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Results for "

cross the blood-brain barrier

" in MCE Product Catalog:

99

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1

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3

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10

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Products

12

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-B0692A
    Cefepime chloride

    BMY-28142 chloride

    Antibiotic Infection
    Cefepime (BMY-28142) chloride is a broad-spectrum and cross the blood-brain barrier cephalosporin. Cefepime chloride shows antibacterial effects against both Gram-positive and Gram-negative aerobic bacteria. Cefepime chloride induces neurotoxicity.
  • HY-B0692
    Cefepime

    BMY-28142

    Antibiotic Infection Cancer
    Cefepime (BMY-28142) is a broad-spectrum and cross the blood-brain barrier cephalosporin. Cefepime shows antibacterial effects against both Gram-positive and Gram-negative aerobic bacteria. Cefepime induces neurotoxicity.
  • HY-120717
    VU6001966

    mGluR Others
    VU6001966 (compound 15m) is a potent and cross the blood-brain barrier mGlu2 (metabotropic glutamate receptor 2) negative allosteric modulator with IC50s of 78 nM and >30 µM for mGlu2 and mGlu3, respectively. VU6001966 can serve as an mGlu2 PET tracer.
  • HY-143464
    BChE-IN-4

    Cholinesterase (ChE) Neurological Disease
    BChE-IN-4 is a potent and cross the blood-brain barrier BChE inhibitor. BChE-IN-4 attenuates learning and memory deficits caused by cholinergic deficit in mouse model. BChE-IN-4 has the potential for the research of alzheimer’s disease.
  • HY-103461
    FAAH-IN-6

    FAAH Neurological Disease
    FAAH-IN-6 (compound 21d) is a potent, orally active and cross the blood-brain barrier fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 0.72, 0.28 nM for hFAAH, rFAAH, respectively. FAAH-IN-6 shows dose-dependent analgesic efficacy in animal models of both neuropathic and inflammatory pain.
  • HY-147512
    CB1/2 agonist 1

    Cannabinoid Receptor Inflammation/Immunology
    CB1/2 agonist 1 is a potent and cross the blood-brain barrier CB1/2 agonist with EC50s of 56.15, 11.63 nM for CB1R and CB2R, respectively. CB1/2 agonist 1 reduces glutamate release and LPS-induced activation of microglial cells. CB1/2 agonist 1 shows anti-inflammatory and antinociceptive effects. CB1/2 agonist 1 has the potential for the research of multiple sclerosis.
  • HY-B1206
    Neostigmine methyl sulfate

    Cholinesterase (ChE) Neurological Disease
    Neostigmine methyl sulfate is a reversible inhibitor of acetylcholinesterase, can not cross the blood-brain barrier.
  • HY-137441
    Icapamespib

    PU-HZ151

    HSP Neurological Disease
    Icapamespib (PU-HZ151) is a potent HSP90 inhibitor with an EC50 of 5 nM. Icapamespib is able to cross blood-brain barrier.
  • HY-122489
    DL-Laudanosine

    Drug Metabolite Neurological Disease
    DL-Laudanosine, an Atracurium and Cisatracurium metabolite, crosses the blood–brain barrier and may cause excitement and seizure activity.
  • HY-12763
    GNE-317

    PI3K mTOR Cancer
    GNE-317 is a PI3K/mTOR inhibitor, is able to cross the blood-brain barrier (BBB).
  • HY-10231
    PX-478

    HIF/HIF Prolyl-Hydroxylase Autophagy Cancer
    PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier.
  • HY-103240
    Methoxy-X04

    Amyloid-β Others
    Methoxy-X04 is a fluorescent dye that crosses the blood-brain barrier and selectively binds to beta-pleated sheets found in dense core amyloid Aβ plaques.
  • HY-W010936
    Nitrobenzylthioinosine

    NBMPR

    Adenosine Receptor Neurological Disease
    Nitrobenzylthioinosine is an ENT1 transporter inhibitor that binds to ENT1 transporter with high affinity. Nitrobenzylthioinosine is a photoaffinity probe for adenosine uptake sites in brain. Nitrobenzylthioinosine can cross the blood-brain barrier.
  • HY-50098
    Mardepodect

    PF-2545920

    Phosphodiesterase (PDE) Neurological Disease
    Mardepodect (PF-2545920) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect can cross the blood-brain barrier.
  • HY-50098A
    Mardepodect hydrochloride

