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good pharmacokinetic profile

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21

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Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-130251
    DS18561882
    20+ Cited Publications

    Methylenetetrahydrofolate Dehydrogenase (MTHFD) Cancer
    DS18561882 is a highly potent, isozyme-selective methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with an IC50 value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 (IC50=0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile .
    DS18561882
  • HY-164729

    Antibody-Drug Conjugates (ADCs) Topoisomerase Apoptosis Cancer
    FZ-AD005 is a DLL3-targeting antibody-drug conjugate (ADC) with high selectivity, composed of the anti-DLL3 antibody FZ-A038 (HY-P990896), a dipeptide linker (Val-Ala), and DXd (HY-13631D). The Kd value of FZ-AD005 for human DLL3 ranges from 13.29 to 58.3 pmol/L. After binding to DLL3 on the cell surface, FZ-AD005 mediates endocytosis, and the payload DXd is released via cleavage by lysosomal cathepsins. DXd inhibits topoisomerase TopI to induce double-strand DNA breaks, cell cycle arrest and apoptosis, and FZ-AD005 exhibits bystander killing activity against adjacent DLL3-negative cells. FZ-AD005 shows stable circulation in vivo, has good tolerance and acceptable pharmacokinetic profiles in rats and cynomolgus monkeys, and effectively inhibits the growth of DLL3-expressing tumor cells. FZ-AD005 serves as a promising candidate molecule for research on small cell lung cancer and human neuroendocrine prostate cancer .
    FZ-AD005
  • HY-114237

    Sodium Channel Neurological Disease
    GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects .
    GDC-0276
  • HY-143889

    CDK Cancer
    Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability .
    Senexin C
  • HY-150654

    WDR5 Cancer
    WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM .
    WDR5-IN-5
  • HY-112081

    DNA/RNA Synthesis Cancer
    BAY-707, a chemical probe, is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy .
    BAY-707
  • HY-10096

    GSK-3 Neurological Disease
    TCS2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM. TCS2002 shows good pharmacokinetic profiles including favorable BBB penetration. TCS2002 can be used for the research of Alzheimer’s disease .
    TCS2002
  • HY-172914

    ATP Citrate Lyase Cardiovascular Disease Metabolic Disease
    ACLY-IN-1 is an orally active ACLY inhibitor. ACLY-IN-1 exhibits potent ACLY inhibitory activity (IC50 = 8.3 nM) and high binding affinity (KD = 72.0 nM) to ACLY. ACLY-IN-1 demonstrates good pharmacokinetic profiles and a potent in vivo hypolipidemic effect .
    ACLY-IN-1
  • HY-123353

    Neladenoson bialanate; BAY-1067197

    Adenosine Receptor Cardiovascular Disease
    Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases .
    Neladenoson dalanate
  • HY-132867

    Pim Cancer
    MNK/PIM-IN-1 represents an innovative dual MNK/PIM inhibitor with a good pharmacokinetic profile.
    MNK/PIM-IN-1
  • HY-174417

    Reverse Transcriptase HIV Potassium Channel Cytochrome P450 Infection
    NNRT-IN-10 is a potent, selective and orally active non-nucleoside HIV-1 reverse transcriptase (NNRTI) inhibitor with with an EC50 values ranging from 1.16 to 18.3 nM for HIV and its mutant strains. NNRT-IN-10 exhibits good pharmacokinetic properties and favorable safety profiles. NNRT-IN-10 can be used for the study of AIDS, caused by HIV-1 .
    NNRT-IN-10
  • HY-133018

    HCV Infection
    HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity .
    HCV-IN-7
  • HY-133018A

    HCV Cancer
    HCV-IN-7 hydrochloride is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 hydrochloride shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 hydrochloride has anti-viral activity .
    HCV-IN-7 hydrochloride
  • HY-115494

    Neladenoson bialanate hydrochloride; BAY-1067197 hydrochloride

    Adenosine Receptor Cardiovascular Disease
    Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) hydrochloride is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate hydrochloride has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases .
    Neladenoson dalanate hydrochloride
  • HY-170797

    Glycosidase Metabolic Disease
    α-Glucosidase-IN-80 (Compound 10n) is a potent competitive inhibitor of α-glucosidase, with an IC50 of 48.4 μM. α-Glucosidase-IN-80 has good pharmacokinetic properties and toxicity profiles and can be used in the research of diabetes-related diseases .
    α-Glucosidase-IN-80
  • HY-115989

    HCV Infection
    HCV-IN-38 is a potent, selective and orally active HCV inhibitor (EC50=15 nM, SI=431). HCV-IN-38 has high anti-HCV activity and low cytotoxicity. HCV-IN-38 has a good safety and oral pharmacokinetic profile .
    HCV-IN-38
  • HY-151915

    ATM/ATR mTOR Cancer
    ATR-IN-20 is a potent ATR (ATM/ATR) inhibitor with an IC50 of 3 nM. ATR-IN-20 possess an inhibitory effect on mTOR (IC50 of 18 nM) while displaying good selectivity against PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). ATR-IN-20 exhibits excellent pharmacokinetic profile (F = 30%), and has anticancer effects .
    ATR-IN-20
  • HY-170961

    Aminopeptidase Neprilysin Neurological Disease
    SDUY816 is an oral active dual APN/NEP inhibitor, with IC50 values of 0.68 μM for APN and 6.9 μM for NEP. SDUY816 exhibits analgesic effects and demonstrates good safety and pharmacokinetic profiles, with an oral bioavailability of 27% and a half-life of 4.02 hours in rats (oral administration, 10 mg/kg). SDUY816 has potential applications in the research of neuropathic pain disorders .
    SDUY816
  • HY-125279

    Parasite Inflammation/Immunology
    OAT-2068 is a selective, high activity and orally active inhibitor of mouse chitotriosidase (mCHIT1) (IC50=29 nM) and displays 143-fold selectivity over m AMCase (IC50=4170 nM). OAT-2068 displays a good pharmacokinetic profile and is an ideal tool to study the role of CHIT1 in biological systems, including animal models of human diseases .
    OAT-2068
  • HY-157928

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (KD = 0.0029 μM) .
    Keap1-Nrf2-IN-18
  • HY-P11617

    NF-κB ERK JNK p38 MAPK Interleukin Related Inflammation/Immunology
    CLP-d2 is a multi-target anti-inflammatory agent, osteoclastogenesis inhibitor and immunomodulator with superior pharmacokinetic properties to Daptomycin (HY-B0108) and good safety profiles. CLP-d2 inhibits the NF-κB and MAPK signaling pathways by reducing the expression levels of c-Fos and NFATc1, and decreasing the phosphorylation levels of IκBα, p65, ERK and JNK, thereby reducing the secretion of pro-inflammatory cytokines such as IL-6, TNF-α and IL-1β to exert anti-inflammatory activity. CLP-d2 inhibits intra-articular osteoclastogenesis in mice, alleviates bone erosion and joint swelling, reduces synovial hyperplasia and inflammatory cell infiltration, and decreases serum rheumatoid factor (RF) levels. CLP-d2 is applicable to related research on rheumatoid arthritis .
    CLP-d2

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