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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-135910

    OPC-13015

    Drug Metabolite Cardiovascular Disease Cancer
    3,4-Dehydro Cilostazol (OPC-13015) is an active metabolite of Cilostazol (CLZ; HY-17464). 3,4-Dehydro Cilostazol is used for pharmacokinetic study .
    3,4-Dehydro Cilostazol
  • HY-138216

    Bacterial Infection
    Despropylene gatifloxacin is a metabolism of AM-1155 (HY-10581). AM-1155 has potent antibacterial activity and favorable pharmacokinetics .
    Despropylene gatifloxacin
  • HY-136336
    Tofacitinib metabolite-1
    1 Publications Verification

    Drug Metabolite Others
    Tofacitinib metabolite-1 is a metabolite of Tofacitinib, a JAK inhibitor. Tofacitinib metabolite-1 can be used in the pharmacokinetics and metabolism studies of tofacitinib .
    Tofacitinib metabolite-1
  • HY-113018A

    (S)-Ibuprofen glucuronide

    Others Inflammation/Immunology
    (S)-Ibuprofen acyl-β-D-glucuronide ((S)-Ibuprofen glucuronide) is a compound used to study the metabolism and pharmacokinetics of S-ibuprofen, a non-steroidal anti-inflammatory drug. (S)-Ibuprofen acyl-β-D-glucuronide is an acylglucuronic acid metabolite produced by S-ibuprofen in the liver .
    (S)-Ibuprofen acyl-β-D-glucuronide
  • HY-155652

    BCRP Cancer
    ABCG2-IN-1 (compound K2), a Ko143 analog, is an orally active ABCG2 inhibitor with an IC50 of 0.13 μM. ABCG2-IN-1 has favorable oral pharmacokinetic profiles in mice .
    ABCG2-IN-1
  • HY-143316

    Others Neurological Disease
    NPR-C activator 1 (Compound 1) is a potent activator of natriuretic peptide receptor C (NPR-C). C-type natriuretic peptide (CNP) is involved in the regulation of vascular homeostasis. NPR-C activator 1 is identified as a potent agonist (EC50 ∼ 1 μM) with promising in vivo pharmacokinetic properties .
    NPR-C activator 1
  • HY-146662

    PGE synthase Inflammation/Immunology
    HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity .
    HPGDS inhibitor 3
  • 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-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-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-157014

    Tryptophan Hydroxylase Cancer
    TPT-004 is a TPH inhibitor. TPT-004 has superior pharmacokinetic and pharmacodynamic properties. TPT-004 also has good efficacy in preclinical models of peripheral serotonin attenuation and colorectal tumor growth .
    TPT-004
  • HY-139743

    Aditoprim

    Antifolate Bacterial Infection
    Aditoprime (Aditoprim), a selective bacterial dihydrofolate reductase (DHFR) inhibitor, inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime inhibits E.coli and L.casei DHFR with IC50 of 47 and 520 nM, respectively. Aditoprime has a broad antimicrobial spectrum, good antibacterial activity and excellent pharmacokinetics .
    Aditoprime
  • 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-143747

    Influenza Virus Infection
    Cap-dependent endonuclease-IN-5 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-5 inhibits influenza virus well, and/or has lower cytotoxicity, better in vivo pharmacokinetic properties and in vivo pharmacodynamic properties (extracted from patent WO2020078401A1, compound 13-1) .
    Cap-dependent endonuclease-IN-5
  • HY-144437

    TGF-β Receptor Cancer
    ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC50 values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease .
    ALK5-IN-9
  • HY-144660

    Cholinesterase (ChE) Neurological Disease
    AChE-IN-7 (Compound 16) is a selective and potent inhibitor of acetylcholinesterase (eeAChE IC50 = 0.045 μM; eeBuChE IC50 = 19.68 μM). AChE-IN-7 is safe in vivo and in vitro, and shows good overall pharmacokinetic performance and high bioavailability (F = 55.5%). AChE-IN-7 also has high BBB permeability .
    AChE-IN-7
  • 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-15738
    GNF-5
    3 Publications Verification

    Bcr-Abl Cancer
    GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC50 value of 0.22 µM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer .
    GNF-5
  • 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-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-18071
    BI-9627
    1 Publications Verification

    Na+/H+ Exchanger (NHE) Cardiovascular Disease
    BI-9627 is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
    BI-9627
  • HY-18071A
    BI-9627 hydrochloride
    1 Publications Verification

    Na+/H+ Exchanger (NHE) Cardiovascular Disease
    BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
    BI-9627 hydrochloride
  • HY-12995A

    FLAP Inflammation/Immunology
    (S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species agent metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production .
    (S)-BI 665915
  • HY-143881

    FGFR Cancer
    FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity . FGFR4-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    FGFR4-IN-6
  • HY-150654

    Histone Methyltransferase 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-142661

