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Pathways Recommended:	Membrane Transporter/Ion Channel
Targets Recommended:	Sodium Channel Potassium Channel Chloride Channel TRP Channel Calcium Channel HCN Channel CRAC Channel SGLT Na+/K+ ATPase VDAC

Results for "

Sodium Channel

" in MCE Product Catalog:

By Targets:	Calcium Channel (168) Chloride Channel (22) CRAC Channel (8) HCN Channel (4) Potassium Channel (188) Sodium Channel (128) TRP Channel (55) VDAC (1) 5-HT Receptor (16) Adenosine Receptor (1) Adrenergic Receptor (3) AMPK (1) Amyloid-β (2) Angiotensin Receptor (2) Antibiotic (7) Apoptosis (26) Autophagy (29) Bacterial (12) Beta-secretase (1) CaMK (1) Cannabinoid Receptor (3) Carbonic Anhydrase (6) Caspase (2) CDK (1) CFTR (6) Complement System (1) COX (2) Cytochrome P450 (6) Dipeptidyl Peptidase (2) DNA/RNA Synthesis (2) Dopamine Receptor (7) Drug Metabolite (8) Endogenous Metabolite (21) ERK (3) Ferroptosis (2) FKBP (1) GABA Receptor (15) Gap Junction Protein (2) Glucocorticoid Receptor (2) GPCR19 (1) GPR119 (1) GPR139 (1) GPR40 (1) Gutathione S-transferase (2) HCV Protease (2) HIF/HIF Prolyl-Hydroxylase (1) Histamine Receptor (7) HIV (6) HSP (1) iGluR (13) IKK (1) Imidazoline Receptor (1) Influenza Virus (2) Interleukin Related (3) JAK (1) Lipoxygenase (1) mAChR (4) MCHR1 (GPR24) (2) MEK (3) Melatonin Receptor (1) mGluR (2) Mitochondrial Metabolism (2) Mitophagy (2) Monoamine Oxidase (4) Monoamine Transporter (1) Motilin Receptor (1) Na+/Ca2+ Exchanger (5) nAChR (3) Neuropeptide Y Receptor (2) NF-κB (9) NO Synthase (1) Opioid Receptor (1) P-glycoprotein (8) P2X Receptor (5) p38 MAPK (1) Parasite (21) Phosphatase (1) Phosphodiesterase (PDE) (6) Phospholipase (1) PKA (2) PKC (3) PPAR (1) Pyruvate Kinase (1) Reactive Oxygen Species (9) ROCK (2) SARS-CoV (1) Sigma Receptor (2) TGF-beta/Smad (3) TNF Receptor (3) Topoisomerase (3) Virus Protease (3)
By Research Areas:	Cancer (80) Cardiovascular Disease (197) Endocrinology (16) Infection (45) Inflammation/Immunology (86) Metabolic Disease (52) Neurological Disease (296)

By Targets:

Calcium Channel (168)

Chloride Channel (22)

CRAC Channel (8)

HCN Channel (4)

Potassium Channel (188)

Sodium Channel (128)

TRP Channel (55)

VDAC (1)

5-HT Receptor (16)

Adenosine Receptor (1)

Adrenergic Receptor (3)

AMPK (1)

Amyloid-β (2)

Angiotensin Receptor (2)

Antibiotic (7)

Apoptosis (26)

Autophagy (29)

Bacterial (12)

Beta-secretase (1)

CaMK (1)

Cannabinoid Receptor (3)

Carbonic Anhydrase (6)

Caspase (2)

CDK (1)

CFTR (6)

Complement System (1)

COX (2)

Cytochrome P450 (6)

Dipeptidyl Peptidase (2)

DNA/RNA Synthesis (2)

Dopamine Receptor (7)

Drug Metabolite (8)

Endogenous Metabolite (21)

ERK (3)

Ferroptosis (2)

FKBP (1)

GABA Receptor (15)

Gap Junction Protein (2)

Glucocorticoid Receptor (2)

GPCR19 (1)

GPR119 (1)

GPR139 (1)

GPR40 (1)

Gutathione S-transferase (2)

HCV Protease (2)

HIF/HIF Prolyl-Hydroxylase (1)

Histamine Receptor (7)

HIV (6)

HSP (1)

iGluR (13)

IKK (1)

Imidazoline Receptor (1)

Influenza Virus (2)

Interleukin Related (3)

JAK (1)

Lipoxygenase (1)

mAChR (4)

MCHR1 (GPR24) (2)

MEK (3)

Melatonin Receptor (1)

mGluR (2)

Mitochondrial Metabolism (2)

Mitophagy (2)

Monoamine Oxidase (4)

Monoamine Transporter (1)

Motilin Receptor (1)

Na+/Ca2+ Exchanger (5)

nAChR (3)

Neuropeptide Y Receptor (2)

NF-κB (9)

NO Synthase (1)

Opioid Receptor (1)

P-glycoprotein (8)

P2X Receptor (5)

p38 MAPK (1)

Parasite (21)

Phosphatase (1)

Phosphodiesterase (PDE) (6)

Phospholipase (1)

PKA (2)

PKC (3)

PPAR (1)

Pyruvate Kinase (1)

Reactive Oxygen Species (9)

ROCK (2)

SARS-CoV (1)

Sigma Receptor (2)

TGF-beta/Smad (3)

TNF Receptor (3)

Topoisomerase (3)

Virus Protease (3)

By Research Areas:

Cancer (80)

Cardiovascular Disease (197)

Endocrinology (16)

Infection (45)

Inflammation/Immunology (86)

Metabolic Disease (52)

Neurological Disease (296)

649

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas

HY-100257

Sodium Channel inhibitor 2
Sodium Channel Neurological Disease

Sodium Channel inhibitor 2 is a sodium channel blocker extracted from patent WO 2004011439 A2, compound 3c.

*Sodium Channel* inhibitor 2**	Sodium Channel	Neurological Disease
Sodium Channel inhibitor 2 is a sodium channel blocker extracted from patent WO 2004011439 A2, compound 3c.

HY-15736

*Sodium Channel* inhibitor 1**	Sodium Channel	Neurological Disease
Sodium Channel inhibitor1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment.

HY-108505

QX-314 chloride
Sodium Channel Neurological Disease

QX-314 chloride is a membrane-impermeable permanently charged sodium channel blocker.
HY-101350

QX-314 bromide
Sodium Channel Neurological Disease

QX-314 bromide is a membrane-impermeable permanently charged sodium channel blocker.

QX-314 chloride	Sodium Channel	Neurological Disease
QX-314 chloride is a membrane-impermeable permanently charged sodium channel blocker.

QX-314 bromide	Sodium Channel	Neurological Disease
QX-314 bromide is a membrane-impermeable permanently charged sodium channel blocker.

HY-B1243

Propoxycaine hydrochloride	Sodium Channel	Neurological Disease
Propoxycaine hydrochloride inhibits voltage-gated sodium channels, and thereby inhibits the ionic flux required for the initiation and conduction of impulses. Propoxycaine hydrochloride application can lead to a loss of sensation.

HY-107695

Remacemide hydrochloride FPL 12924AA	iGluR Sodium Channel	Neurological Disease
Remacemide hydrochloride (FPL 12924AA), a moderate inhibitor of the Na⁺ channel, is a weak uncompetitive NMDA receptor antagonist with IC₅₀s of 68 μM and 76 μM for MK-801 binding and NMDA currents, respectively. Remacemide hydrochloride is an anticonvulsant agent.

HY-U00135

Calcium channel-modulator-1
Calcium Channel Cardiovascular Disease

Calcium channel-modulator-1 is a calcium channel modulator; blocks aortic contraction with an IC₅₀ of 0.8 μM.
HY-75867

M2 ion channel blocker
Influenza Virus Infection

M2 ion channel blocker is capable of inhibiting and blocking the activity of M2 ion channel;Antiviral agent.

*Calcium channel-modulator-1*	Calcium Channel	Cardiovascular Disease
Calcium channel-modulator-1 is a calcium channel modulator; blocks aortic contraction with an IC₅₀ of 0.8 μM.

*M2 ion channel* blocker**	Influenza Virus	Infection
M2 ion channel blocker is capable of inhibiting and blocking the activity of M2 ion channel;Antiviral agent.

HY-117714

AZD-3161	Sodium Channel	Neurological Disease
AZD-3161 is a potent and selective blocker of Na_V1.7 channel, with a pIC₅₀ of 7.1. AZD-3161 can be used for the research of neuropathic and inflammatory pain.

HY-122001

PF-05186462	Sodium Channel	Neurological Disease
PF-05186462 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channel, with an IC₅₀ of 21 nM. PF-05186462 shows significant selectivity for Nav1.7 versus other sodium channels (Nav 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, and 1.8). PF-05186462 can be used for the research of acute or chronic pain.

HY-16952A

Bepridil hydrochloride hydrate (±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate	Calcium Channel	Cardiovascular Disease
Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca⁺ channel antagonist and Na⁺, K⁺ channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na⁺/Ca2⁺ exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders.

HY-B1704A

Nisoxetine hydrochloride	Monoamine Transporter Sodium Channel	Neurological Disease
Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a K_d of 0.76 nM. Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.

HY-100310

*N-type calcium channel* blocker-1**	Calcium Channel	Neurological Disease
N-type calcium channel blocker-1 is an orally active analgesic agent which shows high affinity to functionally block N-type calcium channels with an IC₅₀ of 0.7 μM in the IMR32 assay.

HY-B0114

Oxcarbazepine GP 47680	Sodium Channel Apoptosis	Cancer Neurological Disease
Oxcarbazepine is a sodium channel blocker. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines. Anti-cancer and anticonvulsant effects.

HY-41076

*Ca2+ channel* agonist 1**	Calcium Channel CDK	Neurological Disease
Ca²⁺ channel agonist 1 is an agonist of N-type Ca²⁺ channel and an inhibitor of Cdk2, with EC₅₀s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.

HY-P1218

Phrixotoxin 3	Sodium Channel	Neurological Disease
Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC₅₀s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.

HY-P1218A

Phrixotoxin 3 TFA	Sodium Channel	Neurological Disease
Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC₅₀s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.

HY-U00280

*Potassium Channel* Activator 1**	Others	Neurological Disease
Potassium Channel Activator 1 is an agent for treating, one or more disorders or conditions wherein the dopaminergic system is disrupted, such as one or more disorders or conditions independently selected from the group consisting of: schizophrenia and other psychotic states; mood disorders ADHD; aggression; movement disorders.

HY-B0834

Indoxacarb (±)-Indoxacarb	Sodium Channel	Neurological Disease
Indoxacarb ((±)-Indoxacarb) is a broad-spectrum oxadiazine insecticide. Indoxacarb is metabolized in vivo to its active N-decarbomethoxyllated metabolite DCJW. Indoxacarb suppresses voltage-gated sodium channel currents in rat dorsal root ganglion neurons.

HY-17612

Evenamide NW-3509	Sodium Channel	Neurological Disease
Evenamide (NW-3509) is an orally available *voltage-gated sodium channel* (VGSC) blocker (K_i**=0.4 µM) for the research of schizophrenia. Evenamide shows efficacy in a broad spectrum of rodent models of psychosis, mania, depression, and aggressiveness.

HY-11079

A-803467	Sodium Channel	Inflammation/Immunology Neurological Disease
A-803467 is a potent and selective tetrodotoxin-resistant Na_v1.8 sodium channel blocker (IC₅₀=8 nM). A-803467 has shown significant anti-nociception in neuropathic and inflammatory pain models. A-803467 enhances the chemosensitivity of conventional anticancer agents through interaction with the ATP-binding cassette subfamily G member 2 (ABCG2) transporter.

HY-P1220

Huwentoxin-IV	Sodium Channel	Neurological Disease
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC₅₀s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain.

HY-P1220A

Huwentoxin-IV TFA	Sodium Channel	Neurological Disease
Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC₅₀s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain.

HY-B0124A

Zonisamide sodium AD 810 Sodium; CI 912 Sodium	Carbonic Anhydrase Calcium Channel Sodium Channel	Neurological Disease
Zonisamide sodium (AD 810 sodium) is an inhibitor of zinc enzyme carbonic anhydrase (CA), with K_is of 35.2 nM and 20.6 nM for human mitochondrial isozyme hCA II and hCA V, respectively. Zonisamide sodium has antiepileptic activity. Zonisamide sodium can be used for the rsearch for epilepsy, seizures and Parkinson's disease.

HY-B0124

Zonisamide AD 810; CI 912	Carbonic Anhydrase Calcium Channel Sodium Channel	Neurological Disease
Zonisamide (AD 810) is an inhibitor of zinc enzyme carbonic anhydrase (CA), with K_is of 35.2 nM and 20.6 nM for human mitochondrial isozyme hCA II and hCA V, respectively. Zonisamide has antiepileptic activity. Zonisamide can be used for the rsearch for epilepsy, seizures and Parkinson's disease.

HY-18940A

Cilobradine hydrochloride
DK-AH 269
HCN Channel Cardiovascular Disease

Cilobradine is an HCN Channel blocker; an open channel blocker of neuronal Ih and related cardiac If channels.

Cilobradine hydrochloride DK-AH 269	HCN Channel	Cardiovascular Disease
Cilobradine is an HCN Channel blocker; an open channel blocker of neuronal Ih and related cardiac If channels.

HY-P1078

Huwentoxin XVI	Calcium Channel	Neurological Disease
Huwentoxin XVI, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC₅₀ of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels.

HY-P1078A

Huwentoxin XVI TFA	Calcium Channel	Neurological Disease
Huwentoxin XVI TFA, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC₅₀ of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI TFA has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels.

HY-17404

Cilnidipine FRC-8653	Calcium Channel	Cardiovascular Disease
Cilnidipine is a long-acting, second-generation dihydropyridine Ca²⁺-channel blocker on L and N-type Ca²⁺ channel. Antihypertensive effects.

HY-N5101

Kobusin	CFTR Chloride Channel	Inflammation/Immunology Neurological Disease
Kobusin is a bisepoxylignan isolated from the Pnonobio biondii Pamp. Kobusin is an activator of CFTR and CaCCgie chloride channels and a inhibitor of ANO1/CaCC (calcium-activated chloride channel) channel.

HY-U00309

YM758
Others Cardiovascular Disease

YM758 is a “funny” I_f current channel (I_f channel) inhibitor.

YM758	Others	Cardiovascular Disease
YM758 is a “funny” I_f current channel (I_f channel) inhibitor.

HY-10588

Bay K 8644	Calcium Channel	Neurological Disease
Bay K 8644, a dihydropyridine compound, is a specific L-type Ca²⁺ channel agonist. Bay K 8644 increases Ca2+ influx through sarcolemmal Ca²⁺ channels by increasing the open time of the channel.

HY-15416

NS309	Potassium Channel	Neurological Disease Cardiovascular Disease
NS309 is a potent and selective activator of the Ca²⁺-activated SK/IK potassium channels, but displays no activity at BK channels.

HY-B1221

Flufenamic acid	COX AMPK Potassium Channel Chloride Channel Calcium Channel Parasite	Inflammation/Immunology
Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca²⁺ channels, modulating non-selective cation channels (NSC), activating K⁺ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.

HY-12949

ML204	TRP Channel	Neurological Disease
ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca²⁺ channels.

HY-P0189

ω-Conotoxin GVIA
Calcium Channel Neurological Disease

ω-Conotoxin GVIA is an inhibitor of the N-type Ca²⁺ channel.

ω-Conotoxin GVIA	Calcium Channel	Neurological Disease
ω-Conotoxin GVIA is an inhibitor of the N-type Ca²⁺ channel.

HY-12949A

ML204 hydrochloride	TRP Channel	Neurological Disease
ML204 hydrochloride is a novel, potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca²⁺ channels.

HY-131942

sFTX-3.3
Calcium Channel Neurological Disease

sFTX-3.3 is a Ca²⁺ channel antagonist with IC₅₀s of approximately 0.24 mM and 0.70 mM against P-type and N-type channels.
HY-P0189A

ω-Conotoxin GVIA TFA
Calcium Channel Neurological Disease

ω-Conotoxin GVIA TFA is an inhibitor of the N-type Ca²⁺ channel.

sFTX-3.3	Calcium Channel	Neurological Disease
sFTX-3.3 is a Ca²⁺ channel antagonist with IC₅₀s of approximately 0.24 mM and 0.70 mM against P-type and N-type channels.

ω-Conotoxin GVIA TFA	Calcium Channel	Neurological Disease
ω-Conotoxin GVIA TFA is an inhibitor of the N-type Ca²⁺ channel.

HY-108592

UCL 2077	Others	Neurological Disease
UCL 2077 is a selective slow-afterhyperpolarization (sAHP) channel blocker (IC₅₀ = 500 nM in hippocampal neurons in culture), having minimal effects on Ca2+ channels, action potentials, input resistance and the medium after hyperpolarization. UCL 2077 is also a subtype-selective blocker of the epilepsy associated KCNQ channels.

HY-105917

Endovion NS3728	Chloride Channel	Others
Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.

HY-18723

Yoda 1
Others Cardiovascular Disease

Yoda 1 is a Piezo1 agonist. Yoda 1 activates purified Piezo1 channels.

Yoda 1	Others	Cardiovascular Disease
Yoda 1 is a Piezo1 agonist. Yoda 1 activates purified Piezo1 channels.

HY-B0545S

Probenecid-d14	TRP Channel Bacterial HIV	Metabolic Disease
Probenecid-d14 is the deuterium labeled Probenecid. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels.

HY-17451

Glibornuride
Potassium Channel Metabolic Disease

Glibornuride is a blocker of ATP-sensitive K⁺ channels (K_ATP channel) with a pK_i of 5.75. Antidiabetic agent.

Glibornuride	Potassium Channel	Metabolic Disease
Glibornuride is a blocker of ATP-sensitive K⁺ channels (K_ATP channel) with a pK_i of 5.75. Antidiabetic agent.

HY-P1221

ProTx II	Sodium Channel	Neurological Disease
ProTx II is a selective blocker of Nav1.7 sodium channels with an IC₅₀ of 0.3 nM, and is at least 100-fold selective for Nav1.7 over other sodium channel subtypes. ProTx-II inhibits sodium channels by decreasing channel conductance and shifting activation to more positive potentials and blocks action potential propagation in nociceptors.

HY-128933

AMP-PNP tetralithium Adenylyl-imidodiphosphate tetralithium	Potassium Channel	Metabolic Disease
AMP-PNP tetralithium (Adenylyl-imidodiphosphate tetralithium) is a non-hydrolysable analogue of ATP and inhibits K_ATP channels.

HY-14183

Vernakalant Hydrochloride RSD1235 hydrochloride	Potassium Channel	Cardiovascular Disease
Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na⁺ and atria-preferred K⁺ channel blocker. IC₅₀ for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for *Kv1.5 channel* wt, Kv1.5 channel I508F, Kv1.5 channel T479A**, respectively.

HY-12796A

Raxatrigine hydrochloride GSK-1014802 hydrochloride; CNV1014802 hydrochloride	Sodium Channel	Neurological Disease
Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.

HY-12796

Raxatrigine GSK-1014802; CNV1014802	Sodium Channel	Neurological Disease
Raxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.

HY-12345

ML365	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-110153

NS19504	Potassium Channel	Neurological Disease
NS19504 is a Ca²⁺-activated K⁺ channel (BK channel, KCa1.1 channel) activator (EC₅₀=11.0 µM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions.

HY-P1073

ProTx-I	Calcium Channel Sodium Channel Potassium Channel	Cancer
ProTx-I, a venom toxin of the tarantula Thrixopelma pruriens, is a potent, selective Ca_V3.1 channel blocker with IC₅₀ values of 0.2 μM and 31.8 μM for hCa_V3.1 and hCa_V3.2 respectively. ProTx-I is also a potent blocker for voltage-gated Na⁺ channels and inhibits K_V 2.1 channels.

HY-B0545

Probenecid	TRP Channel Bacterial HIV	Metabolic Disease
Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels.

HY-135412

N-Methyl Duloxetine hydrochloride	Sodium Channel	Neurological Disease
N-Methyl Duloxetine hydrochloride is an analgesic. N-Methyl Duloxetine (hydrochloride) elicits both tonic and use-dependent block of neuronal Na⁺ channels.

HY-111325

Synta66	CRAC Channel	Neurological Disease
Synta66 is an inhibitor of store-operated calcium entry channel Orai, which forms the pore of the CRAC channel, and used for the research of neurological disease.

HY-100623

Dofetilide N-oxide UK-116856	Potassium Channel	Cardiovascular Disease
Dofetilide N-oxide (UK-116856) is a metabolite of Dofetilide. Dofetilide is a class III antiarrhythmic agent that blocks potassium channels.

HY-B0653A

Levobupivacaine hydrochloride
(S)-(-)-Bupivacaine monohydrochloride
Sodium Channel Neurological Disease

Levobupivacaine hydrochloride is a sodium channel blocker.
HY-N2077

Heteroclitin D
Calcium Channel Metabolic Disease

Heteroclitin D is a lignin from Kadsura medicinal plants with anti-liqid peroxidation. Heteroclitin D inhibits L-type calcium channels.

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-B0341

Nicorandil SG-75	Potassium Channel	Cardiovascular Disease
Nicorandil (SG-75) is a potent potassium channel activator and targets vascular nucleoside diphosphate-dependent K⁺ channels and cardiac ATP-sensitive K⁺ channels (K_ATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases.

HY-P0190

Iberiotoxin	Potassium Channel	Cardiovascular Disease
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca²⁺-activated K⁺ channel inhibitor with a K_d of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels.

HY-101942

Zegocractin CM-4620	CRAC Channel	Neurological Disease
Zegocractin (CM-4620) is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC₅₀s of 119 nM and 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.

HY-133910

Lu AE98134	Sodium Channel	Neurological Disease
Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Na_v1.1 channels positive modulator. Lu AE98134 also increases the activity of Na_v1.2 and Na_v1.5 channels but not of Na_v1.4, Na_v1.6 and Na_v1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Na_v1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al.

HY-16915

RPR-260243	Potassium Channel	Cardiovascular Disease
RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivation of hERG1 channels. RPR260243-modified HERG currents are inhibited by Dofetilide (IC₅₀=58 nM). RPR260243 displays no activator-like effects on other voltage-dependent ion channels, including the closely related ERG3 K+ channel.

HY-P1424

Lei-Dab7	Potassium Channel	Neurological Disease
Lei-Dab7 is a potent and selective SK2 (KCa2.2) channels blocker with a K_d of 3.8 nM. Lei-Dab7 shows low or no activity on KCa1, KCa3, Kv and Kir2.1 channels.

HY-122697

ML418	Potassium Channel	Neurological Disease
ML418 is the first potent, selective and CNS penetrating blocker of Kir7.1 potassium channel (IC₅₀, 310 nM), which also potently inhibits Kir6.2/SUR1, and exhibits superior selectivity over other Kir channels.

HY-Z0816

Dehydronitrosonisoldipine
Calcium Channel Others

Dehydronitrosonisoldipine is a calcium channel antagonist.
HY-101674

Tiapamil hydrochloride
Ro 11-1781
Calcium Channel Cardiovascular Disease

Tiapamil hydrochloride is a calcium channel blocker.
HY-101383

PF-01247324
Sodium Channel Neurological Disease

PF-01247324 is a selective and orally bioavailable Na_v1.8 channel blocker with an IC₅₀ of 196 nM for recombinant human Na_v1.8 channel.

HY-B0262S

Methocarbamol D5	Sodium Channel	Metabolic Disease
Methocarbamol D5 is deuterium labeled Methocarbamol. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel.

HY-108584

Flindokalner BMS-204352	Potassium Channel	Neurological Disease
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (K_i=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.

HY-136232

PSEM 308 hydrochloride	Others	Neurological Disease
PSEM 308 hydrochloride is a pharmacologically selective actuator module (PSAM) agonist. PSEM 308 Activates PSAML141F-GlyR chimeric ion channels.

HY-B1798A

Tocainide hydrochloride	Sodium Channel	Inflammation/Immunology
Tocainide hydrochloride is a sodium channel blocker, it blocks the sodium channels in the pain-producing foci in the nerve membranes. Tocainide hydrochloride is a primary amine analog of lidocaine, can be used for the treatment of tinnitus.

