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brain penetrating

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53

Inhibitors & Agonists

6

Peptides

1

Inhibitory Antibodies

4

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-14533
    K 01-162

    K162

    		 Amyloid-β Neurological Disease
    K 01-162 (K162) inhibits the fibril formation of Aβ peptides and eliminates their neurotoxicity. K 01-162 binds with Aβ42 peptide with an EC50 value of 80 nM. K 01-162 binds directly to AβO with a KD value of 19 μM. K 01-162 is capable of penetrating the brain and can be used for the research of Alzheimer’s disease .
    K 01-162
  • HY-P0285
    Rabies Virus Glycoprotein
    1 Publications Verification

    		 RABV Infection
    Rabies Virus Glycoprotein is a 29-amino-acid cell penetrating peptide derived from a rabies virus glycoprotein that can cross the blood-brain barrier (BBB) and enter brain cells.
    Rabies Virus Glycoprotein
  • HY-P0285A
    Rabies Virus Glycoprotein TFA
    1 Publications Verification

    		 RABV Infection
    Rabies Virus Glycoprotein (TFA) is a 29-amino-acid cell penetrating peptide derived from a rabies virus glycoprotein that can cross the blood-brain barrier (BBB) and enter brain cells .
    Rabies Virus Glycoprotein TFA
  • HY-109058
    Firibastat
    1 Publications Verification

    QGC001; RB150

    		 Aminopeptidase Cardiovascular Disease
    Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats .
    Firibastat
  • HY-100740
    Lanabecestat

    AZD3293; LY3314814

    		 Beta-secretase Neurological Disease
    Lanabecestat (AZD3293) is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Lanabecestat is used for the research of Alzheimer's disease .
    Lanabecestat
  • HY-112305
    AZ32

    		ATM/ATR Cancer
    AZ32 is an orally bioavailable and blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for ATM enzyme, and an IC50 of 0.31 μM for ATM in cell.
    AZ32
  • HY-105235A
    Enadoline hydrochloride

    CI-977 hydrochloride

    		 Opioid Receptor Neurological Disease
    Enadoline (CI-977) hydrochloride is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
    Enadoline hydrochloride
  • HY-105235
    Enadoline

    CI-977

    		 Opioid Receptor Neurological Disease
    Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (Ki=1.25 nM). Antinociceptive effects .
    Enadoline
  • HY-N12038
    Coumarinic acid

    		Amyloid-β Cholinesterase (ChE) Neurological Disease
    Coumarinic acid is a brain-penetrating inhibitor of AChE and β-amyloid. Coumarinic acid can be used in study anti-Alzheimer drug .
    Coumarinic acid
  • HY-125087
    A-304121

    		Histamine Receptor Neurological Disease
    A-304121 is a selective and brain penetrating H3 receptor antagonist. A-304121 is a cognition-enhancing agent .
    A-304121
  • HY-153964
    PF-06478939

    		Oxytocin Receptor Cardiovascular Disease
    PF-06478939 is a non-brain-penetrating peptide that is an agonist at oxytocin (OT) receptor and vasopressin receptor with EC50 values of 0.01 nM and 0.078 nM, respectively .
    PF-06478939
  • HY-100740B
    Lanabecestat camsylate

    LY3314814 camsylate; AZD3293 camsylate

    		 Beta-secretase Neurological Disease
    Lanabecestat camsylate is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Lanabecestat camsylate is used for the research of Alzheimer's disease .
    Lanabecestat camsylate
  • HY-153964A
    PF-06478939 TFA

    		Oxytocin Receptor Cardiovascular Disease
    PF-06478939 TFA is a non-brain-penetrating peptide that is an agonist at oxytocin (OT) receptor and vasopressin receptor with EC50 values of 0.01 nM and 0.078 nM, respectively .
    PF-06478939 TFA
  • HY-111409
    RIP1 kinase inhibitor 1

    		RIP kinase Inflammation/Immunology
    RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pKi=9.04) .
    RIP1 kinase inhibitor 1
  • HY-120710
    DNS-8254

    		Phosphodiesterase (PDE) Neurological Disease
    DNS-8254 is an oral active and brain-penetrating PDE2a inhibitor with the IC50 of 8 nM. DNS-8254 shows memory enhancing effects in a rat model .
    DNS-8254
  • HY-112723
    Apinocaltamide

    ACT-709478

    		 Calcium Channel Neurological Disease
    Apinocaltamide (ACT-709478) is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies .
    Apinocaltamide
  • HY-125287
    (Rac)-Minzasolmin

