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Pathways Recommended:	Membrane Transporter/Ion Channel

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CNS transporters

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By Targets:	Adrenergic Receptor (2) Apoptosis (1) Autophagy (2) Cadherin (1) Chloride Channel (1) Collagen (1) FXR (1) Interleukin Related (1) NF-κB (1) NOD-like Receptor (NLR) (1) Phosphodiesterase (PDE) (2) Reference Standards (2) Serotonin Transporter (3) TGF-β Receptor (1) Toll-like Receptor (TLR) (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (2) Endocrinology (2) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (6)

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Targets Recommended: Nucleoside Transporters GlyT ATP-binding cassette (ABC) transporters ASCT

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0193A

Prazosin hydrochloride Maximum Cited Publications 17 Publications Verification	Adrenergic Receptor Autophagy	Cardiovascular Disease Endocrinology Cancer
Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC₅₀ of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC₅₀s of 1.8, and 13 μM, respectively .

HY-12501A

ITI-214 3 Publications Verification	Phosphodiesterase (PDE)	Neurological Disease
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (K_i of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with K_is of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions .

HY-12501

ITI-214 free base	Phosphodiesterase (PDE)	Neurological Disease
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (K_i of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with K_is of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions .

HY-107128

Ampreloxetine hydrochloride TD-9855 hydrochloride	Serotonin Transporter	Neurological Disease
Ampreloxetine (TD-9855) hydrochloride is an orally active and CNS-penetrant inhibitor of Norepinephrine transporter (NET) and Serotonin 5-HT uptake transporter (SERT), but not Dopamine transporter (DAT). Ampreloxetine hydrochloride binds norepinephrine transporters (NET) and serotonin transporters (SERT) with EC₅₀ values of 11.7 ng/mL and 50.8 ng/mL, respectively, in plasma .

HY-B0193AR

Prazosin hydrochloride (Standard)	Reference Standards Adrenergic Receptor Autophagy	Cardiovascular Disease Endocrinology Cancer
Prazosin (hydrochloride) (Standard) is the analytical standard of Prazosin (hydrochloride). This product is intended for research and analytical applications. Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC₅₀ of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC₅₀s of 1.8, and 13 μM, respectively .

HY-107128R

Ampreloxetine hydrochloride (Standard) TD-9855 hydrochloride (Standard)	Reference Standards Serotonin Transporter	Neurological Disease
Ampreloxetine hydrochloride (Standard) (TD-9855 hydrochloride (Standard)) is the analytical standard of Ampreloxetine (hydrochloride) (HY-107128). This product is intended for research and analytical applications. Ampreloxetine (TD-9855) hydrochloride is an orally active and CNS-penetrant inhibitor of Norepinephrine transporter (NET) and Serotonin 5-HT uptake transporter (SERT), but not Dopamine transporter (DAT). Ampreloxetine hydrochloride binds norepinephrine transporters (NET) and serotonin transporters (SERT) with EC₅₀ values of 11.7 ng/mL and 50.8 ng/mL, respectively, in plasma .

HY-183269

SERT-IN-5	Serotonin Transporter	Neurological Disease
SERT-IN-5 is a potent, selective, and CNS-penetrant serotonin transporter (SERT) inhibitor with a K_i of 0.3 nM. SERT-IN-5 blocks serotonin reuptake to increase synaptic serotonin levels. SERT-IN-5 exhibits anti-anxiety effects in mice. SERT-IN-5 can be used for the research of anxiety, depression .

HY-182571

AK-42	Chloride Channel	Neurological Disease
AK-42 is a selective CLC-2 chloride channel inhibitor with human IC₅₀ of 17 nM and rat IC₅₀ of 14 nM. AK-42 binds to an extracellular vestibule above the channel pore, inhibits CLC-2 currents acutely and reversibly, including with auxiliary subunit GlialCAM coexpression. AK-42 acts as a selective tool compound for acute CLC-2 function modulation to probe CLC-2 neurophysiology. AK-42 can be used for the research of leukodystrophy and idiopathic generalized epilepsies .

