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pharmacodynamics

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7

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-162255

    CDK Cancer
    CDK2-IN-23 (Compound 17) is a kinase selective and highly potent CDK2 inhibitor (IC50 = 0.29 nM). CDK2-IN-23 shows the pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models. CDK2-IN-23 can be used for the research of cancer .
    CDK2-IN-23
  • 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-70002AS

    N-desmethyl MDV 3100-d6

    Androgen Receptor Cancer
    N-desmethyl Enzalutamide-d6 is a deuterium labeled N-desmethyl Enzalutamide. N-desmethyl Enzalutamide is an active metabolite of Enzalutamide. N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide[1].
    N-desmethyl Enzalutamide-d6
  • HY-B0377
    Famotidine
    4 Publications Verification

    MK-208

    Histamine Receptor Metabolic Disease Endocrinology Cancer
    Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
    Famotidine
  • 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-12883A

    Sodium Channel Neurological Disease
    PF-05198007 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor. PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771 .
    PF-05198007
  • 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-113468A

    3-Methoxy-L-tyrosine; 3-O-Methyl-L-DOPA

    Dopamine Receptor Endogenous Metabolite Neurological Disease
    3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine .
    3-O-Methyldopa
  • 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-160251

    (3'R,5k'S)-trans-3'-Hydroxycotinine glucuronide

    Others Others
    3-HC-Gluc ((3’R,5k’s)-trans-3’ -Hydroxycotinine glucuronide) The trans-structure of 3-HC, the main metabolite of nicotine .
    3-HC-Gluc
  • HY-70002A

    N-desmethyl MDV 3100

    Androgen Receptor Cancer
    N-desmethyl Enzalutamide is the active metabolite of Enzalutamide.N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide .
    N-desmethyl Enzalutamide
  • HY-A0147

    OPC-17116; dl-Grepafloxacin

    Antibiotic Bacterial Infection
    Grepafloxacin (OPC-17116) is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin has high tissue penetration and a promising pharmacodynamic profile .
    Grepafloxacin
  • HY-136933

    Na+/K+ ATPase Cardiovascular Disease
    Gitoxin, a Na +/K +-ATPase inhibitor, usually appears as a result of metabolic degradation of Digitoxin, is just the hydroxyl (ZOH) group close to the C-17β position, which changes the pharmacokinetics and pharmacodynamics of these substances considerably .
    Gitoxin
  • HY-B0377R

    Histamine Receptor Metabolic Disease Endocrinology Cancer
    Famotidine (Standard) is the analytical standard of Famotidine. This product is intended for research and analytical applications. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
    Famotidine (Standard)
  • HY-10787
    Ximelagatran
    1 Publications Verification

    H 376/95

    Thrombin Cardiovascular Disease
    Ximelagatran (H 376/95) is an orally active thrombin inhibitor that selectively and competitively inhibits both free and clot-bound thrombin. Ximelagatran is an anticoagulant agent with a rapid onset of anticoagulant effect, predictable, dose-dependent pharmcokinetics and pharmacodynamics .
    Ximelagatran
  • HY-A0147A

    OPC-17116 hydrochloride; dl-Grepafloxacin hydrochloride

    Antibiotic Bacterial Infection
    Grepafloxacin (OPC-17116) hydrochloride is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin hydrochloride has high tissue penetration and a promising pharmacodynamic profile .
    Grepafloxacin hydrochloride
  • HY-B0377S

    Isotope-Labeled Compounds Histamine Receptor Metabolic Disease Endocrinology
    Famotidine- 13C,d3 is the 13C- and deuterium labeled Famotidine. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
    Famotidine-13C,d3
  • HY-101560
    Linrodostat
    4 Publications Verification

    BMS-986205; ONO-7701

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    Linrodostat (BMS-986205) is a selective and irreversible indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 value of 1.1 nM in IDO1-HEK293 cells. Linrodostat is well tolerated with potent pharmacodynamic activity in advanced cancers .
    Linrodostat
  • 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-113468AS

    3-Methoxy-L-tyrosine-d3; 3-O-Methyl-L-DOPA-d3

    Dopamine Receptor Endogenous Metabolite Neurological Disease
    3-O-Methyldopa-d3 is deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine[1].
    3-O-Methyldopa-d3
  • HY-117290

    Factor Xa Cardiovascular Disease
    BMS-962212 is a direct, reversible, selective factor XIa (FXIa) inhibitor . BMS-962212 is well tolerated, with fast onset of pharmacodynamic (PD) responses and rapid elimination. BMS-962212 increases exposure dependently in activated partial thromboplastin time, and decreases exposure dependently in FXI clotting activity .
    BMS-962212
  • HY-18030A

    Anaplastic lymphoma kinase (ALK) Cancer
    CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally bioavailable ALK inhibitor, with an IC50 value of 1.9 nM for recombinant ALK kinase activity. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity .
    CEP-28122 mesylate salt
  • HY-N8265

