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Central permeability

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GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16900
    Rolipram
    Maximum Cited Publications
    19 Publications Verification

    (R,S)-Rolipram; (±)-Rolipram; ZK 62711

    		 Bacterial HIV Phosphodiesterase (PDE) Epigenetic Reader Domain Amyloid-β Infection Neurological Disease Cancer
    Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis .
    Rolipram
  • HY-B0298A
    Clemastine fumarate
    10+ Cited Publications

    HS-592 fumarate; Meclastine fumarate

    		 Histamine Receptor Apoptosis mAChR Pyroptosis Keap1-Nrf2 p62 Autophagy mTOR IKK Neurological Disease Metabolic Disease
    Clemastine (HS-592; Meclastine) fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
    Clemastine fumarate
  • HY-B0520A
    Benztropine mesylate
    5 Publications Verification

    Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate

    		 Dopamine Receptor mAChR Histamine Receptor Infection Neurological Disease Metabolic Disease Cancer
    Benztropine mesylate (Benzatropine mesylate) is an orally active and BBB-permeable centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
    Benztropine mesylate
  • HY-111263
    NIAD-4
    1 Publications Verification

    		 Fluorescent Dye Amyloid-β Others
    NIAD-4 is a blood-brain barrier permeable fluorophore for optical imaging of amyloid-β (Aβ) in the central nervous system (CNS) for Alzheimer’s disease (AD). NIAD-4 binds to the same Aβ site with the binding affinity (Ki) of 10 nM .
    NIAD-4
  • HY-102020
    RG3039
    3 Publications Verification

    PF-06687859

    		 DNA/RNA Synthesis Neurological Disease
    RG3039 (PF-06687859) is an orally active, blood-brain barrier-permeable DcpS inhibitor with an IC50 of 4.2 nM against hDcpS. RG3039 inhibits the decapping activity of DcpS and maintains DcpS in a catalytically inactive conformation in the central nervous system and other tissues. RG3039 extends survival and improves function in spinal muscular atrophy mice. RG3039 is applicable to research related to spinal muscular atrophy .
    RG3039
  • HY-105231
    Bryostatin 1
    2 Publications Verification

    		 PKC HIV Bacterial Infection Neurological Disease Inflammation/Immunology Cancer
    Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties .
    Bryostatin 1
  • HY-101418
    JNJ-47965567
    5 Publications Verification

    		 P2X Receptor Neurological Disease
    JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology .
    JNJ-47965567
  • HY-P99797
    Pabinafusp alfa

    JR-141

    		 Transferrin Receptor Neurological Disease
    Pabinafusp alfa (JR-141) is a transferrin receptor-targeting antibody consisting of Iduronate 2-sulfatase (HY-P76399) and an anti-human transferrin receptor antibody. Pabinafusp alfa is blood-brain permeable and prevents heparan sulfate (HS) deposition in the central nervous system of mucopolysaccharidosis II (MPS II) mice. Pabinafusp alfa improves learning and prevents central nervous system neuronal damage in mice .
    Pabinafusp alfa
  • HY-113413
    Imidazoleacetic acid
    2 Publications Verification

    Imidazolyl-4-acetic acid

    		 Endogenous Metabolite GABA Receptor Cardiovascular Disease Neurological Disease Metabolic Disease
    Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the GABAA receptor. Imidazoleacetic acid forms via histamine oxidation in the mouse brain. Imidazoleacetic acid exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces a range of centrally mediated effects, including analgesia, sedation, hypnosis, as well as reductions in blood pressure, body temperature, isolation-induced aggression and motor activity .
    Imidazoleacetic acid
  • HY-B0298
    Clemastine
    10+ Cited Publications

    HS-592; Meclastine

    		 Histamine Receptor mAChR Autophagy Apoptosis Keap1-Nrf2 p62 mTOR Pyroptosis IKK Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Clemastine (HS-592; Meclastine) is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
    Clemastine
  • HY-15023
    Cligosiban
    5+ Cited Publications

    PF-3274167

    		 Oxytocin Receptor Endocrinology
    Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents [1][2].
    Cligosiban
  • HY-149555
    DNL343

    		Eukaryotic Initiation Factor (eIF) Neurological Disease
    DNL343 is a potent, selective, orally active and brain-penetrant activator of eukaryotic initiation factor eIF2B. DNL343 inhibits the activity of the integrated stress response (ISR) in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 can be used in the study of neurodegenerative diseases .
    DNL343
  • HY-P10502
    L57