    (Rac)-UCB0599; NPT200-11

    		 α-synuclein Neurological Disease
    (Rac)-Minzasolmin ((Rac)-UCB0599) is a brain penetrating inhibitor of accumulation of alpha-synuclein (ASYN) misfolding and aggregation. (Rac)-Minzasolmin can be used for research of Parkinson's disease .
    (Rac)-Minzasolmin
  • HY-161571
    LRRK2-IN-13

    		LRRK2 Neurological Disease
    LRRK2-IN-13 (Compound 13) is an inhibitor of LRRK2 (IC50=0.57 nM). LRRK2-IN-13 has brain penetrating properties .
    LRRK2-IN-13
  • HY-151797
    Ph-HTBA

    		CaMK Neurological Disease
    Ph-HTBA is a high-affinity, brain-penetrating modulator for CaMKIIα. Ph-HTBA has binding affinity for CaMKIIα with a Kd value of 757 nM. Ph-HTBA can be used for the research of ischemia and neurodegenerative disorders .
    Ph-HTBA
  • HY-14880A
    Bavisant dihydrochloride

    JNJ-31001074 dihydrochloride

    		 Histamine Receptor Neurological Disease Endocrinology
    Bavisant (JNJ-31001074) dihydrochloride is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant dihydrochloride can be used for attention-deficit hyperactivity disorder (ADHD) research .
    Bavisant dihydrochloride
  • HY-14880B
    Bavisant dihydrochloride hydrate

    JNJ31001074AAC; JNJ31001074 dihydrochloride hydrate

    		 Histamine Receptor Neurological Disease Endocrinology
    Bavisant dihydrochloride hydrate (JNJ31001074AAC) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant dihydrochloride hydrate can be used for attention-deficit hyperactivity disorder (ADHD) research .
    Bavisant dihydrochloride hydrate
  • HY-14880
    Bavisant

    JNJ-31001074

    		 Histamine Receptor Neurological Disease Endocrinology
    Bavisant (JNJ-31001074) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant can be used for attention-deficit hyperactivity disorder (ADHD) research .
    Bavisant
  • HY-11030
    SNT-207858

    		Melanocortin Receptor Metabolic Disease Endocrinology Cancer
    SNT207858 is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor .
    SNT-207858
  • HY-100740R
    Lanabecestat (Standard)

    AZD3293 (Standard); LY3314814 (Standard)

    		 Reference Standards Beta-secretase Neurological Disease
    Lanabecestat (Standard) is the analytical standard of Lanabecestat. This product is intended for research and analytical applications. Lanabecestat (AZD3293) is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Lanabecestat is used for the research of Alzheimer's disease .
    Lanabecestat (Standard)
  • HY-P99530
    Valanafusp alfa

    AGT-181; HIRMAb-IDUA

    		 Insulin Receptor Metabolic Disease
    Valanafusp alfa (AGT-181) is a chimeric monoclonal antibody that fuses human α-L-iduronidase (IDUA) and targets the human insulin receptor (HIR). Valanafusp alfa has brain penetrating properties, making it useful for research on mucopolysaccharidosis type I (MPS I) .
    Valanafusp alfa
  • HY-111791
    ACY-1083
    1 Publications Verification

    		 HDAC Cancer
    ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy .
    ACY-1083
  • HY-P4073
    ANG1005

    GRN1005; Paclitaxel trevatide

    		 Peptide-Drug Conjugates (PDCs) LDLR Cancer
    ANG1005 (Paclitaxel trevatide) is a brain-penetrating peptide-drug conjugate. ANG1005, a taxane derivative, consists of three paclitaxel (HY-B0015) molecules covalently linked to Angiopep-2, designed to cross the blood-brain and blood-cerebrospinal barriers and to penetrate malignant cells via low density lipoprotein receptor-related protein (LRP1) transport system .
    ANG1005
  • HY-11030A
    SNT-207858 free base

    		Melanocortin Receptor Metabolic Disease Endocrinology Cancer
    SNT207858 free base is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 free base has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor .
    SNT-207858 free base
  • HY-103200
    SR59230A hydrochloride
    Maximum Cited Publications
    11 Publications Verification

    		 Adrenergic Receptor Cardiovascular Disease Metabolic Disease
    SR59230A hydrochloride is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively .
    SR59230A hydrochloride
  • HY-100672
    SR59230A
    Maximum Cited Publications
    11 Publications Verification

    		 Adrenergic Receptor Cardiovascular Disease Metabolic Disease
    SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively .
    SR59230A
  • HY-W016420
    Fosfomycin sodium
    5+ Cited Publications

