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Pathways Recommended:	Membrane Transporter/Ion Channel

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CNS channels

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Calcium Channel (10) Chloride Channel (1) Drug Isomer (1) ERK (1) Ferroptosis (3) GABA Receptor (1) Guanylate Cyclase (1) iGluR (2) Isotope-Labeled Compounds (2) LRRK2 (2) nAChR (1) NF-κB (1) Opioid Receptor (1) P2X Receptor (1) Phosphodiesterase (PDE) (2) Potassium Channel (8) Reference Standards (4) Sodium Channel (7) TRP Channel (3)
By Research Areas:	Cancer (3) Cardiovascular Disease (7) Endocrinology (1) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (29)

Inhibitors & Agonists

Screening Libraries

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12650

Mirogabalin 5 Publications Verification DS5565	Calcium Channel	Neurological Disease
Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.

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-12345

ML365 Maximum Cited Publications 6 Publications Verification	Potassium Channel	Cardiovascular Disease
ML365 is a selective two-pore domain potassium channel KCNK3/TASK1 inhibitor, with an IC₅₀ of 4 nM. ML365 acts as a pharmacological tool that can be used to examine the specific roles of TASK1 channels .

HY-10035

TTA-P2 2 Publications Verification T-Type calcium channel inhibitor	Calcium Channel	Neurological Disease
TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC₅₀ = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy < sup>[4] .

HY-122697

ML418	Potassium Channel	Cardiovascular Disease Neurological Disease Endocrinology
ML418 is a potent, selective and CNS penetrating Kir7.1 potassium channel blocker. ML418 inhibits Kir7.1 with an IC₅₀ value of 0.31 μM. ML418 can be used for the research of neurological, cardiovascular, endocrine and muscle disorders.

HY-B0653A

Levobupivacaine hydrochloride 2 Publications Verification (S)-(-)-Bupivacaine monohydrochloride	Sodium Channel Ferroptosis	Cardiovascular Disease Neurological Disease Cancer
Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .

HY-152107

LRRK2-IN-7	LRRK2	Neurological Disease
LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC₅₀ of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes .

HY-101789

Nav1.7-IN-3	Sodium Channel	Neurological Disease
Nav1.7-IN-3 is a selective, orally bioavailable *voltage-gated sodium channel* Nav1.7 inhibitor with an IC₅₀** of 8 nM. Pain relief. Limited CNS penetration .

HY-137952

NS8593	Potassium Channel TRP Channel	Neurological Disease
NS8593 is an SK channel (small conductance Ca ²⁺-activated K+ channels) inhibitor. NS8593 reversibly inhibited recombinant SK3-mediated currents (human SK3 and rat SK3). NS8593 inhibits all the SK1-3 subtypes Ca ²⁺-dependently (K_d = 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca ²⁺). NS8593 does not affect the Ca ²⁺-activated K channels of intermediate and large conductance (hlk and hBK channels, respectively). NS8593 can also inhibit TRPM7 (melastatin-related TRP cation channel 7) (IC₅₀ = 1.6 mM). NS8593 can be used for the study of central nervous system (CNS) related diseases .

HY-108460

A-784168	TRP Channel	Neurological Disease
A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration .

HY-172182

ONO-2920632 VU6011887	Potassium Channel	Neurological Disease
ONO-2920632 is an orally active and central nervous system (CNS)-penetrant TREK activator, with EC₅₀ values of 0.3 µM and 2.8 μM for TREK-1 and TREK-2, respectively. ONO-2920632 exhibits selectivity for other K2P channels (>91-fold selective versus TASK1, TASK2, TASK3, TRAAK, and TWIK2; 31-fold selective versus TRESK). ONO-2920632 possesses analgesic effects and can be used in research on pain, migraine, and neurological disorders.

HY-B0653

Levobupivacaine 2 Publications Verification (S)-(-)-Bupivacaine	Sodium Channel Ferroptosis	Neurological Disease Cancer
Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .

HY-101809A

CNS 5161	iGluR	Cardiovascular Disease
CNS-5161 is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.

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-179004

ONO-9517601 VU6022856	Potassium Channel	Neurological Disease
ONO-9517601 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC₅₀= 0.067 μM, TREK-2 IC₅₀= 0.23 μM). ONO-9517601 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-9517601 can be used for research on neurological and cognitive disorders .

