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Pharmacokinetics (PK)

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18353
    mTOR inhibitor-3
    3 Publications Verification

    		 mTOR Cancer
    mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
    mTOR inhibitor-3
  • HY-143889
    Senexin C

    		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-163825
    RNB-61

    		Cannabinoid Receptor Neurological Disease Inflammation/Immunology
    RNB-61 is an oral active agonist of cannabinoid CB2 receptor (CB2R), with the Ki ranging from 0.13 nM to 1.81 nM. RNB-61 has nephroprotective and/or antifibrotic effects. RNB-61 has negligible penetration into the brain .
    RNB-61
  • HY-168025
    VU6007496

    		nAChR Neurological Disease
    VU6007496 is a highly selective and CNS penetrant M1 positive allosteric modulator (PAM). VU6007496 shows excellent pharmacokinetics (PK) .
    VU6007496
  • HY-163721
    CDK7-IN-29

    		CDK Cancer
    CDK7-IN-29 (compound 20) is an inhibitor of CDK7 with an IC50 value of 1.4 nM. CDK7-IN-29 has oral activity and good pharmacokinetic (PK) properties .
    CDK7-IN-29
  • HY-126973
    BI-1230

    		HCV Protease Infection
    BI-1230, a chemical probe, is potent and digit nanomolar inhibitor of HCV NS3 protease and of viral replication. BI-1230 is also highly selective against other serine/cysteine proteases. BI-1230 shows good Pharmacokinetic(PK) activity .
    BI-1230
  • HY-159581
    URAT1&XO inhibitor 3

    		URAT1 Others
    URAT1&XO inhibitor 3 (compound 27) is an orally active anti-gout agent targeting XO (IC50: 35 nM) and URAT1 (IC50: 31 nM). URAT1&XO inhibitor 3 has good pharmacological and pharmacokinetic (PK) characteristics and in vivo safety .
    URAT1&XO inhibitor 3
  • HY-152535
    ATV041

    		HSV Infection Inflammation/Immunology
    ATV041 is an orally active Ibuprofen (HY-78131) and nucleotide analogue. ATV041 improves oral pharmacokinetic (PK) profile and tissue distribution with anti-mouse hepatitis virus (MHV) activity. ATV041 reduces viral load, tissue damage and virus-induced inflammation in a dose-dependent manner .
    ATV041
  • HY-149982
    IDO1-IN-22

    		Indoleamine 2,3-Dioxygenase (IDO) Inflammation/Immunology Cancer
    IDO1-IN-22 (Compound 3) is a IDO1 inhibitor (biochemical hIDO1 IC50: 67.4 nM, HeLa hIDO1 IC50: 17.6 nM). IDO1-IN-22 has excellent antitumor efficacy in LLC xenograft model, as well as desirable pharmacokinetic (PK) profile .
    IDO1-IN-22
  • HY-158119A
    PSMA-trillium

    		PSMA Cancer
    PSMA-trillium is a PSMA targeting compound, consisting of a PSMA targeting molecule (PSMA binder), a Macropa chelating molecule, and a group that regulates pharmacokinetics (PK modifier). PSMA-trillium is a non-radioactive form of Actinium-225-PSMA-Trillium (BAY 3563254) with improved PSMA targeting and pharmacokinetic properties. PSMA-trillium can bind Ac through the Macropa chelating molecule, or the radioactive isotope 225Actinium. Actinium-225-PSMA-Trillium is a potent inhibitor of metastatic castration-resistant prostate cancer (mCRPC) .
    PSMA-trillium
  • HY-109052
    Atabecestat
    1 Publications Verification

    JNJ-54861911

    		 Beta-secretase Neurological Disease
    Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment .
    Atabecestat
  • HY-112081
    BAY-707

    		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-158122
    Lys(CO-C3-p-I-Ph)-O-tBu

    		DNA-PK Cancer
    Lys(CO-C3-p-I-Ph)-O-tBu is a pharmacokinetic modifier (PK modifier) that can improve the pharmacokinetic properties of PSMA ligand molecules. Lys(CO-C3-p-I-Ph)-O-tBu can increase the residence time of PSMA ligand in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-O-tBu also reduces salivary gland absorption, possibly extending the half-life of the active compound .
    Lys(CO-C3-p-I-Ph)-O-tBu
  • HY-163507
    ALK5-IN-79

    		Anaplastic lymphoma kinase (ALK) Cancer
    ALK5-IN-79 (compound 57) is an ALK inhibitor with anticancer activity, by blocking TGF-β1/SMAD signaling pathway. ALK5-IN-79 attenuates the production of extracellular matrix (ECM) and deposition of collagen. ALK5-IN-79 exhibits adequate pharmacokinetic (PK) properties and good in vivo tolerance.
    ALK5-IN-79
  • HY-132296
    GSK215
    1 Publications Verification

    		 FAK PROTACs Cancer
    GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect .
    GSK215
  • HY-151915
    ATR-IN-20

    		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-157928
    Keap1-Nrf2-IN-18

    		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-178028
    PRMT5-IN-53

    		Histone Methyltransferase Cancer
    PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis (FAP) .
    PRMT5-IN-53
  • HY-19500
    SC-75416

    		COX Others
    SC-75416 is a selective cyclooxygenase-2 inhibitor. Its pharmacokinetic/pharmacodynamic (PK/PD) model was used for development and clinical trial simulation to design a study protocol to verify its analgesic effect in a post-oral surgery pain model. The simulation results showed that 360 mg of SC-75416 may provide better pain relief than 400 mg of ibuprofen. The actual clinical trial results confirmed this hypothesis, and 360 mg of SC-75416 was indeed superior to 400 mg of ibuprofen in pain relief. The PK/PD model of SC-75416 showed good predictive performance and successfully predicted its clinical effect. These research results show that SC-75416, as a new selective COX-2 inhibitor, has potential clinical application value in the management of post-oral surgery pain.
    SC-75416
  • HY-158118
    Lys(CO-C3-p-I-Ph)-OMe

    		DNA-PK Cancer
    Lys(CO-C3-p-I-Ph)-OMe is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules (such as Ac-PSMA-trillium). Lys(CO-C3-p-I-Ph)-OMe can increase the residence time of Ac-PSMA-trillium in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-OMe also reduces salivary gland absorption of Ac-PSMA-trillium, potentially extending its half-life. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .
    Lys(CO-C3-p-I-Ph)-OMe

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