    Thrombin Neurological Disease
    BAY 1217224 is a neutral, non-proagent Thrombin inhibitor with good oral pharmacokinetics.
    BAY 1217224
  • HY-U00418
    ARS-1620
    5+ Cited Publications

    Ras Cancer
    ARS-1620 is an atropisomeric selective KRAS G12C inhibitor with desirable pharmacokinetics.
    ARS-1620
  • 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-120123

    Prostaglandin Receptor Inflammation/Immunology
    FR181157, an orally active PGI2 agonist activity with especially good pharmacokinetic properties .
    FR181157
  • HY-139401

    FAP Cancer
    FAPI-34 is a fibroblast-activating protein (FAP) inhibitor with favorable pharmacokinetic and biochemical properties. (patent WO2019154886A1).
    FAPI-34
  • HY-18310

    PI3K Cancer
    NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth .
    NIBR-17
  • HY-13829

    HIV Infection
    BMS-585248 is a potent, third-generation HIV-1 attachment inhibitor with a promising initial in vitro and in vivo pharmacokinetic profile .
    BMS-585248
  • HY-W196368

    Others Inflammation/Immunology
    Thymohydroquinone is a monoterpene molecule. Thymohydroquinone has antioxidant and anti-inflammatory properties. Thymohydroquinone can be used for pharmacokinetic studies and regulatory toxicity studies .
    Thymohydroquinone
  • HY-137207
    MK-28
    3 Publications Verification

    PERK Neurological Disease
    MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice .
    MK-28
  • HY-139875

    CDK Cancer
    JH-XVI-178 is a highly potent and selective inhibitor of CDK8/19 that displays low clearance and moderate oral pharmacokinetic properties.
    JH-XVI-178
  • HY-16593

    HCV Protease Infection
    GS-9256 is a selective HCV NS3 protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity .
    GS-9256
  • HY-162163

    Toll-like Receptor (TLR) Cancer
    TLR7 agonist 19 (Compound 14) is a Toll-like receptor 7 (TLR7) agonist with excellent pharmacokinetic properties and synergistic antitumor activity.
    TLR7 agonist 19
  • HY-138171

    Biochemical Assay Reagents Others
    Lipid 5 is an amino lipid that affords efficient mRNA delivery in rodent and primate models. Lipid 5 shows optimal pharmacokinetics and non-toxic side effects .
    Lipid 5
  • HY-109555

    HMR 1964

    Insulin Receptor Metabolic Disease
    Insulin glulisine (HMR 1964) is a rapid-acting insulin analogue, it mimics the pharmacokinetic and pharmacodynamic profiles of physiological human insulin. Insulin glulisine can be used for the research of diabetes .
    Insulin glulisine
  • HY-160471S

    Isotope-Labeled Compounds Cancer
    N-Nitrososertraline-d3 is a Sertraline isotope labeled with deuterium and nitrogen-15. N-Nitrososertraline-d3 can be used to track the metabolism and pharmacokinetics of Sertraline in vivo.
    N-Nitrososertraline-d3
  • HY-122682

    Others Metabolic Disease
    SBI-993 is a SBI-477 analog with improved potency and suitable pharmacokinetic properties for in vivo bioavailability. SBI-993 stimulates insulin signaling by deactivating the transcription factor MondoA .
    SBI-993
  • 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-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-14305A
    BMS-582949 hydrochloride
    1 Publications Verification

    p38 MAPK Autophagy Inflammation/Immunology
    BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease .
    BMS-582949 hydrochloride
  • HY-10493
    Cobicistat
    Maximum Cited Publications
    10 Publications Verification

    GS-9350

    Cytochrome P450 HIV Infection Cancer
    Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC50s of 30-285 nM. Cobicistat is a pharmacokinetic enhancer which increases the overall absorption of several HIV medications.
    Cobicistat
  • HY-131903

    IRAK Inflammation/Immunology
    HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties .
    HS271
  • HY-146214

    CDK Cancer
    As a cdk4/6 inhibitor. Compounds 10B and 10C showed low nanomolar activity, ideal antiproliferative activity, excellent metabolic properties and acceptable pharmacokinetics on cdk4/6.
    CDK4/6-IN-13
  • HY-18030B

    Anaplastic lymphoma kinase (ALK) Others
    CEP-28122 mesylate hydrochloride is a diaminopyrimidine derivative.CEP-28122 mesylate hydrochloride is a potent, selective, and orally bioavailable ALK inhibitor with an IC50 of 1.9 nM. CEP-28122 mesylate hydrochloride has antitumor and good pharmacokinetic activity .
    CEP-28122 mesylate hydrochloride
  • HY-162172

    PARP Cancer
    Parp7-in-18 (Compund 8) is a selective PARP7 inhibitor with an IC50 of 0.11 nM. PARP7-IN-18 exhibits good anticancer activity and pharmacokinetic properties .
    PARP7-IN-18

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