Search Result

Results for "

brain penetrating

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (4) Adrenergic Receptor (6) Aminopeptidase (2) AMPK (2) Amyloid-β (1) Antibiotic (6) Apoptosis (3) Aryl Hydrocarbon Receptor (2) ATM/ATR (1) Autophagy (2) Bacterial (6) Beta-secretase (5) Btk (2) Calcium Channel (2) CaMK (2) Caspase (1) COX (1) Cytochrome P450 (1) Deubiquitinase (1) EGFR (1) Endogenous Metabolite (3) ERK (1) Fc Receptor (FcR) (1) Ferroptosis (1) GLUT (2) HDAC (1) Histamine Receptor (7) iGluR (3) Insecticide (1) Insulin Receptor (2) Keap1-Nrf2 (1) LDLR (1) LRRK2 (1) MEK (1) Melanocortin Receptor (3) Mitophagy (1) NF-κB (1) NO Synthase (1) Opioid Receptor (2) Orexin Receptor (OX Receptor) (1) Oxytocin Receptor (2) p38 MAPK (2) Peptide-Drug Conjugates (PDCs) (1) Phosphodiesterase (PDE) (1) RABV (2) Raf (1) RANKL/RANK (1) Reactive Oxygen Species (ROS) (2) Reference Standards (10) RIP kinase (1) Src (1) STAT (1) Survivin (1) Tau Protein (3) Topoisomerase (2) TRP Channel (1) UGT (1) Virus Protease (1) α-synuclein (1)
By Research Areas:	Cancer (17) Cardiovascular Disease (11) Endocrinology (6) Infection (12) Inflammation/Immunology (9) Metabolic Disease (16) Neurological Disease (39)

By Targets:

5-HT Receptor (4)

Adrenergic Receptor (6)

Aminopeptidase (2)

AMPK (2)

Amyloid-β (1)

Antibiotic (6)

Apoptosis (3)

Aryl Hydrocarbon Receptor (2)

ATM/ATR (1)

Autophagy (2)

Bacterial (6)

Beta-secretase (5)

Btk (2)

Calcium Channel (2)

CaMK (2)

Caspase (1)

COX (1)

Cytochrome P450 (1)

Deubiquitinase (1)

EGFR (1)

Endogenous Metabolite (3)

ERK (1)

Fc Receptor (FcR) (1)

Ferroptosis (1)

GLUT (2)

HDAC (1)

Histamine Receptor (7)

iGluR (3)

Insecticide (1)

Insulin Receptor (2)

Keap1-Nrf2 (1)

LDLR (1)

LRRK2 (1)

MEK (1)

Melanocortin Receptor (3)

Mitophagy (1)

NF-κB (1)

NO Synthase (1)

Opioid Receptor (2)

Orexin Receptor (OX Receptor) (1)

Oxytocin Receptor (2)

p38 MAPK (2)

Peptide-Drug Conjugates (PDCs) (1)

Phosphodiesterase (PDE) (1)

RABV (2)

Raf (1)

RANKL/RANK (1)

Reactive Oxygen Species (ROS) (2)

Reference Standards (10)

RIP kinase (1)

Src (1)

STAT (1)

Survivin (1)

Tau Protein (3)

Topoisomerase (2)

TRP Channel (1)

UGT (1)

Virus Protease (1)

α-synuclein (1)

By Research Areas:

Cancer (17)

Cardiovascular Disease (11)

Endocrinology (6)

Infection (12)

Inflammation/Immunology (9)

Metabolic Disease (16)

Neurological Disease (39)

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B2132

Tryptamine 1 Publications Verification 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine	Endogenous Metabolite 5-HT Receptor Aryl Hydrocarbon Receptor	Neurological Disease Metabolic Disease
Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models .

HY-100740

Lanabecestat 2 Publications Verification AZD3293; LY3314814	Beta-secretase	Neurological Disease
Lanabecestat (AZD3293; LY3314814) is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a K_i of 0.4 nM. Lanabecestat is used for the research of Alzheimer's disease .

HY-W016420

Fosfomycin sodium Maximum Cited Publications 14 Publications Verification 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 .

HY-100672

SR59230A 10+ Cited Publications	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 .

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 .

HY-17402

Nisoldipine 2 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 .

HY-P2048

MOTS-c (human) 1 Publications Verification	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 .

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 .

HY-B1075

Fosfomycin calcium Maximum Cited Publications 14 Publications Verification 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 .

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 .

HY-103200

SR59230A hydrochloride 10+ Cited Publications	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 .

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 .

