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fourth-generation

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20

Inhibitors & Agonists

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0111
    Drospirenone
    1 Publications Verification

    Dihydrospirorenone

    		 Progesterone Receptor Androgen Receptor Endocrinology Cancer
    Drospirenone (Dihydrospirorenone) is an orally active fourth-generation progestin that interacts with the progesterone receptor (PR) and androgen receptor (AR). Drospirenone significantly decreases both plasminogen activator inhibitor-1 (PAI-1) and tissue plasminogen activator (tPA) via the AR. Drospirenone can produce DNA damage in bone marrow cells of female mice. .
    Drospirenone
  • HY-129550
    BI-4020

    		EGFR Cancer
    BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties .
    BI-4020
  • HY-17028
    Besifloxacin Hydrochloride

    		Bacterial Antibiotic DNA/RNA Synthesis Topoisomerase Infection Inflammation/Immunology
    Besifloxacin Hydrochloride is a fourth generation fluoroquinolone antibiotic. Besifloxacin Hydrochloride is a DNA gyrase and topoisomerase IV inhibitor. Besifloxacin Hydrochloride has broad-spectrum antibacterial activity, it is effective against Gram-negative and Gram-positive aerobic and anaerobic strains and reduces the incidence of drug resistance. Besifloxacin Hydrochloride has anti-inflammatory activity. Besifloxacin Hydrochloride can be used in bacterial conjunctivitis research .
    Besifloxacin Hydrochloride
  • HY-100213
    EAI045
    3 Publications Verification

    		 EGFR Cancer
    EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFR L858R, EGFR T790M and EGFR L858R/T790M at 10 μM ATP, respectively.
    EAI045
  • HY-13451
    Finafloxacin
    1 Publications Verification

    		 Antibiotic Bacterial Infection
    Finafloxacin is an orally active fourth-generation fluoroquinolone broad-spectrum antibiotic. Finafloxacin exhibits stronger antibacterial activity in acidic pH environments and is not easily affected by bacterial multidrug efflux transporters. Finafloxacin is effective against a variety of extracellular pathogenic bacteria, and can also accumulate in macrophages, showing excellent antibacterial activity against intracellular Staphylococcus aureus, Listeria monocytogenes, Legionella pneumophila, Burkholderia pseudomallei, and other pathogens. Finafloxacin has been approved by the U.S. FDA for research on acute otitis externa mediated by Pseudomonas aeruginosa. Finafloxacin is also used in studies related to diseases such as melioidosis, inhalational tularemia, and inhalational plague .
    Finafloxacin
  • HY-B0186B
    Cefoselis sulfate

    FK-037

    		 Bacterial Antibiotic Infection
    Cefoselis sulfate (FK-037), the fourth gen-eration of cephalosporin, is a β-lactam antibiotic. Cefoselis sulfate exhibits good activity against a wide range of Gram-positive and Gram-negative organisms. Cefoselis sulfate penetrates the blood-brain barrier .
    Cefoselis sulfate
  • HY-B0755
    Etimicin sulfate

    		Antibiotic Infection
    Etimicin (sulfate), a fourth-generation aminoglycoside antibiotic, is now widely clinically used due to its high efficacy and low toxicity.
    Etimicin sulfate
  • HY-156786
    TLD-1433

    		Reactive Oxygen Species (ROS) Influenza Virus SARS-CoV HSV Infection
    TLD-1433 is the fourth-generation ruthenium (II) based photodynamic compound (PDC). TLD-1433 is activated by green light (525 ± 25 nm) and efficiently generates ROS to achieve pathogen inactivation. After photoinactivation, TLD-1433 significantly induces lipid peroxidation of the cell membrane, which can directly damage the integrity of the viral envelope. TLD-1433 has ID50 for enveloped viruses (such as H1N1 influenza virus, coronavirus OC43, HSV-1, Zika virus) is as low as nanomolar level; for non-enveloped viruses (such as adenovirus Ad5, mammalian rotavirus MRV), a concentration of micro-molar level is required for inactivation. TLD-1433 has antigen retention property and can be used for the preparation of inactivated vaccines .
    TLD-1433
  • HY-130616
    EGFR-IN-11

    		EGFR Apoptosis Cancer
    EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1 .
    EGFR-IN-11
  • HY-B0699
    Cefpirome

    HR 810

    		 Antibiotic Bacterial Infection
    Cefpirome (HR 810) is a fourth generation cephalosporin. Cefpirome shows antibacterial activity. Cefpirome also has in vitro activity against Streptococcus pneumoniae .
    Cefpirome
  • HY-B0186
    Cefoselis

    		Bacterial Antibiotic Infection
    Cefoselis, the fourth gen-eration of cephalosporin, is a β-lactam antibiotic. Cefoselis exhibits good activity against a wide range of Gram-positive and Gram-negative organisms. Cefoselis penetrates the blood-brain barrier .
    Cefoselis
  • HY-156284
    EGFR-IN-89