    		LDLR Infection
    L57 is a low-density lipoprotein receptor-related protein 1 (LRP1)-binding peptide. L57 exhibits high affinity for LRP1, with an EC50 of 45 nM. L57 possesses blood-brain barrier (BBB) permeability and plasma stability. L57 can serve as a carrier for central nervous system drug delivery .
    L57
  • HY-B1343
    Pridinol mesylate

    		Cholinesterase (ChE) Neurological Disease
    Pridinol mesylate is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol mesylate reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol mesylate inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .
    Pridinol mesylate
  • HY-B0520
    Benztropine
    5 Publications Verification

    Benzatropine; Benzotropine

    		 Dopamine Receptor mAChR Histamine Receptor Cancer
    Benztropine (Benzatropine; Benzotropine) is an orally active and BBB-permeable centrally acting anticholinergic agent that can be used for Parkinson's disease research . Benztropine is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
    Benztropine
  • HY-U00050
    (E)-10-Hydroxynortriptyline

    E-10-OH-NT

    		 Drug Metabolite Adrenergic Receptor mAChR Neurological Disease
    (E)-10-Hydroxynortriptyline (E-10-OH-NT) is a blood-brain barrier-permeable norepinephrine uptake inhibitor. (E)-10-Hydroxynortriptyline effectively promotes central norepinephrine neuronal transmission, with little interindividual variation in in vivo potency. (E)-10-Hydroxynortriptyline has low affinity for muscarinic receptors, exhibits only extremely weak anticholinergic activity, and does not inhibit salivary secretion. (E)-10-Hydroxynortriptyline can be used in studies related to depression .
    (E)-10-Hydroxynortriptyline
  • HY-164795
    SBI-810

    		Neurotensin Receptor Arrestin iGluR ERK Sodium Channel Neurological Disease
    SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders .
    SBI-810
  • HY-164795A
    SBI-810 hydrochloride

    		Neurotensin Receptor Arrestin iGluR ERK Sodium Channel Neurological Disease
    SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders .
    SBI-810 hydrochloride
  • HY-N1414
    (E)-3',6-Disinapoylsucrose

    		Trk Receptor NF-κB Amyloid-β Neurological Disease
    (E)-3',6-Disinapoylsucrose is an orally active, blood-brain barrier permeable neuroprotective agent that inhibits Aβ protein aggregation. (E)-3',6-Disinapoylsucrose exerts anxiolytic, anti-inflammatory and cognitive-enhancing effects. (E)-3',6-Disinapoylsucrose regulates the TrkB/BDNF signaling pathway, inhibits the expression of NF-κB p65, reduces pro-inflammatory cytokine levels, and alleviates neuronal damage. (E)-3',6-Disinapoylsucrose also enhances the functions of central 5-HT and noradrenergic systems, thereby improving spatial learning and memory abilities and reducing anxiety-like behaviors. (E)-3',6-Disinapoylsucrose can be used for the research of related diseases such as Alzheimer's disease, depression, memory impairment and anxiety disorder .
    (E)-3',6-Disinapoylsucrose
  • HY-164288
    TDI-6570

    TDI-006570

    		 Cyclic GMP-AMP Synthase STING Neurological Disease Inflammation/Immunology
    TDI-6570 (TDI-006570) is a blood-brain barrier-permeable, orally active cGAS inhibitor with an IC50 of 1.64 μM. TDI-6570 exhibits high gastrointestinal absorption and a long brain half-life in mice, and shows no toxicity to primary neurons. By inhibiting the cGAS-STING-IFN signaling pathway, TDI-6570 reduces STING levels and the activation of TBK1, blocks double-stranded DNA-induced cGAS activation and downstream interferon-stimulated gene expression, thereby reducing tau protein spread and improving synaptic loss. TDI-6570 reverses memory deficits, increases the amplitude of long-term potentiation, enhances the MEF2C transcriptional network, restores PSD-95 and vGAT punctate structures, and significantly improves cognitive resilience. TDI-6570 can be applied to the research of Alzheimer's disease, Parkinson's disease, systemic lupus erythematosus, as well as various central nervous system and autoimmune diseases .
    TDI-6570
  • HY-153615
    CVN636

    		mGluR Neurological Disease
    CVN636 is a potent, orally active and selective mGluR7 allosteric agonist with an EC50 value of 7 nM for hu mGluR7. CVN636 has central nervous system (CNS) permeability .
    CVN636
  • HY-12143
    Vofopitant dihydrochloride

