Glucocorticoid Receptor Metabolic Disease Inflammation/Immunology
    Glucocorticoid receptor modulator 3 (Payload 6) is a thioester-containing glucocorticoid receptor modulator (IC50=0.6 nM). Glucocorticoid receptor modulator 3 is designed to inactivate unconjugated payloads rapidly through liver metabolism, thereby minimizing systemic exposure. Glucocorticoid receptor modulator 3 can be utilized in the development of antibody-drug conjugates (ADCs) targeting autoimmune diseases .
    Glucocorticoid receptor modulator 3
  • HY-147927
    Human enteropeptidase-IN-1

    		Enteropeptidase Metabolic Disease
    Human enteropeptidase-IN-1 (compound 6b) is a highly potent, orally active and low systemic exposure enteropeptidase inhibitor. Human enteropeptidase-IN-1 boosts the increase in fecal protein output, and exhibits potent body weight loss in diet-induced obese (DIO) rat model. Human enteropeptidase-IN-1 can be used for anti-obesity research .
    Human enteropeptidase-IN-1
  • 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-147927A
    (S)-Human enteropeptidase-IN-1

    		Enteropeptidase Metabolic Disease
    (S)-Human enteropeptidase-IN-1 (Compound 6c) is an orally active enteropeptidase inhibitor with low systemic exposure (IC50 (initial): 26 nM; IC50 (app): 1.8 nM). (S)-Human enteropeptidase-IN-1 promotes increased fecal protein output and effectively reduces body weight in a diet-induced obese (DIO) rat model. (S)-Human enteropeptidase-IN-1 inhibits enteropeptidase via a reversible covalent mechanism and prolongs the enzyme inactivation time. (S)-Human enteropeptidase-IN-1 can be used in anti-obesity research .
    (S)-Human enteropeptidase-IN-1
  • 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-15042
    MK 0686

    		Bradykinin Receptor Metabolic Disease
    MK 0686, a potent bradykinin B1 receptor antagonist, demonstrates autoinduction of metabolism in rhesus monkeys after oral administration. It undergoes significant biotransformation primarily via oxidation pathways, leading to the formation of metabolites like M11 and M13 in rhesus liver microsomes. This metabolic induction is mediated by CYP2C75, as evidenced by increased mRNA expression, protein levels, and catalytic activity of this enzyme in hepatocytes and liver microsomes from MK 0686-treated animals. The autoinduction phenomenon suggests that MK 0686 enhances its own metabolism by upregulating CYP2C75, potentially influencing its systemic exposure and pharmacokinetics over time .
    MK 0686
  • HY-185398
    Amikacin liposome

    Amikacin disulfate liposome; Liposomal amikacin

    		 Liposome Antibiotic Bacterial Infection
    Amikacin liposome is a liposome-encapsulated form of Amikacin disulfate (HY-B0509B), an aminoglycoside antibiotic with antibactericidal avtivity. Amikacin liposome prolongs the release of amikacin in the lungs and reduces systemic exposure, thereby lowering systemic toxicity.
    Amikacin liposome
  • HY-123165
    NU7200

    		Drug Metabolite DNA-PK Metabolic Disease
    NU7200 is a metabolite of the DNA-PK inhibitor NU7026 (HY-15719) .
    NU7200
  • HY-181558
    Anticancer agent 303

    		Others Cancer
    Anticancer agent 303 is a selective, orally active anticancer agent belonging to the pyrazolopyridine derivatives. Anticancer agent 303 exhibits low cytotoxicity to healthy cells, with a selective window of approximately 2-fold between cancer cells and healthy cells. Anticancer agent 303 produces detectable systemic exposure in mice following intraperitoneal or oral administration. Anticancer agent 303 effectively inhibits the proliferation of prostate cancer and breast cancer cells .
    Anticancer agent 303
  • HY-182059
    GSTP1-IN-1

    		Glutathione S-transferase Reactive Oxygen Species (ROS) Cancer
    GSTP1-IN-1 is a selective GSTP1 inhibitor with an IC50 of 0.79 μM and a Kd of 0.63 μM. GSTP1-IN-1 inhibits the proliferation of gastric cancer cells, induces ROS production and depletes glutathione. GSTP1-IN-1 achieves systemic exposure and is well tolerated in xenograft mouse models, while inhibiting tumor growth. GSTP1-IN-1 can be used in gastric cancer-related research .
    GSTP1-IN-1
  • HY-181929
    RAI-20

    H018

    		 JAK Inflammation/Immunology
    RAI-20 (H018) is an orally active JAK1/JAK2 dual inhibitor (IC50=15.1 and 22.7 nM). RAI-20 exhibits excellent pharmacokinetic properties, including plasma stability, systemic exposure, and a long half-life. In a collagen-induced arthritis rat model, RAI-20 shows significant anti-inflammatory and anti-arthritic activities, effectively reducing paw swelling volume and arthritis index. RAI-20 can be used for research on the pathogenesis of rheumatoid arthritis .
    RAI-20
  • HY-181711
    nNOS-IN-6

    		NO Synthase Neurological Disease Cancer
    nNOS-IN-6 is a human neuronal nitric oxide synthase (hnNOS) inhibitor with a human hnNOS Ki of 16 nM, ~1800-fold selectivity over human eNOS, ~2900-fold selectivity over human iNOS, and a rat nNOS Ki of 34 nM.nNOS-IN-6 exhibits high effective permeability in PAMPA-BBB assays, crosses the blood-brain barrier, and shows sustained systemic exposure, low clearance, and robust brain penetration in mouse in vivo pharmacokinetic studies.nNOS-IN-6 can be used for the research of neurodegenerative diseases, melanoma .
    nNOS-IN-6
  • HY-138135
    OP-1118

    Fidaxomicin metabolite OP-1118

    		 NF-κB ERK Apoptosis Bacterial Infection
    OP-1118 (Fidaxomicin metabolite OP-1118) is an orally active dual inhibitor of NF-κB and ERK1/2, with low systemic plasma exposure, no accumulation, and primary excretion via feces. By inhibiting the phosphorylation of NF-κB and ERK1/2 and reducing the expression of pro-inflammatory cytokines, OP-1118 exerts significant anti-inflammatory, cytoprotective, anti-apoptotic and antibacterial activities. In Clostridium difficile infection models, OP-1118 effectively blocks toxin-mediated intestinal inflammation, cell rounding, histological damage and apoptosis, and its protective effect can be reversed by PMA (HY-18739) .
    OP-1118

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