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Microsomal stability

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37

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-155354
    Antimalarial agent 33

    		Parasite Infection
    Antimalarial agent 33 (compound 5g) has antiplasmodial activity against erythrocytic and hepatic stages of Plasmodium with an EC50 of 1.1 μM for K1 P. falciparum strain. Antimalarial agent 33 demonstrats enhanced microsomal stability (T1/2=29 min). Antimalarial agent 33 has no significant cytotoxicity against primary hepatocytes .
    Antimalarial agent 33
  • HY-163350
    TUG-2208

    		GPR84 Inflammation/Immunology
    TUG-2208 (compound 42a) is a GPR84 agonist (pEC50=8.98) with low lipophilicity and good solubility, in vitro permeability and microsomal stability .
    TUG-2208
  • HY-146397
    TD-802

    		PROTACs Androgen Receptor Cancer
    TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research .
    TD-802
  • HY-163004
    Type II TRK inhibitor 2

    		Trk Receptor Cancer
    Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor with plasma stability and moderate hepatic microsomal stability. Type II TRK inhibitor 2 significantly inhibits Km-12, Ba/F3-TRKA G595R and Ba/F3-TRKA G667C cell proliferation (IC50: 4.1 nM, 41.5 nM, 1.4 nM). Type II TRK inhibitor 2 can be used to study NTRK fusion cancers .
    Type II TRK inhibitor 2
  • HY-146380
    S1427

    		Histone Demethylase Cancer
    S1427 is a tranylcypromine-derived LSD1 inhibitor with the IC50 of 390 nM and Ki of 80 nM. S1427 exhibits desirable hERG channel inhibition and microsomal stability profiles. Inhibition of LSD1 partially reduces the proliferation of cancer cells .
    S1427
  • HY-159174
    EPHA2/A4/GAK-IN-1

    		Ephrin Receptor Cyclin G-associated Kinase (GAK) Dengue virus Infection
    EPHA2/A4/GAK-IN-1 (compound 55) is a potent inhibitor of EPHA2/EPHA4 and GAK with KD values of 180.5 nM for EPHA2 and 19.2 nM for GAK, respectively. EPHA2/GAK-IN-1 shows an extrapolated half-life time of 4.6 h in a microsomal stability assay. EPHA2/GAK-IN-1 shows antiviral activity and prevents dengue virus infection of Huh7 liver cells .
    EPHA2/A4/GAK-IN-1
  • HY-155687
    PDE5-IN-10

    		Phosphodiesterase (PDE) Neurological Disease
    PDE5-IN-10 (compound 4b) is a potent PDE5 inhibitor with an IC50 of 20 nM. PDE5-IN-10 improves in vitro microsomal stability (t1/2 = 44.6 min) as well as excellent efficacy in restoring long-term potentiation. PDE5-IN-10 can be used for Alzheimer’s disease (AD) research .
    PDE5-IN-10
  • HY-146018
    HIV-1 inhibitor-23

    		HIV Infection
    HIV-1 inhibitor-23 (compound 12a) is a highly potent HIV-1 non-nucleoside reverse transcriptase inhibitor, with EC50s of 24.9 nM and 10.4 nM for HIV-1 WT and HIV-1 K103N, respectively. HIV-1 inhibitor-23 has low cytotoxicity (CC50 > 221 μM) and a favorable in vitro microsomal stability .
    HIV-1 inhibitor-23
  • HY-143757
    Cap-dependent endonuclease-IN-10

    		Influenza Virus Infection
    Cap-dependent endonuclease-IN-10 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-10 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo pharmacokinetic and in vivo pharmacodynamic properties, and better hepatic microsomal stability. Cap-dependent endonuclease-IN-10 has the potential for the research of viral infections (including influenza A, influenza B and influenza C) (extracted from patent WO2021129799A1, compound 1-1) .
    Cap-dependent endonuclease-IN-10
  • HY-160647
    CCR8 antagonist 3

    		CCR Inflammation/Immunology
    CCR8 antagonist 3 (compound 2) is a CCR8 antagonist with an IC50 value of 0.062 µM. CCR8 antagonist 3 shows human microsomal stability .
    CCR8 antagonist 3
  • HY-157932
    MR24

    		Hippo (MST) Cancer
    MR24, a G-5555 (HY-19635) derivative, is a mammalian STE20-like (MST) kinase inhibitor. MR24 selectively target MST3/4, with EC50 values of 57 and 583 nM, respectively .
    MR24
  • HY-168118
    Ferroptosis-IN-14

    		Ferroptosis Cancer
    Ferroptosis-IN-14 (compund 36) exhibits the potent anti-ferroptosis activity with an EC50 value of 0.58 ± 0.02 μM and possessed excellent anti-ferroptosis activity, microsomal and plasma stability .
    Ferroptosis-IN-14
  • HY-160031
    GLP-1R agonist 19

