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pharmacokinetics

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565

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2

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-138171
    Lipid 5
    3 Publications Verification

    		 Liposome 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-10493
    Cobicistat
    10+ Cited Publications

    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-P99250
    Onartuzumab
    2 Publications Verification

    MetMAb

    		 c-Met/HGFR Cancer
    Onartuzumab (MetMAb) is a unique, humanized and affinity-matured monovalent (one-armed) monoclonal antibody against the MET receptor. Onartuzumab potently inhibits HGF binding and receptor phosphorylation and signaling. Onartuzumab has antibody-like pharmacokinetics and antitumor activity .
    Onartuzumab
  • HY-122682
    SBI-993

    		Drug Derivative 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-175510
    TREM2 agonist-5

    		TREM receptor Neurological Disease
    TREM2 agonist-5 is the microglial lipid-sensing receptor (TREM2) agonist with a Kd of 71.36 μM. TREM2 agonist-5 is a racemic structural analog of the TREM2 agonist VG-3927 and exhibits superior microglial phagocytosis and activates TREM2 signaling in HEK293-hTREM2/DAP12 cells. TREM2 agonist-5 displays a superior in vitro pharmacokinetic profile to VG-3927. TREM2 agonist-5 can used for the study of Alzheimer’s disease .
    TREM2 agonist-5
  • HY-151424
    Vimentin-IN-1

    		Proteasome Mitosis Cancer
    Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1 .
    Vimentin-IN-1
  • HY-U00418
    ARS-1620
    10+ Cited Publications

    		 Ras Cancer
    ARS-1620 is an atropisomeric selective KRAS G12C inhibitor with desirable pharmacokinetics.
    ARS-1620
  • HY-137207
    MK-28
    5+ Cited Publications

    		 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-15023
    Cligosiban
    5+ Cited Publications

    PF-3274167

    		 Oxytocin Receptor Endocrinology
    Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents [1][2].
    Cligosiban
  • HY-101447A
    SI-2 hydrochloride

    EPH 116 hydrochloride

    		 Estrogen Receptor/ERR Cancer
    SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI). SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability .
    SI-2 hydrochloride
  • HY-15738
    GNF-5
    4 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-50175
    Laropiprant

    MK-0524

    		 Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Laropiprant is a potent and selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively .
    Laropiprant
  • 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-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-18071
    BI-9627
    3 Publications Verification

    		 Na+/H+ Exchanger (NHE) Autophagy Cardiovascular Disease
    BI-9627, a chemical probe, is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 decreases autophagy in HTR-8/SVneo cells. BI-9627 can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 prolongs Ca 2+ recovery time in KO hiPSC-CMs. 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-150654
    WDR5-IN-5

    		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-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-178324
    T2M-010

    		TREM receptor Syk Neurological Disease Inflammation/Immunology
    T2M-010 is a potent, brain-penetrant TREM2 agonist (Kd = 0.83 μM). T2M-010 activates receptor-proximal signaling, inducing SYK phosphorylation in TREM2-expressing cells, and promotes microglial phagocytosis. T2M-010 can be used for the study of protective microglial responses relevant to Alzheimer’s disease (AD) .
    T2M-010
  • HY-153245
    JNJ-64264681

    		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-105090
    Lerisetron

    		5-HT Receptor Cardiovascular Disease Neurological Disease
    Lerisetron is a potent 5-HT3 antagonists and possess high-affinity binding for the 5-HT3 receptors with pKi value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats .
    Lerisetron
  • HY-135910
    3,4-Dehydro Cilostazol

    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-125290
    MU1210

    		CDK DYRK Cancer
    MU1210 (compound 12f), a chemical probe, 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-10096
    TCS2002

    		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-18071A
    BI-9627 hydrochloride
    3 Publications Verification

    		 Na+/H+ Exchanger (NHE) Autophagy Cardiovascular Disease
    BI-9627 hydrochloride is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride decreases autophagy in HTR-8/SVneo cells. BI-9627 hydrochloride can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 hydrochloride prolongs Ca 2+ recovery time in KO hiPSC-CMs. 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-14305A
    BMS-582949 hydrochloride
    2 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-161993
    BI-9787

    		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-138627A
    AST5902 trimesylate