    PF-2545920 hydrochloride

    Phosphodiesterase (PDE) Cancer
    Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect hydrochloride can cross the blood-brain barrier.
  • HY-105077A
    Nemifitide diTFA

    INN 00835 diTFA

    5-HT Receptor Neurological Disease
    Nemifitide diTFA (INN 00835 diTFA) is a synthetic pentapeptide antidepressant with a potential for rapid onset of action. Nemifitide diTFA is a peptide analog of melanocyte-inhibiting factor (MIF). Nemifitide diTFA can cross the blood-brain barrier.
  • HY-101485
    AUTEN-99 hydrobromide

    Autophagy enhancer-99 hydrobromide

    Others Neurological Disease
    AUTEN-99 (hydrobromide) is a novel inhibitor of the myotubularin phosphatase Jumpy (also called MTMR14). AUTEN-99 (hydrobromide) crosses the blood-brain barrier and exerts potent neuroprotective effects.
  • HY-10959
    RG7112

    RO5045337

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC50 of 18 nM and a KD of 11 nM for binding to MDM2.
  • HY-B0309
    Felodipine

    Calcium Channel Autophagy Cardiovascular Disease
    Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
  • HY-B1395S
    Mecamylamine-d3 hydrochloride

    nAChR Neurological Disease
    Mecamylamine-d3 hydrochloride is the deuterium labeled Mecamylamine hydrochloride. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier.
  • HY-B0627
    Metformin

    1,1-Dimethylbiguanide

    AMPK Autophagy Mitophagy Cancer Metabolic Disease Cardiovascular Disease
    Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin can cross the blood-brain barrier and triggers autophagy.
  • HY-100642
    3-O-Methyltolcapone

    Ro 40-7591

    COMT Neurological Disease
    3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease.
  • HY-122015
    ASP2905

    Potassium Channel Neurological Disease
    ASP2905 is a potent and selective potassium channel Kv12.2 inhibitor encoded by the Kcnh3/BEC1 gene. ASP2905 can cross the blood-brain barrier and has antipsychotic activities.
  • HY-N0304
    L-DOPA

    Levodopa; 3,4-Dihydroxyphenylalanine

    Dopamine Receptor Endogenous Metabolite Neurological Disease
    L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease.
  • HY-15615A
    TIC10

    ONC-201

    TNF Receptor Apoptosis Cancer
    TIC10 (ONC-201) is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can cross the blood-brain barrier.
  • HY-10835
    DG-041

    Prostaglandin Receptor Cardiovascular Disease
    DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier.
  • HY-129441
    Metoprine

    BW 197U

    Histone Methyltransferase Antifolate Cancer Neurological Disease
    Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT. Metoprine is an antifolate and antitumor agent.
  • HY-N0304A
    L-DOPA sodium

    Levodopa sodium; 3,4-Dihydroxyphenylalanine sodium

    Dopamine Receptor Endogenous Metabolite Neurological Disease
    L-DOPA (Levodopa) sodium is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA sodium can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA sodium has anti-allodynic effects, and can be used for Parkinson's disease research.
  • HY-B0309S
    Felodipine-d8

    Calcium Channel Autophagy Cardiovascular Disease
    Felodipine-d8 is the deuterium labeled Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
  • HY-B0309S1
    Felodipine-d5

    Calcium Channel Autophagy Cardiovascular Disease
    Felodipine-d5 is deuterium labeled Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
  • HY-B0309S2
    Felodipine-d3

    Calcium Channel Autophagy Cardiovascular Disease
    Felodipine-d3 is the deuterium labeled Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
  • HY-144309
    Cholesterol 24-hydroxylase-IN-1

    Cytochrome P450 Neurological Disease
    Cholesterol 24-hydroxylase-IN-1 (compound 17) is a potent, orally active, and highly selective cholesterol 24-hydroxylase (CH24H or CYP46A1) inhibitor (IC50=8.5 nM). Cholesterol 24-hydroxylase-IN-1 can cross blood-brain barrier.
  • HY-N6608
    Physostigmine

    Eserine

    Cholinesterase (ChE) Neurological Disease
    Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning.
  • HY-120738
    p-MPPI hydrochloride