    		GLP Receptor Cardiovascular Disease
    GLP-1R agonist 19 (M3190) is a potent and selective GLP-1R agonist. GLP-1R agonist 19 has excellent plasma stability, liver microsomal stability, and low hERG toxicity .
    GLP-1R agonist 19
  • HY-156188
    AChE-IN-41

    		Others Others
    AChE-IN-41 (Compound 2) is a compound of the Galantamine Memantine hybrid. AChE-IN-41 has the inhibition ability of cholinesterase. AChE-IN-41 shows higher plasma stability and comparable microsomal stability in vitro, while showing lower half-life and faster clearance in vivo .
    AChE-IN-41
  • HY-121088
    Ceefourin 2

    		Others Cardiovascular Disease Others
    Ceefourin 2 is a potent and highly selective inhibitor of MRP4. Ceefourin 2 inhibits the transport of MRP4 substrates but is not selective for other ABC transporters. Ceefourin 2 shows lower cytotoxicity and higher microsomal and acid stability .
    Ceefourin 2
  • HY-D2095
    Medical fluorophore 33

    		Fluorescent Dye Cancer
    Medical fluorophore 33 is a novel quinoline-isoquinoline salt. Medical fluorophore 33 exhibits a strong fluorescent signal, good microsomal stability and high biocompatibility in vivo. Medical fluorophore 33 has antitumor activity in colorectal cancer mice .
    Medical fluorophore 33
  • HY-155047
    BDM91514

    		Bacterial Infection
    BDM91514 improves antibiotic potency through AcrB inhibition. BDM91514 prevents the growth of E. coliBW25113 (EC90: 8 μM) in the presence of 8 μg/mL Pyridomycin. BDM91514 has suitable plasma and microsomal stability .
    BDM91514
  • HY-162118
    RGH-122

    		Vasopressin Receptor Neurological Disease
    RGH-122 (compound 43) is an orally active, potent, selective, and hV1a receptor antagonist with Ki value of 0.3 nM and IC50 of 0.9 nM. RGH-122 showes microsomal stability with CLint value of 13/28/25 μL/min/mg .
    RGH-122
  • HY-147950
    PDE4-IN-10

    		Phosphodiesterase (PDE) TNF Receptor Inflammation/Immunology
    PDE4-IN-10 (compound 7a) is a potent PDE4 inhibitor, with an IC50 of 7.01 μM for PDE4B. PDE4-IN-10 shows selectivity, microsomal stability, inhibition of TNF-α and no major toxicities in vitro .
    PDE4-IN-10
  • HY-126254
    BI-4924
    1 Publications Verification

    		 Phosphoglycerate Dehydrogenase (PHGDH) Cancer
    BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h .
    BI-4924
  • HY-132174
    CHIKV-IN-2

    		Flavivirus Dengue virus Dihydroorotate Dehydrogenase Infection
    CHIKV-IN-2 is a potent inhibitor against Chikungunya virus (CHIKV), with excellent cellular antiviral activity (EC90=270 nM) and improved liver microsomal stability. CHIKV-IN-2 shows inhibitory activity against a cellular target Dihydroorotate Dehydrogenase (DHODH), which interacts with various viruses and regulate their replication via depleting intracellular pyrimidine pools .
    CHIKV-IN-2
  • HY-153970
    URAT1 inhibitor 7

    		URAT1 Inflammation/Immunology
    URAT1 inhibitor 7 (compound 10f) is a potent URAT1 inhibitor, with an IC50 of 12 nM. URAT1 inhibitor 7 exhibits microsomal stability (HLM <13 µL/min/mg). URAT1 inhibitor 7 also inhibits CYP2C9, with an IC50 of 4.2 μM. URAT1 inhibitor 7 can be used for gout research .
    URAT1 inhibitor 7
  • HY-147397
    PKM2 activator 3

    		Pyruvate Kinase Cancer
    PKM2 activator 3 is a potent PKM2 activator with an AC50 value of 90 nM. PKM2 activator 3 has good Caco-2 permeability, a low efflux ratio and high microsomal stability. PKM2 activator 3 can be used for researching anticancer .
    (AC50: the concentration which gives 50% activation of enzyme.)
    PKM2 activator 3
  • HY-152614
    Antimalarial agent 19

    		Parasite Infection
    Antimalarial agent 19 (compound 6e) is an antimalarial active agent. Antimalarial agent 19 has antimalarial activity for the blood stage of P. falciparum K1 and P. berghei with EC50 values of 0.3 µM, 15.3 µM, respectively. Antimalarial agent 19 has good aqueous solubility, intestinal permeability and microsomal stability compared to gamhepathiopine .
    Antimalarial agent 19
  • HY-163797
    WRN inhibitor 10