HY-N0762

Isobavachin 5 Publications Verification	Cytochrome P450 UGT p38 MAPK NF-κB NO Synthase COX Fc Receptor (FcR) RANKL/RANK Keap1-Nrf2 Reactive Oxygen Species (ROS) Apoptosis Autophagy	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Isobavachin is an orally active, blood-brain barrier-penetrating prenylated flavonoid present in Psoralea corylifolia. Isobavachin inhibits human CYP2B6, CYP2C9, CYP2C19, UGT1A1, UGT1A9, and UGT2B7. Isobavachin suppresses MAPK activation, NF-κB nuclear translocation, overexpression of iNOS/COX-2, FcεRI-mediated signaling pathways, and RANKL-induced osteoclastogenesis. Isobavachin induces autophagy, cytotoxicity, neuronal differentiation, and NRF2 activation; it alleviates oxidative damage, inflammatory responses, apoptosis, iron accumulation, mitochondrial biogenesis, and mast cell degranulation. Isobavachin is applicable to research related to liver injury, inflammatory diseases, osteoporosis, liver cancer, prostate cancer, glioma, periodontitis-induced bone loss, and Alzheimer's disease .

HY-14880

Bavisant JNJ-31001074	Histamine Receptor	Neurological Disease Metabolic Disease
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 .

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 .

HY-B0609

Fosfomycin tromethamine Maximum Cited Publications 14 Publications Verification 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 .

HY-109058

Firibastat 1 Publications Verification QGC001; RB150	Aminopeptidase	Cardiovascular Disease Neurological Disease
Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (K_i=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats .

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.

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 .

HY-P2048A

MOTS-c(human) acetate 1 Publications Verification	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 .

HY-P10861A

RI-AG03 acetate	Tau Protein	Neurological Disease
RI-AG03 acetate is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. RI-AG03 acetate inhibits tau aggregation and promotes the formation of alternative amorphous aggregates that are non-amyloidogenic. RI-AG03 acetate mediates cellular uptake through direct membrane penetration and macropinocytosis, and its conjugation with cell-penetrating peptide sequences (CPPs) enhances the binding of cells to liposomes. RI-AG03 acetate suppresses aggregation-dependent neurodegenerative and behavioral phenotypes, and extends the lifespan of Drosophila models of tauopathy. RI-AG03 acetate can be used for research on tau-related diseases such as Alzheimer's disease .

HY-160167

Birelentinib DZD8586	Src Btk	Inflammation/Immunology Cancer
Birelentinib (DZD8586) is an orally effective, selective, non-covalent inhibitor targeting LYN tyrosine kinase and BTK tyrosine kinase, capable of penetrating the blood-brain barrier. Birelentinib exhibits concentration-dependent antiproliferative effects in RI-1 cells and diffuse large B-cell lymphoma (DLBCL) cell lines carrying BTK resistance mutations (such as C481X, V416L, etc.). Birelentinib blocks both BTK-dependent and independent signaling of the B-cell receptor (BCR), thereby inhibiting tumor cell proliferation and inducing cell death. Birelentinib can be used in research to overcome resistance to existing covalent and non-covalent BTK inhibitors in B-cell non-Hodgkin lymphoma (B-NHL) .

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.

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 (pK_i=9.04) .

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 .

HY-109118A

Masupirdine mesylate SUVN-502 mesylate	5-HT Receptor	Neurological Disease
Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally active, and brain-penetrating 5-HT₆ receptor antagonist (K_i of 2.04 nM for human 5-HT₆ receptor). Masupirdine mesylate has pro-cognitive effects on all stages of cognition (acquisition, consolidation, and retention), and can reverse Scopolamine (HY-N0296), MK-801 (HY-15084B)-induced and aging-related memory deficits. Masupirdine mesylate can be used in the research of Alzheimer's disease .

HY-100777

DACA	Topoisomerase	Neurological Disease Cancer
DACA (XR 5000) is a potential and blood-brain barrier-penetrating topoisomerase I and II inhibitor. DACA can be used in the research of colorectal cancer, leukemia and lung cancer .

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) .

HY-148236

BAY-390 1 Publications Verification	TRP Channel	Inflammation/Immunology
BAY-390, a chemical probe, 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 .

HY-P10861

RI-AG03	Tau Protein	Neurological Disease
RI-AG03 is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. RI-AG03 inhibits tau aggregation and promotes the formation of alternative amorphous aggregates that are non-amyloidogenic. RI-AG03 mediates cellular uptake through direct membrane penetration and macropinocytosis, and its conjugation with cell-penetrating peptide sequences (CPPs) enhances the binding of cells to liposomes. RI-AG03 suppresses aggregation-dependent neurodegenerative and behavioral phenotypes, and extends the lifespan of Drosophila models of tauopathy. RI-AG03 can be used for research on tau-related diseases such as Alzheimer's disease .

