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Results for "

brain exposures

" in MedChemExpress (MCE) Product Catalog:

19

Inhibitors & Agonists

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-155672
    JPC0323

    		5-HT Receptor Neurological Disease
    JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
    JPC0323
  • HY-163087
    PT-91

    		Orphan Receptor 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-116565
    Usmarapride

    SUVN-D4010

    		 5-HT Receptor Neurological Disease
    Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease .
    Usmarapride
  • HY-116565A
    Usmarapride free base

    SUVN-D4010 free base

    		 5-HT Receptor Neurological Disease
    Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease .
    Usmarapride free base
  • 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[1][2].
    JNJ-6204
  • 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-164512
    NRMA-I

    		Drug Intermediate Neurological Disease
    NRMA-I is the amide produrg of the small molecule nuclear receptor modulator. NRMA-I exhibits a higher exposure in the brain, indicating that a good blood-brain barrier (BBB) penetration. NRMA-I can be used for research of central nervous system diseases related to nuclear receptors, such as Alzheimer's disease and Parkinson's disease .
    NRMA-I
  • HY-130609
    Aβ42-IN-1

    		γ-secretase Neurological Disease
    Aβ42-IN-1, compound 1v, is a novel, potent and orally active?γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50?value of 0.091?μM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
    Aβ42-IN-1
  • 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-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-164505
    NRMA-9

    		Drug Intermediate Neurological Disease
    NRMA-9 is the amide produrg of the small molecule nuclear receptor modulator. NRMA-9 exhibits a higher exposure in the brain, indicating that a good blood-brain barrier (BBB) penetration. NRMA-9 can be used for research of central nervous system diseases related to nuclear receptors, such as Alzheimer's disease and Parkinson's disease .
    NRMA-9
  • HY-124713
    ML372

    		DNA/RNA Synthesis Neurological Disease
    ML372 inhibits survival motor neuron (SMN) protein ubiquitination, increases SMN protein stability without affecting mRNA expression. ML372 improves spinal muscular atrophy (SMA) in mice. ML372 is brain penetrant and has a reasonable exposure and half-life in vivo .
    ML372
  • 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-158627
    JPC0323 Oleate

    		5-HT Receptor Others
    JPC0323 Oleate is a derivative of JPC0323 (HY-155672). JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
    JPC0323 Oleate
  • HY-169310
    ATM Inhibitor-11

    		ATM/ATR Cancer
    ATM Inhibitor-11 (Compound 1) is an inhibitor for ATM with an IC50 of 0.32 nM. ATM Inhibitor-11 inhibits the KAP1 phosphorylation with an IC50 of 0.97 nM. ATM Inhibitor-11 exhibits high exposure in the brain, heart and plasma of ICR mouse. ATM Inhibitor-11 exhibits anti-tumor efficacy in NCI-H441 xenograft mouse model .
    ATM Inhibitor-11
  • HY-155992
    WLB-89462

    		Sigma Receptor Neurological Disease
    WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (Ki: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .
    WLB-89462
  • HY-104044A
    Pamiparib maleate

    BGB-290 maleate

    		 Apoptosis Neurological Disease
    Pamiparib maleate (BGB-290 maleate) is a highly potent and selective PARP inhibitor with neurotoxicity-inducing activity. Pamiparib maleate can effectively penetrate the blood-brain barrier and cause cerebral hemorrhage, brain atrophy, and movement disorders in zebrafish embryos exposed. Pamiparib maleate exposure downregulates the activities of acetylcholinesterase (AChE) and adenosine triphosphatase (ATPase) and leads to upregulation of oxidative stress, which triggers apoptosis and interferes with the expression of neurodevelopment-related genes. The use of pamiparib maleate is also accompanied by downregulation of the Notch signaling pathway, while activation of the Notch signaling pathway can partially rescue neurodevelopmental toxicity. Therefore, pamiparib maleate provides a reference for evaluating its potential neurotoxicity during embryonic development .
    Pamiparib maleate
  • HY-120144
    SR-8993

    		Opioid Receptor Neurological Disease
    SR-8993 is a highly selective nociceptin receptor agonist that can penetrate the blood-brain barrier and has the activity of reducing alcohol intake and relieving withdrawal anxiety. SR-8993 has shown mild anxiolytic effects in animal models and can effectively reverse anxiety caused by acute alcohol withdrawal. SR-8993 further reduces restricted drinking, operant responses for alcohol, and increased drinking induced by long-term intermittent exposure to alcohol. SR-8993 also reduces stress- and cue-related alcohol-seeking relapse .
    SR-8993