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safety

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79

Inhibitors & Agonists

126

Screening Libraries

1

Biochemical Assay Reagents

3

Inhibitory Antibodies

5

Natural
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3

Isotope-Labeled Compounds

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

    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.
  • HY-143499
    hMAO-B-IN-3

    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 drug-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.
  • HY-144389
    hAChE/Aβ1-42-IN-1

    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).
  • HY-105040
    Pomaglumetad methionil

    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.
  • HY-146019
    HIV-1 inhibitor-24

    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.
  • HY-146371
    COX-2-IN-13

    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.
  • HY-146370
    COX-2-IN-12

    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.
  • HY-115494
    Neladenoson dalanate hydrochloride

    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.
  • HY-123353
    Neladenoson dalanate

    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.
  • HY-130000
    Pirmitegravir

    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.
  • HY-150550
    COX-2-IN-26

    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.
  • HY-146883A
    As-358 hydrochloride

    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.
  • HY-103583
    KDU731

    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 drug candidate for the treatment of diarrhea caused by Cryptosporidium and meets a broad range of safety.
  • HY-147657
    GABAA receptor modulator-2

    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.
  • HY-115864
    TAK-653

    iGluR Neurological Disease
    TAK-653, an AMPA receptor potentiator with minimal agonistic activity, produces an antidepressant-like effect with a favorable safety profile in rats.
  • HY-16997A
    Itacitinib adipate

    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.
  • HY-108711
    GPR120 Agonist 1

    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.
  • HY-116489
    Pyribenzoxim

    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.
  • HY-124623
    DNDI-8219

    Parasite Infection
    DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.
  • HY-114301
    PF-06305591

    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.
  • HY-148504
    5'-ODMT cEt G Phosphoramidite (Amidite)

    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.
  • HY-114301A
    PF-06305591 dihydrate

    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.
  • HY-128337
    AN7973

    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 drug candidate for treating cryptosporidiosis.
  • HY-P99789
    Praluzatamab ravtansine

    CX-2009; CD166

    Antibody-Drug Conjugates (ADCs) Cancer
    Praluzatamab ravtansine (CX-2009) is an anti-CD166 antibody drug conjugate (ADC) with an Kd value of 25.15 nM. Praluzatamab ravtansine shows safety, tolerance and anticancer in phase 1/2 test.
  • HY-148506
    5'-ODMT cEt m5U Phosphoramidite (Amidite)

    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.
  • HY-100427
    Imazamox

    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.
  • HY-145574
    Iruplinalkib

    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.
  • HY-111021
    ASP-4058

    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.
  • HY-111021A
    ASP-4058 hydrochloride

    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.
  • HY-133167
    Clothianidin

    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.
  • HY-14670
    Firocoxib

    ML 1785713

    COX Inflammation/Immunology
    Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects.
  • HY-109083
    Cilofexor

    GS-9674

    FXR Autophagy Inflammation/Immunology
    Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.
  • HY-B0743A
    Pipecuronium bromide

    nAChR Neurological Disease
    Pipecuronium bromide is a potent long-acting nondepolarizing steroidal neuromuscular blocking agent (NMBA), and a bisquaternary ammonium compound. Pipecuronium bromide is a powerful competitive nAChR antagonist with a Kd of 3.06 μM.
  • HY-114300
    DSP-0565

    Others Neurological Disease
    DSP-0565 (compound 17a) is a strong, broad-spectrum anti-epileptic drug (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.
  • HY-113603
    Tildacerfont

    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.
  • HY-100375
    Diroximel fumarate

    ALKS 8700; BIIB098

    Others Others
    Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) prodrug in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS).
  • HY-115989
    HCV-IN-38

    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.
  • HY-144829
    PI3Kα-IN-5

    PI3K mTOR Cancer
    PI3Kα-IN-5 (Compound 6ab) is a potent PI3Kα inhibitor with an IC50 of 0.7 nM. PI3Kα-IN-5 shows antitumor activity with good metabolic stabilities and safety profiles.
  • HY-145311
    Bis-Pro-5FU

    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.
  • HY-134790
    GST-HG131

    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.
  • HY-105327
    P11149

    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.
  • HY-114196
    Aclimostat

    ZGN-1061

    Others Metabolic Disease
    Aclimostat (ZGN-1061) is a potent inhibitor of the MetAP2 enzyme and displays favorable efficacy and safety in preclinical studies. ZGN-1061 produced similar efficacy as beloranib for weight loss, improvements in metabolic parameters in a mouse model of obesity and insulin resistance, and concordant changes in gene transcription in HepG2 cells.
  • HY-107784
    Ectoine

