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orally efficacious

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46

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2

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2

Isotope-Labeled Compounds

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-141535A
    IL-17 modulator 1 disodium

    		Interleukin Related Infection Inflammation/Immunology
    IL-17 modulator 1 (disodium) is an orally active, highly efficacious IL-17 modulator extracted from patent WO 2020127685. IL-17 modulator 1 (disodium) can be used for the research of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis .
    IL-17 modulator 1 disodium
  • HY-14390
    LAS101057
    1 Publications Verification

    		 Adenosine Receptor Inflammation/Immunology
    LAS101057 is a potent, selective, and orally efficacious A2B receptor antagonist.
    LAS101057
  • HY-A0287
    Clomifene

    Clomiphene

    		 Others Endocrinology
    Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation .
    Clomifene
  • HY-A0287A
    Clomifene hydrochloride

    Clomiphene hydrochloride

    		 Others Endocrinology
    Clomifene hydrochloride is an orally active compound used for infertility. Clomifene hydrochloride is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation .
    Clomifene hydrochloride
  • HY-A0287S
    Clomifene-d5 hydrochloride

    Clomiphene-d5 (hydrochloride)

    		 Isotope-Labeled Compounds Others
    Clomifene-d5 (hydrochloride) is a deuterium labeled Clomifene. Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation[1].
    Clomifene-d5 hydrochloride
  • HY-147642
    ChemR23-IN-4

    		Others Inflammation/Immunology
    ChemR23-IN-4 (Compound 13) is a potent and orally efficacious ChemR23 inhibitor with an IC50 of 17 nM against human ChemR23 .
    ChemR23-IN-4
  • HY-141535
    IL-17 modulator 1

    		Interleukin Related Infection Inflammation/Immunology
    IL-17 modulator 1 is an orally active, highly efficacious small molecule IL-17 modulators extracted from patent WO 2020127685. IL-17 modulator 1 can be used for the research of preventing, researching or ameliorating a variety of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis .
    IL-17 modulator 1
  • HY-118709
    Ro 23-7637

    		Others Metabolic Disease
    Ro 23-7637 is an orally active, efficacious antiobesity agent .
    Ro 23-7637
  • HY-15199
    Agerafenib hydrochloride

    CEP-32496 hydrochloride; RXDX-105 hydrochloride

    		 Raf Cancer
    Agerafenib hydrochloride is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM.
    Agerafenib hydrochloride
  • HY-111368
    EBI-1051

    		MEK Cancer
    EBI-1051 is a highly potent and orally efficacious MEK inhibitor with an IC50 of 3.9 nM.
    EBI-1051
  • HY-115721
    Antimalarial agent 2

    		Parasite Infection
    Antimalarial agent 2 is a novel orally efficacious antimalarials that suggests a fast in vitro killing profile.
    Antimalarial agent 2
  • HY-145352
    ChemR23-IN-2

    		Others Inflammation/Immunology
    ChemR23-IN-2 is a potent and orally efficacious ChemR23 inhibitor with an IC50 value of 3.2 nM.
    ChemR23-IN-2
  • HY-15200
    Agerafenib
    Maximum Cited Publications
    8 Publications Verification

    CEP-32496; RXDX-105

    		 Raf Cancer
    Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM.
    Agerafenib
  • HY-122078
    FR-190809

    		Acyltransferase Metabolic Disease
    FR-190809 is a potent, nonadrenotoxic, orally efficacious acyl-CoA:cholesterol O-acyltransferase (ACAT) inhibitor, with an IC50 of 45 nM .
    FR-190809
  • HY-15253
    Tiplaxtinin
    5+ Cited Publications

    PAI-039; Tiplasinin

    		 PAI-1 Apoptosis Metabolic Disease Cancer
    Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM .
    Tiplaxtinin
  • HY-132922
    EEDi-5273

    APG-5918

    		 Histone Methyltransferase Cancer
    EEDi-5273 is an exceptionally potent and orally efficacious EED inhibitor (IC50 = 0.2 nM) capable of achieving complete and persistent tumor regression.
    EEDi-5273
  • HY-142162
    LSN3318839

    		GCGR Metabolic Disease
    LSN3318839 is an orally efficacious positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R).
    LSN3318839
  • HY-10268S
    Betrixaban-d6