    HSV DNA/RNA Synthesis ATP Synthase Infection
    Abyssinone V is a prenylated flavonoid with predicted anti-viral activity. Abyssinone V can be isolated from the stem bark of Erythrina melanacantha. Abyssinone V possesses good pharmacodynamics properties. Abyssinone V is predicted to be antivirals including anti-herpes (HSV) agent, with mechanisms comprising inhibition of polymerase, ATPase and membrane integrity .
    Abyssinone V
  • HY-19517

    Others Cardiovascular Disease
    R1663 is a factor Xa inhibitor with anticoagulant activity. R1663 does not affect bleeding time. The pharmacodynamic effects (such as inhibition of thrombin generation) and plasma concentrations of R1663 are dose-dependent. R1663 prolongs clotting time in a concentration-dependent manner and inhibits the peak height of thrombin generation and endogenous thrombin potential .
    R1663
  • HY-113468AS1

    3-Methoxy-L-tyrosine-d3 hydrate; 3-O-Methyl-L-DOPA-d3 hydrate

    Isotope-Labeled Compounds Dopamine Receptor Endogenous Metabolite Neurological Disease
    3-O-Methyldopa-d3 (hydrate) is the deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine[1].
    3-O-Methyldopa-d3 hydrate
  • HY-161672

    Liposome IRE1 Cancer
    G-5758 is an orally available IRE1α inhibitor with an IC50 of 38 nM for XBP1s. G-5758 is well tolerated in multiple myeloma models (KMS-11) at oral doses up to 500 mg/kg in rats. G-5758 exhibits pharmacodynamics comparable to that of induced IRE1 knockdown .
    G-5758
  • 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-132296

    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-118374

    PI3K Akt Inflammation/Immunology
    AM-9635 is a selective PI3Kδ inhibitor with oral bioavailability, good in vitro and in vivo activity and pharmacodynamic properties. AM-9635 inhibits PI3Kδ-dependent B cell receptor-mediated AKT phosphorylation and suppresses the production of specific IgG and IgM antibodies in rats immunized with Aplysia leocyanin (KLH).
    AM-9635
  • HY-136805

    Others Neurological Disease
    Kv1.5-IN-1 is a Kv1.5 channel inhibitor. Its target selectivity and pharmacodynamic effects were evaluated in an in vitro rat model. After the introduction of a methoxy group at the R5 position, Kv1.5-IN-1 showed inhibitory potency similar to that of the unsubstituted compound. Its IC50 value for hKv1.5 channels was 0.51 μM. Kv1.5-IN-1 exhibited a high degree of selectivity, nearly 2,600 times higher than compound Ik and 300 times higher than compound IId, indicating that it may be a safe inhibitor. Due to its good pharmacological behavior, Kv1.5-IN-1 deserves further pharmacodynamic and pharmacokinetic evaluation. These properties make Kv1.5-IN-1 a potential Kv1.5 channel inhibitor that may have application prospects in the treatment of related diseases.
    Kv1.5-IN-1
  • HY-D1460

    Bacterial Infection
    Fluorescein Di-β-D-Glucuronide, a fluorescent probe, can be utilized to non-invasively image the intestinal bacterial β-glucuronidase activity in nude mice. Fluorescein Di-β-D-Glucuronide-based imaging reveals the in vitro and in vivo activity of intestinal bacterial β-glucuronidase, which would facilitate pharmacodynamic studies of specific bacterial β-glucuronidase inhibitors in animal studies .
    Fluorescein Di-β-D-Glucuronide
  • HY-W401531S

    Dopamine Receptor Endogenous Metabolite Neurological Disease
    (R)-3-O-Methyldopa-d3 is a deuterium labeled (R)-3-O-Methyldopa, and (R)-3-O-Methyldopa is an R-enantiomer of 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of L-DOPA and dopamine[1][2].
    (R)-3-O-Methyldopa-d3
  • HY-W401531S1

    Dopamine Receptor Endogenous Metabolite Neurological Disease
    (R)-3-O-Methyldopa-d3 (hydrochloride) is a deuterium labeled (R)-3-O-Methyldopa, and (R)-3-O-Methyldopa is an R-enantiomer of 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of L-DOPA and dopamine[1][2].
    (R)-3-O-Methyldopa-d3 hydrochloride
  • HY-161349

    Aminopeptidase Inflammation/Immunology
    LTA4H-IN-4 (compound 3) is an orally active LTA4H inhibitor. The IC50 value of LTA4H-IN-4 for hERG is 156 μM. LTA4H-IN-4 can be used in inflammation related studies .
    LTA4H-IN-4
  • HY-103196

    Adrenergic Receptor Potassium Channel Cardiovascular Disease Neurological Disease
    Sotalol is an orally active, non-selective β-adrenergic receptor blocker. Sotalol is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol blocks β-receptors, and potassium KCNH2 channels. Antiepileptic Agent .
    Sotalol
  • HY-B0437
    Sotalol hydrochloride
    2 Publications Verification

