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pharmacokinetic characteristics

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79

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Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-153701

    JAK Cancer
    JAK-IN-26 (compound 2) is an orally active JAK inhibitor with good pharmacokinetic characteristics. JAK-IN-26 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC50=17.2 nM) .
    JAK-IN-26
  • HY-125290

    CDK DYRK Cancer
    MU1210 (compound 12f) is an inhibitor of CDC-like kinases Clk1, Clk2, and Clk4 (with IC50 values of 8, 20, and 12 nM respectively), with IC50 for HIPK1 and DYRK2 are 187 and 1309 nM. MU1210 also has favorable pharmacokinetic characteristics (in mice, 10 mg/kg, intraperitoneal injection: Cmax=1.24 μM, T1/2=58 minutes; no acute toxicity observed) .
    MU1210
  • HY-153245

    Btk Inflammation/Immunology Cancer
    JNJ-64264681 is a potent, orally active, selective and irreversible covalent BTK inhibitor. JNJ-64264681 exhibits good pharmacokinetic characteristics and can be used for cancer and autoimmune diseases research .
    JNJ-64264681
  • HY-W096171

    3-Hydroxy-D-tyrosine

    Carboxypeptidase Neurological Disease
    D-Dopa is a non-competitive, allosteric inhibitor for glutamate carboxypeptidase II (GCPII) with an IC50 of 200 nM. D-Dopa exhibits good pharmacokinetic characteristics, and low blood-brain barrier permeability in mouse model .
    D-Dopa
  • HY-161993

    Ketohexokinase Metabolic Disease
    BI-9787 is a zwitterionic inhibitior for ketohexokinase, with an IC50 of 12 and 12.8 nM for hKHK-A and hKHK-C. BI-9787 exhibits good metabolic stability in rat hepatocyte and good pharmacokinetic characteristics in rats .
    BI-9787
  • HY-153699

    SHP2 Cancer
    SHP2-IN-14 (compound 27) is an orally active and potent SHP2 allosteric inhibitor (IC50=7 nM) with anti-tumor activity. SHP2-IN-14 inhibits tumor progression in NCI-H358 tumor bearing mice, exhibits good pharmacokinetic characteristics and safty .
    SHP2-IN-14
  • HY-160073A

    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-162662

    Cytochrome P450 mAChR Neurological Disease
    VU6008677 is a positive allosteric modulator (PAM) for M4, with EC50 of 120 nM for hM4. VU6008677 inhibits cytochrome P450, exhibits good pharmacokinetic characteristics in rats .
    VU6008677
  • HY-117443

    Guanylate Cyclase Cardiovascular Disease
    IWP-051 is an agonist for soluble guanylate cyclase with an EC50 of 290 nM. IWP-051 stimulates the generation of cGMP, and exhibits the synergistic effect with NO. IWP-051 exhibits good pharmacokinetic characteristics in rats .
    IWP-051
  • HY-120481

    FAAH Neurological Disease
    JNJ-40413269 is an inhibitor for FAAH, that inhibits human FAAH and rats FAAH with IC50 of 28 nM and 270 nM. JNJ-40413269 exhibits analgesic efficacy in rat spinal nerve ligation model and exhibits good pharmacokinetic characteristics in rats .
    JNJ-40413269
  • HY-164478

    Wnt PARP Cancer
    G-631 is a selective inhibitor for tankyrase. G-631 inhibits tankyrase auto-PARsylation (poly ADP ribosylation) with an IC50 of 7 nM, and inhibits Wnt signaling pathway. G-631 exhibits good pharmacokinetic characteristics in mice .
    G-631
  • HY-16983

    ROR Inflammation/Immunology
    GNE-3500 is a selective, orally active antagonist for Retinoic Acid Receptor-Related Orphan Receptor C (RORc, also known as RORγ or NR1F3) with an EC50 of 12 nM. GNE-3500 exhibits good pharmacokinetic characteristics in rats .
    GNE-3500
  • HY-163702

    Adrenergic Receptor mAChR Inflammation/Immunology
    CHF-6550 is an antagonist for muscarinic M3 receptor and an agonist for β2 adrenoceptor (MABA), with pKi of 9.3 and 10.6, respectively. CHF-6550 exhibits good hepatocyte clearance in rat models and good pharmacokinetic characteristics in guinea pigs .
    CHF-6550
  • HY-115796

    mGluR Others
    VU0477886 is a metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator with potent activating activity on mGlu4 (EC50 = 95nM, 89% Glu Max), good pharmacokinetic characteristics (brain: plasma Kp = 1.3), and significant therapeutic efficacy in Parkinson's disease models.
    VU0477886
  • HY-P10427

