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blood-brain barrier-penetrant

" in MedChemExpress (MCE) Product Catalog:

64

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1

Biochemical Assay Reagents

2

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4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13324
    Bardoxolone methyl
    Maximum Cited Publications
    41 Publications Verification

    RTA 402; NSC 713200; CDDO Methyl ester

    		 Keap1-Nrf2 SARS-CoV Virus Protease Cardiovascular Disease Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Bardoxolone (CDDO; RTA 401) methyl is an orally active and blood-brain-barrier-penetrant activator of Nrf2 and an inhibitor of SARS-CoV-2 3CL protease. Bardoxolone methyl inhibits SARS-CoV-2 replication in Vero cells with an EC50 value of 0.29 μM. Bardoxolone methyl increases levels of pNrf2 and HO-1, inhibits inflammatory mediators like pNFκB and MCP-1. Bardoxolone methyl activates the Nrf2 pathway to enhance antioxidant and anti-inflammatory responses, inhibits viral replication, and improves mitochondrial function. Bardoxolone methyl can be used in research on chemotherapy-induced neuropathic pain (CINP), COVID-19, and chronic kidney disease (CKD) .
    Bardoxolone methyl
  • HY-109521A
    Manganese chloride tetrahydrate, molecular biology grade,≥99.0% (KT)

    Manganese(Ⅱ) chloride tetrahydrate, molecular biology grade,≥99.0% (KT)

    		 Biochemical Assay Reagents Histone Acetyltransferase HDAC Neurological Disease
    Manganese chloride (tetrahydrate), molecular biology grade,≥99.0% (KT) is an orally active and a blood-brain barrier penetrant compound. It affects the activities of multiple enzymes in cells, such as regulating the activities of histone acetyltransferase (HAT) and histone deacetylase (HDAC), thereby affecting gene expression. It has multiple activities such as neurotoxicity, embryotoxicity, and reproductive toxicity. It is currently mainly used in neurodegenerative diseases and toxicology research.
    Manganese chloride tetrahydrate, molecular biology grade,≥99.0% (KT)
  • HY-12355
    Siponimod
    5+ Cited Publications

    BAF-312

    		 LPL Receptor Potassium Channel Infection Inflammation/Immunology
    Siponimod (BAF-312) is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis .
    Siponimod
  • HY-10328
    Neflamapimod
    5+ Cited Publications

    VX-745

    		 p38 MAPK Autophagy Inflammation/Immunology
    Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
    Neflamapimod
  • HY-13314
    Tesevatinib
    4 Publications Verification

    XL-647; EXEL-7647; KD-019

    		 EGFR VEGFR Src Cancer
    Tesevatinib (XL-647) is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib can inhibit tumor proliferation and exhibits antitumor activity .
    Tesevatinib
  • HY-112870A
    Firmonertinib mesylate
    5+ Cited Publications

    Alflutinib mesylate; Furmonertinib mesylate; AST2818 mesylate

    		 EGFR Inflammation/Immunology Cancer
    Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
    Firmonertinib mesylate
  • HY-15976
    P7C3
    5+ Cited Publications

    		 Others Neurological Disease
    P7C3 is an orally bioavailable and blood-brain barrier penetrant aminopropyl carbazole, with neuroprotective effects. P7C3 can be used for the research of neurodegenerative diseases, including Parkinson's disease .
    P7C3
  • HY-17387
    (-)-Huperzine A
    5+ Cited Publications

    Huperzine A

    		 Cholinesterase (ChE) iGluR Infection Neurological Disease Inflammation/Immunology
    (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
    (-)-Huperzine A
  • HY-P3281
    FGL peptide

    		FGFR Neurological Disease
    FGL peptide is a fibroblast growth factor receptor (FGFR) modulator and blood-brain barrier-penetrant. FGL peptide activates NCAM-FGFR and FGFR1 signaling pathways. FGL peptide alters expression of apoptosis, signal transduction and metabolism regulator genes in traumatic brain injury contexts. FGL peptide can be used for the research of traumatic brain injury .
    FGL peptide
  • HY-10996A
    KHS101 hydrochloride
    1 Publications Verification