HY-W040265

Fenamic acid
N-Phenylanthranilic acid
Chloride Channel Inflammation/Immunology

Fenamic acid is a chloride channel blocker.
HY-B0246

Carbamazepine
CBZ; NSC 169864
Sodium Channel Autophagy Mitophagy Neurological Disease Cancer

Carbamazepine, a sodium channel blocker, is an anticonvulsant drug.
HY-B0984

Fendiline hydrochloride
Calcium Channel Cardiovascular Disease

Fendiline hydrochloride is a nonselective calcium channel blocker.
HY-101621

Teludipine hydrochloride
GR53992B; GX1296B
Calcium Channel Cancer

Teludipine is a lipophilic calcium channel blocker.
HY-14290A

Pinacidil monohydrate
Potassium Channel Others

Pinacidil monohydrate, an antihypertensive drug, is a potassium channel activator.
HY-101069

Y-26763
Potassium Channel Cardiovascular Disease

Y-26763 is a K⁺ channel opener and active metabolite of Y-27152. Y-26763 is an ATP-sensitive K⁺ (K_ATP) channel activator.

HY-N2338

Cholesterol myristate Cholesteryl myristate; Cholesteryl tetradecanoate	nAChR GABA Receptor Potassium Channel Endogenous Metabolite	Cancer
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.

HY-108586

NS3623	Potassium Channel	Neurological Disease
NS3623 is an activator of human ether-a-go-go-related gene (hERG1/K_V11.1) potassium channels. NS3623 activates the IKr and Ito currents and has antiarrhythmic effect. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels.

HY-13103

NS 11021	Potassium Channel	Others
NS 11021 is a potent and specific Ca²⁺-activated big-conductance K⁺ Channels (KCa1.1 channels) activator. NS 11021 at concentrations above 0.3 μM activates KCa1.1 in a concentration-dependent manner by parallelshifting the channel activation curves to more negative potentials.

HY-136564A

DAD	Potassium Channel	Neurological Disease
DAD is a type of ion channel blocker that blocks voltage-gated potassium channels. DAD is a third-generation photoswitch that responds to visible light. DAD has the potential for restoring visual function.

HY-14462

NP118809 39-1B4	Calcium Channel	Cardiovascular Disease
NP118809 is a potent N-type calcium channel blocker, with an IC₅₀ of 0.11 μM; also less potently inhibits L-type calcium channel with an IC₅₀ of 12.2 μM.

HY-101012

NPPB
Chloride Channel Neurological Disease

NPPB is a blocker of the outwardly rectifying chloride channel (ORCC).
HY-105117

Fantofarone
SR 33557
Calcium Channel Parasite Infection

Fantofarone is a highly potent Calcium Channel antagonist.

HY-12515A

Nicardipine hydrochloride YC-93	Calcium Channel Autophagy	Neurological Disease
Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC₅₀ of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.

HY-101428

NS-638	Calcium Channel	Neurological Disease
NS-638 is a small nonpeptide molecule with Ca²⁺-channel blocking properties. K⁺-stimulated intracellular Ca²⁺-elevation is blocked with an IC₅₀ value of 3.4 μM.

HY-18662

RQ-00203078	TRP Channel	Cancer Neurological Disease
RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC₅₀s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels.

HY-P1080

ω-Agatoxin IVA	Calcium Channel	Neurological Disease
ω-Agatoxin IVA is a potent, selective P/Q type Ca²⁺ channel blocker with IC₅₀s of 2 nM and 90 nM for P-type and Q-type Ca²⁺ channels, respectively. ω-Agatoxin IVA (IC₅₀, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA has no effect on L-type or N-type calcium channels.

HY-16126

Carboxyamidotriazole L-651582; CAI	Calcium Channel	Cancer Inflammation/Immunology
Carboxyamidotriazole (L-651582) is a cytostatic inhibitor of nonvoltage-operated calcium channels and *calcium channel-mediated signaling pathways*. Carboxyamidotriazole shows anti-tumor, anti-inflammatory and antiangiogenic effects.

HY-135407S

N-Desethyl Oxybutynin D5 hydrochloride	Drug Metabolite	Neurological Disease
N-Desethyl Oxybutynin D5 hydrochloride is deuterium labeled N-Desethyl Oxybutynin hydrochloride. N-Desethyl Oxybutynin is the the active metabolite Oxybutynin. Oxybutynin is an anticholinergic agent that inhibits voltage-dependent K⁺ channels.

HY-U00218

McN5691
RWJ26240
Calcium Channel Cardiovascular Disease

McN5691 is a voltage-sensitive calcium channel blocker.
HY-B0768A

Lomerizine dihydrochloride
KB-2796
Calcium Channel Neurological Disease

Lomerizine dihydrochloride is an antagonist of L- and T-type voltagegated calcium channels.
HY-B0567

Dequalinium Chloride
Potassium Channel Infection

Dequalinium Chloride is a selective blocker of apamin-sensitive K+ channels.
HY-101740

SQ-31765
SQ31765; SQ 31765
Calcium Channel Cardiovascular Disease

SQ-31765 is a benzazepine calcium channel blocker.
HY-B0419

Manidipine
Calcium Channel Cardiovascular Disease

Manidipine is a calcium channel blocker that is used clinically as an antihypertensive.

HY-U00201

KRN4884	Potassium Channel	Cardiovascular Disease
KRN4884 is a K⁺ channel opener. In the presence of intracellular ATP (1 mM), KRN4884 (0.1-3 μM) activates K_ATP channels in a concentration-dependent manner (EC₅₀=0.55 μM).

HY-136564

DAD dichloride	Potassium Channel	Neurological Disease
DAD dichloride is a type of ion channel blocker that blocks voltage-gated potassium channels. DAD dichloride is a third-generation photoswitch that responds to visible light. DAD dichloride has the potential for restoring visual function.

HY-12515

Nicardipine YC-93 free base	Calcium Channel	Neurological Disease
Nicardipine (YC-93 free base) is a calcium channel blocker with an IC₅₀ of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.

HY-12545

Brevetoxin-3 PbTx-3	Sodium Channel	Inflammation/Immunology
Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na⁺ channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na⁺ channels, inhibits the inactivation of Na⁺ channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.

HY-B0341S

Nicorandil-d4	Potassium Channel	Cardiovascular Disease
Nicorandil-d4 (SG-75-d4) is the deuterium labeled Nicorandil. Nicorandil (SG-75) is a potent potassium channel activator and targets vascular nucleoside diphosphate-dependent K⁺ channels and cardiac ATP-sensitive K⁺ channels (K_ATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases.

HY-110358

QAQ dichloride	Sodium Channel	Inflammation/Immunology
QAQ dichloride, a photoswitchable voltage-gated Na_v and K_v channels blocker, blocks channels in its trans form (of the azobenzene photoswitch), but not in its cis form. QAQ dichloride is membrane-impermeant and only infiltrates pain-sensing neurons that express endogenous import channels. QAQ dichloride acts as a light-sensitive analgesic and can be used for studying of signaling mechanisms in acute and chronic pain.

HY-112075

Lidoflazine	Potassium Channel Calcium Channel	Cardiovascular Disease
Lidoflazine is a high affinity blocker of the HERG (human ether-a-go-go-related gene) K⁺ channel. Lidoflazine is an antianginal calcium channel blocker that carries a significant risk of QT interval prolongation and ventricular arrhythmia.

HY-W011509

CyPPA	Potassium Channel	Neurological Disease
CyPPA is a positive modulator of hSK3 and hSK2, with EC₅₀ values of 14 μM and 5.6 μM, repectively. CyPPA is inactive on both hSK1 and hIK channels^[1]

HY-14255

Levcromakalim
(-)-Cromakalim; BRL 38227
Potassium Channel Cardiovascular Disease

Levcromakalim ((-)-Cromakalim) is an ATP-sensitive K⁺ channel (K_ATP) activator.
HY-B0347

Lacidipine
Calcium Channel Reactive Oxygen Species Apoptosis Cardiovascular Disease

Lacidipine (Lacipil, Motens) is a L-type calcium channel blocker.
HY-101422

GAL-021
Potassium Channel Inflammation/Immunology

GAL-021 a new intravenous BKCa-channel blocker.
HY-U00173

U89232
Potassium Channel Cardiovascular Disease

U-89232 appears to be a cardioselective K_ATP channel opener.
HY-103315

Bepridil hydrochloride
CERM 1978
Calcium Channel Cardiovascular Disease

Bepridil hydrochloride (CERM 1978) is a calcium channel blocker, with antianginal activity.
HY-101843

ML213
Potassium Channel Neurological Disease

ML213 is a selective activator of Kv7.2 and Kv7.4 channels, enhances Kv7.2 and Kv7.4 channels with EC₅₀s of 230 and 510 nM, respectively.

HY-108582

Y-27152	Potassium Channel	Cardiovascular Disease
Y-27152, a prodrug of the K_ATP (Kir6) channel opener Y-26763, is a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state.

HY-108335

Sipatrigine 619C89; BW 619C89	Sodium Channel Calcium Channel	Neurological Disease
Sipatrigine (619C89), a neuroprotective agent, is a glutamate release inhibitor, voltage-dependent sodium channel and calcium channel inhibitor, penetrating the central nervous system. Has the potential in the study for focal cerebral ischemia and stroke.

HY-112705

VU0529331	Potassium Channel	Neurological Disease
VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC₅₀s of 5.1 µM and 5.2 µM for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.

HY-110105

NS8593 hydrochloride	Potassium Channel	Neurological Disease
NS8593 hydrochloride is a potent and selective small conductance Ca²⁺-activated K⁺ channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a K_d value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca²⁺-dependently (K_ds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca²⁺), and does not affect the Ca²⁺-activated K⁺ channels of intermediate and large conductance (hIK and hBK channels, respectively).

HY-B1378S

Ethosuximide-d3	Calcium Channel	Neurological Disease
Ethosuximide-d3 is the deuterium labeled Ethosuximide. Ethosuximide, a widely prescribed anti-epileptic drug, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.

HY-Z1897S

N-Methyl duloxetine-d7	Sodium Channel	Neurological Disease
N-Methyl duloxetine-d7 is the deuterium labeled N-Methyl Duloxetine. N-Methyl Duloxetine is an analgesic. N-Methyl Duloxetine elicits both tonic and use-dependent block of neuronal Na⁺ channels.

HY-116448

Metaflumizone
BAS-320I
Sodium Channel Parasite Infection

Metaflumizone is a semicarbazone insecticide, acts as a potent sodium channel blocker.
HY-B0401

Tolbutamide
Potassium Channel Autophagy Metabolic Disease Cancer

Tolbutamide is a first generation potassium channel blocker, sulfonylurea oral hypoglycemic drug.
HY-B1109

N-Acetylprocainamide
Acecainide; NAPA
Potassium Channel Drug Metabolite Cardiovascular Disease

N-Acetylprocainamide is a class III antiarrhythmic, which blocks K⁺ channels.
HY-B2136

Tannic acid
Potassium Channel Cancer Inflammation/Immunology

Tannic acid is a novel hERG channel blocker with IC₅₀ of 3.4 μM.
HY-100572

Nicainoprol
RU-42924
Sodium Channel Cardiovascular Disease

Nicainoprol is a fast-sodium-channel blocking drug, which is a potent antiarrhythmic agent.
HY-14256

BMS-191095
Potassium Channel Metabolic Disease

BMS-191095 is an activators of mitochondrial ATP-sensitive potassium (mitoKATP) channels.
HY-U00236

PD0176078
Calcium Channel Cardiovascular Disease

PD0176078 is a newly found N-type Calcium channel blocker.
HY-N2164

3-Deoxyaconitine
Sodium Channel Others

3-Deoxyaconitine a diterpenoid alkaloid, is a sodium channel activator.

HY-15553A

Mibefradil dihydrochloride Ro 40-5967 dihydrochloride	Calcium Channel	Cardiovascular Disease
Mibefradil dihydrochloride (Ro 40-5967 dihydrochloride) is a calcium channel blocker with moderate selectivity for T-type Ca²⁺ channels (IC₅₀s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively).

HY-B0285

Amiloride MK-870	Sodium Channel TRP Channel Apoptosis	Metabolic Disease Cardiovascular Disease
Amiloride (MK-870) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride is a blocker of polycystin-2 (PC2; TRPP2) channel.

HY-B0285A

Amiloride hydrochloride MK-870 hydrochloride	Sodium Channel TRP Channel Apoptosis	Metabolic Disease Cardiovascular Disease
Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride is a blocker of polycystin-2 (PC2; TRPP2) channel.

HY-P1079

ω-Agatoxin TK	Calcium Channel	Neurological Disease
ω-Agatoxin TK, a peptidyl toxin of the venom of Agelenopsis aperta, is a potent and selective P/Q type Ca²⁺ channel blocker. ω-Agatoxin TK inhibits the high K⁺ depolarisation-induced rise in internal Ca²⁺ in cerebral isolated nerve endings with an IC₅₀ of of 60 nM. ω-Agatoxin TK has no effect on L-type, N-type, or T-type calcium channels.

HY-P1077

CALP1	Calcium Channel mGluR Phosphodiesterase (PDE) Apoptosis	Inflammation/Immunology
CALP1 is a calmodulin (CaM) agonist (K_d of 88 µM) with binding to the CaM EF-hand/Ca²⁺-binding site. CALP1 blocks calcium influx and apoptosis (IC₅₀ of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity.

HY-15553

Mibefradil Ro 40-5967	Calcium Channel	Cardiovascular Disease
Mibefradil (Ro 40-5967) is a calcium channel blocker with moderate selectivity for T-type Ca²⁺ channels displaying IC₅₀s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively.

HY-N2433

Paederosidic acid methyl ester	Potassium Channel	Neurological Disease
Paederosidic acid methyl ester is a ATP‐sensitive K⁺ channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K⁺ channel in the brain and spinal cord level.

HY-12507

GSK-7975A
Calcium Channel Inflammation/Immunology

GSK-7975A is a potent and orally available CRAC channel inhibitor.
HY-N3463

Isopimaric acid
Potassium Channel Neurological Disease

Isopimaric acid is a potent opener of large conductance calcium activated K⁺ (BK) channels.
HY-P0191

Charybdotoxin
Potassium Channel Inflammation/Immunology

Charybdotoxin, a 37-amino acid peptide, is a K⁺ channel blocker.
HY-P0163

Gramicidin
Bacterial Antibiotic Infection

Gramicidin is an antimicrobial peptide assembling as channels in membranes and increasing their permeability towards cations.
HY-109077

Tigolaner
GABA Receptor Infection Neurological Disease

Tigolaner is a GABA antagonist that regulates chloride channel. Tigolaner is an antiparasitic agent.
HY-U00044

Anipamil
Calcium Channel Cardiovascular Disease

Anipamil is a long-acting calcium channel blocker, used for the treatment of cardiovascular disease.

HY-12778

Ivabradine metabolite N-Demethyl Ivabradine hydrochloride N-Demethyl ivabradine hydrochloride	Drug Metabolite	Cardiovascular Disease Endocrinology Cancer
N-Demethyl Ivabradine Hcl is a metabolite of Ivabradine, which is a specific inhibitor of the funny channel.

HY-14284

Nilvadipine
FK235; FR34235
Calcium Channel Cardiovascular Disease

Nilvadipine is a potent calcium channel antagonist, and the IC₅₀ value is around 0.1 nM.
HY-14656

Diltiazem hydrochloride
CRD-401
Calcium Channel Cardiovascular Disease

Diltiazem hydrochloride is a Ca²⁺ influx inhibitor (slow channel blocker or calcium antagonist).

HY-B1448

Benidipine hydrochloride KW-3049	Calcium Channel	Cardiovascular Disease
Benidipine hydrochloride is a dihydropyridine calcium channel blocker for the treatment of high blood pressure (hypertension).

HY-113147

L-Palmitoylcarnitine	Potassium Channel Endogenous Metabolite	Metabolic Disease Cardiovascular Disease
L-Palmitoylcarnitine, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia. L-Palmitoylcarnitine inhibits K_ATP channel activity, without affecting the single channel conductance, through interaction with Kir6.2.

HY-12515AS

Nicardipine D3 hydrochloride YC-93 D3	Calcium Channel	Neurological Disease
Nicardipine D3 hydrochloride (YC-93 D3) is the deuterium labeled Nicardipine hydrochloride. Nicardipine hydrochloride is a calcium channel blocker with an IC₅₀ of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.

HY-113147A

L-Palmitoylcarnitine chloride	Potassium Channel Endogenous Metabolite	Metabolic Disease Cardiovascular Disease
L-Palmitoylcarnitine chloride, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia. L-Palmitoylcarnitine chloride inhibits K_ATP channel activity, without affecting the single channel conductance, through interaction with Kir6.2.

HY-W032013

1-Octanol Octanol	Calcium Channel Endogenous Metabolite	Metabolic Disease Neurological Disease
1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC₅₀ of 4 μM for native T-currents. 1-Octanol is a highly attractive biofuel with diesel-like properties.

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 Ca²⁺ 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-108573

P-1075	Potassium Channel	Cardiovascular Disease
P-1075 is a potent activator of *sulfonylurea receptor 2-associated ATP-sensitive potassium channels* (SUR2-K_IR6), with an EC₅₀** value of 45 nM for SUR2B-K_IR6 channel activation. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts.

HY-P1077A

CALP1 TFA	Calcium Channel mGluR Phosphodiesterase (PDE) Apoptosis	Inflammation/Immunology
CALP1 TFA is a calmodulin (CaM) agonist (K_d of 88 µM) with binding to the CaM EF-hand/Ca²⁺-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC₅₀ of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity.

HY-B0317

Amlodipine	Calcium Channel	Cancer Cardiovascular Disease
Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer.

HY-12515B

(S)-Nicardipine (S)-YC-93 free base	Others	Neurological Disease Cardiovascular Disease
(S)-Nicardipine ((S)-YC-93 free base) is the less active S enantiomer of Nicardipine. Nicardipine is a calcium channel blocker with an IC₅₀ of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.

HY-50722

NNC 55-0396 NNC 55-0396 dihydrochloride	Calcium Channel	Cardiovascular Disease
NNC 55-0396, Mibefradil derivative, is a highly selective T-type calcium channel blocker; displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells.

HY-B0285B

Amiloride hydrochloride dihydrate MK-870 hydrochloride dihydrate	Sodium Channel Apoptosis TRP Channel	Metabolic Disease Cardiovascular Disease
Amiloride hydrochloride dihydrate (MK-870 hydrochloride dihydrate) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride dihydrate is a blocker of polycystin-2 (PC2; TRPP2) channel.

HY-B1090S

Cinnarizine D8	Calcium Channel Histamine Receptor	Endocrinology Cardiovascular Disease
Cinnarizine D8 is a deuterium labeled Cinnarizine. Cinnarizine is an antihistamine and a calcium channel blocker.

HY-B0612D

(R)-Lercanidipine hydrochloride	Calcium Channel	Cardiovascular Disease
(R)-Lercanidipine hydrochloride is the R-enantiomer of Lercanidipine. (R)-lercanidipine hydrochloride is a calcium channel blocker.

HY-14657

Dantrolene sodium
F 440
Calcium Channel Metabolic Disease

Dantrolene sodium is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm.

HY-B0552A

Dibucaine hydrochloride Cinchocaine hydrochloride	Sodium Channel	Neurological Disease
Dibucaine hydrochloride (Cinchocaine hydrochloride) is a sodium channel inhibitor. Dibucaine hydrochloride is a potent SChE inhibitor.

HY-14187

Amiodarone
Potassium Channel Autophagy Cardiovascular Disease

Amiodarone is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with an IC₅₀ of 19.1 μM.
HY-U00086

Darodipine
PY 108-068; PY-108068
Calcium Channel Neurological Disease Cardiovascular Disease

Darodipine (PY 108-068, PY-108068) is a potent calcium channel antagonist.

HY-U00026

Semotiadil recemate fumarate	Calcium Channel	Cardiovascular Disease
Semotiadil recemate fumarate is the recemate of Semotiadil fumarate. Semotiadil fumarate is a novel vasoselective Ca²⁺ channel antagonist.

HY-P0191A

Charybdotoxin TFA
Potassium Channel Inflammation/Immunology

Charybdotoxin TFA, a 37-amino acid peptide, is a K⁺ channel blocker.
HY-B0552

Dibucaine
Cinchocaine
Sodium Channel Neurological Disease

Dibucaine (Cinchocaine) is a sodium channel inhibitor. Dibucaine is a potent SChE inhibitor.

HY-12498

GV-58	Calcium Channel	Neurological Disease
GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.

HY-113147B

L-Palmitoylcarnitine TFA	Endogenous Metabolite Potassium Channel	Metabolic Disease Cardiovascular Disease
L-Palmitoylcarnitine TFA, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia. L-Palmitoylcarnitine TFA inhibits K_ATP channel activity, without affecting the single channel conductance, through interaction with Kir6.2.

HY-B0317A

Amlodipine maleate	Calcium Channel	Cancer Cardiovascular Disease
Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer.

HY-120355A

AP14145 hydrochloride	Potassium Channel	Cardiovascular Disease
AP14145 hydrochloride is a potent K_Ca2 (SK) channel negative allosteric modulator with an IC₅₀ of 1.1 μM for K_Ca2.2 (SK2) and K_Ca2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF).

HY-D0143

Quinine	Parasite Potassium Channel	Infection
Quinine is an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine is a potassium channel inhibitor that inhibits WT mouse Slo3 (K_Ca5.1) channel currents evoked by voltage pulses to +100 mV with an IC₅₀ of 169 μM.

HY-B0262

Methocarbamol	Sodium Channel	Neurological Disease
Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research.

HY-B1140

Diazoxide Sch-6783; SRG-95213	Potassium Channel Autophagy	Cardiovascular Disease
Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.

HY-B0612E

(S)-Lercanidipine hydrochloride	Calcium Channel	Cardiovascular Disease
(S)-Lercanidipine hydrochloride is the S-enantiomer of Lercanidipine hydrochloride. (S)-lercanidipine hydrochloride is a potent calcium channel blocker.

HY-B0284

Nifedipine
BAY-a-1040
Calcium Channel Autophagy Cardiovascular Disease Cancer

Nifedipine (BAY-a-1040) is a potent calcium channel blocker and drug of choice for cardiac insufficiencies.

HY-107319

Almitrine mesylate Almitrine bismesylate; Almitrine bismethanesulfonate; Almitrine dimesylate	Potassium Channel	Neurological Disease Cardiovascular Disease
Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca²⁺-dependent K⁺ channel.

HY-U00212

Aranidipine
MPC1304
Calcium Channel Cardiovascular Disease

Aranidipine (MPC1304) is a Ca²⁺ channel antagonist with potent and long-lasting antihypertensive effects.
HY-16723

Funapide
TV 45070; XEN402
Sodium Channel Inflammation/Immunology

Funapide (TV 45070; XEN402) is a potent Sodium Channel Nav1.7 inhibitor.
HY-N9404

6-Benzoylheteratisine
Sodium Channel Neurological Disease

6-Benzoylheteratisine is a naturally occurring antagonist of the Na⁺ channel activator aconitine.

HY-B0162A

Ivabradine hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Ivabradine hydrochloride is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.

HY-N1378

(E)-Cardamonin (E)-Cardamomin; (E)-Alpinetin chalcone	TRP Channel Apoptosis	Neurological Disease Cancer
(E)-Cardamonin ((E)-Cardamomin) is a novel antagonist of hTRPA1 cation channel with an IC₅₀ of 454 nM.

HY-B0023S

Azelnidipine D7
CS-905 D7
Calcium Channel Cardiovascular Disease

Azelnidipine D7 is deuterium labeled Azelnidipine, which is a L-type calcium channel blocker.

HY-B1304

(-)-Sparteine sulfate pentahydrate (-)-Lupinidine sulfate pentahydrate	Sodium Channel	Cardiovascular Disease
(-)-Sparteine sulfate pentahydrate ((-)-Lupinidine sulfate pentahydrate) is a class 1a antiarrhythmic agent and a sodium channel blocker.

HY-P2324

Gramicidin A	Bacterial HIF/HIF Prolyl-Hydroxylase	Infection
Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α).

HY-12515C

(R)-Nicardipine (R)-YC-93 free base	Others	Neurological Disease Cardiovascular Disease
(R)-Nicardipine ((R)-YC-93 free base) is the less active R enantiomer of Nicardipine. Nicardipine (YC-93) is a calcium channel blocker with an IC₅₀ of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.

HY-118628

N-(p-amylcinnamoyl) Anthranilic Acid ACA	Phospholipase TRP Channel	Cardiovascular Disease
N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A₂ (PLA₂) inhibitor and TRP channel blocker. N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia.