    GR 205171A

    		 Neurokinin Receptor Neurological Disease
    Vofopitant dihydrochloride (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant dihydrochloride blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant dihydrochloride exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant dihydrochloride improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant dihydrochloride can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .
    Vofopitant dihydrochloride
  • HY-164495
    Sob-AM2

    		FAAH Thyroid Hormone Receptor Inflammation/Immunology Endocrinology
    Sob-AM2 is a potent substrate (Km=1.3 μM) targeting fatty acid amide hydrolase (FAAH) expressed in the brain and has blood-brain barrier permeability. Sob-AM2 delivers high concentrations of Sobetirome (HY-14823) to the central nervous system with minimal peripheral systemic dose, thereby stimulating central thyroid hormone receptor β (TRβ). In addition, Sob-AM2 can prevent myelin and axon degeneration in experimental autoimmune encephalomyelitis (EAE) mice .
    Sob-AM2
  • HY-173396
    VU0467319

    VU319

    		 mAChR Neurological Disease
    VU0467319 (Compound VU319) is a highly selective and blood-brain-permeable, orally active M1 positive allosteric modulator (PAM) (EC50: 492 nM). VU0467319 is selective (EC50 > 30 μM) versus M2-5 for both human and rat. VU0467319 improves cognitive impairment in Alzheimer's disease (AD) through central M1 muscarinic receptors. VU0467319 does not induce cholinergic adverse reactions and has potential in AD research .
    VU0467319
  • HY-177498
    M1 mAChR modulator-1

    		mAChR Neurological Disease
    M1 mAChR modulator-1 (Example 66) is a muscarinic M1 receptor (mAChR1) positive allosteric modulator. M1 mAChR modulator-1 effectively promotes gastrointestinal motility and defecation in mouse models with low central permeability. M1 mAChR modulator-1 can be used for constipation research .
    M1 mAChR modulator-1
  • HY-13976A
    PRL-8-53

    		Drug Derivative Neurological Disease
    PRL-8-53 is an orally active, blood-brain barrier-permeable benzoate derivative with potent spasmolytic activity and central nervous system regulatory activity. PRL-8-53 acts on dopamine, serotonin and cholinergic-related targets, enhances dopamine activity, partially inhibits serotonin function and elicits cholinergic responses, thereby maintaining neurotransmitter balance in the central nervous system. PRL-8-53 improves learning ability, short-term memory and long-term memory in animals. PRL-8-53 can be used in central nervous system-related research .
    PRL-8-53
  • HY-161712
    IMPDH-IN-4

    		IMPDH Cancer
    IMPDH-IN-4 is a derivative of N-pyridinylthiophene carboxamid that exhibits activity against peripheral nerve sheath carcinoma cells. IMPDH-IN-4 is metabolized by NAMPT and NMNAT1 to an adenine dinucleotide (AD) derivative, which is an NAD analog and can inhibit inosine monophosphate dehydrogenase (IMPDH), leading to the accumulation of inosine monophosphate (IMP) in cells. IMPDH-IN-4 has good blood-brain barrier permeability and can be used in the study of central and peripheral nervous system cancers .
    IMPDH-IN-4
  • HY-12678S1
    Entrectinib-d8

    NMS-E628-d8; RXDX-101-d8

    		 Isotope-Labeled Compounds Autophagy Anaplastic lymphoma kinase (ALK) Trk Receptor ROS Kinase Cancer
    Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
    Entrectinib-d8
  • HY-110176
    ASP2535

    		GlyT Neurological Disease
    ASP2535 is a potent, orally bioavailable, selective, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor. ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease .
    ASP2535
  • HY-12142
    Vofopitant

    GR 205171

    		 Neurokinin Receptor Neurological Disease
    Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .
    Vofopitant
  • HY-175482
    PARP1-IN-43

    		PARP Neurological Disease Cancer
    PARP1-IN-43 (Compound 5350) is a blood-brain barrier (BBB) permeable PARP1 inhibitor, with an IC50 of 5 nM. PARP1-IN-43 can be used for the study of homologous recombination (HR)-deficient central nerve system (CNS) cancers .
    PARP1-IN-43
  • HY-B1343A
    Pridinol