    		 Autophagy HSP Apoptosis Aurora Kinase Microtubule/Tubulin Polo-like Kinase (PLK) Neurological Disease Cancer
    KHS101 is a blood-brain barrier-penetrant anticancer agent that primarily functions by inhibiting HSPD1 (IC50 = 14.4 μM) and TACC3 across different cellular backgrounds. KHS101 promotes the aggregation of HSPD1 with client proteins, destabilizes TACC3, and reduces the levels of TACC3, Aurora A and PLK1. KHS101 induces autophagy, apoptosis, cell cycle exit and neuronal differentiation; it suppresses cancer cell growth, motility, EMT and stemness; it also impairs mitochondrial bioenergetics and glycolysis in glioblastoma cells. KHS101 can be used in research related to glioblastoma multiforme and breast cancer .
    KHS101 hydrochloride
  • HY-157839
    PROTAC α-Synuclein/Tau degrader 1

    		PROTACs α-synuclein Tau Protein Neurological Disease
    PROTAC α-Synuclein/Tau degrader 1 is a blood-brain barrier-penetrant dual PROTAC degrader of α-synuclein (α-Syn) and tau, with DC50 of 1.57 μM and 4.09 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 binds to α-Syn and tau PFF, with KDs of 0.47 and 2.78 μM, respectively. PROTAC α-Synuclein/Tau degrader 1 exhibits degradation effect mediated by the ubiquitin-proteasome system (UPS). PROTAC α-Synuclein/Tau degrader 6 can be used for the study of Parkinson’s disease (PD) (Pink: α-Synuclein/Tau ligand (HY-151035); Blue: CRBN ligase ligand (HY-14658); Black: Linker (HY-128803)) .
    PROTAC α-Synuclein/Tau degrader 1
  • HY-45661
    Inixaciclib

    NUV-422

    		 CDK Neurological Disease Cancer
    Inixaciclib (NUV-422) is a blood-brain barrier-penetrant inhibitor of CDK2, CDK4 and CDK6. Inixaciclib inhibits cancer cell growth. Inixaciclib induces anti-tumor activity in xenograft models of glioblastoma, CDK4/CDK6 inhibitor-resistant HR + HER2 - metastatic breast cancer, and anti-androgen-resistant prostate cancer. Inixaciclib can be used for the research of relapsed or metastatic castration-resistant prostate cancer .
    Inixaciclib
  • HY-17388
    (±)-Huperzine A
    1 Publications Verification

    		 Drug Isomer Cholinesterase (ChE) iGluR Neurological Disease
    (±)-Huperzine A is the racemate of (-)-Huperzine A (HY-17387). (-)-Huperzine A is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
    (±)-Huperzine A
  • HY-111455
    LP-211
    2 Publications Verification

    		 5-HT Receptor Neurological Disease Metabolic Disease
    LP-211 is a selective and blood brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).
    LP-211
  • HY-15010
    L-371,257
    1 Publications Verification

    		 Oxytocin Receptor Vasopressin Receptor Cardiovascular Disease Endocrinology
    L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM) .
    L-371,257
  • HY-147294
    Nivasorexant

    ACT-539313

    		 Orexin Receptor (OX Receptor) Cytochrome P450 Neurological Disease
    Nivasorexant (ACT-539313) is an orally active, blood-brain barrier penetrant, selective orexin OX1R inhibitor. Nivasorexant specifically blocks central OX1Rs without affecting OX2Rs, and exhibits competitive inhibitory activity against CYP2C8, CYP2C9, CYP2C19 and CYP3A4 (IC50 values are 25 μM, 8.6 μM, 1.6 μM, 19 μM/44 μM, respectively). Nivasorexant significantly reduces binge-like eating behavior of highly palatable food in rat models and has long-acting properties. Nivasorexant shows no relevant off-target activity against over 130 selected proteins, exhibits favorable safety profiles, and can be used for studies related to binge eating disorder .
    Nivasorexant
  • HY-162566
    REM127

