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118

Inhibitors & Agonists

154

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3

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2

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3

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3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-122620

    Thrombopoietin Receptor Inflammation/Immunology Cancer
    Hetrombopag is a potent thrombopoietin receptor agonist. Hetrombopag is efficacious and well tolerated with a manageable safety profile. Hetrombopag has the potential for the research of immune thrombocytopenia .
    Hetrombopag
  • HY-143499

    Monoamine Oxidase Neurological Disease
    hMAO-B-IN-3 (Compound 15) is a potent inhibitor of hMAO-B with an IC50 of 47.4 nM. hMAO-B-IN-3 is playing favourable agent-like properties and a broad safety window. hMAO-B-IN-3 is thus a suitable candidate for lead optimization and the development of multitarget-directed ligands .
    hMAO-B-IN-3
  • HY-144389

    Cholinesterase (ChE) Amyloid-β Neurological Disease
    hAChE/Aβ1-42-IN-1 (Compound 16) is a potent inhibitor of hAChE and Aβ1-42 aggregation. hAChE/Aβ1-42-IN-1 shows acceptable relative safety upon hepG2 cell line and excellent BBB penetration with wide safety margin. hAChE/Aβ1-42-IN-1 has the potential for the research of Alzheimer disease (AD) .
    hAChE/Aβ1-42-IN-1
  • HY-105040

    LY2140023 hydrate

    mGluR Neurological Disease
    Pomaglumetad methionil (LY2140023 hydrate) is an oral methionine prodrug of the potent specific mGlu2/3 receptor agonist LY404039 (HY-50906). Pomaglumetad methionil is well-tolerated and has a distinct safety profile, and can be used for schizophrenia .
    Pomaglumetad methionil
  • HY-146371

    COX Inflammation/Immunology
    COX-2-IN-13 (compound 13e) is a potent and selective inhibitor of COX-2 with an IC50 of 0.98 μM. COX-2-IN-13 is an anti-inflammatory agent. COX-2-IN-13 shows safety in-vivo acute toxicity study .
    COX-2-IN-13
  • HY-146370

    COX Inflammation/Immunology
    COX-2-IN-12 (compound 3b) is a potent and selective inhibitor of COX-2 with an IC50 of 19.98 μM. COX-2-IN-12 is an anti-inflammatory agent. COX-2-IN-12 shows safety in-vivo acute toxicity study .
    COX-2-IN-12
  • HY-P9989

    REGN5458

    CD3 TNF Receptor Cancer
    Linvoseltamab is a bispecific antibody targeting to both BCMA (TNFRSF17) and CD3 epsilon. Linvoseltamab shows safety profile and encouraging efficacy in relapsed/refractory multiple myeloma (RRMM) models .
    Linvoseltamab
  • HY-115494

    Neladenoson bialanate hydrochloride; BAY-1067197 hydrochloride

    Adenosine Receptor Cardiovascular Disease
    Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) hydrochloride is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate hydrochloride has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases .
    Neladenoson dalanate hydrochloride
  • HY-123353

    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-130000

    STP0404

    HIV Integrase HIV Infection
    Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties .
    Pirmitegravir
  • HY-150550

    COX Inflammation/Immunology
    COX-2-IN-26 is a potent, selective and orally active COX-2 inhibitor with IC50 values of 10.61, 0.067, 1.96 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-26 shows anti-inflammatory activity. COX-2-IN-26 shows gastrointestinal safety profile .
    COX-2-IN-26
  • HY-149949

    Apoptosis Cancer
    Anticancer agent 105 is a compound based on thienopyrimidine scaffold, with with good safety and anticancer properties. Anticancer agent 105 shows selective toxicity towards melanoma cancer, and induces apoptosis. And Anticancer agent 105 significantly inhibits the metastatic nodules, even in pulmonary metastatic melanoma mouse model .
    Anticancer agent 105
  • HY-146019

    HIV Infection
    HIV-1 inhibitor-24 (compound S-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 9.5 nM. HIV-1 inhibitor-24 has high antiretroviral activity against WT HIV-1 with an EC50 of 1.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 9.07 μM in MT-4 cells. HIV-1 inhibitor-24 is well tolerated at a dose of 2 g/kg in mice and has a significant cardiovascular safety .
    HIV-1 inhibitor-24
  • HY-16997A
    Itacitinib adipate
    Maximum Cited Publications
    10 Publications Verification

    JAK Cancer
    Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.
    Itacitinib adipate
  • HY-108711

    Free Fatty Acid Receptor Metabolic Disease
    GPR120 Agonist 1 is a potent and selective GPR120 agonist, and possesses promising antidiabetic effect and good safety profile to be a development candidate .
    GPR120 Agonist 1
  • HY-116489

    LGC-40863

    Others Others
    Pyribenzoxim (LGC-40863) is a broad-spectrum herbicide. Pyribenzoxim has a higher safety level in bentgrass and a stronger herbicidal activity on grass weeds .
    Pyribenzoxim
  • HY-155465