    		Factor Xa Cardiovascular Disease
    Betrixaban-d6 is a deuterium labeled Betrixaban. Betrixaban is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor[1].
    Betrixaban-d6
  • HY-10268
    Betrixaban
    4 Publications Verification

    PRT054021

    		 Factor Xa Cardiovascular Disease
    Betrixaban (PRT054021) is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban shows antithrombotic effect .
    Betrixaban
  • HY-128354
    CWHM-1552

    		Parasite Infection
    CWHM-1552 is an orally efficacious inhibitor of P. falciparum with IC50s of 51 nM and 53 nM for 3D7 and Dd2 strain, respectively .
    CWHM-1552
  • HY-10268B
    Betrixaban hydrochloride

    PRT054021 hydrochloride

    		 Factor Xa Cardiovascular Disease
    Betrixaban (PRT054021) hydrochloride is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban hydrochloride shows antithrombotic effect .
    Betrixaban hydrochloride
  • HY-10268A
    Betrixaban maleate

    PRT054021 maleate

    		 Factor Xa Cardiovascular Disease
    Betrixaban (PRT054021) maleate is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban maleate shows antithrombotic effect .
    Betrixaban maleate
  • HY-145704
    Antimalarial agent 8

    		Parasite Infection
    Antimalarial agent 8 (Compound 7e) is a novel orally active class of antimalarials. Antimalarial agent 8 is potent in vitro against P. falciparum and is orally efficacious (40 mg/kg) in an in vivo mouse model of malaria .
    Antimalarial agent 8
  • HY-112542
    Nemadectin

    CL-287088; LL-F28249 α

    		 Parasite Antibiotic Infection
    Nemadectin (CL-287088), an orally active broad-spectrum endectocide, is highly efficacious against natural infections of all the major canine gastrointestinal helminthes. Anthelmintic activity .
    Nemadectin
  • HY-120608
    BMS-814580

    		MCHR1 (GPR24) Metabolic Disease
    BMS-814580 is an orally active, highly efficacious MCHR1 inhibitor with a Ki of 16.9 nM against hMCHR1. BMS-814580 shows antiobesity activities .
    BMS-814580
  • HY-102036
    G-744

    		Btk Inflammation/Immunology
    G-744 is a highly potent, selective and orally active Btk inhibitor with an IC50 of 2 nM. G-744 is metabolically stable, well tolerated and efficacious to treat arthritis .
    G-744
  • HY-N1428C
    Ferric citrate
    1 Publications Verification

    Iron(III) citrate; Zerenex

    		 Reactive Oxygen Species Antibiotic Metabolic Disease
    Ferric citrate (Iron(III) citrate), an orally active iron supplement, is an efficacious phosphate binder. Ferric citratee can be used for iron deficiency anemia and chronic kidney disease (CKD) research .
    Ferric citrate
  • HY-130253
    IRAK4-IN-6

    		IRAK Cancer
    IRAK4-IN-6 is an orally efficacious and selective IRAK4 inhibitor with an IC50 of 4 nM, and targetes MyD88 L265P mutant diffuse large B cell lymphoma .
    IRAK4-IN-6
  • HY-141692A
    IL-17 modulator 4 sulfate

    		Interleukin Related Inflammation/Immunology
    IL-17 modulator 4 sulfate is a proagent of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator .
    IL-17 modulator 4 sulfate
  • HY-112542R
    Nemadectin (Standard)

    		Parasite Antibiotic Infection
    Nemadectin (Standard) is the analytical standard of Nemadectin. This product is intended for research and analytical applications. Nemadectin (CL-287088), an orally active broad-spectrum endectocide, is highly efficacious against natural infections of all the major canine gastrointestinal helminthes. Anthelmintic activity .
    Nemadectin (Standard)
  • HY-12738
    PF-3882845

    		Mineralocorticoid Receptor Progesterone Receptor Cardiovascular Disease Metabolic Disease
    PF-3882845 is a remarkably high affinity selective and orally efficacious mineralocorticoid receptor (MR binding IC50=2.7 nM) antagonist for hypertension and nephropathy. PF-3882845 also binds to progesterone receptor (PR) with the binding IC50 of 310 nM .
    PF-3882845
  • HY-10596
    BMS-688521
    1 Publications Verification

    		 Integrin Inflammation/Immunology
    BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC50 of 2.5 nM in the adhesion assay and an IC50 of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model .
    BMS-688521
  • HY-115987
    MAO-B-IN-6

