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pharmacodynamics

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39

Inhibitors & Agonists

1

Fluorescent Dye

1

Peptides

3

Natural
Products

6

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0377
    Famotidine
    3 Publications Verification

    MK-208

    		 Histamine Receptor Metabolic Disease Endocrinology
    Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
    Famotidine
  • HY-109555
    Insulin glulisine

    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-162255
    CDK2-IN-23

    		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
    TPT-004

    		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-143747
    Cap-dependent endonuclease-IN-5

    		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-HC-Gluc

    (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-12883A
    PF-05198007

    		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-O-Methyldopa

    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-70002A
    N-desmethyl Enzalutamide

    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
    Grepafloxacin

    OPC-17116; dl-Grepafloxacin
    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
    Gitoxin

    		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-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
    Grepafloxacin hydrochloride

    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
    Famotidine-13C,d3

    		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
    3 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
    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-113468AS
    3-O-Methyldopa-d3

    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
    BMS-962212

    		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
    CEP-28122 mesylate salt

    		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-70002AS
    N-desmethyl Enzalutamide-d6

    N-desmethyl MDV 3100-d6
    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-N8265
    Abyssinone V

    		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-113468AS1
    3-O-Methyldopa-d3 hydrate

    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-109052
    Atabecestat

    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
    GSK215

    		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-D1460
    Fluorescein Di-β-D-Glucuronide

    		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
    (R)-3-O-Methyldopa-d3

    		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
    (R)-3-O-Methyldopa-d3 hydrochloride

    		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
    LTA4H-IN-4

    		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-111745
    Tyk2-IN-5

    		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
    Cap-dependent endonuclease-IN-3

    		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
    Cap-dependent endonuclease-IN-2

    		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
    Cap-dependent endonuclease-IN-9

    		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-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-139920
    Oritinib

    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
    TCS 1102

    		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 modulator 10

    		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
    Tyk2-IN-7

    		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-15790
    Elobixibat

    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

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