    MK-0955 sodium

    		 Bacterial Antibiotic Infection Cancer
    Fosfomycin (MK-0955) sodium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin sodium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
    Fosfomycin sodium
  • HY-100740C
    (1α,1'S,4β)-Lanabecestat

    (1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814

    		 Beta-secretase Neurological Disease
    (1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat. Lanabecestat is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM .
    (1α,1'S,4β)-Lanabecestat
  • HY-148236
    BAY-390

    		TRP Channel Inflammation/Immunology
    BAY-390 is a selective, across species active and brain penetrating TRPA1 inhibitor. BAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC50s of 16, 82, 63 and 35 nM, respectively. BAY-390 can be used for the research of inflammation .
    BAY-390
  • HY-B1075A
    Fosfomycin

    MK-0955

    		 Bacterial Antibiotic Infection Cancer
    Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
    Fosfomycin
  • HY-163565
    BIIB129

    		Btk Neurological Disease
    BIIB129 is a covalent, selective, small molecule inhibitor of Bruton's tyrosine kinase (BTK) capable of penetrating the blood-brain barrier. BIIB129 inhibits the activity of BTK by covalently binding to Cys481 in BTK, thereby affecting the function of B cells and myeloid cells. BIIB129 can be used in multiple sclerosis (MS) research .
    BIIB129
  • HY-137440B
    (2R,3R)-Firazorexton

    (2R,3R)-TAK-994 free base

    		 Orexin Receptor (OX Receptor) Neurological Disease
    (2R,3R)-Firazorexton ((2R,3R)-TAK-994 free base) is an isomer of Firazorexton (HY-137440). Firazorexton is an orally active, brain-penetrating orexin type 2 receptor (OX2R) agonist that may improve narcolepsy-like symptoms ..
    (2R,3R)-Firazorexton
  • HY-B1075
    Fosfomycin calcium
    5+ Cited Publications

    MK-​0955 calcium

    		 Bacterial Antibiotic Infection Cancer
    Fosfomycin (MK-0955) calcium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin calcium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
    Fosfomycin calcium
  • HY-B0609
    Fosfomycin tromethamine
    5+ Cited Publications

    MK-0955 tromethamine

    		 Bacterial Antibiotic Infection Cancer
    Fosfomycin (MK-0955) tromethamine is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin tromethamine shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
    Fosfomycin tromethamine
  • HY-19917
    JNJ-39220675

    		Histamine Receptor Neurological Disease
    JNJ-39220675 is a selective and brain-penetrating histamine H3 receptor antagonist with activity in regulating alcohol stimulation and reward. JNJ-39220675 is effective in reducing alcohol intake and preference in alcohol-preferring rats. JNJ-39220675 does not affect the ataxic effects of alcohol, the rate of alcohol elimination, or alcohol-induced nucleocapsid dopamine release .
    JNJ-39220675
  • HY-160019
    MTX115325

    		Deubiquitinase Mitophagy Neurological Disease
    MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine .
    MTX115325
  • HY-169951
    Lu AF90103

    		iGluR Neurological Disease
    Lu AF90103 (Compound 42e) is a methyl ester prodrug of compound 42d capable of penetrating the blood-brain barrier. Compound 42d acts as a partial agonist of the GluN1/GluN2B complex, exhibiting 24% efficacy, and has an EC50 value of 78 nM. Lu AF90103 plays an important role in neuropsychiatric diseases research .
    Lu AF90103
  • HY-14790
    Esreboxetine

    (S,S)-Reboxetine

    		 Adrenergic Receptor Neurological Disease
    Esreboxetine ((S,S)-Reboxetine) is a selective norepinephrine reuptake inhibitor with activity in increasing urethral resistance. Esreboxetine has been reported to be effective in patients with stress urinary incontinence in a Phase IIa clinical study, achieving this effect by increasing urethral closure. The mechanism of action of esreboxetine involves inhibition of norepinephrine transporters in the central and peripheral nervous systems. The peripheral selectivity of esreboxetine helps it significantly increase urethral resistance without penetrating the brain .
    Esreboxetine
  • HY-17402
    Nisoldipine
    1 Publications Verification

    BAY-k 5552

    		 Calcium Channel Reactive Oxygen Species (ROS) Infection Cardiovascular Disease Neurological Disease
    Nisoldipine (BAY-k 5552; Sular) is an orally active and blood-brain barrier-penetrating dihydropyridine calcium antagonist, with greater vascular selectivity than other calcium channel antagonists. Nisoldipine inhibits calcium influx and blocks voltage-gated calcium channels. Nisoldipine dilates coronary and systemic arteries. Nisoldipine has antihypertensive and anti-anginal activity. Nisoldipine also displays neuroprotective and antiviral activity .
    Nisoldipine
  • HY-100672B
    (2R)-SR59230A

