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AUC

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9

Inhibitors & Agonists

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-146012
    HIV-1 protease-IN-4

    		HIV Infection
    HIV-1 protease-IN-4 (Compound II-22) is a potent HIV-1 protease inhibitor. HIV-1 protease-IN-4 is a proagent of atazanavir. HIV-1 protease-IN-4 as a proagent that delivers the parent 1 to rat plasma with a 5-fold higher AUC and 67-fold higher C24 when compared to oral administration of the parent agent .
    HIV-1 protease-IN-4
  • 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-132596
    Tivanisiran

    SYL1001

    		 Small Interfering RNA (siRNA) TRP Channel Neurological Disease
    Tivanisiran (SYL1001) is a siRNA used for the study of dry eye disease. Tivanisiran was designed to silence transient receptor potential vanilloid 1 (TRPV1) .
    Tivanisiran
  • HY-153256
    EP3 antagonist 4

    		Prostaglandin Receptor Metabolic Disease
    EP3 antagonist 4 (Compound 28) is an EP3 antagonist, with a Ki value of 2 nM for hEP. EP3 antagonist 4 shows low in vivo clearance, high oral AUC, and good bioavailability in the rat full PK studies. EP3 antagonist 4 can be used for research of beta cell dysfunction in diabetes .
    EP3 antagonist 4
  • HY-118683
    KR-31378

    		Potassium Channel Others
    KR-31378 is a neuroprotectant with dose-dependent pharmacokinetic properties and relevant activity in rats. After intravenous and oral administration of KR-31378 in rats, its pharmacokinetic parameters showed dose-dependent changes, such as decreased clearance with increasing doses, good oral absorption, and comparable AUCs for intravenous and oral administration at different doses.
    KR-31378
  • HY-168595
    CSNK2-IN-2

    		Casein Kinase Infection
    CSNK2-IN-2 (compound 2) is an orally active CSNK2 inhibitor. CSNK2-IN-2 has an IC50 of 29 μM against CLK11. CSNK2-IN-2 has a half-life of 2.5 h and an AUC of 10,100 h × nM. CSNK2-IN-2 can be used in antiviral studies .
    CSNK2-IN-2
  • HY-114770
    (E,E)-GLL398

    		Estrogen Receptor/ERR Cancer
    (E,E)-GLL398 is a selective estrogen receptor degrader with potent binding activity to ERα (IC50 = 1.14 nM). (E,E)-GLL398 can effectively degrade ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM). The introduced boronic acid group of (E,E)-GLL398 gives it superior oral bioavailability, with an AUC of 36.9 μg·h/mL in rats, which is significantly higher than that of GW7604 .
    (E,E)-GLL398
  • HY-163982
    FOXJ1 agonist 1

    		NF-κB FOXO Inflammation/Immunology
    FOXJ1 agonist 1 (compound 16c) is an orally effective small molecule that can effectively enhance the expression of FOXJ1. Foxj1-IN-1 acts on the mammalian airway system composed of multiciliated cells (MCC) to prevent the development and onset of chronic obstructive pulmonary disease (COPD). Foxj1-IN-1 can induce the production of motile cilia in the respiratory system of zebrafish and mammals, and inhibit elastase-induced COPD mouse models. Foxj1-IN-1 has good liver microsomal stability, in vivo PK curve and AUC; it has no significant inhibition of CYP and hERG, and does not have significant cytotoxicity .
    FOXJ1 agonist 1
  • HY-159912
    pan-TEAD-IN-1

    		YAP Cancer
    pan-TEAD-IN-1 (Compound 3) is an orally active pan-TEAD inhibitor targeting the palmitoylation site of TEAD, disrupting its interaction with the coactivators YAP/TAZ, thereby suppressing the transcriptional upregulation of oncogenes (e.g., Ctgf and Cyr61) in the Hippo signaling pathway. pan-TEAD-IN-1 exhibits excellent activity with a luciferase IC50 of 0.36 nM and an H226 cell IC50 of 1.52 nM. It also shows favorable pharmacokinetics (AUC0–∞ = 228.7 μg/mL·min, T1/2 = 183.9 min). In TEAD-dependent xenograft mouse models, pan-TEAD-IN-1 significantly inhibited tumor growth, showing promise for research in TEAD-dependent cancers .
    pan-TEAD-IN-1

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