HY-116330A

Hyperforin dicyclohexylammonium salt Hyperforin DCHA	TRP Channel Calcium Channel	Neurological Disease
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca²⁺ levels by activating Ca²⁺-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.

HY-B0317B

Amlodipine besylate Amlodipine benzenesulfonate	Calcium Channel	Cancer Cardiovascular Disease
Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer.

HY-D0143B

Quinine hemisulfate hydrate	Parasite Potassium Channel	Infection
Quinine hemisulfate hydrate, an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine hemisulfate hydrate is a potassium channel inhibitor that inhibits WT mouse Slo3 (K_Ca5.1) channel currents evoked by voltage pulses to +100 mV, with an IC₅₀ of 169 μM.

HY-117825

RU-TRAAK-2	Potassium Channel	Neurological Disease
RU-TRAAK-2 is a completely reversible TRAAK (TWIK-related arachidonic acid-stimulated K⁺ channel) inhibitor. RU-TRAAK-2 exerts no activity for non-K2P channels (Kv1.2, Slo1 and GIRK2).

HY-N0172

Caffeic acid
TRP Channel Lipoxygenase Endogenous Metabolite Inflammation/Immunology Cancer

Caffeic acid is an inhibitor of both TRPV1 ion channel and 5-Lipoxygenase (5-LO).

HY-B0023

Azelnidipine CS 905	Calcium Channel	Cardiovascular Disease
Azelnidipine(CS 905; Calblock) is a novel dihydropyridine derivative, a L-type calcium channel blocker, and an antihypertensive.

HY-12502B

Efonidipine hydrochloride
NZ-105 hydrochloride
Calcium Channel Cardiovascular Disease

Efonidipine Hcl (NZ-105) is a dual T-type and L-type calcium channel blocker (CCB).
HY-12502

Efonidipine
NZ-105; (±)-Efonidipine
Calcium Channel Cardiovascular Disease

Efonidipine(NZ-105) is a dual T-type and L-type calcium channel blocker (CCB).
HY-101096

Suvecaltamide
MK-8998
Calcium Channel Neurological Disease

Suvecaltamide (MK-8998; compound 33) is a potent and selective inhibitor of the T-type calcium channel.
HY-19721

ABT-639
Calcium Channel Neurological Disease

ABT-639 is a novel, peripherally acting, selective T-type Ca²⁺ channel blocker.
HY-B0369A

Orphenadrine citrate
iGluR Neurological Disease

Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.
HY-17001A

Flupirtine
D 9998
Potassium Channel iGluR Neurological Disease

Flupirtine(D 9998) is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.
HY-101616

ABT-639 hydrochloride
Calcium Channel Neurological Disease

ABT-639 hydrochloride is a novel, peripherally acting, selective T-type Ca²⁺ channel blocker.
HY-15551

E-4031
Potassium Channel Cardiovascular Disease

E-4031 is a class III antiarrhythmic agent which selectively blocks hERG potassium channel.

HY-B0151

Pregnenolone 3β-Hydroxy-5-pregnen-20-one	Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy	Neurological Disease
Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

HY-135809

A2764 dihydrochloride	Potassium Channel	Neurological Disease
A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K⁺ channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC₅₀=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception.

HY-P1440A

BeKm-1 TFA	Potassium Channel
BeKm-1 TFA is a potent and selective KV11.1 (hERG) channel blocker. BeKm-1 TFA is selective for KV11.1 over a panel of 14 other potassium channels. BeKm-1 TFA dose-dependently prolongs QTc interval in isolated rabbit heart.

HY-W009724

2-Aminoethyl diphenylborinate 2-APB	Calcium Channel TRP Channel	Others
2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R. 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca²⁺ (SOC) channel and activates some TRP channels (V1, V2 and V3).

HY-136909

SR33805	Calcium Channel	Cardiovascular Disease
SR33805 is a potent Ca²⁺ channel antagonist, with EC₅₀s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively. SR33805 blocks L-type but not T-type Ca²⁺ channels. SR33805 can be used for the research of acute or chronic failing hearts.

HY-127106

VU0810464	Potassium Channel	Neurological Disease
VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC₅₀=165 nM) and GIRK1/4 (EC₅₀=720 nM) channels with improved brain penetration.

HY-N7395

Cyclic ADP-ribose cADPR	Calcium Channel TRP Channel Endogenous Metabolite	Infection Endocrinology Inflammation/Immunology Neurological Disease Cardiovascular Disease
Cyclic ADP-ribose (cADPR) is a potent second messenger for calcium mobilization that is synthesized from NAD⁺ by an ADP-ribosyl cyclase. Cyclic ADP-ribose increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels.

HY-16125

Carboxyamidotriazole Orotate L-651582 Orotate; CAI Orotate	Calcium Channel	Cancer Inflammation/Immunology
Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and *calcium channel-mediated signaling pathways*. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects.

HY-100545

BAPTA-AM	Potassium Channel	Cardiovascular Disease
BAPTA-AM is a well-known membrane permeable Ca²⁺ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC₅₀s of 1.3 μM, 1.45 μM and 1.23 μM, respectively.

HY-121519

GSK2332255B	TRP Channel	Cardiovascular Disease
GSK2332255B is a potent, selective TRPC3 and TRPC6 antagonist with IC₅₀s of 5 nM and 4 nM for rat TRPC3 and rat TRPC6. GSK2332255B shows ≥100-fold selectivity for TRPC3/6 over other calcium-permeable channels.

HY-16973

Fluralaner A1443; AH252723	Parasite	Infection
Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.

HY-B1302

Quinidine hydrochloride monohydrate	Potassium Channel Parasite	Infection Cardiovascular Disease
Quinidine hydrochloride monohydrate is an anti-arrythmic agent which is also a potent blocker of K⁺ channel with an IC₅₀ of 19.9 μM.

HY-N0601

Ginsenoside Rf Panaxoside Rf	Calcium Channel Endogenous Metabolite	Cancer Neurological Disease
Ginsenoside Rf is a trace component of ginseng root. Ginsenoside Rf inhibits N-type Ca²⁺ channel.

HY-112279

GNE-131
Sodium Channel Neurological Disease

GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC₅₀ of 3 nM.
HY-N7511

O-Nornuciferine
Potassium Channel Metabolic Disease

O-Nornuciferine, an aporphine-type alkaloid from lotus leaf, is a potent hERG channel inhibitor.

HY-W016498

Paraxanthine	Endogenous Metabolite	Neurological Disease
Paraxanthine, a caffeine metabolite, provides protection against Dopaminergic cell death via stimulation of Ryanodine Receptor Channels.

HY-12082A

GSK369796 Dihydrochloride	Potassium Channel Parasite	Infection
GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization with an IC₅₀ of 7.5 μM.

HY-103309A

ML218 hydrochloride	Calcium Channel	Neurological Disease
ML218 hydrochloride is a potent, selective and orally active *T-type Ca²⁺ channels* (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC₅₀s of 310 nM and 270 nM for Cav3.2 and Cav3.3*, respectively. ML218 hydrochloride inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 hydrochloride has no significant inhibition of L- or N-type calcium channels, K_ATP or hERG potassium channels*. ML218 hydrochloride can penetrate the blood-brain barrier.

HY-103309

ML218	Calcium Channel	Neurological Disease
ML218 is a potent, selective and orally active *T-type Ca²⁺ channels* (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC₅₀s of 310 nM and 270 nM for Cav3.2 and Cav3.3*, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, K_ATP or hERG potassium channels*. ML218 can penetrate the blood-brain barrier.

HY-B1739

Pregnenolone monosulfate 3β-Hydroxy-5-pregnen-20-one monosulfate	Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy	Neurological Disease
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication. Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

HY-110189

Pregnenolone monosulfate sodium salt 3β-Hydroxy-5-pregnen-20-one monosulfate Sodium salt	Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy	Neurological Disease
Pregnenolone monosulfate sodium salt (3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

HY-P1441

Mambalgin 1	Sodium Channel	Others
Mambalgin-1 is a toxin isolated from black mamba venom. Mambalgin-1 is a disulfide-rich polypeptide consisting of 57 amino acids and belongs to the family of three-finger toxins. Mambalgin-1 can bind to and stabilize ASICs (acid-sensing ion channels) in a physiologically relevant closed-channel conformation.

HY-B0682A

Mitiglinide calcium hydrate KAD-1229; S-21403	Potassium Channel	Metabolic Disease
Mitiglinide calcium hydrate (KAD-1229), an insulinotropic agent, is an ATP-sensitive K⁺ (K_ATP) channel antagonist. Mitiglinide calcium hydrate is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell K_ATP channel). Mitiglinide Calcium hydrate can be used for the research of type 2 diabetes.

HY-B0262S1

Methocarbamol-d3	Sodium Channel	Neurological Disease
Methocarbamol-d3 is the deuterium labeled Methocarbamol. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research.

HY-50694

Senicapoc ICA-17043	Potassium Channel	Others
Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca²⁺-activated K⁺ channel; KCa3.1) blocker with an IC₅₀ of 11 nM. Senicapoc blocks Ca²⁺-induced rubidium flux from human RBCs with an IC₅₀ value of 11 nM and inhibits RBC dehydration with IC₅₀ of 30 nM.

HY-18996

Adjudin AF-2364	Chloride Channel Mitochondrial Metabolism	Cancer
Adjudin is an extensively studied male contraceptive with a superior mitochondria-inhibitory effect. Adjudin is also a potent Cl^- channel blocker.

HY-P0173A

Chlorotoxin	Chloride Channel	Cancer
Chlorotoxin is a 36 amino-acid peptide from the venom of the Israeli scorpion Leiurus quinquestriatus with anticancer activity. Chlorotoxin is a chloride channel blocker.

HY-B0703

Eslicarbazepine acetate BIA 2-093	Beta-secretase Sodium Channel	Neurological Disease
Eslicarbazepine acetate (BIA 2-093), an antiepileptic drug, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.

HY-108451

Ononetin
TRP Channel Neurological Disease

Ononetin, a natural deoxybenzoin, is a potent and selective TRPM3 channel blocker with an IC₅₀ of 0.3 μM.

HY-17403

Manidipine dihydrochloride CV-4093	Calcium Channel	Cardiovascular Disease
Manidipine dihydrochloride (CV-4093) is a dihydropyridine compound and a calcium channel blocker for Ca2+ current with IC50 of 2.6 nM.

HY-12502A

Efonidipine hydrochloride monoethanolate NZ-105 hydrochloride monoethanolate	Calcium Channel	Cardiovascular Disease
Efonidipine hydrochloride monoethanolate (NZ-105 hydrochloride monoethanolate) is a dual T-type and L-type calcium channel blocker (CCB).

HY-17398

Mitiglinide calcium KAD-1229 anhydrous; S21403 anhydrous	Potassium Channel	Metabolic Disease
Mitiglinide Calcium (KAD-1229 anhydrous), an insulinotropic agent, is an ATP-sensitive K⁺ (K_ATP) channel antagonist. Mitiglinide Calcium is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell K_ATP channel). Mitiglinide Calcium can be used for the research of type 2 diabetes.

HY-117639

AUT1	Potassium Channel	Cancer
AUT1 is a Kv3 potassium channel modulator, with pEC₅₀s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC₅₀, 4.5).

HY-N7395A

Cyclic ADP-ribose ammonium cADPR ammonium	Calcium Channel TRP Channel Endogenous Metabolite	Infection Endocrinology Inflammation/Immunology Neurological Disease Cardiovascular Disease
Cyclic ADP-ribose ammonium (cADPR ammonium) is a potent second messenger for calcium mobilization that is synthesized from NAD⁺ by an ADP-ribosyl cyclase. Cyclic ADP-ribose ammonium increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels.

HY-17611

Etripamil MSP-2017; (-)-MSP-2017	Calcium Channel	Cardiovascular Disease
Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist, can be used for the research of Paroxysmal Supraventricular Tachycardia (PSVT). Etripamil (MSP-2017) slows atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells.

HY-12546

Brevetoxin B Brevetoxin-2; PbTx-2	Sodium Channel	Neurological Disease
Brevetoxin B (Brevetoxin-2; PbTx-2) is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. Brevetoxin B binds to site 5 on the alpha subunit of voltage-gated sodium channels (IC₅₀=15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively.

HY-101396

ICA-069673
Potassium Channel Neurological Disease

ICA-069673 is a KCNQ2/Q3 potassium channel activator with an IC₅₀ of 0.69 μM.
HY-101346

ZD7288
ICI D7288
HCN Channel Neurological Disease

ZD7288 (ICI D7288) is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.

HY-A0093

Mexiletine hydrochloride KOE-1173 hydrochloride	Sodium Channel	Cardiovascular Disease
Mexiletine hydrochloride (KOE-1173 hydrochloride), a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker.

HY-B0284S

Nifedipine D6 BAY-a-1040 D6	Calcium Channel	Cardiovascular Disease Cancer
Nifedipine D6 (BAY-a-1040 D6) is deuterium labeled nifedipine, and nifedipine is a potent calcium channel blocker.

HY-B0887

Permethrin NRDC-143	Parasite	Infection
Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.

HY-14149

Cisapride
R 51619; (±)-Cisaprid
5-HT Receptor Neurological Disease

Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.

HY-108425A

AMG8380	Sodium Channel	Neurological Disease
AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channel NaV1.7 with IC₅₀s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC₅₀ of 2560 nM.

HY-N6778

Paxilline	Potassium Channel Calcium Channel	Neurological Disease
Paxilline is an indole alkaloid mycotoxin from Penicillium paxilli, acts as a potent BK channels inhibitor by an almost exclusively closed-channel block mechanism. Paxilline also inhibits the sarco/endoplasmic reticulum Ca²⁺ ATPase (SERCA) with IC₅₀s between 5 μM and 50 μM for differing isoforms. Paxilline possesses significant anticonvulsant activity.

HY-111747

TBAJ-587	Bacterial	Infection Cardiovascular Disease
TBAJ-587, a potent anti-tuberculosis agent, inhibits M.tb strain H37Rv growth with MIC₉₀s of 0.006 and <0.02 µg/mL in MABA and LORA assay, respectively. TBAJ-587 inhibits hERG channel minimally, attenuates inhibition of the cardiac potassium channel protein coded by the hERG, which is important for cardiac repolarization.

HY-130354

Dibutyryl-cGMP sodium Bt2cGMP Sodium	Potassium Channel	Cardiovascular Disease
Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [³H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K⁺ channels.

HY-N0239

Bulleyaconitine A	Sodium Channel	Neurological Disease
Bulleyaconitine A is an analgesic and antiinflammatory drug isolated from Aconitum plants; has several potential targets, including voltage-gated Na+ channels.

HY-B0267A

Oxybutynin chloride	mAChR Potassium Channel	Neurological Disease
Oxybutynin chloride is an anticholinergic agent, which inhibits vascular K_v channels in a concentration-dependent manner, with an IC₅₀ of 11.51 μM.

HY-16916

NS1643
Potassium Channel Autophagy Others

NS1643 is a partial agonist of human ether-a-go-go-related gene (hERG) K(+) channels with an EC₅₀ of 10.5 μM.

HY-B0267

Oxybutynin	mAChR Potassium Channel	Neurological Disease
Oxybutynin is an anticholinergic agent, which inhibits vascular K_v channels in a concentration-dependent manner, with an IC₅₀ of 11.51 μM.

HY-14744

Levamlodipine (S)-Amlodipine; Levoamlodipine	Calcium Channel	Others
Levamlodipine ((S)-Amlodipine) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina.

HY-B0493

Niflumic acid	Chloride Channel	Inflammation/Immunology
Niflumic acid, a Ca2+-activated Cl- channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.

HY-100244

NS1652
Chloride Channel Neurological Disease

NS1652 is a reversible anion conductance inhibitor, blocks chloride channel, with an IC₅₀ of 1.6 μM in human and mouse red blood cells.
HY-U00137

YS-201
Calcium Channel Cardiovascular Disease

YS-201 is a dihydropyridine-type calcium channel antagonist. YS-201 has the potential for angina pectoris and hypertension treatment.
HY-131261

Ibuprofen alcohol
Others Inflammation/Immunology

Ibuprofen alcohol, a nonsteroidal antiinflammatory drug (NSAID), exhibits very little activity for acid-sensing ion channels (ASICs).

HY-U00250

β-Amino Acid Imagabalin Hydrochloride PD-0332334	Calcium Channel	Neurological Disease
β-Amino Acid Imagabalin Hydrochloride (PD-0332334) is a ligand for the α2δ subunit of the voltage-dependent calcium channel.

HY-B0419S

Manidipine-d4	Calcium Channel	Cardiovascular Disease
Manidipine-d4 is the deuterium labeled Manidipine. Manidipine is a calcium channel blocker that is used clinically as an antihypertensive.

HY-103318

PD173212
Calcium Channel Neurological Disease

PD173212 is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC₅₀ of 36 nM in IMR-32 assays.
HY-13519

TRAM-34
Potassium Channel Neurological Disease

TRAM-34 is a highly selective blocker of intermediate-conductance calcium-activated K⁺ channel (IKCa1) (K_d=20 nM).
HY-19366

Nav1.7-IN-2
Sodium Channel Neurological Disease

Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels (Nav), in particular Nav 1.7, with IC50 of 80 nM.

HY-122560A

VU0134992 hydrochloride	Potassium Channel	Cardiovascular Disease
VU0134992 hydrochloride is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC₅₀ of 0.97 µM. VU0134992 hydrochloride is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC₅₀=9 µM) at -120 mV.

HY-102070

NS13001	Potassium Channel	Neurological Disease
NS13001 is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC₅₀s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.

HY-122560

VU0134992	Potassium Channel	Cardiovascular Disease
VU0134992 is the first subtype-preferring, orally active and selective Kir4.1 potassium channel pore blocker, with an IC₅₀ of 0.97 µM. VU0134992 is 9-fold selective for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC₅₀=9 µM) at -120 mV.

HY-108594

PD-118057
Potassium Channel Metabolic Disease

PD-118057 is a human ether-a-go-go-related gene (hERG) channel activator that does not cause hERG blockade.

HY-W011641

(±)-Naringenin	Potassium Channel	Cardiovascular Disease
(±)-Naringenin is a naturally-occurring flavonoid. (±)-Naringenin displays vasorelaxant effect on endothelium-denuded vessels via the activation of BK_Ca channels in myocytes.

HY-B0799

Dihydroergotoxine mesylate Ergoloid mesylates	GABA Receptor	Neurological Disease
Dihydroergotoxine mesylate is a complex of closely related alkaloid salts; Binds with high affinity to the GABAA receptor Cl- channel, producing an allosteric interaction with the benzodiazepine site.

HY-101547

TRPC6-IN-1
TRP Channel Cancer

TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC₅₀ of 4.66 μM.

HY-Y0258

Benzocaine	Sodium Channel	Neurological Disease
Benzocaine shares a common receptor with all othe rLAs in the voltage-gated Na⁺ channel, with an IC₅₀ of 0.8 mM tested with a potential of +30 mV.

HY-B0575

Triamterene	Sodium Channel GPCR19	Metabolic Disease
Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic. Triamterene as an inhibitor of the TGR5 receptor.

HY-15763

Erastin
Ferroptosis VDAC Cancer

Erastin is a ferroptosis inducer. Erastin binds and inhibits voltage-dependent anion channels (VDAC2/VDAC3).

HY-135356

m-Nifedipine	Others	Cardiovascular Disease
m-Nifedipine is an impurity of Nifedipine (BAY-a-1040). Nifedipine is a potent calcium channel blocker and drug of choice for cardiac insufficiencies.

HY-107301

Dehydrosoyasaponin I Soyasaponin Be; DHS-I	Potassium Channel	Neurological Disease
Dehydrosoyasaponin I (Soyasaponin Be;DHS-I), a triterpene glycoside, is a potent and reversible calcium-activated potassium (maxi-K) channels activator.

HY-19664

Pranidipine
OPC-13340
Calcium Channel Cardiovascular Disease

Pranidipine (OPC-13340) is a potent, long acting 1,4-dihydropyridine calcium channel blocker with antihypertensive activity.

HY-131281

Ivabradine impurity 1	Others	Others
Ivabradine impurity 1 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.

HY-106855

Almokalant H 234/09	Potassium Channel	Cardiovascular Disease
Almokalant is a class III antiarrhythmic drug, acts as a potassium channel blocker, and inhibits a specific component (Ikr) of the time-dependent delayed rectifier K⁺ current.

HY-131282

Ivabradine impurity 2	Others	Others
Ivabradine impurity 2 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.

HY-B0347S

Lacidipine-d10	Calcium Channel Reactive Oxygen Species Apoptosis	Cardiovascular Disease
Lacidipine-d10 is the deuterium labeled Lacidipine. Lacidipine (Lacipil, Motens) is a L-type calcium channel blocker.

HY-108690

Fluxametamide	GABA Receptor	Others
Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC₅₀ of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.

HY-N0714

Berbamine	NF-κB Autophagy	Cancer
Berbamine is a natural compound extracted from traditional Chinese medicine Barberry with anti-tumor, immunomodulatory and cardiovascular effects. Berbamine is a calcium channel blocker.

HY-101507

Pico145 HC-608	TRP Channel	Cancer
Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC₅₀s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.

HY-N6708

Alamethicin	Bacterial Antibiotic	Infection
Alamethicin, isolated from Trichoderma viride, is a channel-forming peptide antibiotic and induces voltage-gated conductance in model and cell membranes.

HY-B1090

Cinnarizine	Calcium Channel Histamine Receptor	Cardiovascular Disease Endocrinology
Cinnarizine is an antihistamine and a calcium channel blocker, promote cerebral blood flow, used to treat cerebral apoplexy, post-trauma cerebral symptoms, and cerebral arteriosclerosis.

HY-B0211

Riluzole PK 26124	Sodium Channel GABA Receptor	Neurological Disease
Riluzole is an anticonvulsant drug and belongs to the family of use-dependent Na⁺ channel blocker which can also inhibit GABA uptake with an IC₅₀ of 43 μM.

HY-P0173B

Chlorotoxin TFA	Chloride Channel	Cancer
Chlorotoxin TFA is a peptide isolated from the venom of the scorpion Leiurus quinquestriatus, acts as a chloride channel blocker. Anti-cancer activity.

HY-B0211A

Riluzole hydrochloride PK 26124 hydrochloride	Sodium Channel GABA Receptor	Neurological Disease
Riluzole hydrochloride is an anticonvulsant drug and belongs to the family of use-dependent Na⁺ channel blocker which can also inhibit GABA uptake with an IC₅₀ of 43 μM.

HY-108593

BMS-191011
BMS-A
Potassium Channel Neurological Disease

BMS-191011 (BMS-A) is an opener of the large-conductance, Ca²⁺-activated potassium (maxi-K) channel, effective in stroke models.
HY-15707

NS6180
Potassium Channel Inflammation/Immunology

NS6180 is a novel potent and selective KCa3.1 channel inhibitor(IC50= 9 nM) prevents T-cell activation and inflammation.

HY-B0612DS

(R)-Lercanidipine D3 hydrochloride	Calcium Channel	Cardiovascular Disease
(R)-lercanidipine D3 (hydrochloride) is a deuterium labeled (R)-Lercanidipine hydrochloride. (R)-Lercanidipine D3 (hydrochloride), the R-enantiomer of Lercanidipine, is a calcium channel blocker.

HY-17436

Clevidipine	Calcium Channel	Cardiovascular Disease
Clevidipine is a short-acting dihydropyridine calcium channel antagonist (IC50= 7.1 nM, V(H) = -40 mV ) under development for treatment of perioperative hypertension.

HY-10388

TTA-Q6
Calcium Channel Neurological Disease

TTA-Q6 is a selective T-type Ca²⁺ channel antagonist, which can be used in the research of neurological disease.
HY-108590

DMP-543
XR-543
Potassium Channel Neurological Disease

DMP-543 (XR-543) is a K_V7 channel blocker, also acts as a potent neurotransmitter release enhancer.

HY-131283

8-Demethyl Ivabradine	Drug Metabolite	Endocrinology
8-Demethyl Ivabradine is a metabolite of Ivabradine. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.

HY-B1793

Tetraethylammonium chloride	Potassium Channel	Cancer Neurological Disease
Tetraethylammonium chloride is a non-selective potassium channel blocker. Tetraethylammonium chloride is a good substrate for organic cation transporter (OCTN1). Tetraethylammonium chloride antitumor properties.