    		Molecular Glues Calcium Channel Amyloid-β Tau Protein Neurological Disease
    REM127 is an orally active, blood-brain barrier-penetrant septin 6/7 molecular glue degrader. REM127 binds to SEPT6 with high affinity and promotes the assembly of SEPT2/6/7 cortical filaments, thereby normalizing cytoplasmic calcium levels, cerebrospinal fluid hyperphosphorylated tau protein levels, synaptic function and cognitive function. REM127 can be used in research related to Alzheimer's disease .
    REM127
  • HY-107982
    VU6005649

    		mGluR Neurological Disease
    VU6005649 is a blood-brain-barrier penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.
    VU6005649
  • HY-141866
    Acid Ceramidase-IN-1
    1 Publications Verification

    		 Ceramidase Neurological Disease
    Acid Ceramidase-IN-1 is orally active and blood-brain barrier penetrant acid ceramidase (AC, ASAH-1) inhibitor (hAC IC50=0.166 μM). Acid Ceramidase-IN-1 reduces AC activity, accumulates ceramide species (Cer (d18:0/16:0), Cer (d18:1/16:0)), and decreases sphingosine levels. Acid Ceramidase-IN-1 can be used for the study of severe neurological lysosomal storage diseases (LSDs) such as Gaucher’s disease (GD) and Krabbe’s disease (KD) .
    Acid Ceramidase-IN-1
  • HY-118301
    ADX71441

    		GABA Receptor 5-HT Receptor Neurological Disease
    ADX71441 is an orally active, blood-brain barrier penetrant positive allosteric modulator of GABAB receptor. ADX71441 potentiates the activity of endogenous GABA at GABAB receptor, with an EC50 of 96 nM. ADX71441 functionally inhibits adenosine transporters and 5-HT2B receptor. ADX71441 produces anxiolytic-like, analgesic, muscle relaxant, hypothermic and overactive bladder inhibitory effects, reduces acute locomotor activity levels, decreases voluntary intake of alcohol and saccharin, attenuates stress-induced neuronal activation, and exhibits anti-hyperalgesic activity .
    ADX71441
  • HY-113603
    Tildacerfont

    SPR001; LY2371712

    		 CRFR Metabolic Disease
    Tildacerfont (SPR001; LY2371712) is an orally active, blood-brain barrier-penetrant selective corticotropin-releasing factor type 1 (CRF1) receptor antagonist. Tildacerfont selectively blocks CRF1 receptors, thereby inhibiting the release of pituitary adrenocorticotropic hormone (ACTH). Tildacerfont can be used in research related to congenital adrenal hyperplasia .
    Tildacerfont
  • HY-P10019
    Pegsebrenatide

    NLY01

    		 GCGR Neurological Disease Inflammation/Immunology
    Pegsebrenatide (NLY01) is a blood-brain barrier-penetrant GLP-1R agonist. Pegsebrenatide alleviates retinal inflammation and neuronal death secondary to ocular hypertension . Pegsebrenatide significantly delays onset and reduces disease severity in experimental autoimmune encephalomyelitis . Pegsebrenatide inhibits the formation of A1 reactive astrocytes in nerve cells and reduces the loss of retinal ganglion cells and dopaminergic neurons. Pegsebrenatide exerts neuroprotective effects in a mouse model of Parkinson's disease by directly preventing microglia-mediated conversion of astrocytes to the A1 neurotoxic phenotype. Pegsebrenatide can be used for research on glaucoma, Parkinson's disease, and multiple sclerosis .
    Pegsebrenatide
  • HY-B2029
    Phosalone
    1 Publications Verification

    		 Insecticide Cholinesterase (ChE) Infection Inflammation/Immunology
    Phosalone is an orally active, blood-brain barrier penetrant Insecticide and acaricide. Phosalone inhibits the activity of Acetylcholinesterase. Phosalone acts as a substrate for detoxifying esterases. Phosalone induces symptoms of cholinergic hyperactivity, toxic reactions, mortality, oxidative stress, and changes in pro-inflammatory protein levels, and exerts toxic effects on colonic tissues and cells. Phosalone controls pistachio psyllids. Phosalone can be used in studies related to colitis .
    Phosalone
  • HY-160939
    ASK1-IN-6

    		ASK1 Interleukin Related Neurological Disease Inflammation/Immunology
    ASK1-IN-6 is a selective, orally active, and blood-brain barrier penetrant inhibitor of ASK1 (biochemical IC50: 7 nM; cellular IC50: 25 nM). ASK1-IN-6 exhibits anti-inflammatory and can be used in the research of neurodegenerative diseases such as Alzheimer's disease .
    ASK1-IN-6
  • HY-173066
    NU227326

