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Results for "

Central permeability

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Anaplastic lymphoma kinase (ALK) (1) Autophagy (1) Bacterial (1) Cholinesterase (ChE) (4) Eukaryotic Initiation Factor (eIF) (1) FAAH (1) GlyT (1) HIV (1) IMPDH (1) IPK Superfamily (1) Isotope-Labeled Compounds (2) mAChR (2) mGluR (1) Oxytocin Receptor (2) P-glycoprotein (1) P2X Receptor (1) PARP (1) PKC (1) Reference Standards (1) ROS Kinase (1) Thyroid Hormone Receptor (1) Transferrin Receptor (1) Trk Receptor (1)
By Research Areas:	Cancer (4) Endocrinology (3) Infection (1) Inflammation/Immunology (2) Neurological Disease (16)

By Targets:

5-HT Receptor (1)

Anaplastic lymphoma kinase (ALK) (1)

Autophagy (1)

Bacterial (1)

Cholinesterase (ChE) (4)

Eukaryotic Initiation Factor (eIF) (1)

FAAH (1)

GlyT (1)

HIV (1)

IMPDH (1)

IPK Superfamily (1)

Isotope-Labeled Compounds (2)

mAChR (2)

mGluR (1)

Oxytocin Receptor (2)

P-glycoprotein (1)

P2X Receptor (1)

PARP (1)

PKC (1)

Reference Standards (1)

ROS Kinase (1)

Thyroid Hormone Receptor (1)

Transferrin Receptor (1)

Trk Receptor (1)

By Research Areas:

Cancer (4)

Endocrinology (3)

Infection (1)

Inflammation/Immunology (2)

Neurological Disease (16)

Inhibitors & Agonists

Screening Libraries

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-164495

Sob-AM2	FAAH Thyroid Hormone Receptor	Inflammation/Immunology Endocrinology
Sob-AM2 is a potent substrate (K_m=1.3 μM) targeting fatty acid amide hydrolase (FAAH) expressed in the brain and has blood-brain barrier permeability. Sob-AM2 delivers high concentrations of Sobetirome (HY-14823) to the central nervous system with minimal peripheral systemic dose, thereby stimulating central thyroid hormone receptor β (TRβ). In addition, Sob-AM2 can prevent myelin and axon degeneration in experimental autoimmune encephalomyelitis (EAE) mice .

HY-15023

Cligosiban Maximum Cited Publications 6 Publications Verification PF-3274167	Oxytocin Receptor	Endocrinology
Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents ^[1][2].

HY-153615

CVN636	mGluR	Neurological Disease
CVN636 is a potent, orally active and selective mGluR7 allosteric agonist with an EC₅₀ value of 7 nM for hu mGluR7. CVN636 has central nervous system (CNS) permeability .

HY-101418

JNJ-47965567 5 Publications Verification	P2X Receptor	Neurological Disease
JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pK_is of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology .

HY-110176

ASP2535	GlyT	Neurological Disease
ASP2535 is a potent, orally bioavailable, selective, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor. ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease .

HY-P99797

Pabinafusp alfa JR-141	Transferrin Receptor	Neurological Disease
Pabinafusp alfa (JR-141) is a transferrin receptor-targeting antibody consisting of Iduronate 2-sulfatase (HY-P76399) and an anti-human transferrin receptor antibody. Pabinafusp alfa is blood-brain permeable and prevents heparan sulfate (HS) deposition in the central nervous system of mucopolysaccharidosis II (MPS II) mice. Pabinafusp alfa improves learning and prevents central nervous system neuronal damage in mice .

HY-177498

M1 mAChR modulator-1	mAChR	Neurological Disease
M1 mAChR modulator-1 (Example 66) is a muscarinic M1 receptor (mAChR1) positive allosteric modulator. M1 mAChR modulator-1 effectively promotes gastrointestinal motility and defecation in mouse models with low central permeability. M1 mAChR modulator-1 can be used for constipation research .

HY-162821

LI-3948	IPK Superfamily	Neurological Disease
IP6K-IN-2 (compound 29c) is an orally bioavailable and blood-brain barrier permeable IP6K inhibitor (IC₅₀: 15.8 nM) that can be used in the study of central nervous system diseases .