HY-19062

SM-6586	Calcium Channel Na+/Ca2+ Exchanger	Cardiovascular Disease
SM-6586 is a calcium channel antagonist and inhibitor of Na⁺/H⁺ and Na⁺/Ca²⁺ exchange transport, potentially for the treatment of cerebrovasular diseases and hypertension.

HY-A0176

Glisoxepide	Potassium Channel	Metabolic Disease Cardiovascular Disease
Glisoxepide, a sulphonamide derivative, is an orally available nonselective K(ATP) channel blocker, with antihyperglycemic activity and cardiovascular regulation effect.

HY-14744A

Levamlodipine besylate (S)-Amlodipine besylate; Levoamlodipine besylate	Calcium Channel	Cardiovascular Disease
Levamlodipine besylate ((S)-Amlodipine besylate) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina.

HY-P1084

β-Pompilidotoxin β-PMTX	Sodium Channel	Neurological Disease
β-Pompilidotoxin (β-PMTX), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells.

HY-B1494

Picrotoxinin	Chloride Channel GABA Receptor	Neurological Disease
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABA_A receptor antagonist, which negatively modulates the action of GABA on GABA_A receptors.

HY-108577

XE 991 dihydrochloride	Potassium Channel	Neurological Disease
XE 991 dihydrochloride, a Kv7 (KCNQ) channels blocker, potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current with IC₅₀s of 0.75 µM, 0.71 µM, 0.6 μM, and 0.98 µM, respectively.

HY-108425

AMG8379	Sodium Channel	Neurological Disease
AMG8379 is a potent, orally active and selective sulfonamide antagonist of the *voltage-gated sodium channel* NaV1.7, with IC₅₀*s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels* in dorsal root ganglia (DRG) neurons with an IC₅₀ of 3.1 nM.

HY-16671

CFTR(inh)-172	CFTR Autophagy	Others
CFTR(inh)-172 is a potent and selective blocker of the CFTR chloride channel; reversibly inhibits CFTR short-circuit current in less than 2 minutes with a K_i of 300 nM.

HY-N0663

Talatisamine	Potassium Channel	Neurological Disease
Talatisamine, a aconitum alkaloid, is specific K⁺ channel blocker. Talatisamine attenuates beta-amyloid oligomers induced neurotoxicity in cultured cortical neurons.

HY-13044

ADL-5859	Opioid Receptor	Neurological Disease
ADL5859 is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel.

HY-B1378

Ethosuximide	Calcium Channel	Neurological Disease
Ethosuximide, a widely prescribed anti-epileptic drug, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.

HY-100750

Norverapamil hydrochloride (±)-Norverapamil hydrochloride; D591 hydrochloride	Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

HY-B0246S

Carbamazepine-D10	Sodium Channel Autophagy Mitophagy	Neurological Disease Cancer
Carbamazepine-D10 (CBZ-D10) is the deuterium labeled Carbamazepine. Carbamazepine (CBZ), a sodium channel blocker, is an anticonvulsant agent.

HY-103623

PF-05241328
Sodium Channel Neurological Disease

PF-05241328 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (Nav1.7), with an IC₅₀ of 31 nM.

HY-B0575S

Triamterene D5	Sodium Channel	Metabolic Disease
Triamterene D5 is deuterium labeled Triamterene, which can block epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic.

HY-17360

Tiotropium Bromide BA679 BR	mAChR	Neurological Disease
Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.

HY-108585

VU591 hydrochloride
Potassium Channel Others

VU591 hydrochloride is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC₅₀ of 0.24 μM.

HY-17402

Nisoldipine BAY-k 5552	Calcium Channel Reactive Oxygen Species	Cardiovascular Disease
Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.

HY-108585A

VU591
Potassium Channel Others

VU591 is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC₅₀ of 0.24 μM.
HY-100230A

ML133 hydrochloride
Potassium Channel Others

ML133 hydrochloride is a selective K_ir2 family channels inhibitor, with an IC₅₀ of 1.8 μM at pH 7.4 and 290 nM at pH 8.5.

HY-100611

CaCCinh-A01	Chloride Channel	Cancer Inflammation/Immunology
CaCCinh-A01 is an inhibitor of both TMEM16A and calcium-activated chloride channel (CaCC) with IC₅₀s of 2.1 and 10 μM, respectively.

HY-135328

Norverapamil (±)-Norverapamil; D591	Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

HY-115681

(2R/S)-6-PNG 6-Prenylnaringenin	Calcium Channel	Neurological Disease
(2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Ca_v3.2 T-type Ca²⁺ channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice.

HY-13422

Zatebradine hydrochloride UL-FS-49; UL-FS-49CL	HCN Channel	Cardiovascular Disease
Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC₅₀ values 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC₅₀ values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively.

HY-P1075

CALP3	Calcium Channel	Cancer Neurological Disease
CALP3, a Ca²⁺-like peptide, is a potent Ca²⁺ channel blocker that activates EF hand motifs of Ca²⁺-binding proteins. CALP3 can functionally mimic increased [Ca²⁺]_i by modulating the activity of Calmodulin (CaM), Ca²⁺ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.

HY-113618A

RO2959 hydrochloride	CRAC Channel Interleukin Related	Cardiovascular Disease
RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC₅₀ of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC₅₀ of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.

HY-103371

DCPIB	Chloride Channel Potassium Channel	Neurological Disease
DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB voltage-dependently activates potassium channels TREK1 and TRAAK and inhibits TRESK, TASK1 and TASK3 (IC₅₀s of 0.14, 0.95, 50.72 μM, respectively). DCPIB is also a selective blocker of swelling-induced chloride current (I_Cl,swell), with an IC₅₀ of 4.1 μM in CPAE cells.

HY-14187S

Amiodarone-d10 hydrochloride	Potassium Channel Autophagy	Cardiovascular Disease
Amiodarone-d10 hydrochloride is the deuterium labeled Amiodarone. Amiodarone hydrochloride is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with an IC₅₀ of 19.1 μM.

HY-19960

BCTC
TRP Channel Cancer

BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.

HY-101238

Agmatine sulfate	Imidazoline Receptor NO Synthase Endogenous Metabolite	Neurological Disease Cancer
Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.

HY-101437A

Ralfinamide mesylate FCE-26742A mesylate	Sodium Channel	Neurological Disease
Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na⁺ channel blocker derived from α-aminoamide, with function of suppressing pain.

HY-132813

Evifacotrep	TRP Channel	Neurological Disease
Evifacotrep, a short transient receptor potential channel 5 (TRPC5) antagonist (WO2020061162, compound 100), can be used for the research of neurological diseases.

HY-112729

HC-056456 3,4-Bis(2-thienoyl)-1,2,5-oxadiazole-N-oxide	Others	Others
HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na⁺]_i rise is slowed by HC-056456 (IC₅₀~3 µM).

HY-W013093

Uridine triphosphate trisodium salt UTP triSodium salt; Uridine 5'-triphosphate triSodium salt	Others	Cancer Inflammation/Immunology Cardiovascular Disease
Uridine triphosphate trisodium salt is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.

HY-N3710

Dehydrocrenatidine Kumujian G; O-Methylpicrasidine I	JAK Apoptosis	Cancer Neurological Disease
Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain.

HY-103368

Eact	Chloride Channel	Neurological Disease
Eact is a selective and potent activator of TMEM16A, directly activates the TRPV1 channels in sensory nociceptors and produces itch, acute nociception and thermal hypersensitivity.

HY-N8404

Chlorahololide C	Potassium Channel	Inflammation/Immunology
Chlorahololide C, a lindenane sesquiterpenoid dimer, is isolated from Chloranthus holostegius. Chlorahololide C is a potent and selective potassium channel blocker, with an IC₅₀ of 3.6 μM.

HY-12343

ML277
CID-53347902
Potassium Channel Cardiovascular Disease

ML277(CID53347902) is a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator with EC50 of 270 nM.
HY-109987

ISPA-28
Parasite Infection

ISPA-28 is a specific plasmodial surface anion channel (PSAC) antagonist. ISPA-28 binds directly and reversibly to CLAG3.
HY-131012

GoSlo-SR-5-69
Potassium Channel Others

GoSlo-SR-5-69 is a potent activator of large conductance Ca²⁺-activated K⁺ (BK) channels, with an EC₅₀ of 251 nM.

HY-B1655

Fluspirilene R 6218; Redeptin	Calcium Channel	Neurological Disease
Fluspirilene is a non-competitive antagonist of L-type calcium channels with an IC₅₀ of 0.03 μM. Fluspirileneis a long-acting injectable depot antipsychotic drug used for schizophrenia.

HY-P1084A

β-Pompilidotoxin TFA β-PMTX TFA	Sodium Channel	Neurological Disease
β-Pompilidotoxin TFA (β-PMTX TFA), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells.

HY-136190

TRPC6-PAM-C20	TRP Channel
TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) of TRPC6 channels. TRPC6-PAM-C20 is a potent enhancer of channel activation, enabling low basal concentrations of DAG to induce activation of the ion channel. TRPC6-PAM-C20 induces increases in intracellular Ca²⁺ concentrations ([Ca²⁺]i) in TRPC6-expressing HEK293 cells with an EC₅₀ of 2.37 μM. TRPC6-PAM-C20 can be used as a valuable tool to selectively exaggerate TRPC6-dependent signals.

HY-B1671

(+)-Kavain	GABA Receptor Sodium Channel Calcium Channel	Metabolic Disease Neurological Disease
(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na⁺ and Ca²⁺ channels. (+)-Kavain is shown to bind at the α4β2δ GABA_A receptor and potentiate GABA efficacy. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied.

HY-B0563

Ropivacaine	Sodium Channel Potassium Channel	Neurological Disease Cardiovascular Disease
Ropivacain is a potent sodium channel blocker and acts as a local anesthetic agent. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K_2P (two-pore domain potassium channel) TREK-1 with an IC₅₀ of 402.7 μM in COS-7 cell's membrane. Ropivacaine is used for the research of regional anesthesia and neuropathic pain management.

HY-P1075A

CALP3 TFA	Calcium Channel	Cancer Neurological Disease
CALP3 TFA, a Ca²⁺-like peptide, is a potent Ca²⁺ channel blocker that activates EF hand motifs of Ca²⁺-binding proteins. CALP3 TFA can functionally mimic increased [Ca²⁺]_i by modulating the activity of Calmodulin (CaM), Ca²⁺ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.

HY-B0563B

Ropivacaine hydrochloride	Sodium Channel Potassium Channel	Neurological Disease Cardiovascular Disease
Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K_2P (two-pore domain potassium channel) TREK-1 with an IC₅₀ of 402.7 μM in COS-7 cell's membrane. Ropivacaine is a local anesthetic agent widely used for regional anesthesia and neuropathic pain management in vivo.

HY-B0682S

Mitiglinide-d8 calcium hydrate	Potassium Channel	Metabolic Disease
Mitiglinide-d8 calcium hydrate (KAD-1229-d8) is the deuterium labeled Mitiglinide calcium hydrate. Mitiglinide calcium hydrate (KAD-1229), an insulinotropic agent, is an ATP-sensitive K⁺ (K_ATP) channel antagonist. Mitiglinide calcium hydrate is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell K_ATP channel). Mitiglinide Calcium hydrate can be used for the research of type 2 diabetes.

HY-10341A

Fasudil HA-1077; AT877	ROCK Calcium Channel Autophagy PKA PKC	Cancer
Fasudil (HA-1077; AT877), is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an K_i of 0.33 μM for ROCK1, IC₅₀s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil is also a potent Ca2+channel antagonist and vasodilator.

HY-113618B

RO2959 monohydrochloride	CRAC Channel Interleukin Related	Cardiovascular Disease
RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC₅₀ of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC₅₀ of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.

HY-B0563A

Ropivacaine hydrochloride monohydrate	Sodium Channel Potassium Channel	Neurological Disease Cardiovascular Disease
Ropivacaine hydrochloride monohydrate is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K_2P (two-pore domain potassium channel) TREK-1 with an IC₅₀ of 402.7 μM in COS-7 cell's membrane. Ropivacaine is a local anesthetic agent widely used for regional anesthesia and neuropathic pain management in vivo.

HY-P1274

ShK-Dap22	Potassium Channel	Inflammation/Immunology
ShK-Dap22 is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 is a selective Kv1.3 channel blocker with IC₅₀s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively.

HY-100727

AM-2099
Sodium Channel Neurological Disease

AM-2099 is a potent and selective inhibitor of voltage-gated sodium channel Nav1.7 with an IC₅₀ of 0.16 μM for human Nav1.7.

HY-116790A

(+)-Penbutolol (R)-Penbutolol; (+)-Isopenbutolol	Adrenergic Receptor	Metabolic Disease Endocrinology
(+)-Penbutolol is a β-adrenoceptor antagonist, with an IC₅₀ of 0.74 μM. (+)-Penbutolol is an optical isomer of l-penbutolol with Na⁺ channel-blocking action.

HY-B1288

Oxybuprocaine hydrochloride Benoxinate hydrochloride	Sodium Channel	Neurological Disease
Oxybuprocaine hydrochloride (Benoxinate hydrochloride) reversibly blocks sodium channels and prevents propagation of painful nerve impulses in the cornea, conjunctiva, and sclera. Oxybuprocaine hydrochloride is used especially in ophthalmology and otolaryngology.

HY-119373

Cav 2.2 blocker 1
Calcium Channel Neurological Disease

Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain, with an IC₅₀ of 1 nM.
HY-10388A

TTA-Q6(isomer)
Others Others

TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca²⁺ channel antagonist.

HY-B1445

Minoxidil sulfate	Potassium Channel	Metabolic Disease
Minoxidil sulfate, a potent and ATP-sensitive K⁺ channel opener, is the sulfated metabolite of minoxidil. Minoxidil sulfate is considered as a vasodilator to promote hair growth in vivo.

HY-A0084

Procainamide hydrochloride	Autophagy	Cancer
Procainamide hydrochloride is an anti-arrhythmic agent and is used to treat cardiac arrhythmia; induces rapid block of the batrachotoxin(BTX)-activated sodium channels of the heart muscle and acts as antagonist to long gating closures.

HY-137437

Dirocaftor PTI-808	CFTR	Inflammation/Immunology
Dirocaftor (PTI-808) is a CFTR potentiator that enhances the function of CFTR protein by opening chloride channels. Dirocaftor can be used for cystic fibrosis (CF) research.

HY-124687

ROMK-IN-32	Potassium Channel	Cardiovascular Disease
ROMK-IN-32 is a renal outer medullary potassium channel (ROMK) inhibitor with an IC₅₀ of 35 nM. ROMK-IN-32 also inhibits hERG with an IC₅₀ of 22 μM.

HY-15125

(R)-(+)-Bay-K-8644
Calcium Channel Cardiovascular Disease

(R)-(+)-Bay-K-8644 is a calcium channel inhibitor. (R)-(+)-Bay-K-8644 inhibits Ba²⁺ currents (I_Ba) (IC₅₀=975 nM).

HY-20587

CRAC intermediate 1	CRAC Channel	Inflammation/Immunology
CRAC intermediate 1 is a key intermediate in the chemical synthesis of a series of CRAC channel inhibitors, detailed information can be found in Patent WO 2010122089 A1, intermediate 9.

HY-N2060

Evocarpine	Apoptosis Bacterial	Cancer Infection Inflammation/Immunology
Evocarpine, a quinolone alkaloid that could be isolated from Evodiae fructus, inhibitss Ca²⁺ influx through voltage-dependent calcium channels. Antimycobacterial activity.

HY-135013

Umbellulone	TRP Channel	Neurological Disease
Umbellulone is an active constituent of the leaves of Umbellularia californica. Umbellulone stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism.

HY-N0252

Catharanthine (+)-3,4-Didehydrocoronaridine	Calcium Channel	Cancer Cardiovascular Disease
Catharanthine is an alkaloid isolated from Madagascar periwinkle, inhibits voltage-operated L-type Ca²⁺ channel, with anti-cancer and blood pressure-lowering activity.

HY-108465

Pyr3
TRP Channel Others

Pyr3 is a selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC₅₀ of 700 nM for TRPC3-mediated Ca²⁺ influx.

HY-N5006

Guanfu base G	Potassium Channel	Cardiovascular Disease
Guanfu base G is an antiarrhythmic alkaloid isolated from Aconitum coreanum. Guanfu base G inhibits HERG channel current with an IC₅₀ of 17.9 μM.

HY-N1469

Kaurenoic acid	Others	Inflammation/Immunology Neurological Disease
Kaurenoic acid is a diterpene from Sphagneticola trilobata, inhibits Inflammatory Pain by the inhibition of cytokine production and activation of the NO–cyclic GMP–PKG–ATP-sensitive potassium channel signaling pathway.

HY-136189

UK-59811 hydrochloride	Calcium Channel	Neurological Disease
UK-59811 hydrochloride, a Br-dihydropyridine derivative, is a potent bacterial homotetrameric model voltage-gated Ca²⁺ (Ca_V) channel Ca_VAb inhibitor with an IC₅₀ of 194 nM.

HY-101840

EIPA L593754; MH 12-43	TRP Channel Sodium Channel	Cancer Inflammation/Immunology
EIPA (L593754) is a TRPP3 channel inhibitor with an IC₅₀ of 10.5 μM. EIPA also inhibits Na⁺/H⁺-exchanger (NHE) and macropinocytosis.

HY-112723

ACT-709478	Calcium Channel	Neurological Disease
ACT-709478 is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies.

HY-16723A

(R)-Funapide (R)-TV 45070; (R)-XEN402	Sodium Channel	Neurological Disease
(R)-Funapide ((R)-TV 45070) is the less active R-enantiomer of Funapide. Funapide is a potent Nav1.7 sodium channel blocker that can be used for pain research.

HY-N0252A

Catharanthine Tartrate (+)-3,4-Didehydrocoronaridine Tartrate	Calcium Channel	Cancer Cardiovascular Disease
Catharanthine Tartrate is an alkaloid isolated from Madagascar periwinkle, inhibits voltage-operated L-type Ca²⁺ channel, with anti-cancer and blood pressure-lowering activity.

HY-101840A

EIPA hydrochloride L593754 hydrochloride; MH 12-43 hydrochloride	TRP Channel Sodium Channel	Cancer Inflammation/Immunology
EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC₅₀ of 10.5 μM. EIPA hydrochloride also inhibits Na⁺/H⁺-exchanger (NHE) and macropinocytosis.

HY-107372

Uridine triphosphate UTP; Uridine 5'-triphosphate	Endogenous Metabolite	Cancer Inflammation/Immunology Cardiovascular Disease
Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.

HY-103310

MRS1845	Calcium Channel CRAC Channel	Cardiovascular Disease
MRS1845 is a selective store-operated calcium (SOC) channel inhibitor with an IC₅₀ of 1.7 μM. MRS1845 is an ORAI1 inhibitor.

HY-101621S

Teludipine-d6
Calcium Channel Cancer

Teludipine-d6 (GR53992B-d6) is the deuterium labeled Teludipine hydrochloride. Teludipine is a lipophilic calcium channel blocker.

HY-B0612A

Lercanidipine hydrochloride	Calcium Channel	Cardiovascular Disease
Lercanidipine hydrochloride is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine hydrochloride has long lasting antihypertensive action and reno-protective effect.

HY-B0612

Lercanidipine	Calcium Channel	Cardiovascular Disease
Lercanidipine is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine has long lasting antihypertensive action and reno-protective effect.

HY-13422A

Zatebradine UL-FS-49 free base; UL-FS-49CL free base	HCN Channel	Cardiovascular Disease
Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC₅₀ value of 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC₅₀ values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively.

HY-W013712

GI-530159	Potassium Channel	Neurological Disease
GI-530159 is a selective, mechanosensitive opener of TREK1 (K_2P2.1) and TREK2 (K_2P10.1) channels, with an EC₅₀ of 0.76 μM for TREK1. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels. GI-530159 reduces rat dorsal root ganglion neuron excitability.

HY-P1274A

ShK-Dap22 TFA	Potassium Channel	Inflammation/Immunology
ShK-Dap22 TFA is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 TFA is a selective Kv1.3 channel blocker with IC₅₀s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively.

HY-123824

GNE-0439	Sodium Channel	Neurological Disease
GNE-0439 is a novel Nav1.7-selective inhibitor with IC₅₀ of 0.34 uM and inhibits Nav1.5 with an IC₅₀ of 38.3 μM. GNE-0439 inhibits mutant N1742K channels (IC₅₀=0.37 uM) in membrane potential assays. GNE-0439 possesses a carboxylic acid group, binds outside of the channel pore, and is unique compared with known selective VSD4 binders.

HY-P0062

Ziconotide SNX-111	Calcium Channel	Inflammation/Immunology Neurological Disease
Ziconotide (SNX-111), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide reduces synaptic transmission, and can be used for chronic pain research.

HY-B0772A

Nifekalant hydrochloride MS-551	Potassium Channel	Cardiovascular Disease
Nifekalant hydrochloride (MS-551), a class III antiarrhythmic agent, is a IKr potassium channel blocker with an IC₅₀ of 10 µM. Nifekalant hydrochloride can be used for refractory ventricular tachyarrhythmias research.

HY-18600A

Azimilide Dihydrochloride NE-10064 Dihydrochloride	Potassium Channel	Cardiovascular Disease
Azimilide Dihydrochloride (NE-10064 Dihydrochloride) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.

HY-133614

Dihydroisopimaric acid	Potassium Channel	Others
Dihydroisopimaric acid activates large conductance Ca²⁺ activated K⁺ (BK) channels alphabeta1 in the direct measurement of BKalphabeta1 opening under whole-cell voltage clamp.

HY-P1282

Agitoxin-2
Potassium Channel Neurological Disease

Agitoxin-2 is a K+ channel inhibitor, with IC₅₀ values of 201 pM and 144 pM for mK_V1.3 and mK_V1.1, respectively).

HY-15065

Chembridge-5861528 TCS 5861528	TRP Channel	Neurological Disease
Chembridge-5861528 is a TRPA1 channel blocker that antagonizes AITC- and 4-HNE-evoked calcium influx (IC50 values are 14.3 and 18.7μM respectively).

HY-114301

PF-06305591	Sodium Channel	Neurological Disease
PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC₅₀ of 15 nM. An excellent preclinical in vitro ADME and safety profile.

HY-A0148A

Halofantrine hydrochloride SKF-102886; WR-171669	Parasite	Infection
Halofantrine hydrochloride (SKF-102886) is a blocker of delayed rectifier potassium current via the inhibition of human-ether-a-go-go-related gene (HERG) channel and a potent antimalarial compound.

HY-B0405A

Bupivacaine hydrochloride	Sodium Channel	Cancer Neurological Disease
Bupivacaine hydrochloride is a Na⁺ channel blocker which has local narcotic effect. Bupivacaine hydrochloride has direct anti-cancer activities with the dominant inhibitory effects on gastric cancer migration.

HY-18600

Azimilide NE-10064	Potassium Channel	Cardiovascular Disease
Azimilide(NE-10064) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.

HY-B0339

Primidone	Sodium Channel	Neurological Disease
Primidone is a potent anticonvulsant agent of the barbiturate class. Primidone is a neuronal *voltage-gated sodium channel* (VGSC)** blocker and can be used for the study of epilepsy, essential tremor, and Psychiatric disorders.

HY-N6691

Veratridine 3-Veratroylveracevine	Sodium Channel	Neurological Disease
Veratridine (3-Veratroylveracevine), a alkaloid derived from plants in the family Liliaceae, is a sodium channel agonist. Veratridine inhibits the peak current of Nav1.7, with an IC₅₀ of 18.39 µM.

HY-121604

(Rac)-MEM 1003	Calcium Channel	Others
(Rac)-MEM 1003 is the racemate of MEM 1003. MEM 1003, a dihydropyridine compound, is a potent L-type Ca²⁺ channel antagonist and has the potential for Alzheimer’s disease research.

HY-15124

(S)-(-)-Bay-K-8644
Calcium Channel Cardiovascular Disease

(S)-(-)-Bay-K-8644 is an agonist of L-type Ca²⁺ channel. (S)-(-)-Bay-K-8644 activates Ba²⁺ currents (I_Ba) (EC₅₀=32 nM).

HY-B0517A

Mepivacaine hydrochloride	Sodium Channel	Neurological Disease
Mepivacaine hydrochloride is an amide-type local anesthetic agent. Mepivacaine hydrochloride binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.

