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40

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2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15043

    Bradykinin Receptor Inflammation/Immunology Endocrinology
    ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse .
    ELN-441958
  • HY-139981

    Microtubule/Tubulin Cancer
    Microtubule destabilizing agent-1 (Compound 12b) acts as a microtubule destabilizing agent (MDA) based on hydroxamic acid, could serve as a potential MDA for further investigation. Microtubule destabilizing agent-1 shows favorable metabolism stability, high bioavailability, and potent antitumor activity .
    Microtubule destabilizing agent-1
  • HY-151360

    Sodium Channel Metabolic Disease
    NHE3-IN-3 (Compound 1) is a Na +/H + exchanger isoform 3 (NHE3) inhibitor with pIC50 of 6.2 and 6.6 against human and rat NHE3, respectively. NHE3-IN-3 shows high (98%) oral bioavailability in Sprague–Dawley rats .
    NHE3-IN-3
  • HY-101699A

    MCHR1 (GPR24) Metabolic Disease
    AMG-076 is an orally bioavailable and selective MCHR1 antagonist. AMG-076 results in significant reduction in body weight gain in nonobese mice fed a high-fat diet and in high-fat diet-induced obese (DIO) mice .
    AMG-076
  • HY-161061

    Arginase Cancer
    Arginase inhibitor 7 (compound A17) is an arginase (ARG1) inhibitor, with an IC50 of 0.16 μM. Arginase inhibitor 7 has high oral bioavailability .
    Arginase inhibitor 7
  • HY-146223

    Ras Cancer
    AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
    AZD4625
  • HY-135230

    FP3FBZ

    Opioid Receptor Neurological Disease
    LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects .
    LY2444296
  • HY-15023
    Cligosiban
    5 Publications Verification

    PF-3274167

    Oxytocin Receptor Endocrinology
    Cligosiban (PF-3274167), a high oral bioavailability and good brain-penetrant non-peptide oxytocin receptor antagonist, shows a high-affinity (Ki=9.5 nM) and an excellent selectivity versus the vasopressin receptors with almost no affinity for the V1b and V1a subtypes. Cligosiban inhibits ejaculatory physiology in rodents .
    Cligosiban
  • HY-120634

    HCV Infection
    BMS-929075 is a potent and orally active HCV NS5B replicase palm site allosteric inhibitor. BMS-929075 shows high oral bioavailability. BMS-929075 shows cytotoxicity .
    BMS-929075
  • HY-149345

    IRAK Inflammation/Immunology
    IRAK4-IN-24 (compound 16) is a potent IRAK4 inhibitor, with high clearance (Cl) and poor oral bioavailability. IRAK4-IN-24 can be used for research in inflammatory and autoimmune disorders.
    IRAK4-IN-24
  • 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-127105A
    Iptacopan hydrochloride
    3 Publications Verification

    LNP023 hydrochloride

    Complement System Metabolic Disease Inflammation/Immunology
    LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. LNP023 inhibits factor B with an IC50 value of 10 nM .
    Iptacopan hydrochloride
  • HY-15419
    RS-127445 hydrochloride
    2 Publications Verification

    5-HT Receptor Neurological Disease
    RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
    RS-127445 hydrochloride
  • HY-15419A

    5-HT Receptor Neurological Disease
    RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
    RS-127445
  • HY-156593

    ROCK Cancer
    ROCK-IN-9 (Compound T345) is a ROCK inhibitor. ROCK-IN-9 shows cytotoxicity in HepG2 cell, with an IC50 of 40.8 μM. ROCK-IN-9 has good pharmacokinetic properties in mice, and shows high in vivo exposure and oral bioavailability at lower doses .
    ROCK-IN-9
  • HY-139211

    3,4-Difluorobenzylidene curcumin

    Others Cancer
    Difluorinated Curcumin (3,4-Difluorobenzylidene curcumin) is a fluorinated curcumin analog with high bioavailability and anticancer activity. Difluorinated Curcumin inhibits the self-renewal ability of tumor stem/stem-like cells, clonogenicity, invasiveness and angiogenesis of tumor cells. Difluorinated Curcumin also increases cell sensitivity to chemotherapy .
    Difluorinated Curcumin
  • HY-15010

    Oxytocin Receptor Vasopressin Receptor Endocrinology
    L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM) .
    L-371,257
  • HY-127105
    Iptacopan
    3 Publications Verification

    LNP023

    Complement System Metabolic Disease Inflammation/Immunology
    Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G) .
    Iptacopan
  • HY-144878
    VPC-70619
    1 Publications Verification

    c-Myc Cancer
    VPC-70619 is a potent, orally active N-Myc inhibitor. VPC-70619 blocks the N-Myc-Max heterocomplex from binding to DNA E-boxes and demonstrated strong inhibition activity against N-Myc-dependent cell lines as well as high bioavailability in both oral and intraperitoneal administration .
    VPC-70619
  • HY-153256

