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MDCK-MDR1

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-167856
    RTI-122

    		GPR88 Neurological Disease
    RTI-122 is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC50=11 nM), with EC50 values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([ 35S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 exhibits metabolic stability in mice (T1/2=5.8 h) and can be used to investigate alcohol use disorder [1] .
    RTI-122
  • HY-143792
    HTT-D3

    		Huntingtin P-glycoprotein Neurological Disease
    HTT-D3 is an orally active, blood-brain barrier penetrant splicing modulator of huntingtin (HTT). HTT-D3 promotes the inclusion of a pseudo-exon containing a premature termination codon into HTT pre-mRNA, triggers nonsense-mediated mRNA degradation and reduces HTT protein levels. HTT-D3 induces dose-dependent, comparable reductions in mutant HTT protein in both the brain and peripheral tissues of transgenic mouse models. HTT-D3 can be used for the research of Huntington's disease [1].
    HTT-D3
  • HY-169194
    Antimalarial agent 44

    		Parasite Infection
    Antimalarial agent 44 (Compound 3) is an antimalarial agent against parasite. Antimalarial agent 44 has a good permeability across MDCK-MDR1 cell monolayers and a high clearance by mouse liver microsomes [1].
    Antimalarial agent 44
  • HY-155152
    P-gp/BCRP-IN-2

    		P-glycoprotein BCRP Cancer
    P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells [1].
    P-gp/BCRP-IN-2
  • HY-183247
    BRDT-IN-1

    		Epigenetic Reader Domain Cancer
    BRDT-IN-1 is a BRDT-BD1 and BRDT-T inhibitor with BRDT-BD1 IC50 19 nM, Ki 8.8 nM, Ka 1.6 nM, and BRDT-T IC50 56 nM, Ka 5.0 nM. BRDT-IN-1 displays in vitro metabolic stability and limited cellular permeability in MDCK-MDR1 cells. BRDT-IN-1 can be used for the research of multiple myeloma [1].
    BRDT-IN-1
  • HY-168494
    GluN2A Allosteric modulator 1

    		iGluR Neurological Disease
    GluN2A Allosteric modulator 1 (Compound 11) is an orally active, BBB-penetrable and highly selective GluN2A negative allosteric modulator. GluN2A Allosteric modulator 1 has IC50 values of 0.042 μM and 13 μM for GluN2A and GluN2B, respectively. GluN2A Allosteric modulator 1 can be used for the research of nervous system diseases [1].
    GluN2A Allosteric modulator 1
  • HY-181348
    HBV-IN-56

    		HBV Infection
    HBV-IN-56 is an orally active HBsAg production inhibitor. HBV-IN-56 inhibits HBsAg production both in vitro and in vivo. HBV-IN-56 can be used for the research of chronic hepatitis B virus infection [1].
    HBV-IN-56
  • HY-182697
    RTICBM-74

    		Cannabinoid Receptor Metabolic Disease
    RTICBM-74 is a blood-brain barrier-permeable, selective CB1 allosteric modulator with IC50 values of 23 nM (calcium mobilization assay) and 153 nM ([ 35S]GTPγS assay). RTICBM-74 inhibits CB1 receptor signaling. RTICBM-74 reduces alcohol intake in rats. RTICBM-74 can be used for the research of alcohol use disorder [1].
    RTICBM-74

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