    MJ 1999

    Adrenergic Receptor Potassium Channel Cardiovascular Disease Neurological Disease
    Sotalol hydrochloride (MJ 1999) is an orally active, non-selective β-adrenergic receptor blocker. Sotalol hydrochloride is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol hydrochloride blocks β-receptors, and potassium KCNH2 channels. Antiepileptic Agent .
    Sotalol hydrochloride
  • HY-111745

    JAK Inflammation/Immunology
    Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis .
    Tyk2-IN-5
  • HY-143744

    Influenza Virus Infection
    Cap-dependent endonuclease-IN-3 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-3 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-3 has the potential for the research of influenza A and influenza B infection (extracted from patent WO2019141179A1, compound VI-1) .
    Cap-dependent endonuclease-IN-3
  • HY-143743

    Influenza Virus Infection
    Cap-dependent endonuclease-IN-2 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-2 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-2 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent WO2019052565A1, compound 28) .
    Cap-dependent endonuclease-IN-2
  • HY-143755

    Influenza Virus Infection
    Cap-dependent endonuclease-IN-9 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-9 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-9 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent CN112521386A, compound VI-1) .
    Cap-dependent endonuclease-IN-9
  • HY-135495

    Others Inflammation/Immunology
    AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing .
    AM-0466
  • HY-143757

    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-139920

    SH-1028

    EGFR Cancer
    Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFR WT, EGFR L858R, EGFR L861Q, EGFR L858R/T790M, EGFR d746-750 and EGFR d746-750/T790M kinases, with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively .
    Oritinib
  • HY-10900

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    TCS 1102 is a potent, dual orexin receptor antagonist, with Ki values of 0.2 nM and 3 nM for OX2 and OX1 receptors, respectively. TCS 1102 demonstrates excellent blood-brain barrier penetrability and moderate bioavailability in rats .
    TCS 1102
  • HY-155406

    Estrogen Receptor/ERR Caspase Bcl-2 Family Cancer
    Estrogen receptor modulator 10 (compound G-5b) is an Estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 can induce apoptosis. Estrogen receptor modulator 10 can block cells at the G1/G0 phase. Estrogen receptor modulator 10 can be used in cancer studies .
    Estrogen receptor modulator 10
  • HY-126242S

    JAK Inflammation/Immunology
    Tyk2-IN-7 is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model[1].
    Tyk2-IN-7
  • HY-133031A

    Histone Methyltransferase Others
    CSV0C018875 hydrochloride is a G9a (EHMT2) inhibitor that inhibits G9a activity. CSV0C018875 can effectively inhibit G9a activity in both enzyme and cell-based assays, and its toxicity is much lower than that of the known G9a inhibitor BIX-01294. CSV0C018875 binds tightly to the active site cavity of G9a, thereby improving the binding firmness and prolonging the residence time of the compound, further enhancing the inhibitory effect of G9a. CSV0C018875 has the potential to improve its ADME (absorption, distribution, metabolism and excretion) and pharmacodynamic properties through further optimization .
    CSV0C018875 hydrochloride
  • HY-15790

    A 3309; AZD 7806

    Apical Sodium-Dependent Bile Acid Transporter Interleukin Related TNF Receptor Metabolic Disease Inflammation/Immunology
    Elobixibat (A 3309; AZD 7806) is an orally effective Apical Sodium-Dependent Bile (IBAT) inhibitor, with an IC50 value of 0.53 nM (human IBAT ), 0.13 nM (mouse IBAT), 5.8 nM (canine IBAT). Elobixibat lowers LDL cholesterol, increases serum GLP-1, promotes colon motility, and has the potential to treat metabolic syndrome. Elobixibat can be used to study constipation, dyslipidemia, non-alcoholic hepatitis, and liver tumors .
    Elobixibat
  • HY-15790R

    Apical Sodium-Dependent Bile Acid Transporter Interleukin Related TNF Receptor Metabolic Disease Inflammation/Immunology
    Elobixibat (Standard) is the analytical standard of Elobixibat. This product is intended for research and analytical applications. Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ± 0.17 nM, 0.13 ± 0.03 nM, and 5.8 ± 1.6 nM for human IBAT, mouse IBAT, and canine IBAT.
    Elobixibat (Standard)
  • HY-15790H

    (S)-A 3309; (S)-AZD 7806

    Apical Sodium-Dependent Bile Acid Transporter TNF Receptor Interleukin Related Metabolic Disease Inflammation/Immunology
    (S)-Elobixibat is the S enantiomer of Elobixibat (HY-15790). (S)-Elobixibat is an orally effective Apical Sodium-Dependent Bile (IBAT) inhibitor. (S)-Elobixibat decreases LDL cholesterol, increases serum GLP-1, promotes colon motility, and has the potential to treat metabolic syndrome. (S)-Elobixibat can be used to study constipation, dyslipidemia, non-alcoholic hepatitis, and liver tumors .
    (S)-Elobixibat

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