HY-114608

RY785	Sodium Channel	Neurological Disease
RY785 is a potent and selective voltage-gated potassium (K_V2) channel inhibitor with an IC₅₀ of 0.05 μM for K_V2.2. RY785 has analgesic activity.

HY-66010A

Cinepazide		Cardiovascular Disease
Cinepazide is a piperazine derivative and acts as a weak calcium channel blocker. Cinepazide is a potent vasodilator and can be used for the research of cerebrovascular diseases, including ischemic stroke, brain infarct et. al.

HY-B0517

Mepivacaine	Sodium Channel	Neurological Disease
Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.

HY-105170B

ABT-418 hydrochloride	nAChR	Neurological Disease
ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease.

HY-W042039

Methyl homoveratrate	Calcium Channel	Cardiovascular Disease
Methyl homoveratrate, a metabolite of RWJ-26240 in vivo, can be identified in plasma, urine and faecal extract. McN5691 (RWJ-26240) is a voltage-sensitive calcium channel blocker.

HY-B0448A

Phenytoin sodium 5,5-Diphenylhydantoin Sodium salt	Sodium Channel Virus Protease	Neurological Disease
Phenytoin sodium (5,5-Diphenylhydantoin sodium salt) is a potent *Voltage-gated Na⁺ channels* (VGSCs)** blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice.

HY-B0632

Diltiazem	Calcium Channel	Cardiovascular Disease
Diltiazem is an orally active L-type Ca²⁺ channel blocker, with antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris.

HY-114301A

PF-06305591 dihydrate	Sodium Channel	Neurological Disease
PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC₅₀ of 15 nM. An excellent preclinical in vitro ADME and safety profile.

HY-N2197

Hirsuteine	Others	Neurological Disease
Hirsuteine is an indole alkaloid extracted from Uncaria genus. Hirsuteine non-competitively antagonizes nicotine-mediated dopamine release by blocking ion permeation through nicotinic receptor channel complexes.

HY-P1282A

Agitoxin-2 TFA
Potassium Channel Neurological Disease

Agitoxin-2 TFA is a K+ channel inhibitor, with IC₅₀ values of 201 pM and 144 pM for mK_V1.3 and mK_V1.1, respectively).

HY-B0448

Phenytoin 5,5-Diphenylhydantoin	Sodium Channel Virus Protease	Neurological Disease
Phenytoin (5,5-Diphenylhydantoin) is a potent *Voltage-gated Na⁺ channels* (VGSCs)** blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice.

HY-B0551

Doxapram
Potassium Channel Neurological Disease

Doxapram inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.

HY-P0188

ω-Conotoxin MVIIC	Calcium Channel	Neurological Disease
ω-Conotoxin MVIIC is a N- and P/Q-type Ca²⁺ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release.

HY-B0551A

Doxapram hydrochloride hydrate	Potassium Channel	Neurological Disease
Doxapram hydrochloride hydrate inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.

HY-N1584

Halofuginone RU-19110	DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel	Cancer Infection Inflammation/Immunology Cardiovascular Disease
Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

HY-100783A

(-)-Bicuculline methochloride l-Bicuculline methochloride	GABA Receptor	Neurological Disease
(-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABA_A receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca²⁺-activated K⁺ channels in various types of neurons.

HY-A0176S

Glisoxepid-d4	Potassium Channel	Metabolic Disease Cardiovascular Disease
Glisoxepid-d4 is the deuterium labeled Glisoxepide. Glisoxepide, a sulphonamide derivative, is an orally available nonselective K(ATP) channel blocker, with antihyperglycemic activity and cardiovascular regulation effect.

HY-N2412

Irisolidone	Chloride Channel	Cancer Neurological Disease
Irisolidone is a major isoflavone found in Pueraria lobata flowers. Irisolidone exhibits potent hepatoprotective activity. Irisolidone shows the high efficacy for *volume-regulated anion channels* (VRAC)** blockade.

HY-135328S

Norverapamil D7 (±)-Norverapamil D7; D591 D7	Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
Norverapamil D7 is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

HY-P0188A

ω-Conotoxin MVIIC TFA	Calcium Channel	Neurological Disease
ω-Conotoxin MVIIC TFA is a N- and P/Q-type Ca²⁺ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release.

HY-33350

Clofilium tosylate	Potassium Channel Apoptosis	Cancer Cardiovascular Disease
Clofilium tosylate, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Antiarrhythmic agent.

HY-100783

(-)-Bicuculline methobromide l-Bicuculline methobromide	GABA Receptor	Neurological Disease
(-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABA_A receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca²⁺-activated K⁺ channels in various types of neurons.

HY-112217A

PSEM 89S TFA	nAChR	Neurological Disease
PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively.

HY-B0424

Nitrendipine BAY-E-5009	Calcium Channel Autophagy	Cardiovascular Disease
Nitrendipine (BAY-E-5009), an analogue of Nifedipine (HY-B0284), is a dihydropyridine calcium channel blocker with vasodilator action. Nitrendipine has antihypertensive effect.

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-A0093S

Mexiletine D6 hydrochloride KOE-1173 D6 hydrochloride	Sodium Channel	Cardiovascular Disease
Mexiletine D6 hydrochloride (KOE-1173 D6 hydrochloride) is a deuterium labeled Mexiletine hydrochloride (KOE-1173 hydrochloride). Mexiletine hydrochloride, a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker.

HY-136589

Verapamil EP Impurity C hydrochloride NSC-609249 hydrochloride	Calcium Channel P-glycoprotein Cytochrome P450	Metabolic Disease
NSC-609249 hydrochloride is an impurity of Verapamil (HY-14275). Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.

HY-107754

Cesium chloride	Potassium Channel	Cardiovascular Disease
Cesium chloride is a blocker of potassium channel. Cesium chloride prevents the decrease of Na⁺ transport produced by Alloxan. Cesium chloride has induced cardiac arrhythmias, including torsade de pointes in animal models.

HY-130353

Desethylamiodarone hydrochloride N-desethylamiodarone hydrochloride; LB 33020 hydrochloride	Potassium Channel Autophagy	Cardiovascular Disease
Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC₅₀ of 19.1 μM.

HY-B1386

Halazone	Bacterial Carbonic Anhydrase Sodium Channel	Infection
Halazone is an atypical antimicrobial sulfonamide derivative and a carbonic anhydrase II inhibitor with a K_d value of 1.45 µM. Halazone protects sodium channels from inactivation. Halazone is widely used for disinfection of drinking water.

HY-122135

A-317567	Sodium Channel	Neurological Disease
A-317567 is a potent *acid-sensing ion channel* 3 (ASIC-3) inhibitor with an IC₅₀** of 1.025 μM. A-317567 has antidepressant and antinociception effects.

HY-17429

Flecainide acetate R-818	Sodium Channel	Cardiovascular Disease
Flecainide acetate (R-818) is a class 1C antiarrhythmic drug especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential.

HY-B0493S

Niflumic Acid-d5	Chloride Channel	Inflammation/Immunology
Niflumic Acid-d5 is the deuterium labeled Niflumic acid. Niflumic acid, a Ca²⁺-activated Cl^- channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.

HY-B0432B

(S)-Propafenone (S)-SA-79	Others	Cardiovascular Disease
(S)-Propafenone ((S)-SA-79) is the S-enantiomer of Propafenone. (S)-Propafenone ((S)-SA-79) exerts beta-blocking action and the sodium channel-dependent antiarrhythmic class 1 activity.

HY-P0062A

Ziconotide TFA SNX-111 TFA	Calcium Channel	Inflammation/Immunology Neurological Disease
Ziconotide TFA (SNX-111 TFA), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide TFA reduces synaptic transmission, and can be used for chronic pain research.

HY-B1500

2,2,2-Trichloroethanol	Potassium Channel	Neurological Disease
2,2,2-Trichloroethanol, the active form of the sedative hypnotic drug chloral hydrate, is an agonist for the nonclassical K_2P channels TREK-1 (KCNK2) and TRAAK (KCNK4).

HY-13812

QNZ EVP4593	NF-κB TNF Receptor	Inflammation/Immunology Neurological Disease
QNZ (EVP4593) shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC₅₀s of 11 and 7 nM, respectively. QNZ (EVP4593) is a neuroprotective inhibitor of SOC channel.

HY-111828

TTA-A2	Calcium Channel	Neurological Disease
TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a₁G) and Cav3.2 (a₁H) channels with IC₅₀ values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.

HY-N1584A

Halofuginone hydrobromide RU-19110 hydrobromide	DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel	Cancer Infection Inflammation/Immunology Cardiovascular Disease
Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

HY-100080

A-887826	Sodium Channel	Neurological Disease
A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC₅₀ of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo.

HY-N6868

Dimethyl lithospermate B dmLSB	Sodium Channel	Cardiovascular Disease
Dimethyl lithospermate B (dmLSB) is a selective Na⁺ channel agonist. Dimethyl lithospermate B slows inactivation of sodium current (INa), leading to increased inward current during the early phases of the action potential (AP).

HY-14182

Vernakalant RSD1235	Potassium Channel	Cardiovascular Disease
Vernakalant(RSD-1235) is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents; in treatment of antiarrhythmic.

HY-66010

Cinepazide Maleate MD-67350	Calcium Channel	Cardiovascular Disease
Cinepazide Maleate (MD-67350) is a piperazine derivative and acts as a weak calcium channel blocker. Cinepazide Maleate is a potent vasodilator and can be used for the research of cerebrovascular diseases, including ischemic stroke, brain infarct et. al.

HY-N0252B

Catharanthine Sulfate (+)-3,4-Didehydrocoronaridine Sulfate	Calcium Channel	Cancer Cardiovascular Disease
Catharanthine Sulfate ((+)-3,4-Didehydrocoronaridine Sulfate) is an alkaloid isolated from Madagascar periwinkle, inhibits voltage-operated L-type Ca²⁺ channel, with anti-cancer and blood pressure-lowering activities.

HY-N0042

Ginsenoside Rc Panaxoside Rc	GABA Receptor TNF Receptor Interleukin Related	Cancer Inflammation/Immunology Neurological Disease
Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptor_A (GABA_A)-mediated ion channel currents (I_GABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.

HY-P0256

Apamin Apamine	Potassium Channel	Inflammation/Immunology Neurological Disease
Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca²⁺-activated K⁺ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.

HY-N1072

Wilforgine	Others	Inflammation/Immunology
Wilforgine is a bioactive sesquiterpene alkaloid in Tripterygium wilfordii Hook. F. Wilforgine can induce microstructural and ultrastructural changes in the muscles of Mythimna separata larvae, and the sites of action are proposed to be calcium receptors or channels in the muscular system.

HY-19608

GSK1016790A	TRP Channel Calcium Channel	Metabolic Disease Cardiovascular Disease
GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca²⁺ influx and elevate intracellular Ca²⁺ in HEK cells.

HY-N7126

Citronellal	Others	Neurological Disease
Citronellal is a monoterpenea from the essential oils in various aromatic species of plants, with depressant, hypnotic, and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K^⁺ channel pathway.

HY-100831

YM-58483 BTP2	CRAC Channel	Inflammation/Immunology
YM-58483 (BTP2) is the first selective and potent inhibitor of CRAC channels and subsequent Ca²⁺ signals. YM-584832 is a blocker of store-operated Ca²⁺ entry (SOCE).

HY-135328AS

Norverapamil D7 hydrochloride (±)-Norverapamil D7 hydrochloride; D591 D7 hydrochloride	Calcium Channel	Cardiovascular Disease
Norverapamil D7 ((±)-Norverapamil D7) hydrochloride is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

HY-100641

4-Hydroxytolbutamide Hydroxytolbutamide	Potassium Channel Autophagy	Cancer Metabolic Disease
4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic.

HY-101253

AM-92016 hydrochloride	Others	Cardiovascular Disease
AM-92016 hydrochloride is a specific blocker of rectifier potassium current (IK). AM-92016 hydrochloride delays rectifier potassium channel (IK), repolarizes the membrane thereby restricting the duration of the nerve impulse thereby restricting the duration of the nerve impulse.

HY-101436A

Sematilide hydrochloride CK-1752 hydrochloride	Potassium Channel	Cardiovascular Disease
Sematilide hydrochloride (CK-1752 hydrochloride) is a selective I_Kr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K⁺ current (IC₅₀=25 μM). Sematilide is a class III antiarrhythmic agent.

HY-101622

5-HT6/7 antagonist 1	5-HT Receptor Dopamine Receptor
5-HT6/7 antagonist 1 is a multifunctional ligand that antagonizes 5-HT6/7/2A and D2 receptors, without interacting with M1 receptors and hERG channels.

HY-136615

5-Hydroxydecanoate sodium	Potassium Channel	Neurological Disease
5-Hydroxydecanoate sodium is a selective ATP-sensitive K⁺ (K_ATP) channel blocker (IC₅₀ of ~30 μM). 5-Hydroxydecanoate sodium is a substrate for mitochondrial outer membrane acyl-CoA synthetase and has antioxidant activity.

HY-B1837

Cyfluthrin	Sodium Channel	Infection
Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav_1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product.

HY-101436

Sematilide CK-1752	Potassium Channel	Cardiovascular Disease
Sematilide (CK-1752) is a selective I_Kr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K⁺ current (IC₅₀=25 μM). Sematilide is a class III antiarrhythmic agent.

HY-111996

Kv3 modulator 1	Potassium Channel	Inflammation/Immunology
Kv3 modulator 1 is a Kv3 voltage-gated potassium channel modulator extracted from patent WO2018020263A1, Compound X. Kv3 modulator 1 has the potential for inflammatory pain treatment.

HY-14848

Naluzotan PRX 00023	5-HT Receptor Potassium Channel	Neurological Disease
Naluzotan is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC₅₀ and K_i of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K⁺ channel blocker, with IC₅₀ of 3800 nM.

HY-19408

Pyr10	TRP Channel	Others
Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca²⁺ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC₅₀ of 0.72 μM (IC₅₀ of 13.08 μM for store operated Ca²⁺ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels.

HY-16787

ICA-121431	Sodium Channel	Cardiovascular Disease
ICA-121431 is a nanomolar potent and broad-spectrum *voltage-gated sodium channel* (Na_v) blocker, shows equipotent selectivity for human Na_v1.1 and Na_v1.3 subtypes with IC₅₀ values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Na_v1.2 (IC₅₀*=240 nM) and 1,000 fold selectivity against Na_v1.4, Na_v1.6, and the TTX-resistant human Na_v1.5 and Na_v1.8 channels* (IC₅₀s >10 µM).

HY-110237

BX430	P2X Receptor Calcium Channel	Cardiovascular Disease
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC₅₀ of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.

HY-22044

ICA N-[4-(2-Pyridinyl)-2-thiazolyl]-2-pyridinamine	Parasite	Infection Cardiovascular Disease
ICA (N-(pyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine) is a SK channel inhibitor that has antileishmanial activity with an IC₅₀ of 2.1 µM.

HY-16696

SN 2	TRP Channel	Infection
SN 2 is a potent activator of TRPML3 ion channel with an EC₅₀ of 1.8 μM. SN 2 also acts as a potent inhibitor of Dengue virus 2 (DENV2) and Zika virus (ZIKV).

HY-B0358A

Flunarizine dihydrochloride	Calcium Channel Sodium Channel Dopamine Receptor	Neurological Disease
Flunarizine dihydrochloride is a potent dual *Na⁺/Ca²⁺ channel* (T-type) blocker. Flunarizine dihydrochloride is a D₂ dopamine** receptor antagonist. Flunarizine dihydrochloride, a diphenylpiperazine derivative, has the potential for peripheral vessels dilator and migraine prophylaxis.

HY-B0612DS1

Lercanidipine-d3 hydrochloride	Calcium Channel	Cardiovascular Disease
Lercanidipine-d3 hydrochloride is the deuterium labeled Lercanidipine. Lercanidipine is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine has long lasting antihypertensive action and reno-protective effect.

HY-N1462

Atractyloside potassium salt	Others	Cardiovascular Disease
Atractyloside potassium salt is a toxic diterpenoid glycoside that can be isolated from the fruits of Xanthium sibiricum. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart.

HY-128829

Kv3 modulator 2	Potassium Channel	Inflammation/Immunology
Kv3 modulator 2 (formula (I)) is a potent Kv3 channels modulator extracted from patent WO2018109484A1, compound formula (I) , has analgesic activity and is used in the prophylaxis or treatment of related disorders.

HY-18779

PF-4840154	TRP Channel	Inflammation/Immunology
PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel with EC₅₀s of 97 and 23 nM, respectively. PF-4840154 elicits TrpA1-mediated nocifensive behaviour in mouse.

HY-N4097

Incensole	Others	Neurological Disease
Incensole, a 14-membered diterpenoid, is isolated from both essential oils and resins of frankincense. Incensole has shown anti-inflammatory and anti-depression activities due to their ability to activate ion channels in the brain to alleviate anxiety or depression.

HY-N6688

Verruculogen	Potassium Channel Bacterial Antibiotic	Infection
Verruculogen is a toxin produced mainly by Penicillium and Aspergillus spp. and causes severe tremors in affected animals. Verruculogen inhibits Ca²⁺-activated K⁺ channels. Verruculogen is an M phase inhibitor of the mammalian cell cycle.

HY-106916

Unoprostone	Potassium Channel	Neurological Disease
Unoprostone, a prostaglandin F2α analogs (PGAs), activates BK channels to reduce oxidative stress- and light-induced retinal cell death, and phagocytotic dysfunction. Unoprostone reduces intraocular pressure and is used topically for glaucoma or ocular hypertension.

HY-111613

Pinaverium bromide	Calcium Channel	Others
Pinaverium bromide is an L-type calcium channel blocker with selectivity for the gastrointestinal tract, effectively relieves pain, diarrhea and intestinal discomfort, provides good therapeutic efficacies without significant adverse effects on Irritable bowel syndrome (IBS) patients.

HY-P0256A

Apamin TFA Apamine TFA	Potassium Channel	Inflammation/Immunology Neurological Disease
Apamin TFA (Apamine TFA) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca²⁺-activated K⁺ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.

HY-P1441A

Mambalgin 1 TFA	Sodium Channel
Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC₅₀ values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.

HY-B1167

Ajmaline Cardiorythmine; (+)-Ajmaline	Sodium Channel	Cardiovascular Disease
Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC₅₀ of 1 μM in HEK cells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia.

HY-12693

R(+)-IAA-94 R(+)-Methylindazone	Chloride Channel	Others
R(+)-IAA-94 (R(+)-Methylindazone) is a potent indanyloxyacetic acid blocker of epithelial chloride channels. R(+)-IAA-94 inhibits Nef-sdAb19 (single-domain antibody) interaction and binds to negative factor (Nef).

HY-122015

ASP2905	Potassium Channel	Neurological Disease
ASP2905 is a potent and selective *potassium channel* Kv12.2** inhibitor encoded by the Kcnh3/BEC1 gene. ASP2905 can cross the blood-brain barrier and has antipsychotic activities.

HY-19282A

(5R)-BW-4030W92
Others Neurological Disease

(5R)-BW-4030W92 is the R enantiomer of BW-4030W92. BW-4030W92 is a non-selective, voltage-, and use-dependent sodium channel antagonist.

HY-N6016

Bacopaside II	Apoptosis	Cancer
Bacopaside II, an extract from the medicinal herb Bacopa monnieri, blocks the Aquaporin-1 (AQP1) water channel and impairs migration of cells that express AQP1. Bacopaside II induces cell cycle arrest and apoptosis.

HY-75161

(-)-Menthol	TRP Channel Endogenous Metabolite	Cancer
(-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca²⁺-permeable nonselective cation channel, to increase [Ca²⁺]_i. Antitumor activity.

HY-122605

TRPM4-IN-1 CBA	TRP Channel	Cancer Cardiovascular Disease
TRPM4-IN-1 (CBA) is a potent and selective inhibitor of the cation channel TRPM4, with an IC₅₀ of 1.5 μM. TRPM4-IN-1 can be used for the research of cardiac diseases and prostate cancer.

HY-102052

DCEBIO	Potassium Channel	Inflammation/Immunology
DCEBIO, a derivative of 1-EBIO, is an extremely potent activator of Cl^- secretion in T84 colonic cells. DCEBIO stimulates Cl^- secretion via the activation of hIK1 K⁺ channels and the activation of an apical membrane Cl^- conductance.

HY-A0092

Trimethadione 3,5,5,-Trimethyloxazolidine-2,4-dione	Calcium Channel	Neurological Disease
Trimethadione (3,5,5,-Trimethyloxazolidine-2,4-dione) is an oxazolidinedione anticonvulsant agent widely used against absences seizures. Trimethadione also is a T-type calcium channel blocker which has antihyperalgesic effects.

HY-108235

Lanicemine AZD6765	iGluR	Neurological Disease
Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (K_i of 0.56-2.1 μM for NMDA receptor; IC₅₀s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects.

HY-N2941

Bisandrographolide C	TRP Channel	Metabolic Disease Inflammation/Immunology
Bisandrographolide C is an unusual dimer of ent-labdane diterpenoid isolated and identified from Andrographis paniculata. Bisandrographolide C activates TRPV1 and TRPV3 channels with K_d values of 289 and 341 μM respectively, and protects cardiomyocytes from hypoxia-reoxygenation injury.

HY-131868

TRPV3 antagonist 74a	TRP Channel	Neurological Disease
TRPV3 antagonist 74a is a potent and selective TRPV3 antagonist. TRPV3 antagonist 74a displays no significant activity against a panel of other ion channels. TRPV3 antagonist 74a can be used for the research of neuropathic pain.

HY-B0112

Minoxidil U10858	Potassium Channel	Cardiovascular Disease
Minoxidil (U10858) is an ATP-sensitive potassium (K_ATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. Minoxidil is also a potent inhibitor of soybean lipoxygenaseare with an IC₅₀ of 20 μM.

HY-B0887S

Permethrin-d5	Parasite	Infection
Permethrin-d5 (NRDC-143-d5) is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.

HY-B0402A

Amantadine hydrochloride 1-Adamantanamine hydrochloride; 1-Adamantylamine hydrochloride; 1-Aminoadamantane hydrochloride	Influenza Virus	Infection
Amantadine (1-Adamantanamine) hydrochloride is an antiviral agent with activity against influenza A viruses. Amantadine hydrochloride blocks the proton flow through the M2 ion channel and thus prevents the release of viral RNA into the cytoplasm of the infected cells. Amantadine hydrochloride is an antiparkinsonian agent.

HY-119934

NaV1.7 inhibitor-1	Sodium Channel	Neurological Disease
NaV1.7 inhibitor-1 is an efficacious *voltage-gated sodium channel* (NaV) 1.7 inhibitor with an IC₅₀** of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5.

HY-108589

PNU 37883 hydrochloride PNU 37883A	Potassium Channel	Neurological Disease
PNU 37883 hydrochloride (PNU 37883A) is a selective vascular ATP-sensitive potassium (Kir6, K_ATP) channels blocker. PNU 37883 hydrochloride has diuretic effects with specific binding in kidney and vascular smooth muscle rather than in brain or pancreatic beta cells.

HY-N1934

Dihydroberberine	Potassium Channel HSP	Cancer Inflammation/Immunology Cardiovascular Disease
Dihydroberberine inhibits human ether-a-go-go-related gene (hERG) channels and remarkably reduces heat shock protein 90 (Hsp90) expression and its interaction with hERG. Dihydroberberine has anti-inflammatory, anti-atherosclerotic, hypolipidemic and antitumor activities.

HY-108235A

Lanicemine dihydrochloride AZD6765 dihydrochloride; ARL 15896AR	iGluR	Neurological Disease
Lanicemine (AZD6765) dihydrochloride is a low-trapping NMDA channel blocker (K_i of 0.56-2.1 μM for NMDA receptor; IC₅₀s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects.

HY-131614

TPC2-A1-N	Calcium Channel	Others
TPC2-A1-N is a powerful and Ca²⁺-permeable agonist of two pore channel 2 (TPC2), which plays its role by mimicking the physiological actions of NAADP. TPC2-A1-P reproducibly evokes significant Ca²⁺ responses from TPC2 (EC₅₀=7.8 μM), and the effect can be blocked by several TPC blockers. TPC2-A1-N can be used to probe different functions of TPC2 channels in intact cells.

