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Blood-brain barrier penetrant

" in MedChemExpress (MCE) Product Catalog:

108

Inhibitors & Agonists

1

Screening Libraries

1

Biochemical Assay Reagents

5

Peptides

3

Natural
Products

8

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-17355
    Pramipexole dihydrochloride
    10+ Cited Publications

    		 Dopamine Receptor Neurological Disease
    Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .
    Pramipexole dihydrochloride
  • HY-B0410
    Pramipexole
    10+ Cited Publications

    		 Dopamine Receptor Neurological Disease
    Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .
    Pramipexole
  • HY-12947
    GNE-3511
    5+ Cited Publications

    		 MAP3K Neurological Disease
    GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases .
    GNE-3511
  • 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-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-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-15722
    SB-222200
    5+ Cited Publications

    		 Neurokinin Receptor Neurological Disease Endocrinology
    SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders .
    SB-222200
  • 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-105283
    PF 04531083

    		Sodium Channel Neurological Disease
    PF 04531083 is an orally active and selective NaV1.8 blocker with an IC50 of 0.7 μM. PF 04531083 is a blood-brain barrier (BBB) penetrant compound. PF 04531083 can be used for the research of respiratory system and neuropathic/inflammatory pain .
    PF 04531083
  • HY-136731
    APE1-IN-1

    		DNA/RNA Synthesis Cancer
    APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 (APE1) inhibitor with an IC50 value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide (HY-17364) to cancer cells .
    APE1-IN-1
  • 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-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-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-109968
    Irdabisant

    CEP-26401

    		 Histamine Receptor Neurological Disease Metabolic Disease
    Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
    Irdabisant
  • HY-173591
    T0080

    		Formyl Peptide Receptor (FPR) Apoptosis Cardiovascular Disease Neurological Disease Inflammation/Immunology
    T0080 is a central nervous system-penetrant FPR1 inhibitor. By functionally blocking the FPR1 signaling pathway, T0080 effectively reduces neutrophil infiltration into ischemic brain tissue and maintains the integrity of the blood-brain barrier. T0080 alleviates tPA-associated hemorrhagic transformation, inhibits demyelination responses and the expression of NOX2. T0080 also possesses anti-apoptotic (apoptosis) and anti-inflammatory properties, thereby protecting myelin and reducing neurological deficits. T0080 is widely used in studies related to ischemic stroke complicated by hemorrhagic transformation after tPA thrombolysis, as well as multiple sclerosis .
    T0080
  • HY-B0410A
    Pramipexole dihydrochloride hydrate
    10+ Cited Publications

    		 Dopamine Receptor Neurological Disease
    Pramipexole dihydrochloride hydrate is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .
    Pramipexole dihydrochloride hydrate
  • 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-P10580
    Vasculotide

    		Tie PI3K Akt Cadherin Claudin Cardiovascular Disease Infection Inflammation/Immunology
    Vasculotide is a blood-brain barrier (BBB)-penetrant Tie2 agonist. Vasculotide binds to a unique domain of Tie2, induces receptor clustering to drive phosphorylation, activates downstream PI3K/Akt and eNOS pathways, enhances inter-endothelial cell junctions (such as VE-cadherin and claudin-5), and inhibits inflammatory adhesion molecules, ultimately stabilizing the vascular endothelial barrier and reducing its permeability . Vasculotide alleviates pulmonary microvascular leakage and microcirculatory dysfunction caused by cardiopulmonary bypass, acts as an adjuvant radioprotective agent to reduce acute radiation dermatitis, and promotes BBB recovery after focused ultrasound (FUS). Combination of Vasculotide with antibiotics reduces lung injury .
    Vasculotide
  • HY-150700
    RLX-33

    		ERK Metabolic Disease
    RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome .
    RLX-33
  • HY-110278
    ADX71743

    		mGluR Neurological Disease
    ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 can cross the blood-brain barrier (BBB) and possesses anxiolytic activity. .
    ADX71743
  • HY-110123
    ML-00253764 hydrochloride

    		Melanocortin Receptor Neurological Disease Metabolic Disease Cancer
    ML-00253764 hydrochloride is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a Ki and IC50 of 0.16 μM and 0.103 μM, respectively. ML-00253764 can cross blood-brain barrier .
    ML-00253764 hydrochloride
  • 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-147395
    GPR52 agonist-1

    		GPR52 Neurological Disease
    GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity .
    GPR52 agonist-1
  • 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-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-147319
    RTI-7470-44

    		Trace Amine-associated Receptor (TAAR) Neurological Disease
    RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC50 value of 8.4 nM and a Ki value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD) .
    RTI-7470-44
  • 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-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-120717
    VU6001966

    		mGluR Cytochrome P450 Neurological Disease
    VU6001966 is a brain-penetrant and selective mGlu2 receptor inhibitor. VU6001966 blocks mGlu2 receptor activity, counteracts LY379268 (HY-103558)-mediated blood-brain barrier protection and inflammatory cytokine dampening in microglia under inflammatory conditions. VU6001966 enhances antidepressant effects when combined with Scopolamine (HY-N0296). VU6001966 can be used for the research of major depressive disorder .
    VU6001966
  • 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-107731
    SF 11

    		Neuropeptide Y Receptor Neurological Disease
    SF 11 is a potent and brain penetrant neuropeptide Y Y2 receptor antagonist (IC50=199 nM). Antidepressant-like activity .
    SF 11
  • HY-P10580A
    Vasculotide TFA

    		Cadherin Tie Claudin PI3K Akt Cardiovascular Disease Infection Inflammation/Immunology
    Vasculotide TFA is a blood-brain barrier (BBB)-penetrant Tie2 agonist. Vasculotide TFA binds to a unique domain of Tie2, induces receptor clustering to drive phosphorylation, activates downstream PI3K/Akt and eNOS pathways, enhances inter-endothelial cell junctions (such as VE-cadherin and claudin-5), and inhibits inflammatory adhesion molecules, ultimately stabilizing the vascular endothelial barrier and reducing its permeability . Vasculotide TFA alleviates pulmonary microvascular leakage and microcirculatory dysfunction caused by cardiopulmonary bypass, acts as an adjuvant radioprotective agent to reduce acute radiation dermatitis, and promotes BBB recovery after focused ultrasound (FUS). Combination of Vasculotide TFA with antibiotics reduces lung injury .
    Vasculotide TFA
  • 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-17355S1
    Pramipexole-d5 dihydrochloride

    		Isotope-Labeled Compounds Dopamine Receptor Neurological Disease
    Pramipexole-d5 dihydrochloride is deuterium labeled Pramipexole dihydrochloride. Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS) .
    Pramipexole-d5 dihydrochloride
  • 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-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-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-117501
    Dexchlorpheniramine

    		Histamine Receptor Inflammation/Immunology Cancer
    Dexchlorpheniramine is an potent and blood-brain barrier (BBB) penetrant histamine 1 (H1) receptor antagonist with anticholinergic properties. Dexchlorpheniramine can be used for researching allergies .
    Dexchlorpheniramine
  • 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-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

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