    		PROTACs Indoleamine 2,3-Dioxygenase (IDO) Cancer
    NU227326 is a blood-brain barrier penetrant IDO1 PROTAC degrader, with a DC50 of 4.5 nM in HiBiT degradation assays. NU227326 degrades IDO1 in U87 and GBM43 cells, with DC50 values of 7.1 nM and 11.8 nM, respectively (WB assays). NU227326 is applicable to research related to glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer .
    NU227326
  • 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 .
    HTT-D3
  • HY-12355A
    Siponimod hemifumarate
    5+ Cited Publications

    BAF-312 hemifumarate

    		 LPL Receptor Potassium Channel Neurological Disease Inflammation/Immunology
    Siponimod (BAF-312) hemifumarate is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod hemifumarate induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod hemifumarate can be used in research related to multiple sclerosis .
    Siponimod hemifumarate
  • HY-161104
    Kv2.1-IN-1
    1 Publications Verification

    		 Potassium Channel Apoptosis Cardiovascular Disease Neurological Disease
    Kv2.1-IN-1 is an orally active and blood-brain barrier penetrant Kv2.1 inhibitor with an IC50 of 0.07 μM. Kv2.1-IN-1 exhibits a selectivity >130 fold over other K +, Na +, and Ca 2+ ion channels. Kv2.1-IN-1 decreases the apoptosis of HEK293 cells induced by H2O2. Kv2.1-IN-1 produces significant neuroprotection efficacy in middle cerebral artery occlusion (MCAO) rat. Kv2.1-IN-1 can be used for the study of ischemic stroke .
    Kv2.1-IN-1
  • HY-113603S
    Tildacerfont-d8

    SPR001-d8; LY2371712-d8

    		 Isotope-Labeled Compounds CRFR Cancer
    Tildacerfont-d8 (SPR001-d8; LY2371712-d8) is a deuterium labeled Tildacerfont (HY-113603). Tildacerfont (SPR001; LY2371712) is an orally active, blood-brain barrier-penetrant selective corticotropin-releasing factor type 1 (CRF1) receptor antagonist. Tildacerfont selectively blocks CRF1 receptors, thereby inhibiting the release of pituitary adrenocorticotropic hormone (ACTH). Tildacerfont can be used in research related to congenital adrenal hyperplasia .
    Tildacerfont-d8
  • HY-18006
    NKP608
    1 Publications Verification

    		 Neurokinin Receptor Wnt Bcl-2 Family β-catenin Cyclin G-associated Kinase (GAK) VEGFR Caspase Cadherin Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    NKP608 is a non-peptidic derivative of 4-aminopiperidine, a highly selective, orally active, neurokinin-1 (NK1) receptor antagonist with IC50 of 2.6 nM. NKP608 is active both in vitro and in vivo, showing extremely low affinity for NK2, NK3 receptors. NKP608 exerts its effects by blocking the NK₁ receptor, regulate cell proliferation and apoptosis, affect neurotransmitter functions and gastric mucosal repair mechanisms, and suppress the Wnt/β-catenin pathway in antitumor research. NKP608 is applicable to research related to various diseases, including cough, anxiety disorders, depression, gastric mucosal injury, and colorectal cancer .
    NKP608
  • HY-17649
    EIDD-036

    		Progesterone Receptor Neurological Disease
    EIDD-036, is the blood-brain barrier penetrant C-20 oxime of Progesterone (HY-N0437), that binds progesterone receptor (PR) with an IC50 of 171 nM. EIDD-036 is the active metabolite of EIDD-1723 (HY-125547). EIDD-036 exhibits promising challenges for rapid administration in acute trauma. EIDD-036 can be used for the study of traumatic brain injury (TBI) .
    EIDD-036
  • HY-19888
    GSK-1482160

    		P2X Receptor Interleukin Related Neurological Disease Inflammation/Immunology
    GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI) .
    GSK-1482160
  • HY-172419
    Blixeprodil