HY-109177

Icenticaftor QBW251	CFTR	Inflammation/Immunology
Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC₅₀s of 79 nM and 497 nM for F508del and G551D CFTR, respectively. Icenticaftor can be used for chronic obstructive pulmonary disease (COPD) and cystic fibrosis research.

HY-100238

Antihistamine-1	Histamine Receptor Cytochrome P450 Potassium Channel	Neurological Disease Endocrinology
Antihistamine-1 is a H1-antihistamine (K_i=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC₅₀s of 5.4 and 0.8 μM, respectively.

HY-N0219

Bicuculline (+)-Bicuculline; d-Bicuculline	GABA Receptor	Neurological Disease
Bicuculline ((+)-Bicuculline; d-Bicuculline), as a convulsant alkaloid, is a competitive neurotransmitter GABA_A receptor antagonist (IC₅₀=2 μM). Bicuculline also blocks Ca²⁺-activated potassium (SK) channels and subsequently blocks the slow afterhyperpolarization (slow AHP) .

HY-P1074

SNX-482	Calcium Channel	Neurological Disease
SNX-482, a peptidyl toxin of the spider Hysterocrates gigas, is a potent, high affinity, selective and voltage-dependent R-type Ca_V2.3 channel blocker with an IC₅₀ of 30 nM. SNX-482 has antinociceptive effect.

HY-132201

MK-8153	Potassium Channel	Metabolic Disease
MK-8153 is a potent, selective and orally active inhibitor of *renal outer medullary potassium channel* (ROMK), with IC₅₀**s of 5 nM, 34 μM for ROMK electrophysiology (EP) and hERG EP, respectively. MK-8153 can be used as the diuretic/atriuretic.

HY-B0562

Methyclothiazide	Carbonic Anhydrase	Metabolic Disease Cardiovascular Disease
Methyclothiazide is an orally active antihypertensive agent and a diuretic agent. Methyclothiazide leads to a reduction of the vascular response to the action of endogenous vasoconstricting stimuli, such as Norepinephrine (HY-13715). Methyclothiazide is against voltage-dependent Ca-channel (VDCC) activity in vitro.

HY-P1249

Neuropeptide SF(mouse,rat)	Neuropeptide Y Receptor	Neurological Disease
Neuropeptide SF (mouse,rat) is a potent neuropeptide FF receptor agonist with K_i values are 48.4 nM and 12.1 nM for NPFF1 and NPFF2, respectively. Neuropeptide SF increases the amplitude of the sustained current of heterologously expressed acid sensing ion channel 3 (ASIC3) .

HY-120033

RY796	Sodium Channel	Neurological Disease
RY796 is a potent and selective voltage-gated potassium (K_V2) channel inhibitor with IC₅₀s of 0.25 μM and 0.09 μM for K_V2.1 and K_V2.2. RY796 has analgesic activity.

HY-B0166A

L-Ascorbic acid sodium salt Sodium L-ascorbate; Vitamin C Sodium salt	Calcium Channel Reactive Oxygen Species Apoptosis	Cancer
L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively Ca_v3.2 channels with an IC₅₀ of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.

HY-15084B

Dizocilpine MK-801	iGluR	Neurological Disease
Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a K_d of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca²⁺ flux.

HY-14275

Verapamil (±)-Verapamil; CP-16533-1	Calcium Channel P-glycoprotein Cytochrome P450	Metabolic Disease
Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research.

HY-A0064

Verapamil hydrochloride (±)-Verapamil hydrochloride; CP-16533-1 hydrochloride	Calcium Channel P-glycoprotein Cytochrome P450	Cardiovascular Disease
Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research.

HY-12650

Mirogabalin 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-132268

Cav 2.2 blocker 2	Calcium Channel	Neurological Disease
Cav 2.2 blocker 2 is a Cav2.2 calcium channel blocker extracted from patent WO2017046581A1, compound 1. Cav 2.2 blocker 2 can reverses hyperalgesia associated with an injury or inflammation in conjunction with the opioid.

HY-B0233

Isradipine PN 200-110	Calcium Channel Autophagy	Neurological Disease Cardiovascular Disease
Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease.

HY-10015

PAP-1 5-(4-Phenoxybutoxy)psoralen	Potassium Channel	Inflammation/Immunology
PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC₅₀=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC₅₀=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects.

HY-B0309

Felodipine	Calcium Channel Autophagy	Cardiovascular Disease
Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.

HY-113673

A-935142	Potassium Channel	Cardiovascular Disease
A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. A-935142 enhances hERG current in a complex manner by facilitation of activation, reduction of inactivation, and slowing of deactivation, and abbreviates atrial and ventricular repolarization.

HY-B0495

Lamotrigine LTG; BW430C	Sodium Channel Autophagy	Neurological Disease
Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na⁺ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al.

HY-P1249A

Neuropeptide SF(mouse,rat) TFA	Neuropeptide Y Receptor	Neurological Disease
Neuropeptide SF (mouse,rat) TFA is a potent neuropeptide FF receptor agonist with K_i values are 48.4 nM and 12.1 nM for NPFF1 and NPFF2, respectively. Neuropeptide SF TFA increases the amplitude of the sustained current of heterologously expressed acid sensing ion channel 3 (ASIC3) .

HY-137563

A2793	Potassium Channel	Neurological Disease
A2793 is an efficient dual *TWIK-related acid-sensitive K⁺ channel* (TASK)-1/TRESK inhibitor, with an IC₅₀** of 6.8 μM for mTRESK. A2764 is more selective for TRESK, and it only moderately influences TREK-1 and TALK-1.

HY-133168

Englerin A	TRP Channel	Cancer
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC₅₀s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca²⁺ influx and Ca²⁺ cell overload.

HY-B0422

Nateglinide A4166; Senaglinide	Potassium Channel Dipeptidyl Peptidase	Metabolic Disease
Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K⁺ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.

HY-B0778

Milbemycin oxime	Parasite Antibiotic	Infection
Milbemycin oxime is a macrocyclic lactone and has broad-spectrum anti-parasitic activity. Milbemycin oxime is composed of milbemycins A4 and A3. Milbemycin oxime binds glutamate-gated chloride channels. Milbemycin oxime is against intestinal nematodes, pulmonary and cardiac helminths.

HY-15419

RS-127445 hydrochloride	5-HT Receptor	Neurological Disease
RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT_2B receptor antagonist with a pK_i of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.

HY-17402S1

Nisoldipine-d4	Calcium Channel Reactive Oxygen Species	Cardiovascular Disease
Nisoldipine-d4 (BAY-k 5552-d4) is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC₅₀ of 10 nM.

HY-12361

PF 1022A	Parasite	Infection
PF 1022A is a cyclooctadepsipeptide with broadspectrum anthelmintic properties produced by fermentation of the fungus Mycelia sterilia. PF 1022A is a channel-forming ionophore. PF 1022A showes strong anthelmintic activities against *Ascaridia galli* in chickens. PF 1022A also can be used for angiostrongyliasis research.

HY-P1346

APETx2	Sodium Channel	Inflammation/Immunology Neurological Disease
APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC₅₀ of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.

HY-107212

Selamectin	Parasite Chloride Channel P-glycoprotein	Infection
Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, *Lymphatic filariae, and nematode* infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC₅₀ of 120 nM.

HY-17402S2

Nisoldipine-d7	Calcium Channel Reactive Oxygen Species	Cardiovascular Disease
Nisoldipine-d7 (BAY-k 5552-d7) is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC₅₀ of 10 nM.

HY-15419A

RS-127445	5-HT Receptor	Neurological Disease
RS-127445 is a selective, high affinity, orally bioavailable 5-HT_2B receptor antagonist with a pK_i of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.

HY-17437A

Mefloquine hydrochloride Mefloquin hydrochloride	Parasite SARS-CoV Reactive Oxygen Species Autophagy Potassium Channel	Cancer Infection Metabolic Disease Inflammation/Immunology
Mefloquine hydrochloride (Mefloquin hydrochloride), a quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine hydrochloride is also a *K⁺ channel* (KvQT1/minK) antagonist with an IC₅₀** of ~1 μM. Mefloquine hydrochloride can be used for malaria, systemic lupus erythematosus and cancer research.

HY-P1346A

APETx2 TFA	Sodium Channel	Inflammation/Immunology Neurological Disease
APETx2 TFA, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC₅₀ of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.

HY-16953

JNJ 303	Potassium Channel	Cardiovascular Disease
JNJ 303 is a potent I_Ks blocker with an IC₅₀ value of 64 nM. JNJ 303 does not have any effects on other cardiac channels at concentrations of 3.3 μM for I_Na, I_ca, I_to, and I_Kr. JNJ 303 induces QT-prolongations and causes unprovoked torsades de pointes (TdP).

HY-122700

Factor D inhibitor 6	Complement System	Inflammation/Immunology
Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC₅₀ of 30 nM and a K_d of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.

HY-W020468

Linopirdine DuP 996	Potassium Channel TRP Channel	Neurological Disease
Linopirdine (DuP 996) is an orally active, selective M-type K⁺ current (IM; Kv7; KCNQ Channels) inhibitor with an IC₅₀ of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue.

HY-P1422

Spadin	Potassium Channel	Neurological Disease
Spadin, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K_2P2.1) channel activity. Spadin binds specifically to TREK-1 with an affinity of 10 nM. Spadin is an efficient antidepressant in mice.

HY-100612

T16Ainh-A01	Chloride Channel	Others
T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC₅₀ value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC).

HY-100973A

Adenosine 5′-diphosphoribose sodium ADP ribose Sodium	TRP Channel Autophagy	Endocrinology Metabolic Disease
Adenosine 5′-diphosphoribose sodium (ADP ribose sodium) is a nicotinamide adenine nucleotide (NAD⁺) metabolite. Adenosine 5′-diphosphoribose sodium is the most potent and primary intracellular Ca²⁺-permeable cation TRPM2 channel activator. Adenosine 5′-diphosphoribose sodium also can enhance autophagy.

HY-B0824

Bifenthrin	Sodium Channel	Neurological Disease
Bifenthrin is a synthetic pyrethroid insecticide that prolongs opening of sodium channels resulting in membrane depolarization and conductance block in the insect nervous system. Bifenthrin is effective against A. gambiae and C. quinquefasciatus mosquitos (LD₅₀s = 0.15 and 0.16 ng/mg, respectively) and increases O. insidiosus mortality in treated corn and sorghum plants.

HY-B0122

Topiramate McN 4853; RWJ 17021	iGluR GABA Receptor Sodium Channel Calcium Channel Potassium Channel Carbonic Anhydrase	Neurological Disease
Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.

HY-119322

Tifenazoxide NN414	Potassium Channel	Metabolic Disease
Tifenazoxide (NN414) is a potent, orally active and SUR1/Kir6.2 selective K^ATP channels opener. Tifenazoxide has antidiabetic effect, can inhibit glucose stimulated insulin release in vitro and in vivo, and has a beneficial effect on glucose homeostasis.

HY-P1105

GaTx2	Others	Neurological Disease
GaTx2 is a seletive and a high affinity inhibitor of ClC-2 channels with a voltage-dependent apparent K_D of ∼20 pM. GaTx2 is a peptide toxin inhibitor from Leiurus quinquestriatus hebraeus venom. GaTx2 is useful in determining the role and the membrane localization of ClC-2 in specific cell types.

HY-108235B

(Rac)-Lanicemine (Rac)-AZD6765	iGluR	Neurological Disease
(Rac)-Lanicemine ((Rac)-AZD6765) is the racemate of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (K_i of 0.56-2.1 μM for NMDA receptor; IC₅₀s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects.

HY-B0836

λ-Cyhalothrin	Parasite Sodium Channel	Infection Endocrinology Neurological Disease
λ-Cyhalothrin is a high efficiency, broad-spectrum type II synthetic pyrethroid insecticide containing α-cyano group. λ-Cyhalothrin is used to control a wide range of pests in a variety of applications. λ-Cyhalothrin is a neurotoxin that targets sodium channels in the membranes of neurons in the central nervous system.

HY-136205

IA-Alkyne Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide	TRP Channel	Infection Inflammation/Immunology
IA-Alkyne (Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide) is a *TRP channel* (TRPC) agonist and has the potential for the study of respiratory infection. IA-Alkyne can be used to develop an isotopically tagged probe for quantitative cysteine-reactivity** profiling.

HY-12532

Astemizole R 43512	Histamine Receptor Potassium Channel	Inflammation/Immunology Endocrinology
Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC₅₀ of 4 nM. Astemizole also shows potent hERG K⁺ channel blocking activity with an IC₅₀ of 0.9 nM. Astemizole has antipruritic effects.

HY-B0252

Hydrochlorothiazide HCTZ	TGF-beta/Smad Potassium Channel	Metabolic Disease Cardiovascular Disease
Hydrochlorothiazide (HCTZ), an orally active diuretic drug of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.

HY-12962

NMDA-IN-1	iGluR	Neurological Disease
NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.

HY-N6776

Penitrem A	Potassium Channel	Cancer Neurological Disease
Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals.

HY-110199

TC-I 2014	TRP Channel	Neurological Disease
TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC₅₀ values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models.

HY-108588

NS5806	Potassium Channel	Cardiovascular Disease
NS5806, a potent potassium current activator, increases K_V4.3/KChIP2 peak current amplitudes with an EC₅₀ of 5.3 μM. NS5806 slows K_V4.3 and K_V4.2 current dacay in channel complexes containing KChIP2.

HY-134494

MS48107	Others	Neurological Disease
MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice.

HY-128830

Kv3 modulator 3	Potassium Channel	Inflammation/Immunology
Kv3 modulator 3 (Compound 4) is a selective modulator of Kv3.1 and/or Kv3.2 and/or Kv3.3 *channels* extracted from patent WO2017098254A1, compound 4, has analgesic activity for use in the prophylaxis o or treatment of pain.

HY-107642

MA-2029	Motilin Receptor	Metabolic Disease
MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC₅₀=4.9 nM). MA-2029 is selective for the motilin receptor over various other receptors and ion channels. MA-2029 may be useful for gastrointestinal disorders associated with disturbed gastrointestinal motility.

HY-131615

TPC2-A1-P	Sodium Channel	Others
TPC2-A1-P is a powerful and membrane permeable agonist of two pore channel 2 (TPC2) with an EC₅₀ of 10.5 μM. TPC2-A1-P plays its role by mimicking the physiological actions of PI(3,5)P2. TPC2-A1-P also shows higher potency to induce Na²⁺ mobilisation from TPC2 than TPC-A1-N (HY-131614). TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells.

HY-108587

ICA 110381	Potassium Channel	Neurological Disease
ICA 110381 (Compound 16) is a KCNQ2/Q3 potassium channel opener for the treatment of epilepsy. ICA 110381 is a KCNQ2/Q3 agonist (EC₅₀=0.38 μM) as well as KCNQ1 antagonist (IC₅₀=15 μM).

HY-108235C

(R)-Lanicemine (R)-AZD6765	iGluR	Neurological Disease
(R)-Lanicemine ((R)-AZD6765) is the less active R-enantiomer of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (K_i of 0.56-2.1 μM for NMDA receptor; IC₅₀s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects.

HY-12533

Disopyramide Dicorantil; SC-7031	Sodium Channel Potassium Channel	Cardiovascular Disease
Disopyramide (Dicorantil) is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action.

HY-135897

Urolithin C	Calcium Channel Reactive Oxygen Species Apoptosis Endogenous Metabolite	Metabolic Disease
Urolithin C, a gut-microbial metabolite of Ellagic acid, is a glucose-dependent activator of insulin secretion. Urolithin C is a L-type Ca²⁺ channel opener and enhances Ca²⁺ influx. Urolithin C induces cell apoptosis through a mitochondria-mediated pathway and also stimulates reactive oxygen species (ROS) formation.

HY-A0236A

Aprindine hydrochloride	Potassium Channel	Cardiovascular Disease
Aprindine hydrochloride is a class I-b anti-arrhythmic agent and a hERG channel blocker with an IC₅₀ of 0.23 μM. Aprindine hydrochloride has inhibitory effects on Na⁺/Ca²⁺ exchanger currents, which is partly responsible for their antiarrhythmic and cardioprotective effects. Aprindine hydrochloride is widely used for trial and ventricular tachyarrhythmias treatment research.

HY-19838

JNJ-63533054	GPR139	Neurological Disease
JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC₅₀ of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB).

HY-B1193

Terfenadine (±)-Terfenadine; MDL-991	Potassium Channel Histamine Receptor Na+/Ca2+ Exchanger Caspase Apoptosis	Cancer Inflammation/Immunology Endocrinology
Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC₅₀ of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca²⁺ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.

HY-B0254

Glipizide CP 28720; K 4024	Potassium Channel	Metabolic Disease
Glipizide (CP 2872; K 4024) a potent, orally active and sulfonylurea class anti-diabetic agent and can be used for type 2 diabetes mellitus research but not type 1. Glipizide acts by partially blocking ATP-sensitive potassium (K_ATP) channels among β cells of pancreatic islets of Langerhans.

HY-B0422S

Nateglinide D5 A4166 D5; Senaglinide D5	Potassium Channel Dipeptidyl Peptidase	Metabolic Disease
Nateglinide D5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K⁺ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.

HY-P1422A

Spadin TFA	Potassium Channel	Neurological Disease
Spadin TFA, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K_2P2.1) channel activity. Spadin TFA binds specifically to TREK-1 with an affinity of 10 nM. Spadin TFA is an efficient antidepressant in mice.

HY-B0114S

Oxcarbazepine-D4 GP 47680-D4	Sodium Channel Apoptosis	Cancer Neurological Disease
Oxcarbazepine-D4 (GP 47680-D4) is the deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines. Anti-cancer and anticonvulsant effects.

HY-133596

12,14-Dichlorodehydroabietic acid	Potassium Channel GABA Receptor	Neurological Disease
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca²⁺-activated K⁺ (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABA_A antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca²⁺ and stimulates transmitter release.

HY-A0082

Diphenidol hydrochloride Difenidol hydrochloride	mAChR Sodium Channel	Neurological Disease
Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M₁-M₄ receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na⁺, K⁺, and Ca²⁺) in neuronal cells. Diphenidol hydrochloride is a potential drug of choice for experimental spinal anesthesia.

HY-19765

GSK2798745	TRP Channel	Cardiovascular Disease
GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC₅₀s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 is used in research for the treatment of pulmonary edema associated with congestive heart failure.

HY-130605

BAY-1797	P2X Receptor	Neurological Disease
BAY-1797 is a potent, orally active, and selective P2X4 antagonist, with an IC₅₀ of 211 nM against human P2X4. BAY-1797 displays no or very weak activity on the other P2X ion channels. BAY-1797 shows anti-nociceptive and anti-inflammatory effects.

HY-108579

UCL 1684 dibromide	Potassium Channel	Cardiovascular Disease
UCL 1684 (dibromide) is a first nanomolar, non-peptidic small conductance calcium-activated potassium (SK) channel blocker. UCL 1684 (dibromide) is effective in preventing the development of atrial fibrillation due to potent atrial-selective inhibition of I_Na. UCL 1684 (dibromide) causes atrial-selective prolongation of ERP secondary to induction of postrepolarization refractoriness.

HY-122114

ICA-27243	Potassium Channel	Neurological Disease
ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC₅₀ of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects.

HY-108512

PD 144418	Sigma Receptor	Neurological Disease
PD 144418 is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (K_i values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 shows potential antipsychotic activity.

HY-135746

OR-1896	Potassium Channel Phosphodiesterase (PDE) Drug Metabolite Apoptosis	Cardiovascular Disease
OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K⁺ channels and has Ca²⁺-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation.

HY-131897

1-Stearoyl-2-arachidonoyl-sn-glycerol	PKC TRP Channel	Neurological Disease
1-Stearoyl-2-arachidonoyl-sn-glycerol is a diacylglycerol (DAG) containing polyunsaturated fatty acids. 1-Stearoyl-2-arachidonoyl-sn-glycerol can activate PKC. 1-Stearoyl-2-arachidonoyl-sn-glycerol also can augment *nonselective cation channel* (NSCC)** activity.

HY-108512A

PD 144418 oxalate	Sigma Receptor	Neurological Disease
PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (K_i values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows potential antipsychotic activity.

HY-117833

PXS-4681A	Monoamine Oxidase	Inflammation/Immunology
PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a K_i of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects.

HY-110234

Topiramate D12 McN 4853 D12 ; RWJ 17021 D12	iGluR GABA Receptor Sodium Channel Calcium Channel Potassium Channel Carbonic Anhydrase	Neurological Disease
Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.

HY-12496

NS-1619	Potassium Channel Apoptosis	Cancer Cardiovascular Disease
NS-1619 is an opener of large conductance Ca²⁺-activated K⁺ (BK) channel. NS-1619 is a highly effective relaxant with an EC₅₀ of about 10 – 30 μM in several smooth muscles of blood vessels and other tissues. NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells.

HY-B1546

Benzamil Benzylamiloride	Sodium Channel Na+/Ca2+ Exchanger	Neurological Disease
Benzamil (Benzylamiloride), an Amiloride analogue, is a Na⁺/Ca²⁺ exchanger (NCX) inhibitor (IC₅₀~100 nM). Benzamil also is a non-selective *Deg/epithelial sodium channels* (ENaC)** blocker, and can potentiate myogenic vasoconstriction. Benzamil inhibits TRPP3-mediated Ca²⁺-activated currents, with an IC₅₀ of 1.1 μM.

HY-19976

RN-1747	TRP Channel	Cardiovascular Disease
RN-1747 is a selective *transient receptor potential cation channel* subfamily V member 4 (TRPV4) agonist, with EC₅₀** values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC₅₀ of 4 μM.

HY-N0747

Oxypeucedanin	Potassium Channel	Cancer Cardiovascular Disease
Oxypeucedanin is a furocoumarin derivative isolated from Angelica dahurica. Oxypeucedanin is a selective open-channel blocker, inhibits the hKv1.5 current with an IC₅₀ value of 76 nM. Oxypeucedanin prolongs cardiac action potential duration (APD), is a potential antiarrhythmic agent for atrial fibrillation. Oxypeucedanin induces cell apoptosis through inhibition of cancer cell migration.

HY-B1546A

Benzamil hydrochloride Benzylamiloride hydrochloride	Na+/Ca2+ Exchanger Sodium Channel	Neurological Disease
Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na⁺/Ca²⁺ exchanger (NCX) inhibitor (IC₅₀~100 nM). Benzamil hydrochloride also is a non-selective *Deg/epithelial sodium channels* (ENaC)** blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca²⁺-activated currents, with an IC₅₀ of 1.1 μM.

HY-23196S

Minoxidil-d10	Potassium Channel
Minoxidil-d10 (U10858-d10) is the deuterium labeled Minoxidil. Minoxidil (U10858) is an ATP-sensitive potassium (K_ATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. Minoxidil is also a potent inhibitor of soybean lipoxygenaseare with an IC₅₀ of 20 μM.

HY-B0185A

Lidocaine hydrochloride Lignocaine hydrochloride	Sodium Channel MEK ERK NF-κB Apoptosis	Cancer Cardiovascular Disease
Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative commonly used to anesthetize. hydrochloride is a a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.

HY-120348

ML67-33	Potassium Channel	Neurological Disease Cardiovascular Disease
ML67-33 is a selective activator of temperature- and mechano-sensitive K_2P channels. ML67-33 rapidly and reversibly affects K_2P2.1 (TREK-1) with EC₅₀s of 36.3 μM and 9.7 μM in cell-free and HEK293 cells, respectively.

HY-14600

Rosiglitazone maleate BRL 49653C	PPAR TRP Channel Autophagy Ferroptosis	Cancer Metabolic Disease Inflammation/Immunology
Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC₅₀s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a K_d of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).

HY-12811

PF-04856264	Sodium Channel	Neurological Disease
PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC₅₀s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect.

HY-103370

Talniflumate BA 7602-06	Chloride Channel	Inflammation/Immunology
Talniflumate (BA 7602-06) is the prodrug of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase. Talniflumate is an orally active *Ca²⁺-activated Cl^- channel* (CaCC)** blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome.

HY-B0233S

Isradipine-d3	Calcium Channel Autophagy	Neurological Disease Cardiovascular Disease
Isradipine-d3 (PN 200-110-d3) is the deuterium labeled Isradipine. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease.