    CXCR HIV Infection
    DV1 is a selective antagonist for CXC chemokine receptor 4 (CXCR4). DV1 exhibits antiviral activity by blocking HIV-1 entry through the CXCR4 co-receptor. DV1 is stable in rat plasma and exhibits good pharmacokinetic characteristics in rat models .
    DV1
  • HY-12586

    Thrombin Others
    AZD6564 is an orally active inhibitor for fibrinolysis through disruption of plasma kinase-fibrin interaction. AZD6564 dissolves human plasma clot with an IC50 of 0.44 μM. AZD6564 ameliorates hemorrhage in rats with EC50 of 1.62 μM, and exhibits good pharmacokinetic characteristics in rats .
    AZD6564
  • HY-159581

    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-155553

    GPR119 Metabolic Disease
    GPR119 agonist 2 (compound 43) is an orally active GPR119 agonist. GPR119 agonist 2 shows good pharmacokinetic characteristics in rodents and can effectively improve glucose tolerance in mice and rats. GPR119 agonist 2 has the potential to study type 2 diabetes .
    GPR119 agonist 2
  • HY-12580

    MDM-2/p53 Cancer
    RO5353 is an orally active inhibitor for p53-MDM2 with an IC50 of 7 nM for MDM2. RO5353 inhibits the proliferation of wild-type p53 cancer cells with an average IC50 of 7 nM. RO5353 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice .
    RO5353
  • HY-164320

    Others Cancer
    Anticancer agent 245 (Compound 115) inhibits proliferation of cancer cell SKOV3, MDA-MB-231 and HCT-116 with IC50 of 0.021, 0.056 and 0.11 μM, respectively. Anticancer agent 245 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
    Anticancer agent 245
  • HY-120454

    MEK Potassium Channel Cancer
    G-479 is the inhibitor for MEK and hERG channel (IC50=14 μM). G-479 inhibits the proliferation of HCT-116 and A375 with IC50 of 0.049 μM and 0.004 μM. G-479 exhibits good metabolic stability in liver microsomes and good pharmacokinetic characteristics in rats .
    G-479
  • HY-109052

    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-159099

    Molecular Glues Histone Acetyltransferase Others
    HbF inducer 3 (Compound dWIZ-2) is an orally active molecular glue, which degrades the WIZ transcription factor (DC50=13 nM in primary human erythroid precursor cell) and induces the expression of fetal hemoglobin (HbF) (EC50=100 nM). HbF inducer 3 exhibits good pharmacokinetic characteristics in cynomolgus monkeys .
    HbF inducer 2
  • HY-164311

    Transmembrane Glycoprotein Neurological Disease
    GPR17 modulator-1 (Compound 2-046) is a modulator for G protein-coupled receptor 17 GPR17, with an IC50<10 nM for hGPR17 in CHO. GPR17 modulator-1 exhibits moderate pharmacokinetic characteristics in mice. GPR17 modulator-1 ix blood-brain barrier (BBB) permeable .
    GPR17 modulator-1
  • HY-172426

    Anaplastic lymphoma kinase (ALK) Cancer
    Dirozalkib (Compound 4) is the inhibitor for ALK with an IC50 of 0.9 nM. Dirozalkib exhibits anti-proliferative activity in cancer cells NCI-H3122, Karpas-299 and NCI-H2228 with IC50s of 130.4, 0.71 and 15.11 nM, respectively. Dirozalkib exhibits good pharmacokinetics characteristics with an bioavailbility of 30%~50% .
    Dirozalkib
  • HY-163797

    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-111073

    Y101

    HBV Infection Inflammation/Immunology
    Bentysrepinine (Y101) is an orally active HBV inhibitor with anti-hepatitis B virus infection activity. Bentysrepinine exhibits favorable pharmacokinetic characteristics, with absolute bioavailability of 44.9%, 43.1%, and 19.2% in rats, dogs, and monkeys, respectively, and it does not accumulate in monkeys after 90 days of oral administration. Bentysrepinine is under research in the antiviral and hepatitis fields .
    Bentysrepinine
  • HY-163110

    HIV Reverse Transcriptase Infection
    NNRT-IN-2 (compound 7w) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains. NNRT-IN-2 inhibits HIV-1 reverse transcriptase with an EC50 of 22 nM. NNRT-IN-2 is insensitive to CYP and hERG and has good safety and pharmacokinetic characteristics .
    NNRT-IN-2
  • HY-135216

    Src VEGFR Raf EGFR Cancer
    Antiproliferative agent-54 (Compound 6z) is the inhibitor for multiple kinases, such as ABL WT, B-RAF, EGFR, HCK, LYN A and SRC with IC50 of 6-50 nM. Antiproliferative agent-54 inhibits proliferation of several cancer cell, inhibits HUVEC and HepG2, with EC50 of 34 and 38 nM. Antiproliferative agent-54 exhibits good pharmacokinetic characteristics in rats .
    Antiproliferative agent-54
  • HY-125677