    GM-1020

    		 iGluR Neurological Disease
    Blixeprodil (GM-1020) is an orally active, blood-brain barrier-penetrant NMDA receptor inhibitor with a Ki of 3.25 µM in rat cortical tissues. Blixeprodil binds to the MK-801 ion channel site and blocks NMDA receptor-mediated currents in hyperpolarized states in a voltage-dependent manner. Blixeprodil modulates the power of cortical EEG frequency bands, alters spontaneous motor activity, and induces ataxia at high doses. Blixeprodil can be used in the research of depression .
    Blixeprodil
  • HY-118635
    Cyprodenate

    Actebral

    		 Radionuclide-Drug Conjugates (RDCs) Neurological Disease
    Cyprodenate is an orally active and blood-brain barrier-penetrant stimulant. Cyprodenate can be labeled with 14C. Cyprodenate can be used in the research of psychiatric disorders .
    Cyprodenate
  • HY-12355S
    Siponimod-d11

    BAF-312-d11

    		 Isotope-Labeled Compounds LPL Receptor Potassium Channel Neurological Disease Inflammation/Immunology
    Siponimod-d11 (BAF-312-d11) is deuterium labeled Siponimod (HY-12355). Siponimod is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis.
    Siponimod-d11
  • HY-10996
    KHS101

    		HSP Microtubule/Tubulin Aurora Kinase Polo-like Kinase (PLK) Autophagy Apoptosis Neurological Disease Cancer
    KHS101 is a blood-brain barrier-penetrant anticancer agent that primarily functions by inhibiting HSPD1 (IC50 = 14.4 μM) and TACC3 across different cellular backgrounds. KHS101 promotes the aggregation of HSPD1 with client proteins, destabilizes TACC3, and reduces the levels of TACC3, Aurora A and PLK1. KHS101 induces autophagy, apoptosis, cell cycle exit and neuronal differentiation; it suppresses cancer cell growth, motility, EMT and stemness; it also impairs mitochondrial bioenergetics and glycolysis in glioblastoma cells. KHS101 can be used in research related to glioblastoma multiforme and breast cancer .
    KHS101
  • HY-12355R
    Siponimod (Standard)

    BAF-312 (Standard)

    		 Reference Standards LPL Receptor Potassium Channel Neurological Disease Inflammation/Immunology
    Siponimod (BAF-312) (Standard) is the analytical standard of Siponimod. This product is intended for research and analytical applications. Siponimod is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis.
    Siponimod (Standard)
  • HY-W027553R
    Ipidacrine (Standard)

    NIK-247 free base (Standard); Amiridine free base (Standard)

    		 Reference Standards Cholinesterase (ChE) Potassium Channel Sodium Channel Neurological Disease Metabolic Disease
    Ipidacrine (Standard) is the analytical reference standard of Ipidacrine. This product is used for research and analytical applications. Ipidacrine is orally active and blood-brain-barrier-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
    Ipidacrine (Standard)
  • HY-13314A
    Tesevatinib tosylate

    XL-647 tosylate; EXEL-7647 tosylate; KD-019tosylate

    		 EGFR VEGFR Src Cancer
    Tesevatinib (XL-647) tosylate is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib tosylate significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib tosylate also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib tosylate can inhibit tumor proliferation and exhibits antitumor activity .
    Tesevatinib tosylate
  • HY-13314R
    Tesevatinib (Standard)

    XL-647 (Standard); EXEL-7647 (Standard); KD-019 (Standard)

    		 EGFR VEGFR Src Reference Standards Cancer
    Tesevatinib (Standard) is the analytical standard of Tesevatinib. This product is intended for research and analytical applications. Tesevatinib (XL-647) is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib can inhibit tumor proliferation and exhibits antitumor activity .
    Tesevatinib (Standard)
  • HY-12141
    Vestipitant mesylate

    GW597599 mesylate; GW597599B

    		 Neurokinin Receptor Neurological Disease
    Vestipitant (GW597599) mesylate is a selective, orally active, and blood-brain barrier penetrant NK1 receptor antagonist. Vestipitant mesylate exhibits high affinity for the human NK1 receptor (pKi: 9.65). Vestipitant mesylate can be used in the research of diseases such as depression, anxiety disorders, and nausea and vomiting .
    Vestipitant mesylate
  • HY-17387S1
    (-)-Huperzine A-d4 hydrochloride