HY-106345

ILS-920	FKBP Calcium Channel	Inflammation/Immunology Neurological Disease
ILS-920 is a nonimmunosuppressive Rapamycin analog with reduced immunosuppressive activity and potent neuroprotective activity. ILS-920 binds selectively to the immunophilin FKBP52 and to the β1-subunit of *L-type voltage-gated calcium channels* (VGCC). ILS-920 shows 200-fold selectivity for FKBP52** versus FKBP12.

HY-126010

Dooku1	Others	Cardiovascular Disease
Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel. Dooku1 inhibited 2 μM Yoda1-induced Ca²⁺-entry with IC₅₀ values of 1.3 μM (in HEK 293 cells) and 1.5 μM (in HUVECs). Dooku1 inhibits Yoda1-induced relaxation of aorta.

HY-11062

Icilin AG-3-5	TRP Channel	Inflammation/Immunology Neurological Disease
Icilin (AG-3-5) is a super-agonist of the transient receptor potential M8 (TRPM8) ion channel. Icilin activates TRPM8 in EGTA in a dose-dependent manner (EC₅₀=1.4 μM). Icilin is a “super-cooling agent”. Icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response.

HY-N7503

Psoralenoside	Histamine Receptor CaMK Calcium Channel	Cancer Infection Metabolic Disease
Psoralenoside is a benzofuran glycoside from Psoralea corylifolia. Psoralenoside exhibits high binding affinities against histaminergic H₁, calmodulin, and voltage-gated L-type calcium channels (E-value≥-6.5 Kcal/mol). Psoralenoside shows estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.

HY-12323

ISX-9 Isoxazole 9	Calcium Channel	Neurological Disease
ISX-9 (Isoxazole 9) is a potent inducer of adult neural stem cell differentiation. ISX-9 activates Ca²⁺ influx through both voltage-gated Ca²⁺ channels and NMDA receptors and increases neuroD expression. ISX-9 also induces cardiomyogenic differentiation of Notch-activated epicardium-derived cells (NECs).

HY-111655

SKA-31	Potassium Channel	Cardiovascular Disease
SKA-31 is a potent potassium channel activator with EC_50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure.

HY-13295

Vinpocetine Ethyl apovincaminate	Sodium Channel IKK Phosphodiesterase (PDE)	Inflammation/Immunology Neurological Disease Cardiovascular Disease Cancer
Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na⁺ channels. The IC₅₀ value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.

HY-B0185

Lidocaine Lignocaine	Sodium Channel MEK ERK NF-κB Apoptosis	Cancer Cardiovascular Disease
Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative commonly used to anesthetize. Lidocaine is a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.

HY-N1500

Pulegone	TRP Channel Endogenous Metabolite	Inflammation/Immunology
Pulegone, the major chemical constituent of Calamintha nepeta (L.) Savi essential oil which is an aromatic herb with a mint-oregano flavor, is one of avian repellents. The molecular target for the repellent action of Pulegone in avian species is nociceptive TRP ankyrin 1 (TRPA1). Pulegone stimulates both TRPM8 and TRPA1 channel in chicken sensory neurons and suppresses the former but not the latter at high concentrations.

HY-N0603

20(S)-Ginsenoside Rg3 20(S)-Propanaxadiol; S-ginsenoside Rg3	Sodium Channel Potassium Channel NF-κB COX Amyloid-β Endogenous Metabolite	Cancer Inflammation/Immunology Neurological Disease
20(S)-Ginsenoside Rg3 is the main component of Red ginseng. Ginsenoside Rg3 inhibits Na⁺ and hKv1.4 channel with IC₅₀s of 32.2±4.5 and 32.6±2.2 μM, respectively. 20(S)-Ginsenoside Rg3 also inhibits Aβ levels, NF-κB activity, and COX-2 expression.

HY-16689

VU 0240551	Potassium Channel	Others
VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC₅₀=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca²⁺ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission.

HY-B0166

L-Ascorbic acid L-Ascorbate; Vitamin C	Reactive Oxygen Species Calcium Channel Apoptosis Endogenous Metabolite	Cancer Metabolic Disease Neurological Disease
L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Ca_v3.2 channels with an IC₅₀ of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells.

HY-B1640

Ethacrynic acid	Gutathione S-transferase NF-κB Calcium Channel	Cancer Inflammation/Immunology
Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.

HY-B1193S

Terfenadine-d3	Potassium Channel Histamine Receptor Na+/Ca2+ Exchanger Caspase Apoptosis	Cancer Inflammation/Immunology Endocrinology
Terfenadine-d3 ((±)-Terfenadine-d3) is the deuterium labeled Terfenadine. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC₅₀ of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca²⁺ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.

HY-A0095

Flibanserin BIMT-17; BIMT-17BS	5-HT Receptor	Neurological Disease
Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (K_i=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD).

HY-10341

Fasudil Hydrochloride HA-1077 Hydrochloride; AT-877 Hydrochloride	ROCK Calcium Channel Autophagy PKA PKC HIV	Cancer
Fasudil Hydrochloride (HA-1077 Hydrochloride; AT877 Hydrochloride), is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an K_i of 0.33 μM for ROCK1, IC₅₀s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca²⁺ channel antagonist and vasodilator.

HY-12533S

Disopyramide-d14 tosylate salt	Sodium Channel Potassium Channel	Cardiovascular Disease
Disopyramide-d14 (Dicorantil-d14) tosylate salt is the deuterium labeled Disopyramide. Disopyramide (Dicorantil) is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action.

HY-B0563C

Ropivacaine mesylate	Sodium Channel Potassium Channel	Neurological Disease Cardiovascular Disease
Ropivacaine mesylate is a long-acting amide local anaesthetic agent for a spinal block and effectively blocks neuropathic pain. Ropivacaine blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibressup>[1]. Ropivacaine is also an inhibitor of K_2P (two-pore domain potassium channel) TREK-1 with an IC₅₀ of 402.7 μM in COS-7 cell's membrane.

HY-14336A

SB 271046 Hydrochloride SB 271046A	5-HT Receptor	Neurological Disease
SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pK_i of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC₅₀=0.16 μM).

HY-131335

p38α inhibitor 2	p38 MAPK	Inflammation/Immunology
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC₅₀ of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC₅₀=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets.

HY-125469

ICA-105665 PF-04895162	Potassium Channel	Neurological Disease
ICA-105665 (PF-04895162) is a potent and orally active neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels opener. ICA-105665 inhibits liver mitochondrial function and bile salt export protein (BSEP) transport (IC₅₀ of 311 μM). ICA-105665 can penetrate the blood-brain barrier and has antiseizure effects.

HY-108538

Ethacrynic acid D5	Gutathione S-transferase NF-κB Calcium Channel	Inflammation/Immunology
Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.

HY-15206

Glibenclamide Glyburide	Potassium Channel Mitochondrial Metabolism Autophagy CFTR P-glycoprotein	Metabolic Disease
Glibenclamide (Glyburide) is an orally active ATP-sensitive K⁺ channel (K_ATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of K_ATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.

HY-133012

GFB-8438	TRP Channel	Neurological Disease
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC₅₀s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.

HY-P1280

Margatoxin	Potassium Channel	Neurological Disease
Margatoxin, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (K_d=11.7 pM). Margatoxin inhibits the Kv1.2 (K_d=6.4 pM) and Kv1.1 (K_d=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research.

HY-N0822

Shikonin C.I. 75535; Isoarnebin 4	Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV	Cancer
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC₅₀ of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.

HY-P1136

Gap19	Gap Junction Protein	Cardiovascular Disease
Gap19, a peptide derived from nine amino acids of the Cx43 cytoplasmic loop (CL), is a potent and selective connexin 43 (Cx43) hemichannel blocker. Gap19 inhibits hemichannels caused by preventing intramolecular interactions of the C-terminus (CT) with the CL. Gap19 is not blocking GJ channels or Cx40/pannexin-1 hemichannels. Gap19 has protective effects against myocardial.

HY-121119

MRS 1523	Adenosine Receptor Calcium Channel	Inflammation/Immunology Neurological Disease Cardiovascular Disease
MRS 1523 is a potent and selective adenosine A₃ receptor antagonist with K_i values of 18.9 nM and 113 nM for human and rat A₃ receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A₁ and A_2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons.

HY-103112A

SB 243213 dihydrochloride	5-HT Receptor	Neurological Disease
SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT_2C receptor antagonist with a pK_i of 9.37 and a pK_b of 9.8 for human 5-HT_2C receptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.

HY-111191

ONO-2952	Others	Neurological Disease
ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with K_i of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment.

HY-103112B

SB 243213	5-HT Receptor	Neurological Disease
SB 243213 is an orally active, selective and high-affinity 5-HT_2C receptor antagonist with a pK_i of 9.37 and a pK_b of 9.8 for human 5-HT_2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.

HY-B0185AS

Lidocaine-d10 hydrochloride	Sodium Channel MEK ERK NF-κB Apoptosis	Cancer Cardiovascular Disease
Lidocaine-d10 (Lignocaine-d10) hydrochloride is the deuterium labeled Lidocaine hydrochloride. Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative commonly used to anesthetize. hydrochloride is a a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.

HY-107625A

SNAP 94847 hydrochloride	MCHR1 (GPR24)	Neurological Disease
SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (K_i= 2.2 nM, K_d=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.

HY-108006

Mirogabalin besylate DS 5565 besylate	Calcium Channel	Neurological Disease
Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with K_ds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.

HY-107625

SNAP 94847	MCHR1 (GPR24)	Neurological Disease Endocrinology
SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (K_i= 2.2 nM, K_d=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.

HY-103112

SB 243213 hydrochloride	5-HT Receptor	Neurological Disease
SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT_2C receptor antagonist with a pK_i of 9.37 and a pK_b of 9.8 for human 5-HT_2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.

HY-P1136A

Gap19 TFA	Gap Junction Protein	Cardiovascular Disease
Gap19 TFA, a peptide derived from nine amino acids of the Cx43 cytoplasmic loop (CL), is a potent and selective connexin 43 (Cx43) hemichannel blocker. Gap19 TFA inhibits hemichannels caused by preventing intramolecular interactions of the C-terminus (CT) with the CL. Gap19 TFA is not blocking GJ channels or Cx40/pannexin-1 hemichannels. Gap19 TFA has protective effects against myocardial.

HY-A0170

Trovafloxacin	Bacterial Topoisomerase Antibiotic	Infection
Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active *pannexin 1 channel* (PANX1) inhibitor with an IC₅₀ of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1**.

HY-101855

Anle138b	Amyloid-β	Neurological Disease
Anle138b, an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Anle138b strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Anle138b has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Anle138b blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology.

HY-N1483

Guanfu base A	Potassium Channel	Cardiovascular Disease
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a K_i of 1.20 μM in human liver microsomes (HLMs) and a K_i of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (K_i of 0.38 μM) and dog (K_i of 2.4 μM) microsomes. Guanfu base A also inhibits HERG channel current.

HY-100001

SKF-96365 hydrochloride	TRP Channel CRAC Channel Potassium Channel Autophagy Apoptosis	Cancer Cardiovascular Disease
SKF-96365 hydrochloride is a potent TRP channel blocker and a store-operated Ca²⁺ entry (SOCE) inhibitor. SKF-96365 hydrochloride significantly inhibits hERG, hKCNQ1/hKCNE1, hKir2.1 and hKv4.3 current, and significantly prolongs the QTc interval in isolated guinea pig hearts. SKF-96365 hydrochloride exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal cancer cells.

HY-N0215

L-Phenylalanine (S)-2-Amino-3-phenylpropionic acid	Calcium Channel iGluR Endogenous Metabolite	Metabolic Disease
L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca⁺ channels antagonist with a K_i of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (K_B of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.

HY-103399

Trovafloxacin mesylate	Bacterial Topoisomerase Antibiotic	Infection
Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active *pannexin 1 channel* (PANX1) inhibitor with an IC₅₀ of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1**.

HY-15589

GW9508	GPR40 Potassium Channel	Metabolic Disease Inflammation/Immunology Cardiovascular Disease
GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC₅₀s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (K_ATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.

HY-107535

AS1269574	GPR119 TRP Channel	Metabolic Disease
AS1269574 is a potent, orally available GPR119 agonist, with an EC₅₀ of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes.

HY-13750

Ebselen SPI-1005; PZ-51; CCG-39161	Calcium Channel Virus Protease HIV Phosphatase	Cancer Infection Inflammation/Immunology Neurological Disease
Ebselen (SPI-1005), a glutathione peroxidase mimetic, is a potent *voltage-dependent calcium channel* (VDCC) blocker. Ebselen potently inhibits M^pro (IC₅₀=0.67 μM) and COVID-19 virus (EC₅₀=4.67 μM).Ebselen is an inhibitor of HIV-1** capsid CTD dimerization. Ebselen, an organoselenium compound, can permeate the blood-brain barrier and has anti-inflammatory, antioxidant and anticancer activity.

HY-12501A

ITI-214	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-103369

PG01	CFTR	Endocrinology
PG01 is a potent CFTR Cl^- channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with K_d values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (K_a of 0.3 μM). PG01 increases ΔF508-CFTR Cl^- current after adding Forskolin.

HY-134542

CaV1.3 antagonist-1	Calcium Channel	Neurological Disease
CaV1.3 antagonist-1 is a potent and highly selective *Ca_V1.3 L-type calcium channel* (LTCC) antagonist with an IC₅₀** of 1.7 μM. CaV1.3 antagonist-1 inhibits Ca_V1.3 LTCC >600-fold more potently than Ca_V1.2 LTCC. CaV1.3 antagonist-1, a cyclopentyl derivative, has the potential for Parkinson's disease research.

HY-103399S

Trovafloxacin-d4 mesylate	Bacterial Topoisomerase Antibiotic	Infection
Trovafloxacin-d4 mesylate is the deuterium labeled Trovafloxacin mesylate. Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active *pannexin 1 channel* (PANX1) inhibitor with an IC₅₀ of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1**.

HY-108464A

Phenamil methanesulfonate	Sodium Channel TRP Channel	Metabolic Disease Inflammation/Immunology
Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible *epithelial sodium channel* (ENaC) blocker with an IC₅₀ of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca²⁺ transport with an IC₅₀ of 140 nM in a Ca²⁺ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP** signaling pathway. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.

HY-P1424A

Lei-Dab7 TFA	Potassium Channel
Lei-Dab7 TFA is a high affinity, selective K_Ca2.2 (SK2) channel blocker (K_d=3.8 nM). Lei-Dab7 TFA exhibits >200-fold selectivity for K_Ca2.2 over K_Ca2.1, K_Ca2.3, K_Ca3.1, K_v and Kir2.1. Lei-Dab7 TFA increases theta-burst responses and increases LTP in rat hippocampal slices in vitro.

HY-70057

Safinamide FCE 26743; EMD 1195686	Monoamine Oxidase	Neurological Disease
Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC₅₀=0.098 µM) over MAO-A (IC₅₀=580 µM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC₅₀=8 µM) than at resting (IC₅₀=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.

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-B1033

Metergoline	5-HT Receptor Dopamine Receptor Sodium Channel	Neurological Disease
Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pK_is of 8.64, 8.75 and 8.75 for 5-HT_2A, 5-HT_2B and 5-HT_2C, respectively. Metergoline is a high-affinity ligand for the h5-HT₇ receptor, with a K_i of 16 nM. Metergoline is also a reversible neural Na⁺ channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation.

HY-B1371A

Spiperone hydrochloride Spiroperidol hydrochloride	Dopamine Receptor 5-HT Receptor Adrenergic Receptor Chloride Channel	Inflammation/Immunology Neurological Disease
Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D₂ receptor (K_i values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D₂, D₃, D₄, D₁ and D₅ receptors, respectively) and 5-HT_2A/5-HT_1A receptor (K_is of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates *calcium-activated chloride channel* (CaCC)**. Antipsychotic and anti-inflammatory activities.

HY-118607

VU041	Potassium Channel Parasite	Infection
VU041 is a first submicromolar-affinity inhibitor of *Anopheles (An.) gambiae* and **Aedes (Ae.) aegypti inward rectifier potassium 1 (Kir1) channels with IC₅₀ values of 2.5 μM and 1.7 μM, respectively. VU041 inhibits appreciably is mammalian Kir2.1 (IC₅₀** of 12.7 μM), and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2/SUR1, and Kir7.1. VU041 also induces impaired Malpighian tubule function.

HY-19975

RN-1734	TRP Channel	Neurological Disease
RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC₅₀s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM). RN-1734 clearly decreases the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells.

HY-70057A

Safinamide mesylate FCE 26743 mesylate; EMD 1195686 mesylate	Monoamine Oxidase	Neurological Disease Cardiovascular Disease
Safinamide (FCE 26743; EMD 1195686) mesylate is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC₅₀=0.098 µM) over MAO-A (IC₅₀=580 nM). Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC₅₀=8 µM) than at resting (IC₅₀=262 µM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke et.al.

HY-128067

5-(N,N-Hexamethylene)-amiloride Hexamethylene amiloride; HMA	Sodium Channel HIV Apoptosis	Cancer Infection
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na⁺/H⁺ exchanger inhibitor, which decreases the intracellular pH (pH_i) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC₅₀s of 3.91 μM and 1.34 μM, respectively.

HY-12946

BI 653048	Glucocorticoid Receptor Cytochrome P450 HCV Protease	Infection Inflammation/Immunology
BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC₅₀ value of 55 nM. BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC₅₀>30 μM). BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.

HY-105285

Piromelatine Neu-P11	Melatonin Receptor 5-HT Receptor P2X Receptor TRP Channel Sodium Channel	Neurological Disease
Piromelatine (Neu-P11) is a melatonin MT₁/MT₂ receptor agonist, serotonin 5-HT_1A/5-HT_1D agonist, and serotonin 5-HT_2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.

HY-12946A

BI 653048 phosphate	Glucocorticoid Receptor Cytochrome P450 HCV Protease	Infection Inflammation/Immunology
BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC₅₀ value of 55 nM. BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC₅₀>30 μM). BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.

HY-N4267

Yangambin	Calcium Channel	Infection Cardiovascular Disease
Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca²⁺ influx through voltage-gated Ca²⁺ channels, leading to the reduction in [Ca²⁺]i in vascular smooth muscle cells and consequent peripheral vasodilation. Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC₅₀ of 33.8 μM and for anti-inflammatory activity with an IC₅₀ of 37.4 μM.

HY-70057S

Safinamide-d4	Monoamine Oxidase	Neurological Disease
Safinamide-d4 (FCE 26743-d4) is the deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC₅₀=0.098 µM) over MAO-A (IC₅₀=580 µM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC₅₀=8 µM) than at resting (IC₅₀=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.

HY-112544

IK1 inhibitor PA-6 PA-6	Potassium Channel	Cardiovascular Disease
IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent I_K1 (K_IR2.x ion-channel-carried inward rectifier current) inhibitor, with IC₅₀ values of 12-15 nM for human and mouse K_IR2.x currents. IK1 inhibitor PA-6 (PA-6) elevates K_IR2.1 protein expression and induces intracellular K_IR2.1 accumulation. IK1 inhibitor PA-6 (PA-6) has the potential to treat atrial fibrillation and arrhythmia.

HY-108400

SCH-23390 maleate R-(+)-SCH-23390 maleate	Dopamine Receptor 5-HT Receptor Potassium Channel	Neurological Disease
SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D₁-like receptor antagonist with K_is of 0.2 nM and 0.3 nM for the D₁ and D₅ receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT_2C receptor agonist with a K_i of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT₂ and 5-HT_1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC₅₀ of 268 nM.

HY-108596

BL-1249	Potassium Channel	Inflammation/Immunology
BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 potently activates K_2P2.1 (TREK-1) and K_2P10.1 (TREK-2) with EC₅₀ values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K_2P subfamilies. BL-1249 exhibits more selective for the bladder (EC₅₀ of 1.26 μM) than vascular tissue (EC₅₀ of 21.0 μM).

HY-19545A

SCH-23390 hydrochloride R-(+)-SCH-23390 hydrochloride	Dopamine Receptor 5-HT Receptor Potassium Channel	Neurological Disease
SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D₁-like receptor antagonist with K_is of 0.2 nM and 0.3 nM for the D₁ and D₅ receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT_2C receptor agonist with a K_i of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT₂ and 5-HT_1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC₅₀ of 268 nM.

HY-P2141

TRV-120027	Angiotensin Receptor	Cardiovascular Disease
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment.

HY-P2141A

TRV-120027 TFA	Angiotensin Receptor	Cardiovascular Disease
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment.

HY-15568A

A-317491 sodium salt hydrate	P2X Receptor	Inflammation/Immunology Neurological Disease
A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X₃ and P2X_2/3 receptors, with K_is of 22, 22, 9, and 92 nM for hP2X₃, rP2X₃, hP2X_2/3, and rP2X_2/3, respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X₃ and P2X_2/3 receptor-mediated calcium flux.

HY-15568

A-317491	P2X Receptor	Inflammation/Immunology Neurological Disease
A-317491 is a potent, selective and non-nucleotide antagonist of P2X₃ and P2X_2/3 receptors, with K_is of 22, 22, 9, and 92 nM for hP2X₃, rP2X₃, hP2X_2/3, and rP2X_2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X₃ and P2X_2/3 receptor-mediated calcium flux.

HY-19545AS

SCH-23390-d3 hydrochloride	Dopamine Receptor 5-HT Receptor Potassium Channel	Neurological Disease
SCH-23390-d3 (R-(+)-SCH-23390-d3) hydrochloride is the deuterium labeled SCH-23390 hydrochloride. SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D₁-like receptor antagonist with K_is of 0.2 nM and 0.3 nM for the D₁ and D₅ receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT_2C receptor agonist with a K_i of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT₂ and 5-HT_1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC₅₀ of 268 nM.

Cat. No.	Product Name

HY-L0099V

Sodium Ion Channel Library

5,440 compounds

Sodium Ion Channel Library contains about 5,440 compounds, and designed for discovery of new Nav1.7 channel blockers. Sodium voltage-gated ion channel is considered to be an important component in nociception. Therefore, selective Nav1.7 channel blockers are considered as important novel analgesics. The Sodium Ion Channel Library is rich in compounds bearing saturated backbones that can be often seen in structures of other ion-channel blockers.

HY-L0064V

Ion Channel Library 36,800 compounds

A unique collection of 36,800 diverse compounds intended to specifically target ion channels has been offered.

HY-L011

Membrane Transporter/Ion Channel Compound Library

857 compounds

Most of molecules enter or leave cells mainly via membrane transport proteins, which play important roles in several cellular functions, including cell metabolism, ion homeostasis, signal transduction, the recognition process in the immune system, energy transduction, etc. There are three major types of transport proteins, ATP-powered pumps, channel proteins and transporters. Transport proteins such as channels and transporters play important roles in the maintenance of intracellular homeostasis, and mutations in these transport protein genes have been identified in the pathogenesis of a number of hereditary diseases. In the central nervous system, ion channels have been linked to, but not limited to, many diseases such asataxias, paralyses, epilepsies, and deafness. This indicates the roles of ion channels in the initiation and coordination of movement, sensory perception, and encoding and processing of information. Ion channels are a major class of drug targets in drug development.

MCE designs a unique collection of 857 smal-molecule modulators that can be used for the research of Ion Channel and Membrane Transporter or high throughput screening (HTS) related drug discovery.

HY-L0098V

Calcium Ion Channel Library

10,560 compounds

Calcium Ion Channel Library contains about 10,560 compounds, and designed for discovery of new Voltage-gated calcium channel blockers. Calcium ion channels are responsible for an unusually large variety of physiological functions. Calcium ions entering the cell through voltage-gated channels serve as the second messenger of electrical signaling, initiating many different cellular events. Calcium Ion Channel Library encompasses both known chemotypes and molecules based on novel scaffolds identified in their in silico studies and MedChem based scaffold hopping projects.

HY-L070

Neuroprotective Compound Library

653 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 653 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-L046

Anti-Cardiovascular Disease Compound Library

890 compounds

Cardiovascular diseases (CVDs) are a group of disorders of the heart and blood vessels which include coronary heart disease, cerebrovascular disease, peripheral arterial disease, rheumatic heart disease, etc. CVDs are the number 1 cause of death globally. Smoking, unhealthy nutrition, aging population, lack of physical activity, arterial hypertension, or diabetes can promote cardiovascular disease like myocardial infarction or stroke. It is multifactorial and encompasses a multitude of mechanisms, such as eNOS uncoupling, reactive oxygen species formation, chronic inflammatory disorders and abnormal calcium homeostasis. Antioxidant, anti-inflammatory and anti-diabetes agents may reduce the cardiovascular disease risk.