    HPPD Others
    HPPD-IN-2 (compound 28) is a herbicide based on HPPD inhibitors. HPPD-IN-2 potently targets AtHPPD and exhibits enhanced safety in canola crops .
    HPPD-IN-2
  • HY-153624

    Fungal Infection
    Antifungal agent 59 is an antifungal agent, with MIC values of 0.01-1 μg/mL. Antifungal agent 59 prevents the formation of fungi biofilms, but also has safety .
    Antifungal agent 59
  • HY-114301

    Sodium Channel Neurological Disease
    PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile .
    PF-06305591
  • HY-123922

    Bacterial Infection
    NOSO-502 is an inhibitor of bacterial translation. NOSO-502 exhibits inhibitory activity against Enterobacteriaceae. NOSO-502 has good safety and antibacterial properties .
    NOSO-502
  • HY-149253

    Others Neurological Disease
    OY-201 is a potential and BBB-penetrated anti-ischemic stroke agent. OY-201 shows the good safety and neuroprotective activity in both in vitro and in vivo models .
    OY-201
  • HY-114301A

    Sodium Channel Neurological Disease
    PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile .
    PF-06305591 dihydrate
  • HY-148504

    Nucleoside Antimetabolite/Analog Cardiovascular Disease
    5'-ODMT cEt G Phosphoramidite Amidite is a potent nucleic acid analog. 5'-ODMT cEt G Phosphoramidite Amidite shows excellent safety and antisense activity .
    5'-ODMT cEt G Phosphoramidite (Amidite)
  • HY-146883A

    Filovirus Infection
    As-358 (hydrochloride) has inhibitory effects against Ebola virus and Marburg virus with IC50s of 9.1 μM and 18.1 μM, as well as exhibits good in vivo safety .
    As-358 hydrochloride
  • HY-161178

    Bacterial Infection
    LK-60 is a potent DprE1 inhibitor. LK-60 effectively inhibits the proliferation of Mycobacterium tuberculosis. LK-60 has good safety profiles to gut microbiota and human cells .
    LK-60
  • HY-128337

    Parasite Infection
    AN7973 is the 6-carboxamide benzoxaborole, blocks intracellular parasite development and inhibits Cryptosporidium growth. AN7973 is orally active, possesses favorable safety, stability, and PK parameters, and is an exciting agent candidate for treating cryptosporidiosis.
    AN7973
  • HY-153618

    Fungal Infection
    Antifungal agent 53 (A03) is a potent inhibitor of Candida albicans CYP51 with antifungal activity. Antifungal agent 53 prevents the formation of fungi biofilms. Antifungal agent 53 also exhibits good safety .
    Antifungal agent 53
  • HY-100427

    CL29926; (±)-Imazamox

    Acetolactate Synthase (ALS) Others
    Imazamox (CL29926) is a systemic herbicide that inhibits the production of acetolactate synthase (ALS) in plants with high selectivity, high activity, safety and broadspectrum activity, which would then inhibit plant growth and ultimately lead to plant death .
    Imazamox
  • HY-148506

    Nucleoside Antimetabolite/Analog Others
    5'-ODMT cEt m5U Phosphoramidite Amidite is a locked nucleic acid (LNA) analog. 5'-ODMT cEt m5U Phosphoramidite Amidite shows excellent safety and antisense activity .
    5'-ODMT cEt m5U Phosphoramidite (Amidite)
  • HY-145574

    WX-0593

    Anaplastic lymphoma kinase (ALK) ROS Kinase Cancer
    Iruplinalkib (WX-0593) is a potent, selective, and orally active inhibitor of ALK and ROS1 tyrosine kinase. Iruplinalkib (WX-0593) shows favorable safety and promising antitumor activity in advanced NSCLC with ALK or ROS1 rearrangement .
    Iruplinalkib
  • HY-153192

    BI 1015550

    Phosphodiesterase (PDE) Inflammation/Immunology
    Nerandomilast (BI 1015550) is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD) .
    Nerandomilast
  • HY-111021
    ASP-4058
    1 Publications Verification

    LPL Receptor Inflammation/Immunology
    ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile .
    ASP-4058
  • HY-111021A

    LPL Receptor Inflammation/Immunology
    ASP-4058 hydrochloride is a next-generation, selective and orally active agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile .
    ASP-4058 hydrochloride
  • HY-153192A

    BI 1015550 dihydrate

    Phosphodiesterase (PDE) Inflammation/Immunology
    Nerandomilast (BI 1015550) dihydrate is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast (dihydrate) has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD) .
    Nerandomilast dihydrate
  • HY-P5126

    Somatostatin Receptor Cancer
    DOTA-LM3 is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 and 68 Ga-DOTA-LM3. 68 Ga-DOTA-LM3 shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis .
    DOTA-LM3
  • HY-P5126A

    Somatostatin Receptor Cancer
    DOTA-LM3 TFA is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 TFA is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 TFA and 68 Ga-DOTA-LM3 TFA. 68 Ga-DOTA-LM3 TFA shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 TFA can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis .
    DOTA-LM3 TFA
  • HY-133167

