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cross-species

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製品番号 製品名 Target 研究分野 構造式
  • HY-174802
    XL-3158

    		Cyclic GMP-AMP Synthase IKK IFNAR Neurological Disease Inflammation/Immunology Cancer
    XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC50: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 can be used for the study of cGAS-dependent inflammatory diseases.
    XL-3158
  • HY-P3350
    LS-BF1

    		Bacterial Infection
    LS-BF1 is a stable and low toxic cationic antimicrobial peptide. LS-BF1 displays broad spectrum of antibacterial activity, including the challenging ESKAPE pathogens, by cell membrane disruptive mechanism. LS-BF1 shows good in vivo efficacy for elimination of bacteria in a mouse infection model[1].
    LS-BF1
  • HY-12995A
    (S)-BI 665915

    		FLAP Inflammation/Immunology
    (S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species agent metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production .
    (S)-BI 665915
  • HY-175294
    PD-L1/Nampt-IN-1

    		PD-1/PD-L1 NAMPT Cancer
    PD-L1/Nampt-IN-1 is an orally active inhibitor that simultaneously target PD-L1 and NAMPT (nicotinamide phosphoribosyltransferase) with IC50s value of 63 nM and 582 nM. PD-L1/Nampt-IN-1 demonstrates cross-species affinity with comparable KD values for hPD-L1 (52.6 nM) and mPD-L1 (49.1 nM), respectively. PD-L1/Nampt-IN-1 effectively inhibits tumor growth by activating the tumor immune microenvironment. PD-L1/Nampt-IN-1 can be used for the study of melanoma .
    PD-L1/Nampt-IN-1
  • HY-116494
    ML753286

    		BCRP Cancer
    ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .
    ML753286
  • HY-116494A
    (6R)-ML753286

    		BCRP Cancer
    (6R)-ML753286 is an isomer of ML753286 (HY-116494). ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .
    (6R)-ML753286
  • HY-182724
    PSB-18422

    		Transmembrane Glycoprotein Inflammation/Immunology
    PSB-18422 is a GPR17 agonist, with an EC50 of 0.0279 μM for humans, 0.47 μM for rats, 0.753 μM for mice, and a human Ki of 1.46 μM. PSB-18422 triggers intracellular calcium mobilization via cross-species activation of GPR17. PSB-18422 can be used in the research of allergic bronchial inflammation .
    PSB-18422
  • HY-181266
    Antimalarial agent 55

    		Parasite Aminopeptidase Infection
    Antimalarial agent 55 is an orally potent inhibitor of PfA-M1 and PfA-M17 aminopeptidases from Plasmodium falciparum, with Ki values of 27 nM and 81 nM, respectively. Antimalarial agent 55 exhibits potent nanomolar activity against homologous enzymes from Plasmodium vivax and Plasmodium berghei, with Ki values of 2 nM, 4 nM, 190 nM and 18 nM for Pv-M1, Pb-M1, Pv-M17 and Pb-M17, respectively. Antimalarial agent 55 possesses significant antiplasmodial activity, as well as cross-species inhibitory capacity and broad-spectrum activity that is unaffected by existing drug resistance mechanisms. Antimalarial agent 55 can be used in malaria research .
    Antimalarial agent 55
  • HY-182244
    SERT/NET-IN-1

    		Serotonin Transporter 5-HT Receptor Endocrinology
    SERT/NET-IN-1 is a blood-brain barrier-permeable SERT and NET inhibitor, with an IC50 of 11.2 nM against human SERT and an IC50 of 32.0 nM against human NET. SERT/NET-IN-1 blocks 5-HT reuptake to enhance serotonergic signaling. SERT/NET-IN-1 also blocks norepinephrine reuptake to enhance central noradrenergic transmission and inhibits the ejaculatory reflex. SERT/NET-IN-1 prolongs ejaculatory latency, reduces ejaculation frequency and preserves sexual function. SERT/NET-IN-1 exhibits cross-species microsomal metabolic stability, shows acceptable oral brain exposure in rats, and has favorable safety profiles. SERT/NET-IN-1 can be used in studies related to premature ejaculation .
    SERT/NET-IN-1

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