    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.
  • HY-146453
    TGR5 Receptor Agonist 3

    G protein-coupled Bile Acid Receptor 1 Metabolic Disease
    TGR5 Receptor Agonist 3 (Compound 19) is a soft-drug 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.
  • HY-100427S
    Imazamox-13C,d3

    CL29926-13C,d3; (±)-Imazamox-13C,d3

    Isotope-Labeled Compounds Acetolactate Synthase (ALS) Others
    Imazamox- 13C,d3 is the 13C- and deuterium labeled Imazamox. 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[1][2].
  • HY-18767
    Ivosidenib

    AG-120

    Isocitrate Dehydrogenase (IDH) Cancer Metabolic Disease
    Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity.
  • HY-17552
    sn-Glycero-3-phosphocholine

    Choline Alfoscerate; Alpha-GPC; L-α-GPC

    Cholinesterase (ChE) Endogenous Metabolite Neurological Disease
    sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia.
  • HY-147698
    ZLHQ-5f

    CDK Topoisomerase Apoptosis Cancer
    ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile.
  • HY-P99594
    Socazolimab

    ZKAB001; STI-1014; STI-A1014

    PD-1/PD-L1 Cancer
    Socazolimab (ZKAB001) is an anti-PD-L1 monoclonal antibody. Socazolimab has lasting safety and efficacy in the treatment of recurrent or metastatic cervical cancer. Socazolimab also has potential applications in small cell lung cancer, esophageal squamous cell carcinoma (ESCC), advanced urothelial carcinoma and osteosarcoma.
  • HY-151389
    BChE-IN-14

    Cholinesterase (ChE) Neurological Disease
    BChE-IN-14 (compound 19c) is a selective butyrylcholinesterase (BChE) inhibitor with IC50s of 0.23 and 0.011 μM for eqBChE and hBChE, respectively. BChE-IN-14 shows good blood brain barrier permeation and primary cell safety. BChE-IN-14 is able to restore cognitive impairment in vivo, it can be used for the research of Alzheimer’s disease.
  • HY-151813
    NNMT-IN-4

    Others Cancer
    NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT.
  • HY-151933
    HIV-1 inhibitor-49

    HIV Reverse Transcriptase Infection
    HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model.
  • HY-14405A
    Casopitant mesylate

    GW679769B

    Neurokinin Receptor Cytochrome P450 Neurological Disease Cancer
    Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of substance P. Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
  • HY-B1295
    Lithium citrate tetrahydrate

    Litarex tetrahydrate

    ATP Citrate Lyase Bacterial HIF/HIF Prolyl-Hydroxylase Endogenous Metabolite Cancer Infection Metabolic Disease Inflammation/Immunology
    Lithium citrate (Litarex) tetrahydrate is the major active ingredient of Garcinia cambogia. Lithium citrate tetrahydrate competitively inhibits ATP citrate lyase with weight loss benefits. Lithium citrate tetrahydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects.
  • HY-107427
    PF-3644022

    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.
  • HY-W009156
    Hydroxycitric acid tripotassium hydrate

    Potassium citrate monohydrate

    ATP Citrate Lyase HIF/HIF Prolyl-Hydroxylase Bacterial Endogenous Metabolite Cancer Infection Metabolic Disease Inflammation/Immunology
    Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia. Hydroxycitric acid tripotassium hydrate competitively inhibits ATP citrate lyase with weight loss benefits. Hydroxycitric acid tripotassium hydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects.
  • HY-145552
    Azilsartan mepixetil

    Angiotensin Receptor Cardiovascular Disease
    Azilsartan mepixetil is the antagonist of angiotensin II receptor. Azilsartan mepixetil has stronger and longer blood pressure effect, more abvious and longer lasting heart rate lowering effect and high safety. Azilsartan mepixetil achieves ideal protective effect for heart and kidney functions. Azilsartan mepixetil has the potential for the research of hypertension, chronic heart failure and diabetic nephropathy (extracted from patent CN107400122A).
  • HY-133167S
    Clothianidin-d3

    Isotope-Labeled Compounds Others
    Clothianidin-d3 is the deuterium labeled Clothianidin.Clothianidin-d3 is a neonicotinoid insecticide. Clothianidin-d3 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-d3 has various application methods and high safety for crops.
  • HY-111755
    Oral antiplatelet agent 1

    P2Y Receptor Cardiovascular Disease
    Oral antiplatelet agent 1 is a potent P2Y12 receptor antagonist. Oral antiplatelet agent 1 exhibits excellent antiplatelet aggregation potency with an IC50 value of 2.94 μM as well as antithrombotic efficacy in a rat ferric chloride model. Oral antiplatelet agent 1 shows a superior safety profile than Clopidogrel (HY-15283) in a rat tail-bleeding model. Oral antiplatelet agent 1 can be used to research thromboembolic disorders.
  • HY-145284
    APJ receptor agonist 4