    		Monoamine Oxidase Neurological Disease
    MAO-B-IN-6 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.019 µM. MAO-B-IN-6 shows more efficacious than Safinamide in vitro and in vivo. MAO-B-IN-6 has the potential for the research of parkinson's disease (PD) .
    MAO-B-IN-6
  • HY-121212
    Icosabutate

    		Others Metabolic Disease Inflammation/Immunology
    Icosabutate, an orally active ω-3 polyunsaturated fatty acid, is an aeicosapentaenoic acid (EPA) derivative. Icosabutate overcomes the drawbacks of unmodified EPA for liver targeting and improves insulin sensitivity, hepatic inflammation and fibrosis . Icosabutate is well tolerated, and efficacious in lowering non-high-density lipoprotein cholesterol (non-HDL-C) levels in persistent hypertriglyceridemia  .
    Icosabutate
  • HY-141692B
    (R)-IL-17 modulator 4

    		Interleukin Related Inflammation/Immunology
    (R)-IL-17 modulator 4 is the R-configure of IL-17 modulator 4 (HY-141692). IL-17 modulator 4 is a proagent of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator .
    (R)-IL-17 modulator 4
  • HY-11051
    JNJ-20788560

    		Opioid Receptor Inflammation/Immunology
    JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia .
    JNJ-20788560
  • HY-107427
    PF-3644022
    1 Publications Verification

    		 MAPKAPK2 (MK2) p38 MAPK Inflammation/Immunology
    PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect .
    PF-3644022
  • HY-12445
    Asnuciclib
    2 Publications Verification

    CDKI-73; LS-007

    		 CDK Apoptosis Inflammation/Immunology Cancer
    Asnuciclib (CDKI-73; LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. Asnuciclib down-regulates the RNAPII phosphorylation. Asnuciclib is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion .
    Asnuciclib
  • HY-141692
    IL-17 modulator 4

    		Interleukin Related Inflammation/Immunology Cancer
    IL-17 modulator 4 is a proagent of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator. IL-17 modulator 4 is promising for the research of IL-17A mediated diseases, including inflammation, autoimmune diseases, infectious diseases, cancer, and precancerous syndrome .
    IL-17 modulator 4
  • HY-128774
    AM-6494

    		Beta-secretase Neurological Disease
    AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM) . AM-6494 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    AM-6494
  • 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-146399
    AChE/BChE-IN-9

    		Cholinesterase (ChE) ROS Kinase Neurological Disease
    AChE/BChE-IN-9 (Compound 7a) is a potent, orally active AChE and BChE inhibitor with IC50 values of 5.74 μM and 14.05 μM against hAChE and eqBChE, respectively. AChE/BChE-IN-9 is also an efficacious antioxidant with an IC50 of 57.35 μM. AChE/BChE-IN-9 is able to chelate iron and modulates aggregation of amyloid β1-42. AChE-IN-16 can cross the BBB .
    AChE/BChE-IN-9
  • HY-16911
    AFN-1252
    Maximum Cited Publications
    8 Publications Verification

    API-1252; Debio 1452

    		 Bacterial Antibiotic Infection
    AFN-1252 is an orally active and selective inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 exhibits exquisite and highly selective activity against Staphylococcus spp. AFN-1252 exhibits typical MIC90 values of ⩽0.015 μg/ml against diverse clinical isolates of S. aureus. AFN-1252 is efficacious in a mouse model of septicemia providing 100% protection from an otherwise lethal peritoneal infection of S. aureus Smith .
    AFN-1252
  • HY-133011
    nAChR agonist 1

    		nAChR Neurological Disease
    nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease .
    nAChR agonist 1
  • HY-114622
    AFN-1252 tosylate

    API-1252 tosylate; Debio 1452 tosylate

    		 Bacterial Antibiotic Infection
    AFN-1252 (API-1252) tosylate is an orally active and selective inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 tosylate exhibits exquisite and highly selective activity against Staphylococcus spp. AFN-1252 tosylate exhibits typical MIC90 values of ?0.015 μg/ml against diverse clinical isolates of S. aureus. AFN-1252 tosylate is efficacious in a mouse model of septicemia providing 100% protection from an otherwise lethal peritoneal infection of S. aureus Smith .
    AFN-1252 tosylate
  • HY-153321
    NX-5948

    BTK-IN-24

    		 Btk PROTACs Inflammation/Immunology Cancer
    NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
    NX-5948

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