    5-HT Receptor Neurological Disease
    p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with high affinity for 5-HT1A receptors. p-MPPI hydrochloride can crosses the blood-brain barrier, and has clear antidepressant and anxiolytic-like effects.
  • HY-50682
    Azeliragon

    TTP488; PF-04494700

    Amyloid-β Neurological Disease
    Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression in patients with mild Alzheimer’s disease (AD). Azeliragon also can cross the blood-brain barrier (BBB).
  • HY-17547
    NMS-E973

    HSP Cancer
    NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy.
  • HY-N7109
    Erucic acid

    PI3K Endogenous Metabolite Neurological Disease
    Erucic acid, a monounsaturated fatty acid (MUFA), is isolated from the seed of Raphanus sativus L. Erucic acid can readily cross the blood-brain barrier (BBB), it has been reported to normalize the accumulation of very long-chain fatty acids in the brain. Erucic acid can improve cognitive impairment and be effective against dementia .
  • HY-129411
    Sinbaglustat

    ACT-519276; OGT2378

    Others Metabolic Disease
    Sinbaglustat (OGT2378) is a dual inhibitor of glucosylceramide synthase (GCS) and non-lysosomal glucosyl ceramidase (GBA2). Sinbaglustat is an orally available N-alkyl iminosugar that crosses the blood-brain barrier. Sinbaglustat can be used for the research of central neurodegenerative diseases associated with lysosomal dysfunctions.
  • HY-108448
    N-Oleoyldopamine

    OLDA

    TRP Channel Cardiovascular Disease
    N-Oleoyldopamine (OLDA) is a product of condensation of oleic acid and dopamine (DA) and an endogenous TRPV1 selective agonist. N-Oleoyldopamine (OLDA) can crosses the blood-brain barrier. N-oleoyl-dopamine protects the heart against ischemia-reperfusion injury via activation of TRPV1.
  • HY-10202A
    Tandutinib hydrochloride

    MLN518 hydrochloride; CT53518 hydrochloride

    FLT3 c-Kit PDGFR Apoptosis Cancer
    Tandutinib hydrochloride (MLN518 hydrochloride) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib hydrochloride can be used for acute myelogenous leukemia (AML). Tandutinib hydrochloride has the ability to cross the blood-brain barrier.
  • HY-10202
    Tandutinib

    MLN518; CT53518

    FLT3 c-Kit PDGFR Apoptosis Cancer
    Tandutinib (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib can be used for acute myelogenous leukemia (AML). Tandutinib has the ability to cross the blood-brain barrier.
  • HY-N7062
    JNJ-1661010

    Takeda-25

    FAAH Neurological Disease
    JNJ-1661010 (Takeda-25) a potent and selective fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 34 and 33 nM for rat FAAH and human FAAH, respectively. JNJ-1661010 can cross the blood-brain barrier and used as broad-spectrum analgesics.
  • HY-143264
    FAAH/MAGL-IN-2

    FAAH MAGL Neurological Disease
    FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC50s of 11 nM and 36 nM (Kis of 28 nM and 60 nM), respectively . FAAH/MAGL-IN-2 has the potential to treat neuropathic pain without causing locomotion impairment.
  • HY-B1266
    Physostigmine salicylate

    Eserine salicylate

    Cholinesterase (ChE) Neurological Disease
    Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine salicylate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine salicylate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine salicylate is also an antidote for anticholinergic poisoning.
  • HY-A0230
    Spirapril

    SCH 33844

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Spirapril is a potent and cross the blood-brain barrier angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active prodrug of Spiraprilat and can be used for the research of hypertension, congestive heart failure.
  • HY-109012A
    Seltorexant hydrochloride

    JNJ-42847922 hydrochloride

    Orexin Receptor (OX Receptor) Endocrinology Neurological Disease
    Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
  • HY-132670S
    (R)-(-)-Felodipine-d5

    Calcium Channel Autophagy Cardiovascular Disease
    (R)-(-)-Felodipine-d5 is the deuterium labeled (R)-(-)-Felodipine. (R)-(-)-Felodipine is the S enantiomer of Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
  • HY-76772
    Cevimeline hydrochloride hemihydrate

    SNI-2011; AF102B hydrochloride hemihydrate

    mAChR Neurological Disease
    Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).
  • HY-N2320
    Physostigmine hemisulfate