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 .

HY-14880B

Bavisant dihydrochloride hydrate JNJ31001074AAC; JNJ31001074 dihydrochloride hydrate	Histamine Receptor	Neurological Disease Metabolic Disease
Bavisant (JNJ31001074AAC) dihydrochloride hydrate 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 .

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 .

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 .

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 (K_i=1.25 nM). Antinociceptive effects .

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 K_d value of 757 nM. Ph-HTBA can be used for the research of ischemia and neurodegenerative disorders .

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 .

HY-10623

PF-00446687 hydrochloride	Melanocortin Receptor	Endocrinology
PF-00446687 hydrochloride is a potent, brain-penetrating, selective melanocortin 4 receptor (MC4R) agonist with an EC₅₀ of 12 nM. PF-00446687 hydrochloride can be used in the research of sexual dysfunction .

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 ..

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 .

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 .

HY-179008

5-HT2CR agonist 2	5-HT Receptor	Neurological Disease
5-HT2CR agonist 2 (Compound 16k) is a selective, blood-brain barrier-penetrating and Gq-biased 5-HT_2CR agonist, with an EC₅₀ of 36 nM. 5-HT2CR agonist 2 attenuates MK801 (HY-15084B)-induced hyperlocomotion and reverses Phencyclidine-induced hyperlocomotor activity .

HY-B1075R

Fosfomycin calcium (Standard) MK-0955 calcium (Standard)	Reference Standards 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 .

HY-109118

Masupirdine free base SUVN-502 free base	5-HT Receptor	Neurological Disease
Masupirdine free base (SUVN-502 free base) is a potent, selective, orally active, and brain-penetrating 5-HT₆ receptor antagonist (K_i of 2.04 nM for human 5-HT₆ receptor). Masupirdine free base has pro-cognitive effects on all stages of cognition (acquisition, consolidation, and retention), and can reverse Scopolamine (HY-N0296), MK-801 (HY-15084B)-induced and aging-related memory deficits. Masupirdine free base can be used in the research of Alzheimer's disease .

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 (K_i=1.25 nM). Antinociceptive effects .

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 .

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 .

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 .

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 .

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 .

Cat. No.	Product Name	Target	Research Area

HY-P2048

MOTS-c (human) 1 Publications Verification	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 .

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 .

HY-P2048A

MOTS-c(human) acetate 1 Publications Verification	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 .

HY-P10861A

RI-AG03 acetate	Tau Protein	Neurological Disease
RI-AG03 acetate is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. RI-AG03 acetate inhibits tau aggregation and promotes the formation of alternative amorphous aggregates that are non-amyloidogenic. RI-AG03 acetate mediates cellular uptake through direct membrane penetration and macropinocytosis, and its conjugation with cell-penetrating peptide sequences (CPPs) enhances the binding of cells to liposomes. RI-AG03 acetate suppresses aggregation-dependent neurodegenerative and behavioral phenotypes, and extends the lifespan of Drosophila models of tauopathy. RI-AG03 acetate can be used for research on tau-related diseases such as Alzheimer's disease .

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.

HY-P10153

gH625	Peptides	Others
gH625 is a cell-penetrating viral peptide which is a part of glycoprotein H of Herpes simplex virus type I. gH625 is able to cross the cell membrane and to transport many conjugated cargoes into the cytosol. gH625 is permeable to the blood-brain barrier (BBB) and can enter the rat brain in vivo without toxic effects. gH625 can be used for siRNA delivery research .

HY-P4098

SynB1	Peptides	Infection Neurological Disease Cancer
SynB1 is a cell-penetrating peptide with blood-brain barrier permeability, derived from the antimicrobial peptide Protegrin 1. SynB1 enhances the cellular uptake efficiency and cytoplasmic localization level of conjugated constructs. SynB1 can be used in studies related to rabies and glioblastoma .

HY-P10861

RI-AG03	Tau Protein	Neurological Disease
RI-AG03 is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. RI-AG03 inhibits tau aggregation and promotes the formation of alternative amorphous aggregates that are non-amyloidogenic. RI-AG03 mediates cellular uptake through direct membrane penetration and macropinocytosis, and its conjugation with cell-penetrating peptide sequences (CPPs) enhances the binding of cells to liposomes. RI-AG03 suppresses aggregation-dependent neurodegenerative and behavioral phenotypes, and extends the lifespan of Drosophila models of tauopathy. RI-AG03 can be used for research on tau-related diseases such as Alzheimer's disease .