HY-50707

(Rac)-TTA-P2 (Rac)-T-Type calcium channel inhibitor	Calcium Channel Drug Isomer	Neurological Disease
(Rac)-TTA-P2 is the isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .

HY-123481

JNJ-42253432	P2X Receptor	Metabolic Disease
JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pK_i values of 9.1 and 7.9 for rat and human P2X7 channels, respectively .

HY-12596

JNJ-26489112	Calcium Channel Sodium Channel Potassium Channel	Neurological Disease
JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na ⁺ channels and N-type Ca ²⁺ channels, and is effective as a K ⁺ channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC₅₀=35 μM) and CA-I (18 μM) .

HY-152107A

(R,R)-LRRK2-IN-7	LRRK2	Neurological Disease
(R,R)-LRRK2-IN-7 is the isomer of LRRK2-IN-7 (HY-152107). LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes.

HY-12650S

Mirogabalin-13C2,d1 (Mixture of Diastereomers) DS5565-¹³C₂,d₁ (Mixture of Diastereomers)	Isotope-Labeled Compounds	Others
Mirogabalin- ¹³C₂,d₁ (Mixture of Diastereomers) is a ¹³C and deuterium labeled Mirogabalin. Mirogabalin (DS-5565) is a preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS .

HY-179005

ONO-7927846 VU6024391	Potassium Channel	Neurological Disease
ONO-7927846 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC₅₀= 0.11 μM, TREK-2 IC₅₀= 0.29 μM). ONO-7927846 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-7927846 can be used for research on neurological and cognitive disorders .

HY-147639

Cav 2.2/3.2 blocker 1	Calcium Channel	Neurological Disease
Cav 2.2/3.2 blocker 1 (Compound 9e) is a neuronal calcium channel blocker with IC₅₀ values of 78 μM and 80 μM against Ca_v2.2 and Ca_v3.2, respectively. Cav 2.2/3.2 blocker 1 can penetrate the CNS .

HY-10035A

(R)-TTA-P2	Calcium Channel	Neurological Disease
(R)-TTA-P2 is the isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .

HY-101809

CNS-5161 hydrochloride CNS 5161A	iGluR	Cardiovascular Disease
CNS-5161 hydrochloride is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.

HY-163855

KGP-25	Sodium Channel GABA Receptor	Neurological Disease
KGP-25 is an inhibitor of voltage-gated sodium channel 1.8 (Nav1.8), which can be used for analgesia by targeting Nav1.8 in the peripheral nervous system (PNS). KGP-25 can also target γ-aminobutyric acid subtype A receptor (GABA_A) in the central nervous system (CNS) for general anesthesia .

HY-12650R

Mirogabalin (Standard) DS5565 (Standard)	Reference Standards Calcium Channel	Neurological Disease
Mirogabalin (Standard) is the analytical standard of Mirogabalin. This product is intended for research and analytical applications. Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.

HY-B0653AS

Levobupivacaine-d9 hydrochloride (S)-(–)-Bupivacaie-d9hydrochloride	Isotope-Labeled Compounds Ferroptosis Sodium Channel	Cardiovascular Disease Neurological Disease Cancer
Levobupivacaine-d₉ ((S)-(–)-Bupivacaie-d₉) hydrochloride is deuterium labeled Levobupivacaine hydrochloride (HY-B0653A). Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .

HY-147377

N-Salicyloyltryptamine	Calcium Channel ERK Potassium Channel Guanylate Cyclase NF-κB	Cardiovascular Disease Neurological Disease Inflammation/Immunology
N-Salicyloyltryptamine acts on voltage-dependent Na ⁺, Ca ²⁺, and K ⁺ ion channels inhibitor. N-Salicyloyltryptamine inhibits K ⁺ currents with an IC₅₀ value of 34.6 μM (I_to). N-Salicyloyltryptamine also exhibits anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect ^- .

HY-122561

MK-1925	Opioid Receptor	Neurological Disease
MK-1925 is an orally active, CNS-penetrant ORL1 receptor antagonist with an IC₅₀ of 8.2 nM. MK-1925 selectively inhibits the ORL1 receptor and shows no significant activity against other opioid receptors or the hERG potassium channel .

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-101789R

Nav1.7-IN-3 (Standard)	Reference Standards Sodium Channel	Neurological Disease
Nav1.7-IN-3 (Standard) is the analytical standard of Nav1.7-IN-3 (HY-101789). This product is intended for research and analytical applications. Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC₅₀ of 8 nM. Pain relief. Limited CNS penetration .