    Eserine hemisulfate

    Cholinesterase (ChE) Neurological Disease
    Physostigmine hemisulfate (Eserine hemisulfate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine hemisulfate can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine hemisulfate is also an antidote for anticholinergic poisoning.
  • HY-134494
    MS48107

    Others Neurological Disease
    MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice.
  • HY-70020B
    Cevimeline hydrochloride

    AF102B hydrochloride

    mAChR Neurological Disease
    Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride can cross the blood-brain barrier (BBB).
  • HY-12305
    Q-VD-OPh

    QVD-OPH; Quinoline-Val-Asp-Difluorophenoxymethylketone

    Caspase HIV Cancer Infection
    Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPh can inhibits HIV infection. Q-VD-OPh is able to cross the blood-brain barrier.
  • HY-100501
    M2698

    MSC2363318A

    Ribosomal S6 Kinase (RSK) Akt Cancer
    M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.
  • HY-19838
    JNJ-63533054

    GPR139 Neurological Disease
    JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB).
  • HY-13289A
    Nepicastat hydrochloride

    SYN-117 hydrochloride; RS-25560-197 hydrochloride

    Dopamine β-hydroxylase Cardiovascular Disease
    Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB).
  • HY-70020
    Cevimeline

    AF102B

    mAChR Neurological Disease
    Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline can cross the blood-brain barrier (BBB).
  • HY-N0003
    Honokiol

    NSC 293100

    Akt Autophagy HCV ERK Cancer
    Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt. Honokiol can readily cross the blood brain barrier.
  • HY-100642S
    3-O-Methyltolcapone D7

    Ro 40-7591 D7

    COMT Neurological Disease
    3-O-Methyltolcapone D7 (Ro 40-7591 D7) is a deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease.
  • HY-17364
    Temozolomide

    NSC 362856; CCRG 81045; TMZ

    DNA Alkylator/Crosslinker Autophagy Apoptosis Cancer
    Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects.
  • HY-13289
    Nepicastat

    SYN117; RS-25560-197

    Dopamine β-hydroxylase Cardiovascular Disease
    Nepicastat (SYN117) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB).
  • HY-N0304S
    L-DOPA-d6

    Levodopa-d6; 3,4-Dihydroxyphenylalanine-d6

    Dopamine Receptor Endogenous Metabolite Neurological Disease
    L-DOPA-d6 (Levodopa-d6) is the deuterium labeled L-DOPA. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease.
  • HY-109012
    Seltorexant

    JNJ-42847922

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
  • HY-N6608S
    Physostigmine-d3

    Eserine-d3

    Cholinesterase (ChE) Neurological Disease
    Physostigmine-d3 (Eserine-d3) is the deuterium labeled Physostigmine. Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning.
  • HY-132392S
    L-DOPA-2,5,6-d3

    Dopamine Receptor Endogenous Metabolite Neurological Disease
    L-DOPA-2,5,6-d3 (Levodopa-2,5,6-d3) is the deuterium labeled L-DOPA. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain.
  • HY-10974
    MK-0752

    γ-secretase Neurological Disease Cancer
    MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo.
  • HY-130795
    GSK-3β inhibitor 2

    GSK-3 Neurological Disease
    GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.
  • HY-100822
    (R)-(+)-HA-966

    (+)-HA-966

    iGluR Neurological Disease
    (R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine. (R)-(+)-HA-966 can cross the blood-brain barrier and has the potential for neuropathic and acute pain.
  • HY-145845
    HDAC1/MAO-B-IN-1

    HDAC Monoamine Oxidase Neurological Disease
    HDAC1/MAO-B-IN-1 is a potent, selective and cross the blood-brain barrier HDAC1/MAO-B inhibitor with IC50 values of 21.4 nM and 99.0 nM for HDAC1 and MAO-B, respectively. HDAC1/MAO-B-IN-1 has the potential for the research of Alzheimer’s disease.
  • HY-135749
    BN201

    Others Inflammation/Immunology Neurological Disease
    BN201 promotes neuronal differentiation, the differentiation of precursor cells to mature oligodendrocytes (EC50 of 6.3 μM) in vitro, and the myelination of new axons (EC50 of 16.6 μM). BN201 is able to cross the blood-brain barrier by active transport and activate pathways (IGF-1 pathway) associated with the response to stress and neuron survival. BN201 has potently neuroprotective effects.
  • HY-106004
    Zamicastat