    Caspase Reactive Oxygen Species Apoptosis Cancer
    SHetA2 is a derivative of heteroarotinoid, that exhibits cytotoxicity in cancer cells with IC50 of 0.37–4.6 μM. SHetA2 regulates cancer cells differentiation, induces apoptosis through the intrinsic mitochondrial pathway, and arrest cell cycle at G2 phase. SHetA2 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice. SHetA2 is orally active .
    SHetA2
  • HY-163763

    G2A (GPR132) Neurological Disease
    T-10418 is an agonist for G2 accumulation protein (G2A) (also known as G protein-coupled receptor GPR132) with an EC50 of 0.82 μM. T-10418 exhibits a sensitizing effect on mouse primary sensory neurons. T-10418 exhibits good pharmacokinetic characteristics, and no obvious toxicity (at 100 μM) in mouse models .
    T-10418
  • HY-148706

    STAT Infection Cancer
    STAT3-IN-17 is a moderate STAT3 inhibitor (IC50=0.7 μM; HEK-Blue IL-6), with antiproliferative activity in HeLa cells. STAT3-IN-17 has good pharmacokinetic characteristics. STAT3-IN-17 also inhibits pyruvate-ferredoxin oxidoreductase (PFOR), and inhibits Helicobacter pylori .
    STAT3-IN-17
  • HY-162646

    Thrombin Cardiovascular Disease
    FXIIa-IN-5 (Compound 4J) is an orally active, selective inhibitor for factor XIIa (FXIIa), with IC50 of 21 nM. FXIIa-IN-5 inhibits the intrinsic coagulation pathways, and exhibits anti-inflammatory and antithrombotic activity in Carrageenan (HY-125474)-induced mice thrombosis models. FXIIa-IN-5 exhibits moderate pharmacokinetic characteristics and slightly toxicity (at 100 mg/kg) .
    FXIIa-IN-5
  • HY-161767

    Molecular Glues Cancer
    JWJ-01-306 is a molecular glue that targets the C2H2 zinc finger transcription factor ZBTB11. JWJ-01-306 degrades ZBTB11, reduces the oxidative phosphorylation (OXPHOS) and tricarboxylic acid (TCA) cycle, and inhibits the proliferation of KAS-resistant PDAC cells. JWJ-01-306 exhibits good pharmacokinetic characteristics in mouse model .
    JWJ-01-306
  • HY-163768

    β-catenin Inflammation/Immunology Cancer
    Antitumor agent-172 (Compound 28) is an inhibitor for β-catenin/BCL9 interaction with IC50 of 3.92 μM. Antitumor agent-172 exhibits high affinity to β-catenin with Kd of 82 nM. Antitumor agent-172 activates T cells, promotes antigen presentation, and exhibits antitumor efficacy and good pharmacokinetic characteristics in mouse models .
    Antitumor agent-172
  • HY-170790

    TRP Channel Neurological Disease
    HZS60 is a NMDAR/TRPM4 inhibitor with brain permeability that can improve cerebral ischemia. HZS60 has significant neuroprotective effects on primary neuronal ischemic damage caused by NMDA and oxygen-glucose deprivation/reoxygenation. HZS60 exhibits good pharmacokinetic characteristics and can inhibit cerebral ischemia-reperfusion injury. HZS60 can be used as a potential inhibitor of ischemic stroke .
    HZS60
  • HY-172411

    GLP Receptor Metabolic Disease
    GLP-1R agonist 29 (Compound 20) is the agonist for GLP-1R that induces hGLP-1R mediated cAMP stimulation with an EC50 of 0.018 nM. GLP-1R agonist 29 exhibits good pharmacokinetics characteristics with good body exposure of AUC0-∞,sc of 77688 ng·h/mL .
    GLP-1R agonist 29
  • HY-16773

    GS-9451

    HCV Protease BCRP P-glycoprotein Infection
    Vedroprevir (GS-9451) is an inhibitor for HCV NS3/4A protease with an IC50 of 3.2 nM. Vedroprevir is also an inhibitor for breast cancer resistant protein (BCRP) with an IC50 of 1.4 μM. Vedroprevir inhibits P-gp, MRP1 and MRP2 with IC50 of 34, 14.9 and 12 μM, respectively. Vedroprevir exhibits good pharmacokinetic characteristics in rats and dogs .
    Vedroprevir
  • HY-161723

    Dopamine Transporter CDK Neurological Disease
    LH2-051 is a lysosome-enhancing lead compound, which promotes the lysosome biogenesis and the Aβ aggregate clearance through dopamine transporter-cyclin-dependent kinase 9-transcription factor EB (DAT-CDK9-TFEB) pathway. LH2-051 exhibits good pharmacokinetic characteristics in mouse models. LH2-051 is potential for ameliorating Aleheimer’s Disease .
    LH2-051
  • HY-161342