HY-15023R

Cligosiban (Standard)	Oxytocin Receptor	Endocrinology
Cligosiban (Standard) is the analytical standard of Cligosiban. This product is intended for research and analytical applications. Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents .

HY-175482

PARP1-IN-43	PARP	Neurological Disease Cancer
PARP1-IN-43 (Compound 5350) is a blood-brain barrier (BBB) permeable PARP1 inhibitor, with an IC₅₀ of 5 nM. PARP1-IN-43 can be used for the study of homologous recombination (HR)-deficient central nerve system (CNS) cancers .

HY-B1343

Pridinol mesylate	Cholinesterase (ChE)	Neurological Disease
Pridinol mesylate is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol mesylate reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol mesylate inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .

HY-B1343A

Pridinol	Cholinesterase (ChE)	Neurological Disease
Pridinol is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .

HY-149555

DNL343	Eukaryotic Initiation Factor (eIF)	Neurological Disease
DNL343 is a potent, selective, orally active and brain-penetrant activator of eukaryotic initiation factor eIF2B. DNL343 inhibits the activity of the integrated stress response (ISR) in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 can be used in the study of neurodegenerative diseases .

HY-123934

VU6007477	P-glycoprotein	Neurological Disease
VU6007477 is a brain-penetrant, selective M1 positive allosteric modulator (PAM) with an EC₅₀ value of 230 nM. VU6007477 is also a human P-glycoprotein (P-gp) substrate with moderate permeability. VU6007477 displays improved central nervous system (CNS) penetration over the hydroxylated congeners. VU6007477 a pyranyl amide derivative, which is promising for research of robust cholinergic seizure activity .

HY-B1343AS

Pridinol-d5	Cholinesterase (ChE) Isotope-Labeled Compounds	Neurological Disease
Pridinol-d₅ is deuterium labeled Pridinol (HY-B1343A) . Pridinol is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .

HY-105231

Bryostatin 1 2 Publications Verification	PKC HIV Bacterial	Infection Neurological Disease Inflammation/Immunology Cancer
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with K_is of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties .

HY-161712

IMPDH-IN-4	IMPDH	Cancer
IMPDH-IN-4 is a derivative of N-pyridinylthiophene carboxamid that exhibits activity against peripheral nerve sheath carcinoma cells. IMPDH-IN-4 is metabolized by NAMPT and NMNAT1 to an adenine dinucleotide (AD) derivative, which is an NAD analog and can inhibit inosine monophosphate dehydrogenase (IMPDH), leading to the accumulation of inosine monophosphate (IMP) in cells. IMPDH-IN-4 has good blood-brain barrier permeability and can be used in the study of central and peripheral nervous system cancers .

HY-B1343R

Pridinol mesylate (Standard)	Reference Standards Cholinesterase (ChE)	Neurological Disease
Pridinol mesylate (Standard) is the analytical standard of Pridinol mesylate (HY-B1343). This product is intended for research and analytical applications. Pridinol mesylate is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol mesylate reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol mesylate inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .

HY-173396

VU0467319 VU319	mAChR	Neurological Disease
VU0467319 (Compound VU319) is a highly selective and blood-brain-permeable, orally active M1 positive allosteric modulator (PAM) (EC₅₀: 492 nM). VU0467319 is selective (EC₅₀ > 30 μM) versus M2-5 for both human and rat. VU0467319 improves cognitive impairment in Alzheimer's disease (AD) through central M1 muscarinic receptors. VU0467319 does not induce cholinergic adverse reactions and has potential in AD research .

HY-159492

5-HT7 receptor ligand 2	5-HT Receptor	Neurological Disease
5-HT7 receptor ligand 2 (compound 32) is an arylpiperazinehydrazine ligand for 5-HT₇R (K_i=178 nM). 5-HT7 receptor ligand 2 has good membrane permeability, low hepatotoxicity and cardiotoxicity, and high plasma protein binding. 5-HT7 receptor ligand 2 shows neuroprotective effects in SH-SY5Y cells and can be used for the study of central nervous system related diseases .

HY-12678S1

Entrectinib-d8 NMS-E628-d₈; RXDX-101-d₈	Isotope-Labeled Compounds Autophagy Anaplastic lymphoma kinase (ALK) Trk Receptor ROS Kinase	Cancer
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC₅₀ values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .

Cat. No.	Product Name

HY-L0123V

Life Chemicals CNS Focused Screening Library	30,300 compounds
The incidence and significance of central nervous system diseases are increasing at an alarming rate all over the world. Although substantial research efforts have been applied to develop new CNS-active drugs, only a few CNS disorders are addressed satisfactorily, while the remaining ones pose significant clinical challenges. Blood-brain barrier (BBB) permeability is one of the most important limiting factors in the design and development of novel CNS-targeted pharmaceuticals for the treatment of neurological disorders. Carefully selected from the HTS Compound Collection to meet the parameters optimized for high BBB-permeability, our CNS Focused Screening Library comprising over 30,300 structurally-diverse and potentially CNS-active screening compounds. This original Screening Compound Library is aimed at supporting CNS drug design projects and HTS efforts in search for novel neurotherapeutics.

Life Chemicals CNS Focused Screening Library

30,300 compounds

The incidence and significance of central nervous system diseases are increasing at an alarming rate all over the world. Although substantial research efforts have been applied to develop new CNS-active drugs, only a few CNS disorders are addressed satisfactorily, while the remaining ones pose significant clinical challenges. Blood-brain barrier (BBB) permeability is one of the most important limiting factors in the design and development of novel CNS-targeted pharmaceuticals for the treatment of neurological disorders.

Carefully selected from the HTS Compound Collection to meet the parameters optimized for high BBB-permeability, our CNS Focused Screening Library comprising over 30,300 structurally-diverse and potentially CNS-active screening compounds. This original Screening Compound Library is aimed at supporting CNS drug design projects and HTS efforts in search for novel neurotherapeutics.

HY-L028

CNS-Penetrant Compound Library	1,022 compounds
The blood-brain barrier (BBB) is the complex network of brain microvessels. It protects the brain from the external bloodstream environment and supplies the brain with the required nutrients for normal function. However, blood-brain barrier is also the obstacle to deliver beneﬁcial drugs to treat CNS (central nervous system) diseases or brain tumors, as it has the least permeable capillaries in the entire body due to physical barriers (tight junctions). Therefore, it is crucial to discover drugs which can cross this barrier for the treatment of brain-based diseases, such as Alzheimer’s disease (AD), Parkinson’s disease (PD) and epilepsy. MCE offers a unique collection of 1,022 compounds with confirmed CNS-Penetrant property. It’s a useful tool for the discovery of drugs used for brain diseases, such as brain tumors, mental disorders, and neurodegenerative diseases.

CNS-Penetrant Compound Library

1,022 compounds

The blood-brain barrier (BBB) is the complex network of brain microvessels. It protects the brain from the external bloodstream environment and supplies the brain with the required nutrients for normal function. However, blood-brain barrier is also the obstacle to deliver beneﬁcial drugs to treat CNS (central nervous system) diseases or brain tumors, as it has the least permeable capillaries in the entire body due to physical barriers (tight junctions). Therefore, it is crucial to discover drugs which can cross this barrier for the treatment of brain-based diseases, such as Alzheimer’s disease (AD), Parkinson’s disease (PD) and epilepsy.

MCE offers a unique collection of 1,022 compounds with confirmed CNS-Penetrant property. It’s a useful tool for the discovery of drugs used for brain diseases, such as brain tumors, mental disorders, and neurodegenerative diseases.

HY-L920

CNS MPO Lead-like Library	25,622 compounds
With the aging population and increasing competitive pressures, neurodegenerative diseases of the central nervous system (CNS) have become a serious medical challenge in modern society, including Parkinson's disease, Alzheimer's disease, brain tumors, and multiple sclerosis. The CNS MPO (Multi-Parameter Optimization) score is a widely recognized algorithm in medicinal chemistry. Developed by Pfizer, this method is based on an analysis of approved CNS drugs and their interior CNS drug candidates, establishing the CNS MPO rules. It incorporates six key physicochemical properties (ClogP, ClogD, MW, TPSA, HBD, and pKa) to prospectively optimize CNS drug attributes—such as high blood-brain barrier (BBB) permeability, low P-gp efflux liability, low metabolic clearance, and high safety—thereby improving the clinical success rate of CNS drug candidates. The CNS MPO compound library is a collection of compounds with CNS MPO scores greater than 5, specifically designed for CNS drug discovery.