    		DNA/RNA Synthesis Cancer
    WRN inhibitor 10 (Compound P24) is an inhibitor for the Werner helicase WRN with an IC50 of 1.1 nM. WRN inhibitor 10 inhibits the proliferation of cancer cell SW48 with IC50 of 39 nM. WRN inhibitor 10 exhibits good liver microsomal stability and film permeability. WRN inhibitor 10 exhibits good pharmacokinetic characteristics in CD-1 mice .
    WRN inhibitor 10
  • HY-147758
    BACE1/2-IN-1

    		Beta-secretase Amyloid-β Neurological Disease
    BACE1/2-IN-1 (compound 34) is a potent BACE1 and BACE2 inhibitor, with an IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 shows a combination of lower Pgp efflux ratio and improved passive permeability. BACE1/2-IN-1 displays reduced liver microsomal metabolic stability .
    BACE1/2-IN-1
  • HY-150508
    MK-0159

    		CD38 Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    MK-0159 is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD + (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart .
    MK-0159
  • HY-155510
    DprE1-IN-5

    		Bacterial Infection
    DprE1-IN-5 (Compound 10) is a DprE1 inhibitor. DprE1-IN-5 has anti-TB activity against Mtb H37Rv strain (MIC: 4 μM). DprE1-IN-5 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-5 has high microsomal stability .
    DprE1-IN-5
  • HY-155512
    DprE1-IN-7

    		Bacterial Infection
    DprE1-IN-7 (Compound 64) is a DprE1 inhibitor. DprE1-IN-7 has anti-TB activity against Mtb H37Rv strain (MIC: 1 μM). DprE1-IN-7 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-7 has high microsomal stability and medium clearance .
    DprE1-IN-7
  • HY-155511
    DprE1-IN-6

    		Bacterial Infection
    DprE1-IN-6 (Compound 56) is a DprE1 inhibitor. DprE1-IN-6 has anti-TB activity against Mtb H37Rv strain (MIC: 1 μM). DprE1-IN-6 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-6 has high microsomal stability and medium clearance .
    DprE1-IN-6
  • HY-146057
    Antituberculosis agent-2

    		Bacterial Infection
    Antituberculosis agent-2 (Compound 8d) is an antituberculosis agent against agent-sensitive and multidrug-resistant tuberculosis. Antituberculosis agent-2 shows anti-tuberculosis activity with MIC values of 0.454, 1.757 and 1.644 μg/mL against M. tuberculosis H37Rv, 13946 and 14862, respectively. Antituberculosis agent-2 displays favorable mouse and human microsomal stability, low cytotoxicity, and acceptable oral bioavailability .
    Antituberculosis agent-2
  • HY-159588
    Mcl-1 inhibitor 20

    		Bcl-2 Family Cancer
    Mcl-1 inhibitor 20 (compound 47) is a Mcl-1 inhibitor with anti-leukemic effects. Mcl-1 inhibitor 20 can bind to the BH3 binding groove of Mcl-1 (Ki=24 nM), occupy the P1 pocket in Mcl-1, and form interactions with Lys234 and Val249. Mcl-1 inhibitor 20 has good microsomal stability, pharmacokinetic characteristics and low cardiotoxicity .
    Mcl-1 inhibitor 20
  • HY-163403
    VEGFR-2-IN-43

    		VEGFR Cardiovascular Disease Cancer
    VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research .
    VEGFR-2-IN-43
  • HY-163799
    PRMT5-MTA-IN-1

    		Histone Methyltransferase Cancer
    PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor for protein arginine methyltransferase PRMT5-MTA. PRMT5-MTA-IN-1 inhibits the proliferation of colorectal cancer cell HCT116 wildtype and MTAP del mutant, with an IC50 of 16 nM and 2.47 μM. PRMT5-MTA-IN-1 exhibits good liver microsomal stability and film permeability. PRMT5-MTA-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mice .
    PRMT5-MTA-IN-1
  • HY-149916
    A2AR-antagonist-1

    		Adenosine Receptor Cancer
    A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2) .
    A2AR-antagonist-1
  • HY-163982
    FOXJ1 agonist 1

    		FOXO Others 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-123882
    IRAK4-IN-29

    		Others Others
    IRAK4-IN-29 is an IRAK4 inhibitor with good selectivity and low nanomolar activity. IRAK4-IN-29 can effectively block the TLR-mediated signal transduction pathway. IRAK4-IN-29 showed significant inhibitory effects in LPS- and R848-induced cytokine experiments. IRAK4-IN-29 can inhibit LPS-induced TNFα in an in vivo model, showing a similar phenotype to IRAK4 gene-deficient mice. IRAK4-IN-29 has good medicinal chemical properties, such as microsomal stability and solubility, showing potential clinical application value .
    IRAK4-IN-29

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