    Prostaglandin Receptor Metabolic Disease
    EP3 antagonist 4 (Compound 28) is an EP3 antagonist, with a Ki value of 2 nM for hEP. EP3 antagonist 4 shows low in vivo clearance, high oral AUC, and good bioavailability in the rat full PK studies. EP3 antagonist 4 can be used for research of beta cell dysfunction in diabetes .
    EP3 antagonist 4
  • HY-126321

    ROR Cancer
    RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC50 of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy .
    RORγt agonist 1
  • HY-111925
    BI-749327
    10+ Cited Publications

    TRP Channel Cardiovascular Disease
    BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7 .
    BI-749327
  • HY-B0717
    Tocofersolan
    3 Publications Verification

    TPGS; D-α-Tocopherol polyethylene glycol 1000 succinate; Vitamin E-TPGS

    Others Neurological Disease Metabolic Disease
    Tocofersolan is synthetic polyethylene glycol derivative of α-tocopherol. Tocofersolan is an orally active and water-soluble analog of vitamin E. Tocofersolan can reduce neurobehavioral deficits in zebrafish embryos exposed to moderate and high concentrations of BaP during early development. Tocofersolan shows antioxidant activity. Tocofersolan can be used to provide an orally bioavailable source of vitamin E .
    Tocofersolan
  • HY-146223A

    Others Cancer
    (3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
    (3R,10R,14aS)-AZD4625
  • HY-100555

    HSP Infection Cancer
    CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
    CH5138303
  • HY-124634
    PZ-2891
    1 Publications Verification

    Others Neurological Disease
    PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively .
    PZ-2891
  • HY-109118A

    SUVN-502 mesylate

    5-HT Receptor Neurological Disease
    Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate (SUVN-502 mesylate) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease .
    Masupirdine mesylate
  • HY-133747

    JAK Inflammation/Immunology
    JAK3-IN-9 is an orally active JAK3 inhibitor with IC50 value of 1.7 nM. JAK3-IN-9 is highly selective to the JAK3 signal path. JAK3-IN-9 is lowly toxic with high oral bioavailability, shows good anti-arthritis activity. JAK3-IN-9 can be used in autoimmune disease research .
    JAK3-IN-9
  • HY-109118

    SUVN-502 free base

    5-HT Receptor Neurological Disease
    Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base (SUVN-502 free base) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease .
    Masupirdine free base
  • HY-123857

    P2X Receptor Neurological Disease Inflammation/Immunology
    JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain .
    JNJ-55308942
  • HY-N1445
    Isoquercetin
    1 Publications Verification

    Quercetin 3-glucoside

    NF-κB NO Synthase Inflammation/Immunology Cancer
    Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway . Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies .
    Isoquercetin
  • HY-148825

    iGluR Histamine Receptor Potassium Channel Cytochrome P450 Adrenergic Receptor Metabolic Disease Inflammation/Immunology Cancer
    NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC50s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes .
    NP10679
  • HY-111790
    M3258
    1 Publications Verification

    Proteasome Apoptosis Cancer
    M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .
    M3258
  • HY-120184

    AZ13713945

    mAChR Neurological Disease
    VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
    VU0467485
  • HY-13238
    Dolutegravir
    Maximum Cited Publications
    19 Publications Verification

    S/GSK1349572

    HIV Integrase HIV Infection
    Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
    Dolutegravir
  • HY-153460

    Toll-like Receptor (TLR) Inflammation/Immunology
    TLR7/8/9 antagonist 2 is an orally active TLR7/8/9 antagonist. TLR7/8/9 antagonist 2 has inhibitory activities for HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50 values of 0.011 μM, 0.029 μM and 0,052 μM, respectively.TLR7/8/9 antagonist 2 has high bioavailability in vivo.TLR7/8/9 antagonist 2 can be used for the research of auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis .
    TLR7/8/9 antagonist 2
  • HY-13238A
    Dolutegravir sodium
    Maximum Cited Publications
    19 Publications Verification

    S/GSK1349572 sodium

    HIV Integrase HIV Infection
    Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
    Dolutegravir sodium
  • HY-13238S1

    S/GSK1349572-d3

    Isotope-Labeled Compounds HIV Integrase HIV Infection
    Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
    Dolutegravir-d3
  • HY-13238S2

    S/GSK1349572-d5

    Isotope-Labeled Compounds HIV Integrase HIV Infection
    Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
    Dolutegravir-d5
  • HY-144392

    Cholinesterase (ChE) Neurological Disease
    AChE/BuChE-IN-1 (Compound 1), a chrysin derivative, is a selective butyrylcholinesterase (BuChE) inhibitor with an IC50 of 0.48 μM. AChE/BuChE-IN-1 inhibits acetylcholinesterase (AChE) with an IC50 of 7.16 μM. AChE/BuChE-IN-1 shows strong scavenging ·OH activities with a IC50 of 0.1674 μM. AChE/BuChE-IN-1 inhibits reactive oxygen species (ROS), Aβ1-42 aggregation (self-, Cu2+-induced, AChE-induced). AChE/BuChE-IN-1 has high BBB permeability and bioavailability and low cell toxicity. AChE/BuChE-IN-1 has the potential for Alzheimer' disease (AD) research .
    AChE/BuChE-IN-1

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