    		Cholinesterase (ChE) Neurological Disease
    Pridinol is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .
    Pridinol
  • HY-B1343R
    Pridinol mesylate (Standard)

    		Reference Standards Cholinesterase (ChE) Neurological Disease
    Pridinol mesylate (Standard) is the analytical standard of Pridinol mesylate (HY-B1343). This product is intended for research and analytical applications. Pridinol mesylate is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol mesylate reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol mesylate inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .
    Pridinol mesylate (Standard)
  • HY-16900R
    Rolipram (Standard)

    (R,S)-Rolipram (Standard); (±)-Rolipram (Standard); ZK 62711 (Standard)

    		 Reference Standards Bacterial HIV Phosphodiesterase (PDE) Epigenetic Reader Domain Amyloid-β Neurological Disease Cancer
    Rolipram (Standard) is the analytical standard of Rolipram (HY-16900). This product is intended for research and analytical applications. Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis .
    Rolipram (Standard)
  • HY-W018475
    Rizatriptan

    MK 462 free base

    		 5-HT Receptor Neurological Disease
    Rizatriptan (MK 462 free base) is an orally active 5-HT1B/5-HT1D receptor agonist, with BBB permeability. Rizatriptan exerts significant anti-migraine effects by constricting intracranial and extracranial blood vessels and inhibiting neuropeptide release. Rizatriptan exhibits species- and tissue-specific metabolic characteristics; for example, it undergoes oxidative deamination mainly by MAO-A in the liver of brown rats, so co-administration with MAO-A inhibitors is prohibited. Rizatriptan may also exacerbate nitroglycerin-induced cutaneous allodynia, prolong the duration of central sensitization, and increase anxiety-like behavior and active drug-seeking behavior in mice. Rizatriptan has been widely used in studies related to migraine and medication-overuse headache .
    Rizatriptan
  • HY-162821
    LI-3948

    		IPK Superfamily Neurological Disease
    IP6K-IN-2 (compound 29c) is an orally bioavailable and blood-brain barrier permeable IP6K inhibitor (IC50: 15.8 nM) that can be used in the study of central nervous system diseases .
    LI-3948
  • HY-15023R
    Cligosiban (Standard)

    PF-3274167 (Standard)

    		 Oxytocin Receptor Reference Standards Endocrinology
    Cligosiban (Standard) is the analytical standard of Cligosiban. This product is intended for research and analytical applications. Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents .
    Cligosiban (Standard)
  • HY-123934
    VU6007477

    		P-glycoprotein Neurological Disease
    VU6007477 is a brain-penetrant, selective M1 positive allosteric modulator (PAM) with an EC50 value of 230 nM. VU6007477 is also a human P-glycoprotein (P-gp) substrate with moderate permeability. VU6007477 displays improved central nervous system (CNS) penetration over the hydroxylated congeners. VU6007477 a pyranyl amide derivative, which is promising for research of robust cholinergic seizure activity .
    VU6007477
  • HY-B1343AS
    Pridinol-d5

    		Cholinesterase (ChE) Isotope-Labeled Compounds Neurological Disease
    Pridinol-d5 is deuterium labeled Pridinol (HY-B1343A) . Pridinol is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .
    Pridinol-d5
  • HY-113413R
    Imidazoleacetic acid (Standard)

    Imidazolyl-4-acetic acid (Standard)

    		 Reference Standards Endogenous Metabolite GABA Receptor Cardiovascular Disease Neurological Disease Metabolic Disease
    Imidazoleacetic acid (Standard) is the analytical standard of Imidazoleacetic acid (HY-113413). This product is intended for research and analytical applications. Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the GABAA receptor. Imidazoleacetic acid forms via histamine oxidation in the mouse brain. Imidazoleacetic acid exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces a range of centrally mediated effects, including analgesia, sedation, hypnosis, as well as reductions in blood pressure, body temperature, isolation-induced aggression and motor activity .
    Imidazoleacetic acid (Standard)
  • HY-159492
    5-HT7 receptor ligand 2

