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good+bioavailability

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12

Inhibitors & Agonists

1

Screening Libraries

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12839
    p38 MAPK-IN-1
    10+ Cited Publications

    		 p38 MAPK Autophagy Inflammation/Immunology
    p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC50 of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.
    p38 MAPK-IN-1
  • HY-170419
    APJ receptor agonist 10

    		Apelin Receptor (APJ) Cardiovascular Disease
    APJ receptor agonist 10 (Compound I choline salt) modulates the activity of APJ receptor and can be used in research about pulmonary arterial hypertension. APJ receptor agonist 10 exhibits good bioavailability other than its free base form .
    APJ receptor agonist 10
  • HY-148565
    SERT-IN-2

    		Serotonin Transporter Neurological Disease
    SERT-IN-2 is a potent SERT inhibitor (IC50=0.58 nM) with promising anti-depression efficacy. SERT-IN-2 shows good bioavailability of 83.28% in rats. SERT-IN-2 can cross the blood-brain barrier .
    SERT-IN-2
  • HY-160073A
    Florensocatib hydrate

    		Dipeptidyl Peptidase Inflammation/Immunology
    Florensocatib hydrate is a DPP1 inhibitor (IC50: 1.6 nM). Florensocatib hydrate has good bioavailability and pharmacokinetic characteristics, and can be used for research of inflammatory disease .
    Florensocatib hydrate
  • HY-174988
    JAK2-IN-13

    		JAK STAT Cancer
    JAK2-IN-13 is a potent and orally active JAK2 inhibitor with an IC50 of 54.7 nM. JAK2-IN-13 downregulates the expressions of p-STAT3 and p-STAT5. JAK2-IN-13 exhibits good bioavailability and potent inhibition of rhEPO-induced extramedullary erythropoiesis and polycythemia vera. JAK2-IN-13 can be used for the study of myeloproliferative neoplasms .
    JAK2-IN-13
  • HY-161354
    JAK3 covalent inhibitor-2

    		JAK Apoptosis Inflammation/Immunology
    JAK3 covalent inhibitor-2 (compound J1b) is a selective, orally potent JAK3 inhibitor (IC50=7.2 nM) with low toxicity, anti-inflammatory activity and good bioavailability .
    JAK3 covalent inhibitor-2
  • 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-135711
    PDE8B-IN-1

    		Phosphodiesterase (PDE) Metabolic Disease
    PDE8B-IN-1 is a selective inhibitor of phosphodiesterase 8B (PDE8B) with the activity of enhancing insulin secretion. PDE8B-IN-1 showed good efficacy in high-throughput screening and optimized its ligand efficiency through rapid deconstruction. PDE8B-IN-1 showed high target selectivity and good bioavailability in preclinical development, providing a basis for exploring its potential inhibitory use .
    PDE8B-IN-1
  • HY-146460
    Antimicrobial agent-2

    		Reactive Oxygen Species (ROS) Infection
    Antimicrobial agent-2 (compound V-a) is a broad-spectrum antimicrobial agent, possessing inhibitory activity against various Gram-positive and -negative bacteria. Antimicrobial agent-2 has excellent inhibitory effect on Methicillin-resistant Staphylococcus aureus (MRSA) with a MIC of 1 μg/mL. Antimicrobial agent-2 can effectively damage the membrane and lead to the leakage of protein, also can induce the generation of ROS. Antimicrobial agent-2 exhibits low toxicity, no obvious resistance and good bioavailability .
    Antimicrobial agent-2
  • HY-161940
    PCSK9-IN-30

    		PCSK9 Cardiovascular Disease
    PCSK9-IN-30 (Compound 3f) is a PCSK9 inhibitor. PCSK9-IN-30 interacts with a cryptic binding groove of PCSK9, inhibiting the binding of PCSK9 to the low-density lipoprotein receptor (LDLR) (IC50 = 537 nM), restoring the uptake of low-density lipoprotein (LDL) by liver cells, and ultimately reducing plasma cholesterol levels. PCSK9-IN-30 exhibits good bioavailability in mice and can be used for research in the field of cardiovascular diseases .
    PCSK9-IN-30
  • HY-159091
    HIV-1 integrase inhibitor 12

    		HIV Integrase Infection
    HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC50 of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats .
    HIV-1 integrase inhibitor 12
  • HY-122058
    KRH-3955

    		HIV Infection
    KRH-3955 is a CXCR4 antagonist with good bioavailability and potent anti-HIV-1 activity. KRH-3955 can effectively inhibit the replication of X4 HIV-1, including clinical isolates from different donors. KRH-3955 also shows activity against recombinant X4 HIV-1 containing reverse transcriptase, protease and tyrosinase resistance mutations. KRH-3955 can inhibit the binding of SDF-1alpha to CXCR4 and calcium ion signaling through this receptor. KRH-3955 inhibits the binding of an antibody against CXCR4 to CXCR4, showing a potent antagonistic effect on CXCR4. KRH-3955 shows an oral bioavailability of 25.6% in rats and can inhibit the replication of X4 HIV-1 in vivo .
    KRH-3955

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