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BBB penetration

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (3) Adrenergic Receptor (2) Amyloid-β (3) Apoptosis (1) Biochemical Assay Reagents (2) Cannabinoid Receptor (1) Cholinesterase (ChE) (6) DNA Alkylator/Crosslinker (1) Dopamine Receptor (1) Drug Derivative (1) Drug Intermediate (2) Drug Metabolite (2) FAAH (1) Ferroptosis (1) Fungal (1) GABA Receptor (1) GSK-3 (2) Influenza Virus (2) Isotope-Labeled Compounds (1) Keap1-Nrf2 (1) mGluR (1) Neuropeptide S Receptor (2) NO Synthase (3) P2Y Receptor (1) PERK (1) Sodium Channel (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (1) Infection (4) Inflammation/Immunology (3) Metabolic Disease (1) Neurological Disease (26)
Click Chemistry:	Azide (1)

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Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13318

Oseltamivir acid Maximum Cited Publications 75 Publications Verification 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-130795

GSK-3β inhibitor 2 1 Publications Verification	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-137207

MK-28 5+ Cited Publications	PERK	Neurological Disease
MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice .

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-13788

LY 344864 2 Publications Verification	5-HT Receptor Adrenergic Receptor	Neurological Disease
LY 344864 is a selective, orally active 5-HT_1F receptor agonist with a K_i of 6 nM. LY 344864 is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 can cross the blood brain barrier to some extent .

HY-122559

BMS-984923	mGluR	Neurological Disease
BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (K_i = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling .

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-N4134

Ciwujianoside C3	NO Synthase	Inflammation/Immunology
Ciwujianoside C3, an orally active and brain penetrated compound, is isolated the leaves of Acanthopanax henryi Harms. Ciwujianoside C3 has anti-inflammatory effect and can reinforces object recognition memory .

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-10096

TCS2002	GSK-3	Neurological Disease
TCS2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC₅₀ of 35 nM. TCS2002 shows good pharmacokinetic profiles including favorable BBB penetration. TCS2002 can be used for the research of Alzheimer’s disease .

HY-126429

Nav1.1 activator 1	Sodium Channel	Neurological Disease
Nav1.1 activator 1 (compound 4), a highly potent Na_v1.1 activator with **BBB penetration**, increases decay time constant τ of Na_v1.1 currents at 0.03 μM along with significant selectivity against Na_v1.2, Na_v1.5, and Na_v1.6 .

HY-144389

hAChE/Aβ1-42-IN-1	Cholinesterase (ChE) Amyloid-β	Neurological Disease
hAChE/Aβ1-42-IN-1 (Compound 16) is a potent inhibitor of hAChE and Aβ1-42 aggregation. hAChE/Aβ1-42-IN-1 shows acceptable relative safety upon hepG2 cell line and excellent BBB penetration with wide safety margin. hAChE/Aβ1-42-IN-1 has the potential for the research of Alzheimer disease (AD) .

HY-168563

BuChE-IN-15	Cholinesterase (ChE) FAAH	Neurological Disease
BuChE-IN-15 (compound D12) is a selective BuChE/FAAH dual inhibitor with and show IC₅₀ values of 81 and 400 nM for hBuChE and hFFAH, respectively. BuChE-IN-15 possesses good BBB penetration, and shows neuroprotection.BuChE-IN-15 can be used for study of Alzheimer .

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-106768

Trimelamol CB 10-375; NSC 283162	DNA Alkylator/Crosslinker	Cancer
Trimelamol (CB10-375; NSC283162) is a highly efficient acid-catalyzed DNA interstrand crosslinker with low neurotoxicity due to its limited BBB penetration. Trimelamol exhibits anti-tumor activity and overcomes platinum resistance. Trimelamol is investigated for lung and ovarian cancer research ^{[1][2][3][4][5]}.

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-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-144388

ChE/Aβ1-42-IN-1	Cholinesterase (ChE) Amyloid-β	Neurological Disease
ChE/Aβ1-42-IN-1 (compound 28) is a potent ChE and Aβ_1-42 aggregation inhibitor with IC₅₀s of 0.062, 0.767 and 1.227 µM for AChE, BuChE and Aβ_1-42 aggregation, respectively. ChE/β1-42-IN-1 shows excellent BBB penetration. ChE/Aβ1-42-IN-1 is a potent multi-targeted anti-Alzheimer's agent .

HY-147821

CB1-IN-2	Cannabinoid Receptor	Metabolic Disease
CB1-IN-2 (Compound 4g) is a selective CB₁ inhibitor with an IC₅₀ of 0.644 μM. CB1-IN-2 can penetrates BBB and might cause CNS side effect similar with Rimonabant .

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-150972

P163-0892	Fungal	Infection
P163-0892 is a potent and selective antifungal agent against Cryptococcus species. P163-0892 is predicted to show medium BBB penetration .

HY-169287

TriPEX-ClO4	Apoptosis Ferroptosis	Neurological Disease Cancer
TriPEX-ClO4 is a cationic fluorescent anticancer agent capable of BBB penetration. TriPEX-ClO4 can induces apoptosis and ferroptosis and can be used for study of cancer and brain diseases .

HY-13788B

LY 344864 hydrochloride	5-HT Receptor Adrenergic Receptor	Neurological Disease
LY 344864 hydrochloride is a selective, orally active 5-HT_1F receptor agonist with a K_i of 6 nM. LY 344864 hydrochloride is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 hydrochloride can cross the blood brain barrier to some extent .

HY-161029

T14-A24	Cholinesterase (ChE)	Neurological Disease
T14-A24 is an orally active, reversible, competitive, and selective AChE inhibitor (K_i=22 nM, IC₅₀=6 nM). T14-A24 has benign BBB penetration, remarkable neuroprotective effect, and safe toxicological profile .

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-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-D2343

PB0822	Biochemical Assay Reagents	Neurological Disease
PB0822 can be used for in vivo PET imaging when labeled with [ ¹⁸F]fluoride. [ ¹⁸F]PB0822 is a PET radioligand. [ ¹⁸F]PB0822 has a cLogP value of 1.54, which is a good predictive index for BBB penetration. [ ¹⁸F]PB0822 can be used for Alzheimer’s Disease research .

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-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 .

HY-181047

FMJ-01-042	Dopamine Receptor	Neurological Disease
FMJ-01-042 is a blood-brain barrier-permeable, low-efficacy partial agonist with high affinity (Kᵢ = 4.33 nM) and exceptional subtype selectivity for the dopamine D4 receptor. FMJ-01-042 exhibits good metabolic stability and is suitable for research on neurological and psychiatric disorders .

PB0822	Fluorescent Dyes
PB0822 can be used for in vivo PET imaging when labeled with [ ¹⁸F]fluoride. [ ¹⁸F]PB0822 is a PET radioligand. [ ¹⁸F]PB0822 has a cLogP value of 1.54, which is a good predictive index for BBB penetration. [ ¹⁸F]PB0822 can be used for Alzheimer’s Disease research .

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-N4134

Ciwujianoside C3	Structural Classification Acanthopanax henryi (Oliv.) Harms Classification of Application Fields Terpenoids Plants Pentacyclic Triterpenoids Inflammation/Immunology Disease Research Fields Araliaceae Source Classification	NO Synthase
Ciwujianoside C3, an orally active and brain penetrated compound, is isolated the leaves of Acanthopanax henryi Harms. Ciwujianoside C3 has anti-inflammatory effect and can reinforces object recognition memory .

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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BBB penetration

Inhibitors & Agonists

Fluorescent Dyes

Peptides

NaturalProducts

Isotope-Labeled Compounds

Click Chemistry

Natural
Products