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safety properties

" in MedChemExpress (MCE) Product Catalog:

17

Inhibitors & Agonists

15

Screening Libraries

2

Biochemical Assay Reagents

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-151813

    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 .
    NNMT-IN-4
  • 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-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-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-148178

    Parasite Infection
    MMV688533 is an antimalarial agent with rapid anti-plasmodial activity and effective single-dose activity against Plasmodium falciparum infection in humanized mouse models. MMV688533 can inhibit the activity of asexual blood stage parasites with an IC50 value of 1.3 nM. MMV688533 exhibits excellent pharmacokinetic properties and safety .
    MMV688533
  • HY-16505

    Others Neurological Disease
    Triclofos sodium is a drug used to suppress insomnia and for sedation and has sedative activity. Triclofos sodium is used in children for sedation during painless medical procedures, particularly in children with neurocognitive disorders. Triclofos sodium has similar physiological and pharmacological properties to chloral and therefore can be used as a substitute when necessary. The safety and efficacy of Triclofos sodium have been demonstrated in pediatric populations with high rates of neurocognitive disorders .
    Triclofos sodium
  • HY-123479

    Others Infection
    CK0492B is a novel biaminourea antibiotic that has antiplaque properties in vitro and has shown efficacy in an experimental mouse dental disease model. A 12-week study in beagles compared its efficacy in reducing plaque and gingivitis, staining potential, and safety. Dogs were selected as the study subjects because the onset and progression of canine periodontal disease are similar to humans. Chlorhexidine acetate was selected as a positive control for plaque and gingivitis reduction and staining because it is effective in both humans and dogs.
    CK0492B
  • HY-146372

    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 .
    CXCR4 antagonist 5
  • HY-155780

    COX Inflammation/Immunology
    Anti-inflammatory agent 52 (compound 7j) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
    Anti-inflammatory agent 52
  • HY-155781

    COX Inflammation/Immunology
    Anti-inflammatory agent 53 (compound 7c) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in S phase and G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
    Anti-inflammatory agent 53
  • HY-16469

    Others Cancer
    SR13668 is a potent indole analog derived from indole-3-carbinol (I3C), known for its natural anticancer properties but limited by poor metabolic characteristics. Developed to enhance I3C's anticancer efficacy, SR13668 effectively inhibits growth factor-stimulated Akt activation. It demonstrates strong oral anticancer activity across different cancer types in preclinical studies, showing promise in clinical development due to its favorable safety profile and potent therapeutic effects .
    SR 13668
  • HY-115993

    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) .
    CDK4/6-IN-10
  • HY-155005

    EGFR Cancer
    EGFR mutant-IN-2 (Compound D51) is an EGFR mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFR L858R/T790M/C797S mutant with an IC50 value of 14 nM. EGFR mutant-IN-2 inhibits the EGFR del19/T790M/C797S mutant with an IC50 value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity .
    EGFR mutant-IN-2
  • HY-W250129

    Biochemical Assay Reagents Others
    2,3,4,5-Tetrafluorobenzoyl chloride is a fluorinated organic compound that belongs to the class of benzoyl chlorides. It is a colorless liquid with a pungent smell and is mainly used as an intermediate in the synthesis of various pharmaceutical and pesticide compounds. 2,3,4,5-Tetrafluorobenzoyl chloride is an acylating agent that can react with a variety of nucleophiles, including amines, alcohols, and thiols, to form amides, esters, or thioesters, respectively. Its unique fluorine-containing structure can impart desired properties to target molecules, such as increased lipophilicity or increased stability against metabolic degradation. However, due to its high reactivity and potential health hazards, proper safety measures and handling procedures must be followed when using this compound.
    2,3,4,5-Tetrafluorobenzoyl chloride
  • HY-W250172

    Biochemical Assay Reagents Others
    Triton X-405 is a nonionic surfactant commonly used in a variety of industrial and research applications. Triton X-405 belongs to the family of polyethylene glycol (PEG) ethers with a hydrophilic head and lipophilic tail and is suitable for use in emulsions, detergents and solubilizers. Triton X-405 is particularly useful in the study of membrane proteins, where it is used to solubilize and stabilize proteins for structural analysis techniques. It is also used in a variety of other applications, including drug delivery systems, nanotechnology, and diagnostic analysis. Additionally, Triton X-405 is used in the production of microemulsions, salves and lotions due to its emulsifying and solubilizing properties. However, it can be toxic if ingested or inhaled, so proper handling and safety precautions are required.
    Triton X-405
  • HY-137055

    Others Others
    PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
    PF-3774076

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