    Cathepsin SARS-CoV Infection Inflammation/Immunology
    CTSL/CAPN1-IN-2 (Compound 14b) is an orally active inhibitor of both CTSL and CAPN1, with IC50 values of 6.88 nM and 347.6 nM, respectively. CTSL/CAPN1-IN-2 possesses anti-inflammatory properties and favorable pharmacokinetic characteristics. CTSL/CAPN1-IN-2 exhibits broad-spectrum antiviral activity against coronaviruses by blocking viral entry .
    CTSL/CAPN1-IN-2
  • HY-160023

    D3S-001

    Ras Cancer
    Elisrasib is an orally active inhibitor for KRAS. Elisrasib inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2 with an IC50 of 0.6 and 0.44 nM. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
    Elisrasib
  • HY-173029

    Ferroptosis Cancer
    UAMC-4821 is an inhibitor for ferroptosis with an IC50 of 5.2 nM. UAMC-4821 scavenges free radicals, blocks the lipid peroxidation, inhibits ML162 (HY-100002)-induced ferroptosis, and exhibits protective effect in HT-1080 cell. UAMC-4821 exhibits good pharmacokinetics characteristics in mouse with an oral bioavailability of 63%. UAMC-4821 can cross blood-brain barrier .
    UAMC-4821
  • HY-136704

    Glutaminase Cancer
    GLS1 Inhibitor-1 (Compound 27) is an orally active inhibitor for glutaminase 1 (GLS1) with an IC50 of 0.021 μM. GLS1 Inhibitor-1 inhibits the proliferation of PC-3 with an IC50 of 0.3 nM. GLS1 Inhibitor-1 exhibits antitumor efficacy against NCI-H1703 with GI50 of 0.011 μM. GLS1 Inhibitor-1 exhibits moderate pharmacokinetic characteristics .
    GLS1 Inhibitor-1
  • HY-147409

    CDK Cancer
    Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics .
    Ulecaciclib
  • HY-159588

    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-162710

    Aminopeptidase Inflammation/Immunology
    LTA4H-IN-5 (Compound H122) is an orally active inhibitor for leukotriene A4 hydrolase (LTA4H), that inhibits the LTA4H aminopeptidase and LTA4H hydrolase with IC50 of 0.38 nM and 16.93 nM. LTA4H-IN-5 exhibits good pharmacokinetic characteristics in C57 mice and ameliorates the DNBS-induced ulcerative enteritis in rat models .
    LTA4H-IN-5
  • HY-171292

    Casein Kinase p38 MAPK Others
    CK1δ-IN-9 (Compound 8) is the inhibitor for casein kinase 1 that inhibits CK1δ with IC50 of 1.4 nM. CK1δ-IN-9 inhibits p38α and p38β with IC50 of 0.25 μM and 0.78 μM. CK1δ-IN-9 exhibits pharmacokinetic characteristics with a good oral bioavailability (70%) and a moderate clearance .
    CK1δ-IN-9
  • HY-162640

    ROR Cancer
    ROR1-IN-1 (Compound 19h) is an inhibitor for receptor tyrosine kinase-like orphan receptor 1 (ROR 1) with Ki of 0.10 μM. ROR1-IN-1 inhibits proliferation of cancer cells H1975, A549 and MDA-MB-231, with IC50 of 0.36 μM, 1.37 μM and 0.47 μM. ROR1-IN-1 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
    ROR1-IN-1
  • HY-120462

    Dihydroorotate Dehydrogenase Parasite Infection
    Genz-669178 is an inhibitor for dihydroorotate dehydrogenase (DHODH) with IC50 of 0.015-0.05 μM in Plasmodium spp.. Genz-669178 inhibits P. berghei, P. falciparum strains 3D7 and Dd2 with IC50 of 0.068, 0.008 and 0.01 μM, respectively. Genz-669178 exhibits anti-malarial efficacy in P. berghei-infected mice with ED50 of 13-21 mg/kg/day. Genz-669178 exhibits good pharmacokinetic characteristics in mice .
    Genz-669178
  • HY-162645

    TAM Receptor Inflammation/Immunology Cancer
    BPR5K230 is a dual inhibitor for the receptor tyrosine kinase MER and AXL, with IC50 of 4.1 nM and 9.2 nM. BPR5K230 inhibits the proliferation of Ba/F3-MER with IC50 of 5 nM. BPR5K230 exhibits good pharmacokinetic characteristics in mice, exhibits anti-inflammatory and antitumor against 4T1, MDA-MB-231, MC38 and Hepa1?6 in mouse models .
    BPR5K230

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