    		EGFR Cancer
    EGFR-IN-89 (compound 13k) is a potent, fourth-generation EGFR mutation inhibitor with an IC50 of 10.1 nM against Del19/T790M/C797S mutations. EGFR-IN-89 shows higher selectivity over wild type .
    EGFR-IN-89
  • HY-B0186A
    Cefoselis hydrochloride

    		Bacterial Antibiotic Infection
    Cefoselis hydrochloride, the fourth gen-eration of cephalosporin, is a β-lactam antibiotic. Cefoselis hydrochloride exhibits good activity against a wide range of Gram-positive and Gram-negative organisms. Cefoselis hydrochloride penetrates the blood-brain barrier .
    Cefoselis hydrochloride
  • HY-155358
    Os30

    		EGFR Apoptosis Cancer
    Os30, a potent fourth-generation EGFR inhibitor, is a potent EGFRC797S-TK inhibitor with IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. Os30 can suppress EGFR phosphorylation, arrest at G1 phase and induce the apoptosis of KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. Os30 shows potent antitumor efficacy on non-small cell lung cancer (NSCLC) with EGFmRC797S mutation .
    Os30
  • HY-17028A
    (Rac)-Besifloxacin hydrochloride

    		Bacterial Antibiotic DNA/RNA Synthesis Topoisomerase Infection Inflammation/Immunology
    (Rac)-Besifloxacin Hydrochloride is a fourth generation fluoroquinolone antibiotic. (Rac)-Besifloxacin Hydrochloride is a DNA gyrase and topoisomerase IV inhibitor. (Rac)-Besifloxacin Hydrochloride has broad-spectrum antibacterial activity, it is effective against Gram-negative and Gram-positive aerobic and anaerobic strains and reduces the incidence of drug resistance. (Rac)-Besifloxacin Hydrochloride has anti-inflammatory activity. Besifloxacin Hydrochloride can be used in bacterial conjunctivitis research .
    (Rac)-Besifloxacin hydrochloride
  • HY-B0186BR
    Cefoselis sulfate (Standard)

    FK-037 (Standard)

    		 Reference Standards Bacterial Antibiotic Infection
    Cefoselis (sulfate) (Standard) is the analytical standard of Cefoselis (sulfate). This product is intended for research and analytical applications. Cefoselis sulfate (FK-037), the fourth gen-eration of cephalosporin, is a β-lactam antibiotic. Cefoselis sulfate exhibits good activity against a wide range of Gram-positive and Gram-negative organisms. Cefoselis sulfate penetrates the blood-brain barrier[1][2][3].
    Cefoselis sulfate (Standard)
  • HY-17028R
    Besifloxacin Hydrochloride (Standard)

    		Reference Standards Bacterial Antibiotic DNA/RNA Synthesis Topoisomerase Infection
    Besifloxacin (Hydrochloride) (Standard) is a fourth generation fluoroquinolone antibiotic. Besifloxacin Hydrochloride (Standard) is a DNA gyrase and topoisomerase IV inhibitor. Besifloxacin Hydrochloride (Standard) has broad-spectrum antibacterial activity, it is effective against Gram-negative and Gram-positive aerobic and anaerobic strains and reduces the incidence of drug resistance. Besifloxacin Hydrochloride (Standard) has anti-inflammatory activity. Besifloxacin Hydrochloride (Standard) can be used in bacterial conjunctivitis research .
    Besifloxacin Hydrochloride (Standard)
  • HY-B0771AR
    Cefozopran hydrochloride (Standard)

    SCE-2787 hydrochloride (Standard)

    		 Reference Standards Antibiotic Bacterial Penicillin-binding protein (PBP) Infection
    Cefozopran (SCE-2787) hydrochloride (Standard) is the analytical standard of Cefozopran hydrochloride. Cefozopran (SCE-2787) dihydrochloride is a potent antibiotic with broad-spectrum antibacterial activity. Cefozopran dihydrochloride binds PBPs, induces cell wall destruction, cell elongation, filamentation, irregular septa formation, and bactericidal, bacteriolytic activity. Cefozopran dihydrochloride reduces bacterial counts and eradicates bacteria in mouse respiratory, urinary, and thigh muscle infections. Cefozopran dihydrochloride can be used for the research of bacterial infections .
    Cefozopran hydrochloride (Standard)
  • HY-182622
    Etimicin

    		Antibiotic Bacterial Infection
    Etimicin is a fourth-generation semisynthetic aminoglycoside antibiotic. Etimicin exhibits broad spectrum of activity against gram-positive, gram-negative, and aminoglycoside-resistant bacterial strains, with lower ototoxicity and nephrotoxicity. Etimicin exerts rapid, concentration-dependent bactericidal activity against bacteria. Etimicin can be used for the research of bacterial infections .
    Etimicin
  • HY-100213R
    EAI045 (Standard)

    		EGFR Reference Standards Cancer
    EAI045 (Standard) is the analytical standard of EAI045 (HY-100213). This product is intended for research and analytical applications. EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFRL858R, EGFRT790M and EGFRL858R/T790M at 10 μM ATP, respectively.
    EAI045 (Standard)

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