    Apelin Receptor (APJ) Cardiovascular Disease
    APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease.
  • HY-136576
    RP101075

    LPL Receptor Drug Metabolite Inflammation/Immunology
    RP101075, an active metabolite of Ozanimod, is a potent, orally active S1PR (sphingosine-1-phosphate receptor 1) agonist, with an EC50 of 0.27 nM. RP101075 displays >100-fold selectivity over S1PR5 (EC50=5.9 nM) and >10000-fold over S1PR 2, 3, and 4. RP101075 displays superior cardiovascular safety profile.
  • HY-106005
    MMV390048

    Parasite PI4K Infection
    MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kd app=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent.
  • HY-17552S
    sn-Glycero-3-phosphocholine-d9

    Choline Alfoscerate-d9; Alpha-GPC-d9; L-α-GPC-d9

    Cholinesterase (ChE) Endogenous Metabolite Neurological Disease
    sn-Glycero-3-phosphocholine-d9 is the deuterium labeled sn-Glycero-3-phosphocholine. sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia[1][2].
  • HY-145285
    APJ receptor agonist 5

    Apelin Receptor (APJ) Cardiovascular Disease
    APJ receptor agonist 5 (compound 3) is a potent and orally active agonist of apelin receptor (APJ) with an EC50 of 0.4 nM. APJ receptor agonist 5 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 5 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 5 leads to improved cardiac function and can be used for researching the HF disease.
  • HY-125881
    ASP1126

    LPL Receptor Inflammation/Immunology
    ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively. ASP1126 decreases the number of peripheral lymphocytes, naive T cells, central memory T cells and effector memory T cells in the peripheral blood. ASP1126 has the potential to be applied in clinical transplantation with improved safety profile.
  • HY-13499
    CCR2 antagonist 5

    CCR Inflammation/Immunology
    CCR2 antagonist 5 is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). CCR2 antagonist 5 displays a Ki of 9.6 µM for mCCR2 binding. CCR2 antagonist 5 can be used in the research of inflammatory disease.
  • HY-146372
    CXCR4 antagonist 5

    CXCR Cancer
    CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC50 value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately.
  • HY-144122
    HIV-1 inhibitor-15

    HIV Infection
    HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability.
  • HY-151156
    EGFR/HER2-IN-6

    EGFR Apoptosis Cancer
    EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer.
  • HY-120802
    Navafenterol

    AZD-8871; LAS191351

    mAChR Adrenergic Receptor Inflammation/Immunology
    Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile.
  • HY-151161
    EGFR/HER2-IN-8

    EGFR Cancer
    EGFR/HER2-IN-8 (compound 34) is a EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-8 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.45, 0.244 and 5.669 μM, respectively. EGFR/HER2-IN-8 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer.
  • HY-120802A
    Navafenterol saccharinate

    AZD-8871 saccharinate; LAS191351 saccharinate

    mAChR Adrenergic Receptor Infection Inflammation/Immunology
    Navafenterol (AZD-8871) saccharinate is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile.
  • HY-144297
    HDAC1-IN-3

    HDAC Parasite Infection
    HDAC1-IN-3 is a potent Pf HDAC1 inhibitor. HDAC1-IN-3 shows antimalarial activity in wild-type and multidrug-resistant parasite strains. HDAC1-IN-3 shows a significant in vivo killing effect against all life cycles of parasites.
  • HY-115993
    CDK4/6-IN-10

    CDK Apoptosis Cancer
    CDK4/6-IN-10 is a potent, selective and orally active CDK4 and CDK6 inhibitor with IC50s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM).
  • HY-150057
    CB1R Allosteric modulator 4

    Cannabinoid Receptor Others
    CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment.
  • HY-B1075
    Fosfomycin calcium

    MK-​0955 calcium

    Bacterial Antibiotic Infection Cancer
    Fosfomycin (MK-0955) calcium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin calcium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
  • HY-W016420
    Fosfomycin sodium

    MK-0955 sodium

    Bacterial Antibiotic Infection Cancer
    Fosfomycin (MK-0955) sodium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin sodium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
  • HY-B0609
    Fosfomycin tromethamine

    MK-0955 tromethamine

    Bacterial Antibiotic Infection Cancer
    Fosfomycin (MK-0955) tromethamine is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin tromethamine shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
  • HY-B1075A
    Fosfomycin

    MK-0955

    Bacterial Antibiotic Infection
    Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.