    		Adrenergic Receptor Cardiovascular Disease Metabolic Disease
    (2R)-SR59230A is the isomer of SR59230A (HY-100672), and can be used as an experimental control. SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively .
    (2R)-SR59230A
  • HY-B1075AS
    (Rac)-Fosfomycin (benzylamine)-13C3

    MK-0955 (benzylamine)-13C3

    		 Bacterial Antibiotic Infection
    (Rac)-Fosfomycin (benzylamine)- 13C3 is the 13C labeled Fosfomycin . Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
    (Rac)-Fosfomycin (benzylamine)-13C3
  • HY-B1075R
    Fosfomycin (calcium) (Standard)

    		Bacterial Antibiotic Infection Cancer
    Fosfomycin (calcium) (Standard) is the analytical standard of Fosfomycin (calcium). This product is intended for research and analytical applications. Fosfomycin (MK-0955) calcium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin calcium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
    Fosfomycin (calcium) (Standard)
  • HY-P2048
    MOTS-c (human)

    		Apoptosis GLUT AMPK Neurological Disease Metabolic Disease Inflammation/Immunology Endocrinology
    MOTS-c (human) is a blood-brain barrier-penetrating, mitochondrial-derived peptide that modulates the AMPK/PGC-1α pathway to enhance insulin sensitivity. MOTS-c (human) inhibits the folate cycle and de novo purine synthesis, increases AICAR levels to activate AMPK, and then regulates the Nrf2/Keap1 antioxidant pathway and inhibits the NF-κB inflammatory pathway, while promoting mitochondrial biogenesis and energy metabolism. MOTS-c (human) has the effects of improving glucose and lipid metabolism, anti-oxidative stress, anti-inflammatory and neuroprotection, and can be used in the study of type 2 diabetes, traumatic brain injury, inflammatory diseases and aging-related metabolic disorders .
    MOTS-c (human)
  • HY-P2048A
    MOTS-c(human) acetate

    		AMPK GLUT Neurological Disease Metabolic Disease Inflammation/Immunology Endocrinology
    MOTS-c (human) acetate is a blood-brain barrier-penetrating, mitochondrial-derived peptide that modulates the AMPK/PGC-1α pathway to enhance insulin sensitivity. MOTS-c (human) acetate inhibits the folate cycle and de novo purine synthesis, increases AICAR levels to activate AMPK, and then regulates the Nrf2/Keap1 antioxidant pathway and inhibits the NF-κB inflammatory pathway, while promoting mitochondrial biogenesis and energy metabolism. MOTS-c (human) acetate has the effects of improving glucose and lipid metabolism, anti-oxidative stress, anti-inflammatory and neuroprotection, and can be used in the study of type 2 diabetes, traumatic brain injury, inflammatory diseases and aging-related metabolic disorders .
    MOTS-c(human) acetate
  • HY-B0311D
    Carbidopa hydrochloride

    (S)-(-)-Carbidopa hydrochloride

    		 Aryl Hydrocarbon Receptor Cancer
    Carbidopa hydrochloride ((S)-(-)-Carbidopa hydrochloride) is a drug used to inhibit Parkinson's disease, which has the activity of inhibiting the peripheral metabolism of levodopa. Carbidopa hydrochloride can increase the proportion of peripheral levodopa penetrating the blood-brain barrier, thereby enhancing its effect on the central nervous system. Carbidopa hydrochloride has also been found to be an aryl hydrocarbon receptor (AhR) ligand with anticancer activity, which can inhibit the growth of pancreatic cancer cells and tumors. The selective AhR regulation properties of carbidopa hydrochloride provide potential prospects for its clinical application .
    Carbidopa hydrochloride
  • HY-138110
    Toladryl

    4-Methyldiphenhydramine

    		 Endogenous Metabolite iGluR Histamine Receptor Neurological Disease Inflammation/Immunology
    Toladryl is a derivative of Diphenhydramine (HY-B0303), capable of penetrating the blood-brain barrier and possessing oral activity, as well as antihistamine and anticholinergic activities. The anticholinergic activity of Toladryl is approximately one-tenth that of Diphenhydramine (HY-B0303), and its protective effect against lethal doses of histamine in guinea pigs is 2 to 4 times that of Diphenhydramine (HY-B0303). The side effects of Toladryl are fewer and milder than those of Diphenhydramine (HY-B0303), but at higher doses, it may cause central nervous system symptoms such as insomnia, agitation, and disorientation. Toladryl can be used for research in allergic diseases .
    Toladryl

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