HY-108460R

A-784168 (Standard)	Reference Standards TRP Channel	Neurological Disease
A-784168 (Standard) is the analytical standard of A-784168 (HY-108460). This product is intended for research and analytical applications. A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration .

HY-10035R

TTA-P2 (Standard) T-Type calcium channel inhibitor (Standard)	Calcium Channel Reference Standards	Neurological Disease
TTA-P2 (Standard) is the analytical standard of TTA-P2 (HY-10035). This product is intended for research and analytical applications. TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC50 = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy < sup> .

HY-180400

PAM-2	nAChR Calcium Channel	Neurological Disease
PAM-2 is a potent, orally active, CNS-penetrant selective α7 nAChR positive allosteric modulator (human α7 nAChR EC₅₀: 39 μM, rat α7 nAChR EC₅₀: 12 μM) with anti-nociceptive and anti-inflammatory activity. PAM-2 exhibits selectivity over α9α10 nAChR (IC₅₀ = 174 μM) and Ca_V2.2 channel (IC₅₀ = 89 μM). PAM-2 decreases Streptozotocin (STZ) (HY-13753)- and Oxaliplatin (HY-17371)-inducned nuroparhic pain in mice by α7 nAChR potentiation. PAM-2 can be used for the research of neuropathic pain .

Cat. No.	Product Name

HY-L070

Neuroprotective Compound Library	1,748 compounds
Neurodegenerative diseases are characterised by progressive dysfunction and death of neurons, such as Alzheimer’s disease, Parkinson’s disease, and multiple sclerosis (MS). Neuroprotection is an approach to preserve neurons so that neurons cannot be hurt by different pathological factors in neurodegenerative diseases. Neuroprotectors are some agonists and antagonists targeting some key targets in neuroprotactive signal pathways, such as calcium and sodium channel blockers, GABA receptor agonists, NMDA receptor Antagonists, etc. Current neuroprotectors cannot reverse existing damage, but they may protect against further nerve damage and slow down any degeneration of the central nervous system (CNS) and still play important roles in the treatment of neurodegenerative diseases. MCE offers a unique collection of 1,748 compounds with potential neuroprotective activities. These compounds mainly act on some key targets in neuroprotetive signal pathways, such as calcium channel, sodium channel, adenosine A1 receptor, etc. MCE Neuroprotective Compopund Library is a useful tool in neuroprotective drug discovery.

Neuroprotective Compound Library

1,748 compounds

Neurodegenerative diseases are characterised by progressive dysfunction and death of neurons, such as Alzheimer’s disease, Parkinson’s disease, and multiple sclerosis (MS). Neuroprotection is an approach to preserve neurons so that neurons cannot be hurt by different pathological factors in neurodegenerative diseases. Neuroprotectors are some agonists and antagonists targeting some key targets in neuroprotactive signal pathways, such as calcium and sodium channel blockers, GABA receptor agonists, NMDA receptor Antagonists, etc. Current neuroprotectors cannot reverse existing damage, but they may protect against further nerve damage and slow down any degeneration of the central nervous system (CNS) and still play important roles in the treatment of neurodegenerative diseases.

MCE offers a unique collection of 1,748 compounds with potential neuroprotective activities. These compounds mainly act on some key targets in neuroprotetive signal pathways, such as calcium channel, sodium channel, adenosine A1 receptor, etc. MCE Neuroprotective Compopund Library is a useful tool in neuroprotective drug discovery.

HY-L028

CNS-Penetrant Compound Library	1,096 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 1,096 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

1,096 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 1,096 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.

Cat. No.	Product Name	Chemical Structure

HY-12650S

Mirogabalin-13C2,d1 (Mixture of Diastereomers)
Mirogabalin- ¹³C₂,d₁ (Mixture of Diastereomers) is a ¹³C and deuterium labeled Mirogabalin. Mirogabalin (DS-5565) is a preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS .

HY-B0653AS

Levobupivacaine-d9 hydrochloride
Levobupivacaine-d₉ ((S)-(–)-Bupivacaie-d₉) hydrochloride is deuterium labeled Levobupivacaine hydrochloride (HY-B0653A). Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .

Levobupivacaine-d9 hydrochloride

Levobupivacaine-d₉ ((S)-(–)-Bupivacaie-d₉) hydrochloride is deuterium labeled Levobupivacaine hydrochloride (HY-B0653A). Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .

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