    Others Others
    Clothianidin is a neonicotinoid insecticide. Clothianidin shows excellent long-term control effect in small doses against various insect pests such as Coleoptera, Thysanoptera, Lepidoptera, Diptera, Homoptera, Heteroptera, Orthoptera and Isoptera families. Clothianidin has various application methods and high safety for crops .
    Clothianidin
  • HY-114300

    Others Neurological Disease
    DSP-0565 (compound 17a) is a strong, broad-spectrum anti-epileptic agent (AED) candidate with unique GABAergic function. DSP-0565 shows anti-convulsant activity in various models (scPTZ, MES, 6 Hz and amygdala kindling) with good safety margin .
    DSP-0565
  • HY-103583

    PI4K Parasite Infection
    KDU731, an orally active C. parvum PI4K inhibitor with an IC50 value of 25 nM, blocks Cryptosporidium infection in vitro and in vivo . KDU731 is a promising agent candidate for the treatment of diarrhea caused by Cryptosporidium and meets a broad range of safety .
    KDU731
  • HY-113603

    SPR001; LY2371712

    CRFR Cancer
    Tildacerfont is a potent and orally active corticotrophin-releasing factor type 1 (CRF1) receptort antagonis. Tildacerfont effectively reduces adrenocorticotropic hormone (ACTH) and adrenal androgen levels. Tildacerfont has favourable safety profile. Tildacerfont can be used for researching congenital adrenal hyperplasia .
    Tildacerfont
  • HY-115989

    HCV Infection
    HCV-IN-38 is a potent, selective and orally active HCV inhibitor (EC50=15 nM, SI=431). HCV-IN-38 has high anti-HCV activity and low cytotoxicity. HCV-IN-38 has a good safety and oral pharmacokinetic profile .
    HCV-IN-38
  • HY-147657

    GABA Receptor Neurological Disease
    GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety .
    GABAA receptor modulator-2
  • HY-149355

    COX Inflammation/Immunology
    COX-2-IN-33 (compound 5f) is a COX-2 inhibitor (IC50=45.5 nM), as well as a potential anti-inflammatory agent. COX-2-IN-33 inhibits in vivo pro-inflammatory cytokine production and keep gastric safety .
    COX-2-IN-33
  • HY-145311

    Nucleoside Antimetabolite/Analog Cancer
    Bis-Pro-5FU (Compound 4) is a 5-FU precursor that confers oral bioavailability and increase the safety profile of 5-Fluorouracil (5-FU) chemotherapy regimens. 5-FU is an antineoplastic antimetabolite that is widely used for the research of colorectal and pancreatic cancer .
    Bis-Pro-5FU
  • HY-146453

    G protein-coupled Bile Acid Receptor 1 Metabolic Disease
    TGR5 Receptor Agonist 3 (Compound 19) is a soft-agent G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist with reduced gallbladder-filling effects (favorable gallbladder safety), with EC50s of 16.4 and 209 nM for hTGR5 and mTGR5, respectively.
    TGR5 Receptor Agonist 3
  • HY-134790

    HBV Infection
    GST-HG131 is a specific inbihitor of hepatitis B virus (HBV) surface antigen, belongs to dihydrobenzopyridooxazepine (DBP) series. GST-HG131 exhibits excellent and specific HBV antigens inhibition with EC50 of 28.2 nM (HBsAg) and 16.0 nM (HBeAg), respectively, but also it is safety for animal .
    GST-HG131
  • HY-157121

    JAK Inflammation/Immunology
    JAK-IN-34 (compound 11n) is a potent against of JAKs with IC50 values of 0.40, 0.83, 2.10, 1.95 nM target JAK1, JAK2, JAK3, TYK2, respectively. JAK-IN-34 reduces joint swelling with good safety .
    JAK-IN-34
  • HY-107784

    Bacterial Inflammation/Immunology
    Ectoine is a natural cell protectant, an amino acid derivate produced by bacteria living under extremely harsh environmental conditions. Ectoine serves as an osmoregulatory compatible solute, increasing the hydration of the skin surface and stabilizing lipid layers, which is useful in skincare. Ectoine demonstrates a good safety profile for the treatment of allergic rhinitis .
    Ectoine
  • HY-105327

    Cholinesterase (ChE) Neurological Disease
    P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC50 of 1.3 μM for rat BChE/AChE. P11149, a Galanthamine derivative, demonstrates central cholinergic activity, behavioral efficacy and safety. P11149 is used in the study for Alzheimer's disease .
    P11149
  • HY-100427R

    CL29926 (Standard); (±)-Imazamox (Standard)

    Acetolactate Synthase (ALS) Others
    Imazamox (Standard) is the analytical standard of Imazamox. This product is intended for research and analytical applications. Imazamox (CL29926) is a systemic herbicide that inhibits the production of acetolactate synthase (ALS) in plants with high selectivity, high activity, safety and broadspectrum activity, which would then inhibit plant growth and ultimately lead to plant death .
    Imazamox (Standard)

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