    BIA 5-1058

    Dopamine β-hydroxylase P-glycoprotein BCRP Cancer Cardiovascular Disease
    Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively. Zamicastat reduces high blood pressure.
  • HY-100642S1
    3-O-Methyltolcapone-d4

    Ro 40-7591-d4

    COMT Neurological Disease
    3-O-Methyltolcapone-d4 (Ro 40-7591-d4) is the deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease.
  • HY-19918A
    Anatabine dicitrate

    NF-κB Amyloid-β nAChR Inflammation/Immunology Neurological Disease
    Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
  • HY-13821
    Epoxomicin

    BU-4061T

    Proteasome Apoptosis Cancer Inflammation/Immunology
    Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.
  • HY-103441
    JNJ28871063 hydrochloride

    EGFR Cancer
    JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2.
  • HY-70020BS
    Cevimeline-d4 hydrochloride

    AF102B-d4 hydrochloride

    mAChR Neurological Disease
    Cevimeline-d4 (AF102B-d4) hydrochloride is the deuterium labeled Cevimeline hydrochloride. Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride can cross the blood-brain barrier (BBB).
  • HY-101456
    PCPA methyl ester hydrochloride

    4-Chloro-DL-phenylalanine methyl ester hydrochloride

    Tryptophan Hydroxylase 5-HT Receptor Neurological Disease
    PCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride), a reversible tryptophan hydroxylase inhibitor, is a serotonin (5-HT) synthesis inhibitor. PCPA methyl ester hydrochloride crosses the blood brain barrier and reduces 5-HT central availability.
  • HY-16785
    Veledimex

    INXN-1001; RG-115932

    Interleukin Related Cancer Inflammation/Immunology
    Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys.
  • HY-14327
    FAUC 213

    Dopamine Receptor Neurological Disease
    FAUC 213 is an orally active and highly selective dopamine D4 receptor complete antagonist with a Ki of 2.2 nM for hD4.4. FAUC 213 has less activity on D2 and D3 receptors (Kis of 3.4 μM, 5.3 μM for hD2, hD3, respectively). FAUC 213 can cross the blood-brain barrier (BBB). FAUC 213 exhibits atypical antipsychotic characteristic.
  • HY-17364S
    Temozolomide-d3

    DNA Alkylator/Crosslinker Autophagy Apoptosis Cancer
    Temozolomide-d3 (NSC 362856-d3) is the deuterium labeled Temozolomide. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects.
  • HY-15978
    P7C3-A20

    Others Neurological Disease
    P7C3-A20 is a derivative of P7C3 with potent proneurogenic and neuroprotective activity. P7C3-A20 exerts an antidepressant-like effect. P7C3-A20 can cross the blood-brain barrier and therefore has the potential for brain injury treatment.
  • HY-12170
    Prinomastat

    AG3340; KB-R9896

    MMP Apoptosis Cancer
    Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity.
  • HY-12170A
    Prinomastat hydrochloride

    AG3340 hydrochloride; KB-R9896 hydrochloride

    MMP Apoptosis Cancer
    Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity.
  • HY-15196
    TAK-285

    EGFR Cancer
    TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
  • HY-N0303
    Idebenone

    Mitochondrial Metabolism Apoptosis Neurological Disease
    Idebenone, a well-appreciated mitochondrial protectant, exhibits protective efficacy against neurotoxicity and can be used for the research of Alzheimer's disease, Huntington's disease. Idebenone (oxidised form) has a dose-dependent inhibitory effect on the enzymatic metabolism of arachidonic acid in astroglial homogenates (IC50=16.65 μM). Idebenone, a coenzyme Q10 analog and an antioxidant, induces apoptotic cell death in the human dopaminergic neuroblastoma SHSY-5Y cells. Idebenone quickly crosses the blood-brain barrier.
  • HY-115475
    SW-100

    HDAC Neurological Disease
    SW-100, a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 2.3 nM, shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. SW-100 displays a significantly improved ability to cross the blood-brain-barrier.
  • HY-137499
    NT1-O12B

    Endogenous Metabolite Neurological Disease
    NT1-O12B, an endogenous chemical and a neurotransmitter-derived lipidoid (NT-lipidoid), is an effective carrier for enhanced brain delivery of several blood-brain barrier (BBB)-impermeable cargos. Doping NT1-O12B into BBB-impermeable lipid nanoparticles (LNPs) gives the LNPs the ability to cross the BBB. NT-lipidoids formulation not only facilitate cargo crossing of the BBB, but also delivery of the cargo into neuronal cells for functional gene silencing or gene recombination.
  • HY-131350
    LXE408

