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Blood-brain barrier permeability in vitro

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By Targets:	Amyloid-β (1) Apoptosis (1) Cholinesterase (ChE) (3) Ferroptosis (1) Fluorescent Dye (1) Histamine Receptor (1) LPL Receptor (1) Microtubule/Tubulin (2) Monoamine Oxidase (1) NOD-like Receptor (NLR) (1) Opioid Receptor (1) Reactive Oxygen Species (ROS) (1) Reference Standards (1) Tau Protein (1) α-synuclein (1)
By Research Areas:	Cancer (2) Neurological Disease (8)

Inhibitors & Agonists

Fluorescent Dyes

Targets Recommended: Dan family AIM2 CD44 NEKs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12098

Verubulin hydrochloride MPC-6827 hydrochloride	Microtubule/Tubulin	Cancer
Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types .

HY-160831

PQQ-trimethylester 1 Publications Verification PQQ-TME	α-synuclein	Neurological Disease
PQQ-trimethylester (PQQ-TME) is a synthetic compound that is a trimethylester derivative of pyrroloquinoline quinone (PQQ). PQQ-trimethylester has twice the blood-brain barrier permeability of PQQ (HY-100196) in vitro. In addition, PQQ-trimethylester shows strong inhibitory activity against α-synuclein, amyloid β1-42 (Aβ1-42) and prion protein fibrillation. PQQ-trimethylester can be used in the study of neurodegenerative diseases .

HY-10486

JDTic	Opioid Receptor	Neurological Disease
JDTic is a blood-brain barrier-permeable κ-opioid receptor antagonist (K_i=0.02 nM) with favorable in vitro ADME properties. JDTic blocks agonist-mediated Gi and β-arrestin signaling pathways as well as analgesic effects by stabilizing the inactive conformation of hKOR and activating JNK. JDTic may also induce transient asymptomatic ventricular tachycardia. JDTic is widely applicable to studies related to depression, anxiety, stress-induced addictive behaviors, and nicotine withdrawal .

HY-157555

NLRP3-IN-29	NOD-like Receptor (NLR)	Neurological Disease
NLRP3-IN-29(Compound 5M) is an inhibitor of NLR family pyrin domain containing 3 (NLRP3). NLRP3-IN-29 has the potential for blood-brain barrier permeability and inflammation inhibition both in vivo and in vitro. NLRP3-IN-29 can be used for research on Alzheimer's disease .

HY-12098R

Verubulin hydrochloride (Standard) MPC-6827 hydrochloride (Standard)	Microtubule/Tubulin Reference Standards	Cancer
Verubulin (hydrochloride) (Standard) is the analytical standard of Verubulin (hydrochloride). This product is intended for research and analytical applications. Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types .

HY-162812

H3R antagonist 4	Apoptosis Cholinesterase (ChE) Tau Protein Ferroptosis Histamine Receptor	Neurological Disease
H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC₅₀ of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ_1-42 induced by itself and Cu ²⁺ (95.48% and 88.63%) , and degraded the Aβ_1-42 fibrils induced by itself and Cu ²⁺ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu ²⁺, Zn ²⁺, Al ³⁺, and Fe ²⁺. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ_1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .

HY-174399

AChE/BChE-IN-27	Cholinesterase (ChE) Reactive Oxygen Species (ROS)	Neurological Disease
AChE/BChE-IN-27 is a blood-brain barrier-permeable mixed inhibitor (Pe = 4.12) of AChE and BChE, with IC₅₀ values of 3.72 μM and 9.65 μM, respectively. AChE/BChE-IN-27 has potent antioxidant activity with an IC₅₀ value of 6.32 μM in the DPPH (HY-112053) assay and also exhibits potent in vitro antioxidant activity. AChE/BChE-IN-27 exhibits metal chelating properties. AChE/BChE-IN-27 has neuroprotective potential against oxidative stress. AChE/BChE-IN-27 significantly reduces intracellular reactive oxygen species (ROS). In in vivo experiments, AChE/BChE-IN-27 effectively restored AChE and BChE levels, improved cognition, and can be used for Alzheimer's disease (AD) .

HY-149090

AChE/BuChE/MAO-B-IN-2	Cholinesterase (ChE) Monoamine Oxidase	Neurological Disease
AChE/BuChE/MAO-B-IN-2 (compound 4b) is a potent AChE/BuChE inhibitor and showed good blood brain barrier (BBB) permeability in vitro with an IC₅₀ value of 5.3 μM, 12.4 μM, 1.9±0.08 μM, for AChE, BuChE, huMAO-B, respectively. AChE/BuChE/MAO-B-IN-2 (compound 4b) can inhibit excess AChE/BuChE in Alzheimer's disease (AD) brain. AChE/BuChE/MAO-B-IN-2 (compound 4b) can be used in anti-Alzheimer's research .

HY-D3220

PTO-41	Fluorescent Dye Amyloid-β	Neurological Disease
PTO-41 is a blood-brain barrier-permeable near-infrared fluorescent probe that targets β-amyloid oligomers (Aβ Oligomers, AβOs) with a K_d of 349 nM. PTO-41 exhibits low cytotoxicity, high sensitivity to β-amyloid oligomers in in vitro phantom imaging, and can be rapidly cleared from the brain. PTO-41 is applicable to the research of Alzheimer's disease (Ex/Em = 538 nM/680 nM) .

HY-164584

S1P5 receptor antagonist 1	LPL Receptor	Neurological Disease
S1P5 receptor antagonist 1 is a selective, blood-brain barrier-permeable S1P5 receptor antagonist with an EC₅₀ of 0.1 nM and a K_i of 4.4 nM. S1P5 receptor antagonist 1 inhibits the migration of natural killer cells towards sphingosine 1-phosphate in vitro, with no effect on T cell migration. S1P5 receptor antagonist 1 can be used in the research of central nervous system diseases .

PTO-41	Fluorescent Dyes
PTO-41 is a blood-brain barrier-permeable near-infrared fluorescent probe that targets β-amyloid oligomers (Aβ Oligomers, AβOs) with a K_d of 349 nM. PTO-41 exhibits low cytotoxicity, high sensitivity to β-amyloid oligomers in in vitro phantom imaging, and can be rapidly cleared from the brain. PTO-41 is applicable to the research of Alzheimer's disease (Ex/Em = 538 nM/680 nM) .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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