    		5-HT Receptor Neurological Disease
    5-HT7 receptor ligand 2 (compound 32) is an arylpiperazinehydrazine ligand for 5-HT7R (Ki=178 nM). 5-HT7 receptor ligand 2 has good membrane permeability, low hepatotoxicity and cardiotoxicity, and high plasma protein binding. 5-HT7 receptor ligand 2 shows neuroprotective effects in SH-SY5Y cells and can be used for the study of central nervous system related diseases .
    5-HT7 receptor ligand 2
  • HY-B0298AS
    Clemastine-d5 fumarate
    1 Publications Verification

    HS-592-d5 fumarate; Meclastine-d5 fumarate

    		 Isotope-Labeled Compounds Histamine Receptor Apoptosis mAChR Pyroptosis Keap1-Nrf2 p62 Autophagy mTOR IKK Neurological Disease Metabolic Disease
    Clemastine (HS-592; Meclastine)-d5 fumarate is the deuterium labeled Clemastine fumarate. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
    Clemastine-d5 fumarate
  • HY-B0298AR
    Clemastine fumarate (Standard)

    HS-592 fumarate (Standard); Meclastine fumarate (Standard)

    		 Reference Standards Histamine Receptor Apoptosis mAChR Pyroptosis Keap1-Nrf2 p62 Autophagy mTOR IKK Neurological Disease Metabolic Disease
    Clemastine (HS-592; Meclastine) fumarate (Standard) is the analytical standard of Clemastine fumarate. This product is intended for research and analytical applications. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
    Clemastine fumarate (Standard)
  • HY-116142
    CP-283097

    		iGluR Neurological Disease
    CP-283097 is an orally active and conformationally restricted and NR2B subtype-selective NMDA antagonist. CP-283097 efficiently competitively inhibits the binding of [³H]CP-101,606 to the rat meninges, with an IC50 value of 18 nM. CP-283097 exhibits nearly complete inhibition of the current mediated by the NR2B receptor (IC50 = 206 nM), while the inhibitory effect on the NR2A or NR2C receptors is very weak. CP-283097 demonstrates excellent central nervous system permeability and in vivo efficacy in animal models. CP-283097 can be used for neurological diseases related to excessive activation of NMDA receptors .
    CP-283097
  • HY-12142S
    rac-Vofopitant-d3

    rac-GR 205171-d3

    		 Isotope-Labeled Compounds Neurokinin Receptor Neurological Disease
    rac-Vofopitant-d3 (rac-GR 205171-d3) is a racemic form of deuterated Vofopitant (HY-12142). Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .
    rac-Vofopitant-d3
  • HY-101418R
    JNJ-47965567 (Standard)

    		P2X Receptor Reference Standards Neurological Disease
    JNJ-47965567 (Standard) is the analytical standard of JNJ-47965567 (HY-101418). This product is intended for research and analytical applications. JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology .
    JNJ-47965567 (Standard)
  • HY-102020A
    RG3039 hydrochloride

    		DNA/RNA Synthesis Neurological Disease
    RG3039 hydrochloride is an orally active, blood-brain barrier-permeable DcpS inhibitor with an IC50 of 4.2 nM against hDcpS. RG3039 hydrochloride inhibits the decapping activity of DcpS and maintains DcpS in a catalytically inactive conformation in the central nervous system and other tissues. RG3039 hydrochloride extends survival and improves function in spinal muscular atrophy mice. RG3039 hydrochloride is applicable to research related to spinal muscular atrophy .
    RG3039 hydrochloride
  • 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-102020R
    RG3039 (Standard)

    PF-06687859 (Standard)

    		 DNA/RNA Synthesis Reference Standards Neurological Disease
    RG3039 (Standard) is the analytical standard of RG3039 (HY-102020). This product is intended for research and analytical applications. RG3039 (PF-06687859) is an orally active, blood-brain barrier-permeable DcpS inhibitor with an IC50 of 4.2 nM against hDcpS. RG3039 inhibits the decapping activity of DcpS and maintains DcpS in a catalytically inactive conformation in the central nervous system and other tissues. RG3039 extends survival and improves function in spinal muscular atrophy mice. RG3039 is applicable to research related to spinal muscular atrophy .
    RG3039 (Standard)
  • HY-16900G
    Rolipram

    		Phosphodiesterase (PDE) Epigenetic Reader Domain Amyloid-β Neurological Disease Inflammation/Immunology Cancer
    Rolipram GMP is Rolipram (HY-16900) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis .
    Rolipram

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