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selective,blood-brain barrier

" in MedChemExpress (MCE) Product Catalog:
Cat. No. 상품명 Target 연구분야 Chemical Structure
  • HY-18768
    NCT-501
    5 Publications Verification

    		 Aldehyde Dehydrogenase (ALDH) Akt β-catenin Necroptosis Cancer
    NCT-501 is a reversible, non-competitive, selective, blood-brain barrier-permeable ALDH1A1 inhibitor with an IC50 of 40 nM. NCT-501 inhibits the AKT-β-catenin signaling pathway, induces necroptosis in nasopharyngeal carcinoma cells, suppresses their proliferation and inhibits stem cell spheroid formation. NCT-501 can be used in research related to nasopharyngeal carcinoma, esophageal squamous cell carcinoma and malignant tumors .
    NCT-501
  • HY-16531
    YF-2
    2 Publications Verification

    		 Histone Acetyltransferase Neurological Disease Cancer
    YF-2 is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease .
    YF-2
  • HY-154959
    AZD4747

    		Ras Cancer
    AZD4747 is a selective, blood-brain barrier-permeable mutant GTPase KRAS G12C inhibitor. AZD4747 has the potential to study cancer .
    AZD4747
  • 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 .
    RTI-122
  • HY-11030A
    SNT-207858 free base

    		Melanocortin Receptor Metabolic Disease Endocrinology Cancer
    SNT207858 free base is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 free base has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor .
    SNT-207858 free base
  • HY-16531A
    YF-2 hydrochloride
    2 Publications Verification

    		 Histone Acetyltransferase Neurological Disease Cancer
    YF-2 hydrochloride is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease .
    YF-2 hydrochloride
  • HY-12716A
    BRL-44408 maleate

    		Adrenergic Receptor ERK p38 MAPK Dopamine Receptor Cardiovascular Disease Neurological Disease
    BRL-44408 maleate is a selective, blood-brain barrier-permeable α2A-adrenergic receptor antagonist with a Ki value of 8.56 nM against human targets. BRL-44408 maleate exhibits activities such as antidepressant, analgesic effects and attenuation of sepsis-induced acute lung injury by regulating the release of neurotransmitters such as norepinephrine and dopamine, or inhibiting signaling pathways including ERK1/2, p38MAPK and p65. BRL-44408 maleate can be used in studies related to acute respiratory distress syndrome, depression and visceral pain .
    BRL-44408 maleate
  • HY-137466
    ARN-21934

    		Topoisomerase Cancer
    ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research .
    ARN-21934
  • HY-159527
    Glovadalenum

    Glovadalen

    		 Dopamine Receptor Neurological Disease
    Glovadalenum (Glovadalen) is an orally active, selective, blood-brain barrier permeable positive allosteric modulator of dopamine D1 receptor. Glovadalenum selectively enhances the efficacy of dopamine in activating dopamine D1 receptor. Glovadalenum can be used for the research of Parkinson's disease .
    Glovadalenum
  • HY-155939
    M4K2163 dihydrochloride

    		TGF-β Receptor Cancer
    M4K2163 dihydrochloride is a potent, selective, blood-brain barrier (BBB) permeable activin receptor-like kinase-2 (ALK2) inhibitor, with an IC50 of 19 nM. M4K2163 dihydrochloride can be used in the research of diffuse intrinsic pontine glioma (DIPG) .
    M4K2163 dihydrochloride
  • HY-12716
    BRL-44408

    		Adrenergic Receptor p38 MAPK Dopamine Receptor ERK Cardiovascular Disease Neurological Disease
    BRL-44408 is a selective, blood-brain barrier-permeable α2A-adrenergic receptor antagonist with a Ki value of 8.56 nM against human targets. BRL-44408 exhibits activities such as antidepressant, analgesic effects and attenuation of sepsis-induced acute lung injury by regulating the release of neurotransmitters such as norepinephrine and dopamine, or inhibiting signaling pathways including ERK1/2, p38MAPK and p65. BRL-44408 can be used in studies related to acute respiratory distress syndrome, depression and visceral pain .
    BRL-44408
  • HY-124698
    MRK-A