HY-N17383

Ligusticum cycloprolactam	Toll-like Receptor (TLR) NF-κB Collagen Interleukin Related Cadherin NOD-like Receptor (NLR) TGF-β Receptor FXR Apoptosis	Metabolic Disease Inflammation/Immunology
Ligusticum cycloprolactam is a potent, orally active, and CNS-penetrant TLR4/NF-κB inhibitor, exhibiting anti-inflammatory and neuroprotective activity. Ligusticum cycloprolactam reduces FPR1 expression, inhibits NLRP3 inflammasome, TLR4/NF-κB, hepatic MAPK and TGF-β signaling, and selectively activates hepatic FXR. Ligusticum cycloprolactam attenuates pro-inflammatory mediator production, enhances anti-inflammatory cytokine secretion, regulates renal uric acid transporters, and preserves intestinal microbiota composition. Ligusticum cycloprolactam can be used for the research of ischemic stroke, hyperuricemic nephropathy, neuroinflammation, and metabolic dysfunction-associated fatty liver disease .

Cat. No.	Product Name

HY-L906

*Norepinephrine Transporter* (NET) Compound Library**	647 compounds
On May 15, 2024, "Dimerization and antidepressant recognition at noradrenaline transporter" was published online by Nature. The research findings were an effort from Shanghai Institute of Materia Medica, Chinese Academy of Sciences. This study unraveled the important neural system target - the noradrenaline transporter (NET), obtaining the binding modes of human NET homodimers with the natural substrate norepinephrine (NE) and six selective antidepressants. It laid an important theoretical foundation for understanding the physiological regulation mechanisms of NET and other monoamine transporters. The Norepinephrine Transporter (NET) Compound Library is obtained by computer-aided virtual screening based on the HY-L901 compound library . The specific screening process includes molecular docking screening, key pharmacophore screening, and CNS-MPO screening, which can be used for new drug discovery targeting the noradrenaline transporter.

Norepinephrine Transporter (NET) Compound Library

647 compounds

On May 15, 2024, "Dimerization and antidepressant recognition at noradrenaline transporter" was published online by Nature. The research findings were an effort from Shanghai Institute of Materia Medica, Chinese Academy of Sciences. This study unraveled the important neural system target - the noradrenaline transporter (NET), obtaining the binding modes of human NET homodimers with the natural substrate norepinephrine (NE) and six selective antidepressants. It laid an important theoretical foundation for understanding the physiological regulation mechanisms of NET and other monoamine transporters.

The Norepinephrine Transporter (NET) Compound Library is obtained by computer-aided virtual screening based on the HY-L901 compound library . The specific screening process includes molecular docking screening, key pharmacophore screening, and CNS-MPO screening, which can be used for new drug discovery targeting the noradrenaline transporter.

HY-L919

MCE CNS BBB Lead-like Library	27,503 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

27,503 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	Category	Target	Chemical Structure

HY-N17383

Ligusticum cycloprolactam	Structural Classification Natural Products Umbelliferae Plants Echinacea angustifolia DC. Source Classification	Toll-like Receptor (TLR) NF-κB Collagen Interleukin Related Cadherin NOD-like Receptor (NLR) TGF-β Receptor FXR Apoptosis
Ligusticum cycloprolactam is a potent, orally active, and CNS-penetrant TLR4/NF-κB inhibitor, exhibiting anti-inflammatory and neuroprotective activity. Ligusticum cycloprolactam reduces FPR1 expression, inhibits NLRP3 inflammasome, TLR4/NF-κB, hepatic MAPK and TGF-β signaling, and selectively activates hepatic FXR. Ligusticum cycloprolactam attenuates pro-inflammatory mediator production, enhances anti-inflammatory cytokine secretion, regulates renal uric acid transporters, and preserves intestinal microbiota composition. Ligusticum cycloprolactam can be used for the research of ischemic stroke, hyperuricemic nephropathy, neuroinflammation, and metabolic dysfunction-associated fatty liver disease .

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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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CNS transporters

Inhibitors & Agonists

Screening Libraries

NaturalProducts

Natural
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