    Huperzine A-d4

    		 iGluR Cholinesterase (ChE) Apoptosis Isotope-Labeled Compounds Neurological Disease
    (-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
    (-)-Huperzine A-d4 hydrochloride
  • HY-183766
    HYF038

    		ASK1 Radionuclide-Drug Conjugates (RDCs) Neurological Disease
    HYF038 is a blood-brain barrier-penetrant ligand of apoptosis signal-regulating kinase 1 (ASK1). When labeled with 11C, HYF038 can be used for ASK1 neuroimaging studies .
    HYF038
  • HY-123382
    GSK-1482160 (isomer)

    		Drug Isomer Neurological Disease Inflammation/Immunology
    GSK-1482160 isomer is the isomer of GSK-1482160 (HY-19888). GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI).
    GSK-1482160 (isomer)
  • HY-181178
    (Mor-Cor)Ag(III)

    		Amyloid-β Neurological Disease
    (Mor-Cor)Ag(III) is a blood-brain barrier-penetrant silver(III) corrole complex that penetrates the blood-brain barrier. (Mor-Cor)Ag(III) scavenges reactive oxygen species induced by Aβ42 and disrupts Aβ42 aggregation, attenuating Aβ42-induced neuronal hyperactivity. (Mor-Cor)Ag(III) can be used for the research of Alzheimer's disease .
    (Mor-Cor)Ag(III)
  • HY-181932
    HDM2004

    		MAP4K Cancer
    HDM2004 is a selective, orally active, blood-brain barrier-penetrant HPK1 inhibitor with an IC50 of 1.89 nM. HDM2004 exhibits anticancer activity against colon cancer. HDM2004 shows synergistic activity when combined with anti-PD-L1 in syngeneic mouse models. HDM2004 can be used for the research of colon cancer .
    HDM2004
  • HY-181956
    MPAM-15

    		Opioid Receptor Neurological Disease
    MPAM-15 is a blood-brain barrier-penetrant pan-orthosteric allosteric modulator (PAM) of opioid receptors, with ≥16-fold selectivity for μOR over δOR and κOR. MPAM-15 acts as an anti-nociceptive potentiator and analgesic, and its activity is observed in mouse models via both intracerebroventricular and intraperitoneal administration. MPAM-15 is applicable for pain-related research .
    MPAM-15
  • HY-182440
    AZD3783

    		5-HT Receptor Neurological Disease
    AZD3783 is an orally active, blood-brain barrier-penetrant 5-HT1B receptor antagonist. AZD3783 reverses agonist-induced hypothermia, inhibits separation-induced vocalizations in guinea pig pups, and acts as a moderately permeable glycoprotein substrate with moderate clearance. AZD3783 inhibits hERG channel activity. AZD3783 is applicable for research on depression, anxiety disorders, and other psychiatric diseases associated with serotonergic neurotransmission .
    AZD3783
  • HY-183682
    AZ14289671

    		EGFR p38 MAPK ERK Akt Cancer
    AZ14289671 is an orally active, blood-brain barrier-penetrant tyrosine kinase (tyrosine kinase) inhibitor (TKI) that specifically targets non-small cell lung cancer (NSCLC) harboring EGFR exon 20 insertion mutations (EGFR Exon20Ins), while largely sparing wild-type EGFR to reduce off-target toxicities such as rash and diarrhea. AZ14289671 inhibits the downstream MAPK/ERK/AKT pathway, suppressing tumor cell proliferation, survival and migration. AZ14289671 can be used for NSCLC research .
    AZ14289671
  • HY-174332
    Cholesterol 24-hydroxylase-IN-3

    		Cytochrome P450 Neurological Disease
    Cholesterol 24-hydroxylase-IN-3 is an orally active, selective, and blood-brain barrier-penetrant CH24H inhibitor (IC50 = 23 nM) belonging to 1,3-oxazole derivatives. Cholesterol 24-hydroxylase-IN-3 competitively inhibits CH24H enzyme activity by using the 1,3-oxazole nitrogen atom to coordinate the heme iron and the cyclopropyl group occupying the hydrophobic pocket. Cholesterol 24-hydroxylase-IN-3 can be used for research on epilepsy and other neurological diseases.
    Cholesterol 24-hydroxylase-IN-3

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