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Results for "

brain+exposure

" in MedChemExpress (MCE) Product Catalog:

14

Inhibitors & Agonists

1

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0459
    Scopine
    2 Publications Verification

    6,7-Epoxytropine

    		 Drug Metabolite Neurological Disease Cancer
    Scopine is a metabolite of Scopolamine (HY-N0296) and brain-targeting compound. Scopine significantly increases the brain exposure of Chlorambucil (HY-13593) and enhances its anti-glioma activity. Scopine can be used in targeted therapy research for brain gliomas .
    Scopine
  • HY-B0459A
    Scopine hydrochloride
    2 Publications Verification

    6,7-Epoxytropine hydrochloride

    		 Drug Metabolite Neurological Disease Cancer
    Scopine hydrochloride is a metabolite of Scopolamine (HY-N0296) and brain-targeting compound. Scopine hydrochloride significantly increases the brain exposure of Chlorambucil (HY-13593) and enhances its anti-glioma activity. Scopine hydrochloride can be used in targeted therapy research for brain gliomas .
    Scopine hydrochloride
  • HY-163087
    PT-91

    		Orphan GPCR Neurological Disease Metabolic Disease
    PT-91 is an agonist of GPR27. PT-91 exhibits high metabolic stability and brain exposure in mice .
    PT-91
  • HY-148233S
    JNJ-6204

    		Casein Kinase Others
    JNJ-6204 is a dual inhibitor for CSNK1D (Casein Kinase 1 Delta) and CSNK1E (Casein Kinase 1 Epsilon) (CSNK1D IC50=2.3 nM; CSNK1E IC50=137 nM). JNJ-6204 shows good brain exposure .
    JNJ-6204
  • HY-163671
    PW0729

    		GPR52 Neurological Disease
    PW0729 (compound 15b) is an orphan GPR52 agonist with potential applications in GPR52 activation, signaling bias, and neuropsychiatric and neurological disorders. The brain exposure characteristics of PW0729 need to be further optimized .
    PW0729
  • HY-110146
    XAP044

    		mGluR Neurological Disease
    XAP044 is a potent and selective antagonist of mGlu7. The metabotropic glutamate receptor subtype 7 (mGlu7) is an important presynaptic regulator of neurotransmission in the mammalian CNS. XAP044 demonstrates good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy in rodent behavioral paradigms .
    XAP044
  • HY-147720
    γ-Secretase modulator 11

    		γ-secretase Neurological Disease
    γ-Secretase modulator 11 (1o) showed high potency in vitro and brain exposure, inducing brain a β 42 levels were significantly reduced and showed undetectable inhibition of cytochrome P450 enzymes. In addition, compound 1o showed excellent anti cognitive deficit effect in AD model mice.
    γ-Secretase modulator 11
  • HY-147684
    FGFR-IN-7

    		FGFR Neurological Disease
    FGFR-IN-7 (compound 17) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-7 shows neuroprotective activity. FGFR-IN-7 improves brain exposure and reduced risk of phospholidosis. FGFR-IN-7 can be used for neurodegenerative diseases research .
    FGFR-IN-7
  • HY-130609A
    Aβ42-IN-1 free base

    		γ-secretase Neurological Disease
    Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 μM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease .
    Aβ42-IN-1 free base
  • HY-150306A
    (Rac)-Adibelivir

    (Rac)-IM-250

    		 HSV DNA/RNA Synthesis Infection
    (Rac)-Adibelivir ((Rac)-IM-250) is a blood-brain barrier-penetrant HSV helicase-primase inhibitor and metabolic stabilizer with antiviral activity. (Rac)-Adibelivir is also effective against Acyclovir (HY-17422)-resistant strains, and its deuterated structure exhibits enhanced metabolic stability, reducing the formation of hydroxylated metabolites. (Rac)-Adibelivir prolongs in vivo half-life, reduces administration dosage, improves oral bioavailability, and achieves higher brain exposure in mice. (Rac)-Adibelivir can be used in the research of herpes simplex infection, herpes encephalitis and Alzheimer's disease .
    (Rac)-Adibelivir
  • HY-182254
    AChE/BChE-IN-35

    		Cholinesterase (ChE) Neurological Disease
    AChE/BChE-IN-35, Tacrine (HY-111338) derivative, is a brain-penetrant dual AChE/BChE inhibitor with an Electric Eel AChE IC50 of 123.66 nM, human AChE IC50 of 122.34 nM, and equine BChE IC50 of 488.00 nM. AChE/BChE-IN-35 undergoes LAT1-mediated active transport across cell membranes. AChE/BChE-IN-35 exhibits enhanced brain exposure with slower brain tissue elimination. AChE/BChE-IN-35 can be used for the research of alzheimer's disease .
    AChE/BChE-IN-35
  • HY-181049
    FMJ-01-054

    		Dopamine Receptor Neurological Disease
    FMJ-01-054 is a selective dopamine D4 Receptor (D4R) antagonist with a Ki od 77.7 nM. FMJ-01-054 shows subtype selectivity over D2R and D3R. FMJ-01-054 inhibits D4R-mediated β-arrestin recruitment and cAMP production with IC50 values of 3800 nM and 134 nM, respectively. FMJ-01-054 has desirable plasma half-life and brain exposure in rats. FMJ-01-054 can be used for the research of neurological disorders .
    FMJ-01-054
  • 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
  • HY-180406
    NPY Y2 antagonist 2

    		Neuropeptide Y Receptor Neurological Disease
    NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2, with pKi values of 6.8 nM and 7.2 nM in human and rat brains, respectively, and demonstrating blood-brain barrier penetration. NPY Y2 antagonist 2 shows selectivity for the Y1 and Y5 receptors. NPY Y2 antagonist 2 blocks the negative feedback regulation mediated by the NPY Y2 receptor, thereby increasing endogenous NPY release and enhancing Y1 receptor activation, resulting in the modulation of central neurotransmitter release. NPY Y2 antagonist 2 exhibits moderate in vivo clearance, high free fraction in rat brain, and a favorable brain/plasma ratio and brain exposure. NPY Y2 antagonist 2 is applicable for research in conditions such as mood disorders, anxiety induced by alcohol withdrawal, and social anxiety associated with nicotine withdrawal .
    NPY Y2 antagonist 2

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