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Blood-Brain Barrier (BBB) Penetration

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By Targets:	5-HT Receptor (1) Amyloid-β (1) Biochemical Assay Reagents (1) Cholinesterase (ChE) (2) Drug Derivative (1) Drug Intermediate (2) Drug Metabolite (2) GABA Receptor (1) Influenza Virus (2) Isotope-Labeled Compounds (1) Keap1-Nrf2 (1) Neuropeptide S Receptor (2) NO Synthase (2) P2Y Receptor (1) PROTACs (1) RET (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (2) Neurological Disease (12)
Click Chemistry:	Azide (1)

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Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13318

Oseltamivir acid 70+ Cited Publications GS 4071; Ro 64-0802; Oseltamivir carboxylate	Influenza Virus Drug Metabolite	Infection Neurological Disease
Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC₅₀=2 nM) with activity against both influenza A and B viruses. Oseltamivir acid has an extremely weak ability to penetrate the BBB under normal physiological conditions, but its blood-brain barrier penetration is significantly enhanced under inflammatory conditions .

HY-108625

SHA 68 1 Publications Verification	Neuropeptide S Receptor	Neurological Disease
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC₅₀s of 22.0 and 23.8 nM for NPSR Asn ¹⁰⁷ and NPSR Ile ¹⁰⁷, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia .

HY-13318S

Oseltamivir acid-d3 GS 4071-d₃; Ro 64-0802-d₃; Oseltamivir carboxylate-d₃	Isotope-Labeled Compounds Influenza Virus Drug Metabolite	Infection
Oseltamivir acid-d₃ is a deuterium labeled Oseltamivir acid (HY-13318). Oseltamivir acid, the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC₅₀=2 nM) with activity against both influenza A and B viruses. Oseltamivir acid has an extremely weak ability to penetrate the BBB under normal physiological conditions, but its blood-brain barrier penetration is significantly enhanced under inflammatory conditions .

HY-P11195

Angiopep-2 azide	Drug Derivative	Neurological Disease
Angiopep-2 azide is a peptide derivative of Angiopep-2 (HY-P2341) bearing a side chain azide (N3) group. Angiopep-2 exhibits high blood-brain barrier (BBB) penetration capability and can be used for brain compound delivery .

HY-114320

BuChE-IN-TM-10 TM-10	Cholinesterase (ChE)	Neurological Disease
BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC₅₀ of 8.9 nM. BuChE inhibitor 1 inhibits and disaggregates self-induced Aβ aggregation, exhibiting potent antioxidant activity and good blood-brain barrier (BBB) penetration. Has potential to treat Alzheimer’s disease .

HY-N4190

Britannilactone diacetate 1,6-O,O-Diacetylbritannilactone; Di-O-acetylbritannilactone	NO Synthase	Neurological Disease Inflammation/Immunology
Britannilactone diacetate (1,6-O,O-Diacetylbritannilactone; Compound 2) exhibits potential NO inhibition effect. Britannilactone diacetate exhibits activity against NO production induced by LPS in BV-2 microglial cells with the EC₅₀ value of 6.3 μM. Britannilactone diacetate exhibits a favorable blood-brain barriers (BBB) penetration and absorption, distribution, metabolism, excretion, and toxicity (ADMET) property .

HY-178964

PROTAC RET Degrader 1	PROTACs RET	Cancer
PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC₅₀ values for RET (WT), RET (G810S), RET (G810C), and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand (HY-179308); Blue: CRBN ligand (HY-179307); Black: Linker) .

HY-175675

P2Y1 antagonist 4	P2Y Receptor Keap1-Nrf2	Cardiovascular Disease Neurological Disease
P2Y1 antagonist 4 is a selective P2Y1 receptor antagonist with excellent blood-brain barrier (BBB) penetration. P2Y1 antagonist 4 inhibits P2Y1 receptor-mediated cytosolic Ca ²⁺ increase (IC₅₀ = 1.95 μM) and platelet aggregation (IC₅₀ = 3.24 μM) induced by ADP in rabbit washed platelets. P2Y1 antagonist 4 significantly upregulates the level of nuclear Nrf2 protein in H2O2-treated HT22 cells. P2Y1 antagonist 4 reduces myocardial infarct size in a mouse acute myocardial infarction (MI) model. P2Y1 antagonist 4 can be used for the study of ischemic stroke and myocardial infarction .

HY-147151

AMCPy	Biochemical Assay Reagents	Others
AMCPy is a potent electron paramagnetic resonance (EPR) brain imaging agent, possessing excellent lipophilicity for blood brain barrier (BBB) penetration .

HY-143413

BuChE-IN-2	Amyloid-β	Neurological Disease Inflammation/Immunology
BuChE-IN-2 is an excellent butyrylcholinesterase (BuChE) inhibitor (IC₅₀s of 1.28 μM and 0.67 μM for BuChE and NO). BuChE-IN-2 can inhibit the aggregation of Aβ, ROS formation and chelate Cu ²⁺, exhibiting proper blood-brain barrier (BBB) penetration. BuChE-IN-2 has potential to research Alzheimer’s disease .

HY-108625R

SHA 68 (Standard)	Neuropeptide S Receptor	Neurological Disease
SHA 68 (Standard) is the analytical standard of SHA 68. This product is intended for research and analytical applications. SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn107 and NPSR Ile107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia .

HY-168241

Flucopride	Cholinesterase (ChE) 5-HT Receptor	Infection
Flucopride (Compound 4a) is an AChE inhibitor (IC₅₀: 24 nM), and a partial 5-HT₄R agonist (K_i: 9.6 nM for (h)5-HT4R). Flucopride promotes the non-amyloidogenic processing of APP in COS-7 transiently expressing (h)5-HT₄R (EC₅₀: 23.0 nM). Flucopride may has good gastrointestinal track (GIT) penetration, and blood-brain barrier (BBB) cross-membrane penetration (PAMPA assay) .

HY-175670

GABAA receptor modulator-10	GABA Receptor	Neurological Disease
GABAA receptor modulator-10 is an orally active, potent positive allosteric modulator (PAM) of the α1β2γ2 GABAA receptor with favorable blood-brain barrier (BBB) penetration. GABAA receptor modulator-10 enhances α1β2γ2 GABAA receptor function and potentiates GABA-evoked currents. GABAA receptor modulator-10 demonstrates potent antiepileptic efficacy in both the Pentetrazol (PTZ)- and Kainic Acid (KA) (HY-N2309)-induced mice epilepsy models. GABAA receptor modulator-10 can be used for the study of epilepsy .

HY-164512

NRMA-I	Drug Intermediate	Neurological Disease
NRMA-I is the amide produrg of the small molecule nuclear receptor modulator. NRMA-I exhibits a higher exposure in the brain, indicating that a good blood-brain barrier (BBB) penetration. NRMA-I can be used for research of central nervous system diseases related to nuclear receptors, such as Alzheimer's disease and Parkinson's disease .

HY-164505

NRMA-9	Drug Intermediate	Neurological Disease
NRMA-9 is the amide produrg of the small molecule nuclear receptor modulator. NRMA-9 exhibits a higher exposure in the brain, indicating that a good blood-brain barrier (BBB) penetration. NRMA-9 can be used for research of central nervous system diseases related to nuclear receptors, such as Alzheimer's disease and Parkinson's disease .

HY-181711

nNOS-IN-6	NO Synthase	Neurological Disease Cancer
nNOS-IN-6 is a human neuronal nitric oxide synthase (hnNOS) inhibitor with a human hnNOS K_i of 16 nM, ~1800-fold selectivity over human eNOS, ~2900-fold selectivity over human iNOS, and a rat nNOS K_i of 34 nM.nNOS-IN-6 exhibits high effective permeability in PAMPA-BBB assays, crosses the blood-brain barrier, and shows sustained systemic exposure, low clearance, and robust brain penetration in mouse in vivo pharmacokinetic studies.nNOS-IN-6 can be used for the research of neurodegenerative diseases, melanoma .

Cat. No.	Product Name	Target	Research Area

HY-P11195

Angiopep-2 azide	Drug Derivative	Neurological Disease
Angiopep-2 azide is a peptide derivative of Angiopep-2 (HY-P2341) bearing a side chain azide (N3) group. Angiopep-2 exhibits high blood-brain barrier (BBB) penetration capability and can be used for brain compound delivery .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N4190

Britannilactone diacetate 1,6-O,O-Diacetylbritannilactone; Di-O-acetylbritannilactone	Structural Classification Terpenoids Sesquiterpenes Plants Compositae Piptanthus nepalensis (Hook.) D. Don Source Classification	NO Synthase
Britannilactone diacetate (1,6-O,O-Diacetylbritannilactone; Compound 2) exhibits potential NO inhibition effect. Britannilactone diacetate exhibits activity against NO production induced by LPS in BV-2 microglial cells with the EC₅₀ value of 6.3 μM. Britannilactone diacetate exhibits a favorable blood-brain barriers (BBB) penetration and absorption, distribution, metabolism, excretion, and toxicity (ADMET) property .

Cat. No.	Product Name	Chemical Structure

HY-13318S

Oseltamivir acid-d3
Oseltamivir acid-d₃ is a deuterium labeled Oseltamivir acid (HY-13318). Oseltamivir acid, the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC₅₀=2 nM) with activity against both influenza A and B viruses. Oseltamivir acid has an extremely weak ability to penetrate the BBB under normal physiological conditions, but its blood-brain barrier penetration is significantly enhanced under inflammatory conditions .

Oseltamivir acid-d3

Oseltamivir acid-d₃ is a deuterium labeled Oseltamivir acid (HY-13318). Oseltamivir acid, the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC₅₀=2 nM) with activity against both influenza A and B viruses. Oseltamivir acid has an extremely weak ability to penetrate the BBB under normal physiological conditions, but its blood-brain barrier penetration is significantly enhanced under inflammatory conditions .

Cat. No.	Product Name		Classification

HY-P11195

Angiopep-2 azide		Azide
Angiopep-2 azide is a peptide derivative of Angiopep-2 (HY-P2341) bearing a side chain azide (N3) group. Angiopep-2 exhibits high blood-brain barrier (BBB) penetration capability and can be used for brain compound delivery .

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Blood-Brain Barrier (BBB) Penetration

Inhibitors & Agonists

Peptides

NaturalProducts

Isotope-Labeled Compounds

Click Chemistry

Natural
Products