    		EGFR Drug Metabolite Cancer
    AST5902 trimesylate is the principal metabolite of Alflutinib (AST2818) both in vitro and in vivo. AST5902 trimesylate exerts antineoplastic activity. Alflutinib is an EGFR inhibitor .
    AST5902 trimesylate
  • HY-N0343A
    4-Formylpyrnyl-β-D-glucopyranoside

    p-Formylphenyl-β-D-glucopyranoside; p-Hydroxybenzaldehyde glucoside

    		 Others Others
    4-Formylpyrnyl-β-D-glucopyranoside (p-Formylphenyl-β-D-glucopyranoside) is a metabolite of Gastrodin (HY-N0115) in rat plasma. 4-Formylpyrnyl-β-D-glucopyranoside can be used to study the effects of multiple doses and food on the pharmacokinetic behavior of oral Gastrodin and its metabolites .
    4-Formylpyrnyl-β-D-glucopyranoside
  • HY-143316
    NPR-C activator 1

    		Guanylate Cyclase 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-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
  • HY-158119A
    PSMA-trillium

    Felivotide mopaxetan

    		 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-131903
    HS271

    		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-W440913
    DSPE-PEG5000-Cy5

    		Liposome Fluorescent Dye Cancer
    DSPE-PEG-Cy5, MW 5000 is a fluorescently labeled PEGylated phospholipid with a molecular weight of 5000 Da. After intravenous injection, DSPE-PEG-Cy5, MW 5000 shows only extremely low fluorescence accumulation at tumor sites in orthotopic tumor-bearing mice, and can be used as a negative control for evaluating tumor accumulation of nanoparticles. DSPE-PEG-Cy5, MW 5000 can serve as a fluorescent marker to prepare Cy5-labeled NPs-DPPA and NPs-DPPA (C3F8) for pharmacokinetic and biodistribution studies in mice. DSPE-PEG-Cy5, MW 5000 is widely applicable to research in fields related to triple-negative breast cancer, hepatocellular carcinoma and so on .
    DSPE-PEG5000-Cy5
  • HY-123353
    Neladenoson dalanate

    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-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-158125
    PSMA binder-2

    		PSMA Cancer
    PSMA binder-2 is a ligand for PSMA and can be used to synthesize Ac-PSMA-trillium. Ac-PSMA-trillium is a suitable PSMA-targeting compound with improved PSMA binding properties and pharmacokinetic properties. PSMA ligands have different biological applications after being modified 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) .
    PSMA binder-2
  • HY-12769
    Mebeverine acid

    Mebeverine metabolite Mebeverine acid

    		 Drug Metabolite Neurological Disease
    Mebeverine acid (Mebeverine metabolite Mebeverine acid) is a secondary metabolite of the intestinal antispasmodic agent Mebeverine (HY-A0078). Mebeverine acid is generated by the hydrolysis of Mebeverine in the body and is considered a key circulating metabolite. Mebeverine acid is an important marker for oral Mebeverine .
    Mebeverine acid
  • HY-146214
    CDK4/6-IN-13

    		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-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-105454
    Recainam

    Wy-42362

    		 Sodium Channel Cardiovascular Disease
    Recainam (Wy-42362) is an orally active anti-arrhythmic agent with Class I electrophysiological properties. Recainam suppresses complex ventricular arrhythmias. Racainam exhibits a good pharmacokinetic character in Sprague Dawley rats .
    Recainam
  • HY-146662
    HPGDS inhibitor 3

    		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-W043170
    PRL3-CNNM4 PPI-IN-1

    		Phosphatase Cancer
    PRL3-CNNM4 PPI IN 1 (Compound C28d52) is an inhibitor of the PRL3-CNNM4 interaction and also inhibits PRL-mediated suppression of CNNM. PRL3-CNNM4 PPI IN 1 is capable of penetrating epithelial cell layers, exhibits metabolic stability, possesses favorable pharmacokinetic and pharmacodynamic properties, and holds potential for drug development based on this compound .
    PRL3-CNNM4 PPI-IN-1
  • HY-144437
    ALK5-IN-9

    		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-174417
    NNRT-IN-10

    		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-12995A
    (S)-BI 665915

    		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-142661
    BAY 1217224

    		Thrombin Neurological Disease
    BAY 1217224 is a neutral, non-proagent Thrombin inhibitor with good oral pharmacokinetics.
    BAY 1217224
  • HY-132867
    MNK/PIM-IN-1

    		Pim Cancer
    MNK/PIM-IN-1 represents an innovative dual MNK/PIM inhibitor with a good pharmacokinetic profile.
    MNK/PIM-IN-1
  • HY-13829
    BMS-585248

    		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-160073A
    Florensocatib hydrate

    		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-177123
    Refinicopan

    		Complement System Inflammation/Immunology
    Refinicopan is a complement factor D inhibitor with an IC50 of 10 nM. Refinicopan inhibits rabbit erythrocyte hemolysis with an IC50 of 41 nM. Refinicopan exhibits excellent pharmacokinetic and pharmacodynamic activity .
    Refinicopan

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