CNS MPO Lead-like Library

25,622 compounds

HY-L919

MCE CNS BBB Lead-like Library	28,722 compounds
With the aging population and increasing competitive pressures, neurodegenerative diseases of the central nervous system (CNS) have become a serious medical challenge in modern society, including Parkinson's disease, Alzheimer's disease, brain tumors, and multiple sclerosis. However, the success rate of CNS drug development remains remarkably low, primarily due to the blood-brain barrier (BBB). The blood-brain barrier (BBB) is a semipermeable barrier structure that surrounds the microvasculature of the CNS. In capillaries, the wedged endothelial cells are tightly packed and wedge-shaped, lining the interior of the vessels to form extensive tight junctions. Along with a range of receptors, transporters, efflux pumps, and other cellular components, this barrier regulates the entry and exit of molecules between the bloodstream and the brain. The intact BBB blocks the passage of most blood-borne substances into the brain, preventing nearly 100% of large-molecule drugs and over 98% of small-molecule drugs from entering. Compared to non-CNS drugs, physicochemical properties such as hydrogen bonds, lipophilicity, and molecular weight significantly influence a compound's ability to cross the BBB. Using artificial intelligence (AI) algorithms to predict BBB permeability, a predicted value greater than 0.75 indicates that the compound has strong potential to cross the BBB, providing a promising starting point for CNS drug discovery.

MCE CNS BBB Lead-like Library

28,722 compounds

With the aging population and increasing competitive pressures, neurodegenerative diseases of the central nervous system (CNS) have become a serious medical challenge in modern society, including Parkinson's disease, Alzheimer's disease, brain tumors, and multiple sclerosis. However, the success rate of CNS drug development remains remarkably low, primarily due to the blood-brain barrier (BBB). The blood-brain barrier (BBB) is a semipermeable barrier structure that surrounds the microvasculature of the CNS. In capillaries, the wedged endothelial cells are tightly packed and wedge-shaped, lining the interior of the vessels to form extensive tight junctions. Along with a range of receptors, transporters, efflux pumps, and other cellular components, this barrier regulates the entry and exit of molecules between the bloodstream and the brain. The intact BBB blocks the passage of most blood-borne substances into the brain, preventing nearly 100% of large-molecule drugs and over 98% of small-molecule drugs from entering. Compared to non-CNS drugs, physicochemical properties such as hydrogen bonds, lipophilicity, and molecular weight significantly influence a compound's ability to cross the BBB. Using artificial intelligence (AI) algorithms to predict BBB permeability, a predicted value greater than 0.75 indicates that the compound has strong potential to cross the BBB, providing a promising starting point for CNS drug discovery.

Cat. No.	Product Name	Target	Research Area

HY-P99797

Pabinafusp alfa JR-141	Transferrin Receptor	Neurological Disease
Pabinafusp alfa (JR-141) is a transferrin receptor-targeting antibody consisting of Iduronate 2-sulfatase (HY-P76399) and an anti-human transferrin receptor antibody. Pabinafusp alfa is blood-brain permeable and prevents heparan sulfate (HS) deposition in the central nervous system of mucopolysaccharidosis II (MPS II) mice. Pabinafusp alfa improves learning and prevents central nervous system neuronal damage in mice .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-105231

Bryostatin 1 2 Publications Verification	Structural Classification Anti-inflammation/Immunoregulatory Neurological Disease Classification of Application Fields Marine natural products Source classification Other marine organisms Disease Research Infection Macrolide Antibiotics Animals Antibiotics Anticancer Inflammation/Immunology Disease Research Fields	PKC HIV Bacterial
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with K_is of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties .

Cat. No.	Product Name	Chemical Structure

HY-12678S1

Entrectinib-d8
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC₅₀ values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .

Entrectinib-d8

Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC₅₀ values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .

HY-B1343AS

Pridinol-d5
Pridinol-d₅ is deuterium labeled Pridinol (HY-B1343A) . Pridinol is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .

Pridinol-d5

Pridinol-d₅ is deuterium labeled Pridinol (HY-B1343A) . Pridinol is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .

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