    		Isocitrate Dehydrogenase (IDH) Cancer
    MRK-A is a selective, blood-brain-barrier permeable mutant IDH1 inhibitor with an IC50 value of 5 nM. MRK-A inhibits 2-HG production. MRK-A has anti-cancer activity against brain tumors .
    MRK-A
  • HY-179008
    5-HT2CR agonist 2

    		5-HT Receptor Neurological Disease
    5-HT2CR agonist 2 (Compound 16k) is a selective, blood-brain barrier-penetrating and Gq-biased 5-HT2CR agonist, with an EC50 of 36 nM. 5-HT2CR agonist 2 attenuates MK801 (HY-15084B)-induced hyperlocomotion and reverses Phencyclidine-induced hyperlocomotor activity .
    5-HT2CR agonist 2
  • HY-11030
    SNT-207858

    		Melanocortin Receptor Metabolic Disease Endocrinology Cancer
    SNT207858 is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor .
    SNT-207858
  • HY-182384
    VU6015241

    		mAChR Neurological Disease
    VU6015241 is a selective, blood-brain barrier-permeable M4 mAChR Antagonist with a Ki value of 43.3 nM. VU6015241 is used for the research of dystonia and related movement disorders .
    VU6015241
  • HY-103477
    MAO-B-IN-51

    		Monoamine Oxidase Neurological Disease
    MAO-B-IN-51 (Compound 8f) is a selective, blood-brain-barrier permeable, orally active MAO-B inhibitor with an IC50 of 48．9 nM (MDS). MAO-B-IN-51 enhances long-term memory .
    MAO-B-IN-51
  • HY-183565
    HYF031

    		HDAC Neurological Disease
    HYF031 is a selective, blood-brain barrier-permeable HDAC8 inhibitor with an IC50 of 5.7 nM, and exhibits extremely low activity against most other HDAC subtypes. HYF031 is applicable for HDAC8 imaging studies .
    HYF031
  • HY-181021
    Kir4.1-IN-1

    		Potassium Channel Neurological Disease
    Kir4.1-IN-1 (Compound 37) is a potent, selective, blood-brain barrier permeable Kir4.1 inhibitor with an IC50 of 0.19 μM. Kir4.1-IN-1 exhibits rapid-onset antidepressant effects .
    Kir4.1-IN-1
  • HY-182928
    LRRK2-IN-21

    		LRRK2 Mps1 Neurological Disease
    LRRK2-IN-21 is a selective, blood-brain barrier-permeable LRRK2 kinase inhibitor with an IC50 of 0.35 nM. LRRK2-IN-21 inhibits TTK kinase with an IC50 of 70 nM. LRRK2-IN-21 is applicable to the research of Parkinson's disease .
    LRRK2-IN-21
  • HY-180938
    Fyn-IN-1

    		Src GSK-3 NO Synthase Neurological Disease
    Fyn-IN-1 (Compound 43) is a selective, blood-brain barrier permeable Fyn and GSK-3β inhibitor with IC50 values of 0.044 μM and 0.61 μM, respectively. Fyn-IN-1 significantly downregulates the pro-inflammatory enzyme iNOS. Fyn-IN-1 can be used in the research of neurodegenerative diseases .
    Fyn-IN-1
  • HY-106385
    PRX-03140

    VRX-03011 free base

    		 5-HT Receptor Neurological Disease
    PRX-03140 is a selective, blood-brain-barrier permeable 5-HT4 receptor agonist with a Ki value of 110 nM against rat brain 5-HT4 receptor. PRX-03140 can increase cortical ACh and histamine levels. PRX-03140 can be used in the research of Alzheimer's disease .
    PRX-03140
  • HY-12970B
    EPZ020411 dihydrochloride

    		Histone Methyltransferase Reactive Oxygen Species (ROS) Apoptosis Neurological Disease Cancer
    EPZ020411 dihydrochloride is a selective, blood-brain barrier-permeable PRMT6 inhibitor with an IC50 of 0.010 μM. EPZ020411 dihydrochloride blocks PRMT6-mediated histone H3R2 methylation, reduces ROS production, and inhibits Apoptosis. EPZ020411 dihydrochloride is applicable to research related to neuropathic pain, colorectal cancer, ototoxicity, hearing loss and glioblastoma .
    EPZ020411 dihydrochloride
  • HY-164584
    S1P5 receptor antagonist 1

    		LPL Receptor Neurological Disease
    S1P5 receptor antagonist 1 is a selective, blood-brain barrier-permeable S1P5 receptor antagonist with an EC50 of 0.1 nM and a Ki of 4.4 nM. S1P5 receptor antagonist 1 inhibits the migration of natural killer cells towards sphingosine 1-phosphate in vitro, with no effect on T cell migration. S1P5 receptor antagonist 1 can be used in the research of central nervous system diseases .
    S1P5 receptor antagonist 1
  • HY-181549
    PDE4-IN-32

    		Phosphodiesterase (PDE) Cardiovascular Disease Neurological Disease
    PDE4-IN-32 (Compound B05) is a selective, blood-brain barrier permeable PDE4B and PDE4D inhibitor with IC50 values of 13.7 nM and 23.8 nM, respectively. PDE4-IN-32 promotes the recovery of motor and cognitive function in MCAO/R mouse models. PDE4-IN-32 reduces cerebral edema. PDE4-IN-32 can be used for the research of ischemic stroke .
    PDE4-IN-32
  • HY-167856A
    RTI-122 dihydrochloride

    		GPR88 Neurological Disease
    RTI-122 dihydrochloride 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 dihydrochloride significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 dihydrochloride blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 dihydrochloride exhibits metabolic stability in mice (T1/2=5.8 h) and can be used to investigate alcohol use disorder .
    RTI-122 dihydrochloride
  • HY-W283930
    YHV98-4

    		Tau Protein ATP Synthase Mitophagy Reactive Oxygen Species (ROS) Mitochondrial Metabolism Neurological Disease Inflammation/Immunology
    YHV98-4 is a selective, blood-brain barrier permeable Hv1 channel inhibitor. YHV98-4 specifically inhibits Hv1 with a half-maximal inhibitory concentration of 1 µM without inhibiting other ion channels. YHV98-4 reduces the propagation of p-tau. YHV98-4 increases ATP production, and enhances microglial mitophagy. YHV98-4 attenuates inflammatory pain via inhibition of Hv1 and ROS production. YHV98-4 enhances microglia-to-neuron mitochondrial transfer, promoting the delivery of functional mitochondria to rescue neuronal damage and improve cognitive function. YHV98-4 reduces inflammation. YHV98-4 can be used in the research of Alzheimer's disease .
    YHV98-4
  • HY-W657887
    GSK-3β/G9a-IN-1

    		Histone Methyltransferase GSK-3 Tau Protein Amyloid-β Glucocorticoid Receptor Androgen Receptor Adrenergic Receptor Neurological Disease
    GSK-3β/G9a-IN-1 (Compound T2) is an orally active, selective, blood-brain-barrier permeable, competitive G9a (substrate-competitive, IC50: 1.1 μM) and GSK-3β (ATP competitive, IC50: 0.8 μM) inhibitor. GSK-3β/G9a-IN-1 is a potent H3K9me2 inhibitor that reshapes chromatin landscape. GSK-3β/G9a-IN-1 lowers tau phosphorylation, reduces Aβ aggregation. GSK-3β/G9a-IN-1 displays inhibition toward glucocorticoid receptor, androgen receptor, and alpha-2A adrenergic receptor. GSK-3β/G9a-IN-1 also upregulates SAGA complex members such as Eny2 and Sgf29. GSK-3β/G9a-IN-1 markedly improves memory, restores social behaviors, and increases synaptic complexity in late-onset Alzheimer’s disease .
    GSK-3β/G9a-IN-1

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