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 .

Cat. No.	Product Name	Target	Research Area	Image

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) .

HY-P992048

AGT-182 HIRMab; SHP-631; TAK-531	Insulin Receptor	Metabolic Disease
AGT-182 (HIRMab; SHP-631; TAK-531) is a brain-penetrating anti-human insulin receptor antibody and iduronate-2-sulfatase conjugation. AGT-182 can be used for the research of mucopolysaccharidosis type II (MPS II, Hunter syndrome) .

HY-P992172

ADEL-Y01	Tau Protein	Neurological Disease
ADEL-Y01 is a humanized and parental murine blood-brain barrier-penetrating monoclonal antibody against tau-acK280. ADEL-Y01 specifically recognizes tau-acK280 and its surrounding residues, mediates the neutralization and phagocytosis of acetylated tau aggregates, and interferes with the activity of pathological tau protein. ADEL-Y01 prevents the progression of tauopathies, increases neuronal survival rate, reduces tau-related pathological changes, and improves memory impairment. ADEL-Y01 can be used in research related to Alzheimer's disease and tauopathies .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B2132

Tryptamine 1 Publications Verification 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine	Alkaloids Microorganisms Classification of Application Fields Other Diseases Endogenous metabolite Disease Research Fields Indole Alkaloids	Endogenous Metabolite 5-HT Receptor Aryl Hydrocarbon Receptor
Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models .

HY-W016420

Fosfomycin sodium Maximum Cited Publications 14 Publications Verification MK-0955 sodium	Infection Structural Classification Natural Products Microorganisms Classification of Application Fields Disease Research Fields Source Classification	Bacterial Antibiotic
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 .

HY-N0762

Isobavachin 5 Publications Verification	Structural Classification Flavonoids Neurological Disease Classification of Application Fields Leguminosae Flavonones Phenols Polyphenols Psoralea corylifolia L. Plants Disease Research Fields Source Classification	Cytochrome P450 UGT p38 MAPK NF-κB NO Synthase COX Fc Receptor (FcR) RANKL/RANK Keap1-Nrf2 Reactive Oxygen Species (ROS) Apoptosis Autophagy
Isobavachin is an orally active, blood-brain barrier-penetrating prenylated flavonoid present in Psoralea corylifolia. Isobavachin inhibits human CYP2B6, CYP2C9, CYP2C19, UGT1A1, UGT1A9, and UGT2B7. Isobavachin suppresses MAPK activation, NF-κB nuclear translocation, overexpression of iNOS/COX-2, FcεRI-mediated signaling pathways, and RANKL-induced osteoclastogenesis. Isobavachin induces autophagy, cytotoxicity, neuronal differentiation, and NRF2 activation; it alleviates oxidative damage, inflammatory responses, apoptosis, iron accumulation, mitochondrial biogenesis, and mast cell degranulation. Isobavachin is applicable to research related to liver injury, inflammatory diseases, osteoporosis, liver cancer, prostate cancer, glioma, periodontitis-induced bone loss, and Alzheimer's disease .

HY-P0285

Rabies Virus Glycoprotein 1 Publications Verification	Infection Structural Classification Natural Products Microorganisms Classification of Application Fields Disease Research Fields Source Classification	RABV
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.

HY-N1988R

Cucurbitacin IIa (Standard) Hemslecin A (Standard)	Triterpenes Structural Classification Terpenoids Cucurbitaceae Plants Hemsleya chinensis Cogn. ex Forbes et Hemsl. Source Classification	Reference Standards Apoptosis EGFR Autophagy MEK Caspase ERK STAT Survivin Raf p38 MAPK CaMK
Cucurbitacin IIa (Hemslecin A) (Standard) is the analytical standard for Cucurbitacin IIa (HY-N1988). This product is used for research and analytical applications. Cucurbitacin IIa is an orally active, blood-brain barrier-penetrating EGFR inhibitor with an IC₅₀ of 1.455 nM for human EGFR. Cucurbitacin IIa induces caspase-3 dependent cell apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton through actin aggregation, blocks the cell cycle at the G2/M phase, and inhibits the EGFR-MAPK signaling pathway to exert anti-inflammatory activity. Cucurbitacin IIa can be used in research on inflammatory-related diseases, depression, and non-small cell lung cancer and other cancers.

Cat. No.	Product Name	Chemical Structure

HY-B1075AS

(Rac)-Fosfomycin (benzylamine)-13C3

(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 .

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