    Proteasome Parasite Infection
    LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 has a low propensity to cross the blood brain barrier. LXE408 has the potential for visceral leishmaniasis (VL) research.
  • HY-128861A
    ACT001

    PAI-1 STAT PI3K Akt Apoptosis Cancer Inflammation/Immunology
    ACT001 is an orally active PAI-1 inhibitor by inhibiting the phosphorylation of PI3K and AKT. ACT001 inhibits the phosphorylation of STAT3 and PD-L1 expression by directly binding to STAT3. ACT001, a fumarate salt form of DMAMCL (a prodrug of Micheliolide), can cross the blood-brain barrier. ACT001 exerts synergistic effects in combination with Cisplatin (HY-17394) by inhibiting PI3K/AKT pathway in glioma. ACT001 has potent anti-glioblastoma (GBM) activity and immunomodulatory effects.
  • HY-124619
    GPI-1046

    FKBP HIV Infection Neurological Disease
    GPI-1046 is a immunophilin ligand without antibiotic action and attenuates ethanol intake in part through the upregulation of glutamate transporter 1 (GLT1) in PFC and NAc-core. GPI-1046 is an analog of FK506, which is an immunophilin ligand that has been shown neuroprotective effects in neurodegenerative disease models. GPI-1046 readily crosses the blood-brain barrier and promotes the regeneration of dopamine (DA) cells in the CNS in association with functional recovery in rodent models. GPI-1046 improves HIV-associated injury of peripheral nerves.
  • HY-132246
    WWL123

    MAGL Neurological Disease
    WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM. WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice.
  • HY-123960
    Raphin1

    Phosphatase Neurological Disease
    Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease.
  • HY-123960A
    Raphin1 acetate

    Phosphatase Neurological Disease
    Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease.
  • HY-N0148
    Rutin

    Rutoside; Quercetin 3-O-rutinoside

    Amyloid-β Autophagy Inflammation/Immunology Cancer
    Rutin (Rutoside) is a flavonoid found in many plants and shows a wide range of biological activities including anti-inflammatory, antidiabetic, antioxidant, neuroprotective, nephroprotective, hepatoprotective and reducing Aβ oligomer activities. Rutin can cross the blood brain barrier. Rutin attenuates vancomycin-induced renal tubular cell apoptosis via suppression of apoptosis, mitochondrial dysfunction, and oxidative stress.
  • HY-125374
    Larotaxel

    XRP9881

    Apoptosis Cancer
    Larotaxel (XRP9881) is a taxane analogue with preclinical activity against taxane-resistant breast cancer. Larotaxel (XRP9881) exerts its cytotoxic effect by promoting tubulin assembly and stabilizing microtubules, ultimately leading to cell death by apoptosis. It presents the ability to cross the blood brain barrier and has a much lower affinity for P-glycoprotein 1 than Docetaxel.
  • HY-N0148A
    Rutin hydrate

    Rutoside hydrate; Quercetin 3-O-rutinoside hydrate

    Amyloid-β Autophagy Endogenous Metabolite Cancer Neurological Disease
    Rutin (Rutoside) hydrate is a flavonoid found in many plants and shows a wide range of biological activities including anti-inflammatory, antidiabetic, antioxidant, neuroprotective, nephroprotective, hepatoprotective and reducing Aβ oligomer activities. Rutin hydrate can cross the blood brain barrier. Rutin hydrate attenuates vancomycin-induced renal tubular cell apoptosis via suppression of apoptosis, mitochondrial dysfunction, and oxidative stress.
  • HY-117709
    BRD6688

    HDAC Neurological Disease
    BRD6688 is a selective HDAC2 inhibitor. BRD6688 increases H4K12 and H3K9 histone acetylation in primary mouse neuronal cells. BRD6688 crosses the blood brain barrier and rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model.
  • HY-111373
    RapaLink-1

    mTOR Autophagy Cancer
    RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity.
  • HY-102064
    SR 57227A

    5-HT Receptor Neurological Disease
    SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
  • HY-124569
    NAB-14

    iGluR Neurological Disease
    NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier.