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brain penetrate

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295

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-50706
    Selumetinib
    Maximum Cited Publications
    90 Publications Verification

    AZD6244; ARRY-142886

    MEK Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation. Selumetinib can penetrate the blood brain barrier (BBB) .
    Selumetinib
  • HY-13909
    RGFP966
    50+ Cited Publications

    HDAC Cancer
    RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM. RGFP966 can penetrate the blood brain barrier (BBB).
    RGFP966
  • HY-90001
    Ritonavir
    30+ Cited Publications

    ABT 538; RTV

    HIV Protease HIV SARS-CoV Apoptosis Infection Neurological Disease Inflammation/Immunology Cancer
    Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.61 μM. Ritonavir (ABT 538) can penetrate the blood brain barrier (BBB) .
    Ritonavir
  • HY-14842
    Givinostat
    10+ Cited Publications

    ITF-2357

    HDAC Inflammation/Immunology Cancer
    Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat can be used for Duchenne muscular dystrophy (DMD) research. Givinostat can penetrate the blood-brain barrier (BBB) .
    Givinostat
  • HY-14136
    Rimonabant
    10+ Cited Publications

    SR141716

    Cannabinoid Receptor Bacterial Infection Metabolic Disease Cancer
    Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
    Rimonabant
  • HY-14842B

    ITF-2357 hydrochloride monohydrate

    HDAC Infection Neurological Disease Inflammation/Immunology Cancer
    Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride monohydrate can penetrate the blood-brain barrier (BBB) .
    Givinostat hydrochloride monohydrate
  • HY-18236
    MDL-28170
    15+ Cited Publications

    Calpain Inhibitor III

    Proteasome Neurological Disease Inflammation/Immunology
    MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration . MDL-28170 also block γ-secretase .
    MDL-28170
  • HY-171306

    Liposome Others
    MK16 is a lipid material that can be used to construct blood-brain barrier penetrable lipid nanoparticles for mRNA delivery. MK16 facilitates blood-brain barrier crossing via γ-secretase-mediated and caveolae-mediated transcytosis. MK16 can be used for drug delivery research .
    MK16
  • HY-W014423
    L-Histidine hydrochloride hydrate
    3 Publications Verification

    H-His-OH.HCl.H2O

    Endogenous Metabolite Apoptosis Reactive Oxygen Species (ROS) Inflammation/Immunology Cancer
    L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable .
    L-Histidine hydrochloride hydrate
  • HY-P4073

    GRN1005; Paclitaxel trevatide

    Peptide-Drug Conjugates (PDCs) LDLR Cancer
    ANG1005 (Paclitaxel trevatide) is a brain-penetrating peptide-drug conjugate. ANG1005, a taxane derivative, consists of three paclitaxel (HY-B0015) molecules covalently linked to Angiopep-2, designed to cross the blood-brain and blood-cerebrospinal barriers and to penetrate malignant cells via low density lipoprotein receptor-related protein (LRP1) transport system .
    ANG1005
  • HY-119624

    PIKfyve Cancer
    MOMIPP, a macropinocytosis inducer, is a PIKfyve inhibitor. MOMIPP penetrates the blood-brain barrier (BBB) .
    MOMIPP
  • HY-114452
    LY2940094
    1 Publications Verification

    BTRX-246040

    Opioid Receptor Neurological Disease
    LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models .
    LY2940094
  • HY-111540
    LY-3381916
    2 Publications Verification

    IDO1-IN-5

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    LY-3381916 (IDO1-IN-5) is a potent, selective and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1 .
    LY-3381916
  • HY-B0206

    MK 462

    5-HT Receptor Neurological Disease
    Rizatriptan benzoate is the agonist for 5-HT1B and 5-HT1D. Rizatriptan benzoate has a peripheral vasoconstrictive effect, penetrates the intact blood-brain barrier, and inhibits pain neurotransmission in the central nervous system .
    Rizatriptan benzoate
  • HY-50706A
    Selumetinib sulfate
    Maximum Cited Publications
    90 Publications Verification

    AZD6244 sulfate; ARRY-142886 sulfate

    MEK Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Selumetinib (AZD6244) sulfate is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) sulfate inhibits ERK1/2 phosphorylation. Selumetinib sulfate can penetrate the blood brain barrier (BBB) .
    Selumetinib sulfate
  • HY-104044
    Pamiparib
    3 Publications Verification

    BGB-290

    PARP Cancer
    Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor .
    Pamiparib
  • HY-116477

    FAAH Neurological Disease Inflammation/Immunology
    URB937 is an orally active and peripherally restricted FAAH inhibitor (IC50=26.8 nM) and increases anandamide levels. URB937 fails to affect FAAH activity in the brain (not penetrate the blood-brain barrier) .
    URB937
  • HY-14842A
    Givinostat hydrochloride
    10+ Cited Publications

    ITF-2357 hydrochloride

    HDAC Inflammation/Immunology Cancer
    Givinostat (ITF-2357) hydrochloride is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride can penetrate the blood-brain barrier (BBB). .
    Givinostat hydrochloride
  • HY-107531

    GSK-3 Neurological Disease Cancer
    A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain. A 1070722 decreases spontaneous locomotion .
    A 1070722
  • HY-120085
    PFE-360
    3 Publications Verification

    PF-06685360

    LRRK2 Neurological Disease
    PFE-360 (PF-06685360) is a potent, selective, brain penetrated and orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor with a mean IC50 of 2.3 nM in vivo .
    PFE-360
  • HY-131703
    UGT8-IN-1
    1 Publications Verification

    UGT Metabolic Disease
    UGT8-IN-1 is a brain penetrable and orally active inhibitor of ceramide galactosyltransferase enzyme (UGT8). UGT8-IN-1 can be used in the study for lysosomal storage disorders .
    UGT8-IN-1
  • HY-W040971

    2-Methoxy-4-methylphenol

    Environmental Pollutants ERK Endogenous Metabolite p38 MAPK Akt Reactive Oxygen Species (ROS) FAK Cardiovascular Disease Neurological Disease Metabolic Disease
    Creosol (2-Methoxy-4-methylphenol) is an endogenous metabolite that acts as an important chemical intermediate and potential biofuel mainly derived from lignocellulosic biomass. Creosol is blood brain barrier penetrable .
    Creosol
  • HY-D0873

    EPPS

    Amyloid-β Neurological Disease
    HEPPS (EPPS) is a buffering agent with the useful pH range from 7.3 ~ 8.7. HEPPS reduces -aggregate-induced memory deficits and rescues cognitive deficits in mice. EPPS is orally active and penetrates the blood-brain barrier .
    HEPPS
  • HY-120789

    γ-secretase Neurological Disease
    PF-06648671 is a novel, brain-penetrable, and orally active γ-secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease .
    PF-06648671
  • HY-N0666S8

    Endogenous Metabolite Inflammation/Immunology
    L-Aspartic acid-d3 is the deuterium labeled L-Aspartic acid. L-Aspartic aicd is an amino acid that can penetrate the blood-brain barrier. L-Aspartic aicd is commonly used for preparing prodrugs to target colon and cecal tissues. L-Aspartic aicd commonly used in the study of inflammatory conditions .
    L-Aspartic acid-d3
  • HY-14130

    CRFR Neurological Disease Endocrinology
    CP 376395 is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist .
    CP 376395
  • HY-152839

    BLU-263

    c-Kit Cancer
    Elenestinib (BLU-263) is an orally active inhibitor of Tyrosine kinase with an IC50 value of 6 nM for KIT D816V. Elenestinib minimally penetrates the blood-brain barrier. Elenestinib can be used in the study of systemic mastocytosis .
    Elenestinib
  • HY-14174
    MRK-560
    4 Publications Verification

    γ-secretase Neurological Disease Cancer
    MRK-560, a chemical probe, is an orally active, brain barrier-penetrated γ-Secretase inhibitor, reducing Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimer's disease and T-cell acute lymphoblastic leukaemia (T-ALL) .
    MRK-560
  • HY-B0186B

    FK-037

    Bacterial Antibiotic Infection
    Cefoselis sulfate (FK-037), the fourth gen-eration of cephalosporin, is a β-lactam antibiotic. Cefoselis sulfate exhibits good activity against a wide range of Gram-positive and Gram-negative organisms. Cefoselis sulfate penetrates the blood-brain barrier .
    Cefoselis sulfate
  • HY-15748

    ADX-71149

    mGluR Neurological Disease
    JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM. JNJ-40411813 has orally bioactivity and penetrate the blood-brain barriers. JNJ-40411813 has the potential property of anti-depression .
    JNJ-40411813
  • HY-116578
    Metopimazine
    3 Publications Verification

    EXP999; RP9965

    Dopamine Receptor Neurological Disease
    Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .
    Metopimazine
  • HY-N0666S4

    Endogenous Metabolite Inflammation/Immunology
    L-Aspartic acid- 13C4 is the 13C-labeled L-Aspartic acid. L-Aspartic aicd is an amino acid that can penetrate the blood-brain barrier. L-Aspartic aicd is commonly used for preparing prodrugs to target colon and cecal tissues. L-Aspartic aicd commonly used in the study of inflammatory conditions .
    L-Aspartic acid-13C4
  • HY-P10216

    Biochemical Assay Reagents Neurological Disease
    CAQK peptide selectively binds to injured mouse brain. CAQK peptide selectively targets demyelinating areas and it is absent from healthy tissue. The CAQK peptide target is a proteoglycan complex upregulated in brain injuries and is used for drug delivery. CAQK peptide can penetrate the blood-brain barrier .
    CAQK peptide
  • HY-106000

    Histamine Receptor Neurological Disease
    GSK239512 is a potent and brain penetrated H3 receptor antagonist. GSK239512 can be used for the research of mild-to-moderate Alzheimer's disease (AD) .
    GSK239512
  • HY-114452A
    LY2940094 tartrate
    1 Publications Verification

    BTRX-246040 tartrate

    Opioid Receptor Neurological Disease
    LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models .
    LY2940094 tartrate
  • HY-10900
    TCS 1102
    1 Publications Verification

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    TCS 1102 is a potent, dual orexin receptor antagonist, with Ki values of 0.2 nM and 3 nM for OX2 and OX1 receptors, respectively. TCS 1102 demonstrates excellent blood-brain barrier penetrability and moderate bioavailability in rats .
    TCS 1102
  • HY-157227

    VPC4

    TRP Channel Inflammation/Immunology
    VPC01091.4 (VPC4) is a TRPM7 inhibitor and blocks TRPM7 current at low micromolar concentrations. VPC01091.4 can penetrate the blood-brain barrier. VPC01091.4 is an efficacious anti-inflammatory agent that arrests systemic inflammation in vivo .
    VPC01091.4
  • HY-153175

    RET Neurological Disease
    BT44 is a selective RET activator. BT44 can penetrate through the blood-brain barrier and can be used for the research of neurodegenerative disorders and diabetes mellitus .
    BT44
  • HY-132310

    MAGL Neurological Disease
    MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain .
    MAGL-IN-4
  • HY-136146

    nAChR Neurological Disease
    SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity .
    SUVN-911
  • HY-N4134

    NO Synthase Inflammation/Immunology
    Ciwujianoside C3, an orally active and brain penetrated compound, is isolated the leaves of Acanthopanax henryi Harms. Ciwujianoside C3 has anti-inflammatory effect and can reinforces object recognition memory .
    Ciwujianoside C3
  • HY-101059

    GABA Receptor Neurological Disease
    FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a Ki of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions .
    FGIN 1-27
  • HY-N0666S

    Endogenous Metabolite Inflammation/Immunology
    L-Aspartic acid- 13C is a 13C labeled L-Aspartic acid. L-Aspartic aicd is an amino acid that can penetrate the blood-brain barrier. L-Aspartic aicd is commonly used for preparing prodrugs to target colon and cecal tissues. L-Aspartic aicd commonly used in the study of inflammatory conditions .
    L-Aspartic acid-13C
  • HY-101188

    Histamine Receptor Infection
    INCB38579 is an orally active, highly brain penetrable, and selective histamine H4 receptor (HH4R) antagonist (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities .
    INCB38579
  • HY-134228

    Biochemical Assay Reagents Cancer
    4-Hydroperoxyifosfamide is an anticancer agent that can penetrate the blood-brain barrier (BBB) .
    4-Hydroperoxyifosfamide
  • HY-128351
    SHR1653
    1 Publications Verification

    Oxytocin Receptor Neurological Disease Endocrinology
    SHR1653 is a highly potent, selective and brain penetrated oxytocin receptor (OTR) antagonist, with an IC50 of 15 nM for hOTR .
    SHR1653
  • HY-137279
    Naloxone methiodide
    1 Publications Verification

    Opioid Receptor Inflammation/Immunology
    Naloxone methiodide is a peripherally restricted, nonselective, and competitive opioid receptor antagonist. Naloxone methiodide does not penetrate the blood-brain barrier .
    Naloxone methiodide
  • HY-108295

    CXB-722

    GABA Receptor Neurological Disease
    Pivagabine (CXB 722) is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain .
    Pivagabine
  • HY-148236
    BAY-390
    1 Publications Verification

    TRP Channel Inflammation/Immunology
    BAY-390, a chemical probe, is a selective, across species active and brain penetrating TRPA1 inhibitor. BAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC50s of 16, 82, 63 and 35 nM, respectively. BAY-390 can be used for the research of inflammation .
    BAY-390
  • HY-P10235

    Amylin Receptor Neurological Disease
    Cyclic AC253 is an antagonist for amylin receptor, with IC50 of 0.3 μM. Cyclic AC253 exhibits neuroprotective efficacy against Aβ toxicity and abrogates Aβ-induced impairment of hippocampal long-term potentiation. Cyclic AC253 penetrate blood-brain barrier (BBB) .
    Cyclic AC253

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