MCE supplies a unique collection of 890 compounds with confirmed anti-cardiovascular activity. These compounds mainly target metabolic enzyme, membrane transporter, ion channel, inflammation related signaling pathways. MCE Anti-Cardiovascular Disease Compound Library can be used for cardiovascular diseases related research and high throughput and high content screening for new drugs.

HY-L062

Neurotransmitter Receptor Compound Library

1144 compounds

Neurotransmitter (NT) receptors, also known as neuroreceptors, are a broadly diverse group of membrane proteins that bind neurotransmitters for neuronal signaling. There are two major types of neurotransmitter receptors: ionotropic and metabotropic. Ionotropic receptors are ligand-gated ion channels, meaning that the receptor protein includes both a neurotransmitter binding site and an ion channel. The binding of a neurotransmitter molecule (the ligand) to the binding site induces a conformational change in the receptor structure, which opens, or gates, the ion channel. The term “metabotropic receptors” is typically used to refer to transmembrane G-protein-coupled receptors. Metabotropic receptors trigger second messenger-mediated effects within cells after neurotransmitter binding.

In some neurological diseases, the neurotransmitter receptor itself appears to be the target of the disease process. Many neuroactive drugs act by modifying neurotransmitter receptors. A better understanding of neurotransmitter receptor changes in disease may lead to improvements in therapy.

MCE designs a unique collection of 1144 compounds targeting a variety of neurotransmitter receptors. MCE Neurotransmitter Receptor Compound Library is a useful tool for neurological diseases drug discovery.

HY-L0074V

Aquaporins Library	1,500 compounds
The library was designed to find molecules which target both end-chains of water channels (Aquaporins) AQ1, AQ4, AQ5 monomers and internal central pore of AQ5, which possess same physico-chemical properties as those in AQ1 and AQ4.

HY-L028

CNS-Penetrant Compound Library

550 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 550 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-L0065V

CNS Library	56,320 compounds
A unique collection of 56,320 novel small molecules with high CNS MPO (Central Nervous System Multiparameter Optimization) scores. The CNS-active molecules which are able to penetrate blood-brain barrier (BBB) were low polar surface area, low degree of possible hydrogen bond formation and low ClogP values.

Cat. No.	Product Name	Type

HY-100545

BAPTA-AM	Biochemical Assay Reagents
BAPTA-AM is a well-known membrane permeable Ca²⁺ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC₅₀s of 1.3 μM, 1.45 μM and 1.23 μM, respectively.

HY-107754

Cesium chloride	Biochemical Assay Reagents
Cesium chloride is a blocker of potassium channel. Cesium chloride prevents the decrease of Na⁺ transport produced by Alloxan. Cesium chloride has induced cardiac arrhythmias, including torsade de pointes in animal models.

Cat. No.	Product Name	Target	Research Area

HY-P1886

*Kv3, Channel* Containing Protein (567-585)**	Peptides	Neurological Disease
Kv3, Channel Containing Protein (567-585) corresponds to amino acids 567 to 585 fragment of the Kv3.1b channel containing protein. Kv3 channel protein is expressed by parvalbumin (PV)-containing pallidal neurons .

HY-P1218A

Phrixotoxin 3 TFA	Sodium Channel	Neurological Disease
Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC₅₀s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.

HY-P1220

Huwentoxin-IV	Sodium Channel	Neurological Disease
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC₅₀s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain.

HY-P1220A

Huwentoxin-IV TFA	Sodium Channel	Neurological Disease
Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC₅₀s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain.

HY-P1078

Huwentoxin XVI	Calcium Channel	Neurological Disease
Huwentoxin XVI, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC₅₀ of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels.

HY-P1078A

Huwentoxin XVI TFA	Calcium Channel	Neurological Disease
Huwentoxin XVI TFA, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC₅₀ of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI TFA has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels.

HY-P0189

ω-Conotoxin GVIA
Calcium Channel Neurological Disease

ω-Conotoxin GVIA is an inhibitor of the N-type Ca²⁺ channel.
HY-P0189A

ω-Conotoxin GVIA TFA
Calcium Channel Neurological Disease

ω-Conotoxin GVIA TFA is an inhibitor of the N-type Ca²⁺ channel.

HY-P1221

ProTx II	Sodium Channel	Neurological Disease
ProTx II is a selective blocker of Nav1.7 sodium channels with an IC₅₀ of 0.3 nM, and is at least 100-fold selective for Nav1.7 over other sodium channel subtypes. ProTx-II inhibits sodium channels by decreasing channel conductance and shifting activation to more positive potentials and blocks action potential propagation in nociceptors.

HY-P1073

ProTx-I	Calcium Channel Sodium Channel Potassium Channel	Cancer
ProTx-I, a venom toxin of the tarantula Thrixopelma pruriens, is a potent, selective Ca_V3.1 channel blocker with IC₅₀ values of 0.2 μM and 31.8 μM for hCa_V3.1 and hCa_V3.2 respectively. ProTx-I is also a potent blocker for voltage-gated Na⁺ channels and inhibits K_V 2.1 channels.

HY-P0190

Iberiotoxin	Potassium Channel	Cardiovascular Disease
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca²⁺-activated K⁺ channel inhibitor with a K_d of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels.

HY-P1424

Lei-Dab7	Potassium Channel	Neurological Disease
Lei-Dab7 is a potent and selective SK2 (KCa2.2) channels blocker with a K_d of 3.8 nM. Lei-Dab7 shows low or no activity on KCa1, KCa3, Kv and Kir2.1 channels.

HY-P1080

ω-Agatoxin IVA	Calcium Channel	Neurological Disease
ω-Agatoxin IVA is a potent, selective P/Q type Ca²⁺ channel blocker with IC₅₀s of 2 nM and 90 nM for P-type and Q-type Ca²⁺ channels, respectively. ω-Agatoxin IVA (IC₅₀, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA has no effect on L-type or N-type calcium channels.

HY-P1079

ω-Agatoxin TK	Calcium Channel	Neurological Disease
ω-Agatoxin TK, a peptidyl toxin of the venom of Agelenopsis aperta, is a potent and selective P/Q type Ca²⁺ channel blocker. ω-Agatoxin TK inhibits the high K⁺ depolarisation-induced rise in internal Ca²⁺ in cerebral isolated nerve endings with an IC₅₀ of of 60 nM. ω-Agatoxin TK has no effect on L-type, N-type, or T-type calcium channels.

HY-P1077

CALP1	Calcium Channel mGluR Phosphodiesterase (PDE) Apoptosis	Inflammation/Immunology
CALP1 is a calmodulin (CaM) agonist (K_d of 88 µM) with binding to the CaM EF-hand/Ca²⁺-binding site. CALP1 blocks calcium influx and apoptosis (IC₅₀ of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity.

HY-P0191

Charybdotoxin
Potassium Channel Inflammation/Immunology

Charybdotoxin, a 37-amino acid peptide, is a K⁺ channel blocker.

HY-P1077A

CALP1 TFA	Calcium Channel mGluR Phosphodiesterase (PDE) Apoptosis	Inflammation/Immunology
CALP1 TFA is a calmodulin (CaM) agonist (K_d of 88 µM) with binding to the CaM EF-hand/Ca²⁺-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC₅₀ of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity.

HY-P0191A

Charybdotoxin TFA
Potassium Channel Inflammation/Immunology

Charybdotoxin TFA, a 37-amino acid peptide, is a K⁺ channel blocker.

HY-P2324

Gramicidin A	Bacterial HIF/HIF Prolyl-Hydroxylase	Infection
Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α).

HY-P1440A

BeKm-1 TFA	Potassium Channel
BeKm-1 TFA is a potent and selective KV11.1 (hERG) channel blocker. BeKm-1 TFA is selective for KV11.1 over a panel of 14 other potassium channels. BeKm-1 TFA dose-dependently prolongs QTc interval in isolated rabbit heart.

HY-P1410

GsMTx4	Peptides	Inflammation/Immunology
GsMTx4 is a spider venom peptide that selectively inhibits cation-permeable *mechanosensitive channels* (MSCs)** belonging to the Piezo and TRP channel families. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology. GsMTx4 significantly attenuates bladder hyperactivity.

HY-128696

Amlodipine aspartic acid impurity Amlodipine aspartate	Peptides	Cardiovascular Disease
Amlodipine aspartic acid impurity is the impurity of Amlodipine aspartic acid. Amlodipine aspartic acid is a calcium channel blocker with antihypertensive and antianginal properties.

HY-P1441

Mambalgin 1	Sodium Channel	Others
Mambalgin-1 is a toxin isolated from black mamba venom. Mambalgin-1 is a disulfide-rich polypeptide consisting of 57 amino acids and belongs to the family of three-finger toxins. Mambalgin-1 can bind to and stabilize ASICs (acid-sensing ion channels) in a physiologically relevant closed-channel conformation.

HY-P1410A

GsMTx4 TFA	Peptides	Inflammation/Immunology
GsMTx4 TFA is a spider venom peptide that selectively inhibits cation-permeable *mechanosensitive channels* (MSCs)** belonging to the Piezo and TRP channel families. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology. GsMTx4 TFA significantly attenuates bladder hyperactivity.

HY-P0173A

Chlorotoxin	Chloride Channel	Cancer
Chlorotoxin is a 36 amino-acid peptide from the venom of the Israeli scorpion Leiurus quinquestriatus with anticancer activity. Chlorotoxin is a chloride channel blocker.

HY-P1411

Psalmotoxin 1
PcTx1; Psalmopoeus cambridgei toxin-1
Peptides Neurological Disease

Psalmotoxin 1, a protein toxin from a tarantula, inhibits H⁺-gated acid-sensing ion channel (ASIC1a).

HY-P0173B

Chlorotoxin TFA	Chloride Channel	Cancer
Chlorotoxin TFA is a peptide isolated from the venom of the scorpion Leiurus quinquestriatus, acts as a chloride channel blocker. Anti-cancer activity.

HY-P1084

β-Pompilidotoxin β-PMTX	Sodium Channel	Neurological Disease
β-Pompilidotoxin (β-PMTX), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells.

HY-P1075

CALP3	Calcium Channel	Cancer Neurological Disease
CALP3, a Ca²⁺-like peptide, is a potent Ca²⁺ channel blocker that activates EF hand motifs of Ca²⁺-binding proteins. CALP3 can functionally mimic increased [Ca²⁺]_i by modulating the activity of Calmodulin (CaM), Ca²⁺ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.

HY-P1084A

β-Pompilidotoxin TFA β-PMTX TFA	Sodium Channel	Neurological Disease
β-Pompilidotoxin TFA (β-PMTX TFA), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells.

HY-P1075A

CALP3 TFA	Calcium Channel	Cancer Neurological Disease
CALP3 TFA, a Ca²⁺-like peptide, is a potent Ca²⁺ channel blocker that activates EF hand motifs of Ca²⁺-binding proteins. CALP3 TFA can functionally mimic increased [Ca²⁺]_i by modulating the activity of Calmodulin (CaM), Ca²⁺ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.

HY-P1274A

ShK-Dap22 TFA	Potassium Channel	Inflammation/Immunology
ShK-Dap22 TFA is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 TFA is a selective Kv1.3 channel blocker with IC₅₀s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively.

HY-P0062

Ziconotide SNX-111	Calcium Channel	Inflammation/Immunology Neurological Disease
Ziconotide (SNX-111), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide reduces synaptic transmission, and can be used for chronic pain research.

HY-P1282

Agitoxin-2
Potassium Channel Neurological Disease

Agitoxin-2 is a K+ channel inhibitor, with IC₅₀ values of 201 pM and 144 pM for mK_V1.3 and mK_V1.1, respectively).
HY-P1282A

Agitoxin-2 TFA
Potassium Channel Neurological Disease

Agitoxin-2 TFA is a K+ channel inhibitor, with IC₅₀ values of 201 pM and 144 pM for mK_V1.3 and mK_V1.1, respectively).

HY-P0188

ω-Conotoxin MVIIC	Calcium Channel	Neurological Disease
ω-Conotoxin MVIIC is a N- and P/Q-type Ca²⁺ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release.

HY-P0188A

ω-Conotoxin MVIIC TFA	Calcium Channel	Neurological Disease
ω-Conotoxin MVIIC TFA is a N- and P/Q-type Ca²⁺ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release.

HY-P0062A

Ziconotide TFA SNX-111 TFA	Calcium Channel	Inflammation/Immunology Neurological Disease
Ziconotide TFA (SNX-111 TFA), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide TFA reduces synaptic transmission, and can be used for chronic pain research.

HY-P0256

Apamin Apamine	Potassium Channel	Inflammation/Immunology Neurological Disease
Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca²⁺-activated K⁺ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.

HY-P0256A

Apamin TFA Apamine TFA	Potassium Channel	Inflammation/Immunology Neurological Disease
Apamin TFA (Apamine TFA) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca²⁺-activated K⁺ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.

HY-P1441A

Mambalgin 1 TFA	Sodium Channel
Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC₅₀ values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.

HY-P1074

SNX-482	Calcium Channel	Neurological Disease
SNX-482, a peptidyl toxin of the spider Hysterocrates gigas, is a potent, high affinity, selective and voltage-dependent R-type Ca_V2.3 channel blocker with an IC₅₀ of 30 nM. SNX-482 has antinociceptive effect.

HY-P1249

Neuropeptide SF(mouse,rat)	Neuropeptide Y Receptor	Neurological Disease
Neuropeptide SF (mouse,rat) is a potent neuropeptide FF receptor agonist with K_i values are 48.4 nM and 12.1 nM for NPFF1 and NPFF2, respectively. Neuropeptide SF increases the amplitude of the sustained current of heterologously expressed acid sensing ion channel 3 (ASIC3) .

HY-P1249A

Neuropeptide SF(mouse,rat) TFA	Neuropeptide Y Receptor	Neurological Disease
Neuropeptide SF (mouse,rat) TFA is a potent neuropeptide FF receptor agonist with K_i values are 48.4 nM and 12.1 nM for NPFF1 and NPFF2, respectively. Neuropeptide SF TFA increases the amplitude of the sustained current of heterologously expressed acid sensing ion channel 3 (ASIC3) .

HY-P1346

APETx2	Sodium Channel	Inflammation/Immunology Neurological Disease
APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC₅₀ of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.

HY-P1422

Spadin	Potassium Channel	Neurological Disease
Spadin, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K_2P2.1) channel activity. Spadin binds specifically to TREK-1 with an affinity of 10 nM. Spadin is an efficient antidepressant in mice.

HY-P1422A

Spadin TFA	Potassium Channel	Neurological Disease
Spadin TFA, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K_2P2.1) channel activity. Spadin TFA binds specifically to TREK-1 with an affinity of 10 nM. Spadin TFA is an efficient antidepressant in mice.

HY-P1280

Margatoxin	Potassium Channel	Neurological Disease
Margatoxin, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (K_d=11.7 pM). Margatoxin inhibits the Kv1.2 (K_d=6.4 pM) and Kv1.1 (K_d=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research.

HY-P1136

Gap19	Gap Junction Protein	Cardiovascular Disease
Gap19, a peptide derived from nine amino acids of the Cx43 cytoplasmic loop (CL), is a potent and selective connexin 43 (Cx43) hemichannel blocker. Gap19 inhibits hemichannels caused by preventing intramolecular interactions of the C-terminus (CT) with the CL. Gap19 is not blocking GJ channels or Cx40/pannexin-1 hemichannels. Gap19 has protective effects against myocardial.

HY-P1136A

Gap19 TFA	Gap Junction Protein	Cardiovascular Disease
Gap19 TFA, a peptide derived from nine amino acids of the Cx43 cytoplasmic loop (CL), is a potent and selective connexin 43 (Cx43) hemichannel blocker. Gap19 TFA inhibits hemichannels caused by preventing intramolecular interactions of the C-terminus (CT) with the CL. Gap19 TFA is not blocking GJ channels or Cx40/pannexin-1 hemichannels. Gap19 TFA has protective effects against myocardial.

HY-P1424A

Lei-Dab7 TFA	Potassium Channel
Lei-Dab7 TFA is a high affinity, selective K_Ca2.2 (SK2) channel blocker (K_d=3.8 nM). Lei-Dab7 TFA exhibits >200-fold selectivity for K_Ca2.2 over K_Ca2.1, K_Ca2.3, K_Ca3.1, K_v and Kir2.1. Lei-Dab7 TFA increases theta-burst responses and increases LTP in rat hippocampal slices in vitro.

HY-P2141

TRV-120027	Angiotensin Receptor	Cardiovascular Disease
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment.

HY-P2141A

TRV-120027 TFA	Angiotensin Receptor	Cardiovascular Disease
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment.

Cat. No.	Product Name	Target	Category

HY-B0114

Oxcarbazepine GP 47680	Sodium Channel Apoptosis	Alkaloids
Oxcarbazepine is a sodium channel blocker. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines. Anti-cancer and anticonvulsant effects.

HY-N5101

Kobusin	CFTR Chloride Channel	Natural Products
Kobusin is a bisepoxylignan isolated from the Pnonobio biondii Pamp. Kobusin is an activator of CFTR and CaCCgie chloride channels and a inhibitor of ANO1/CaCC (calcium-activated chloride channel) channel.

HY-N2077

Heteroclitin D
Calcium Channel Phenylpropanoids

Heteroclitin D is a lignin from Kadsura medicinal plants with anti-liqid peroxidation. Heteroclitin D inhibits L-type calcium channels.

HY-P0190

Iberiotoxin	Potassium Channel	Acids and Aldehydes
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca²⁺-activated K⁺ channel inhibitor with a K_d of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels.

HY-N2338

Cholesterol myristate Cholesteryl myristate; Cholesteryl tetradecanoate	nAChR GABA Receptor Potassium Channel Endogenous Metabolite	Steroids
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.

HY-12515

Nicardipine YC-93 free base	Calcium Channel	Natural Products
Nicardipine (YC-93 free base) is a calcium channel blocker with an IC₅₀ of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.

HY-12545

Brevetoxin-3 PbTx-3	Sodium Channel	Natural Products
Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na⁺ channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na⁺ channels, inhibits the inactivation of Na⁺ channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.

HY-B2136

Tannic acid
Potassium Channel Phenols

Tannic acid is a novel hERG channel blocker with IC₅₀ of 3.4 μM.
HY-N2164

3-Deoxyaconitine
Sodium Channel Alkaloids

3-Deoxyaconitine a diterpenoid alkaloid, is a sodium channel activator.

HY-N2433

Paederosidic acid methyl ester	Potassium Channel	Terpenoids and Glycosides
Paederosidic acid methyl ester is a ATP‐sensitive K⁺ channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K⁺ channel in the brain and spinal cord level.

HY-P0163

Gramicidin
Bacterial Antibiotic Natural Products

Gramicidin is an antimicrobial peptide assembling as channels in membranes and increasing their permeability towards cations.

HY-113147

L-Palmitoylcarnitine	Potassium Channel Endogenous Metabolite	Acids and Aldehydes
L-Palmitoylcarnitine, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia. L-Palmitoylcarnitine inhibits K_ATP channel activity, without affecting the single channel conductance, through interaction with Kir6.2.

HY-W032013

1-Octanol Octanol	Calcium Channel Endogenous Metabolite	Natural Products
1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC₅₀ of 4 μM for native T-currents. 1-Octanol is a highly attractive biofuel with diesel-like properties.

HY-B0552A

Dibucaine hydrochloride Cinchocaine hydrochloride	Sodium Channel	Natural Products
Dibucaine hydrochloride (Cinchocaine hydrochloride) is a sodium channel inhibitor. Dibucaine hydrochloride is a potent SChE inhibitor.

HY-113147B

L-Palmitoylcarnitine TFA	Endogenous Metabolite Potassium Channel	Acids and Aldehydes
L-Palmitoylcarnitine TFA, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia. L-Palmitoylcarnitine TFA inhibits K_ATP channel activity, without affecting the single channel conductance, through interaction with Kir6.2.

HY-D0143

Quinine	Parasite Potassium Channel	Natural Products
Quinine is an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine is a potassium channel inhibitor that inhibits WT mouse Slo3 (K_Ca5.1) channel currents evoked by voltage pulses to +100 mV with an IC₅₀ of 169 μM.

HY-N9404

6-Benzoylheteratisine
Sodium Channel Alkaloids

6-Benzoylheteratisine is a naturally occurring antagonist of the Na⁺ channel activator aconitine.

HY-N1378

(E)-Cardamonin (E)-Cardamomin; (E)-Alpinetin chalcone	TRP Channel Apoptosis	Flavonoids
(E)-Cardamonin ((E)-Cardamomin) is a novel antagonist of hTRPA1 cation channel with an IC₅₀ of 454 nM.

HY-B1304

(-)-Sparteine sulfate pentahydrate (-)-Lupinidine sulfate pentahydrate	Sodium Channel	Alkaloids
(-)-Sparteine sulfate pentahydrate ((-)-Lupinidine sulfate pentahydrate) is a class 1a antiarrhythmic agent and a sodium channel blocker.

HY-116330A

Hyperforin dicyclohexylammonium salt Hyperforin DCHA	TRP Channel Calcium Channel	Natural Products
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca²⁺ levels by activating Ca²⁺-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.

HY-D0143B

Quinine hemisulfate hydrate	Parasite Potassium Channel	Alkaloids
Quinine hemisulfate hydrate, an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine hemisulfate hydrate is a potassium channel inhibitor that inhibits WT mouse Slo3 (K_Ca5.1) channel currents evoked by voltage pulses to +100 mV, with an IC₅₀ of 169 μM.

HY-N0172

Caffeic acid
TRP Channel Lipoxygenase Endogenous Metabolite Phenylpropanoids

Caffeic acid is an inhibitor of both TRPV1 ion channel and 5-Lipoxygenase (5-LO).
HY-12502

Efonidipine
NZ-105; (±)-Efonidipine
Calcium Channel Natural Products

Efonidipine(NZ-105) is a dual T-type and L-type calcium channel blocker (CCB).
HY-17001A

Flupirtine
D 9998
Potassium Channel iGluR Alkaloids

Flupirtine(D 9998) is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.

HY-B0151

Pregnenolone 3β-Hydroxy-5-pregnen-20-one	Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy	Steroids
Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

HY-N7395

Cyclic ADP-ribose cADPR	Calcium Channel TRP Channel Endogenous Metabolite	Acids and Aldehydes
Cyclic ADP-ribose (cADPR) is a potent second messenger for calcium mobilization that is synthesized from NAD⁺ by an ADP-ribosyl cyclase. Cyclic ADP-ribose increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels.

HY-B1302

Quinidine hydrochloride monohydrate	Potassium Channel Parasite	Natural Products
Quinidine hydrochloride monohydrate is an anti-arrythmic agent which is also a potent blocker of K⁺ channel with an IC₅₀ of 19.9 μM.

HY-N0601

Ginsenoside Rf Panaxoside Rf	Calcium Channel Endogenous Metabolite	Saccharides and Glycosides Terpenoids and Glycosides
Ginsenoside Rf is a trace component of ginseng root. Ginsenoside Rf inhibits N-type Ca²⁺ channel.

HY-N7511

O-Nornuciferine
Potassium Channel Alkaloids

O-Nornuciferine, an aporphine-type alkaloid from lotus leaf, is a potent hERG channel inhibitor.
HY-W016498

Paraxanthine
Endogenous Metabolite Alkaloids

Paraxanthine, a caffeine metabolite, provides protection against Dopaminergic cell death via stimulation of Ryanodine Receptor Channels.

HY-B1739

Pregnenolone monosulfate 3β-Hydroxy-5-pregnen-20-one monosulfate	Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy	Steroids
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication. Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

HY-110189

Pregnenolone monosulfate sodium salt 3β-Hydroxy-5-pregnen-20-one monosulfate Sodium salt	Cannabinoid Receptor TRP Channel Endogenous Metabolite Autophagy	Steroids
Pregnenolone monosulfate sodium salt (3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

HY-P0173A

Chlorotoxin	Chloride Channel	Natural Products
Chlorotoxin is a 36 amino-acid peptide from the venom of the Israeli scorpion Leiurus quinquestriatus with anticancer activity. Chlorotoxin is a chloride channel blocker.

HY-108451

Ononetin
TRP Channel Phenols

Ononetin, a natural deoxybenzoin, is a potent and selective TRPM3 channel blocker with an IC₅₀ of 0.3 μM.

HY-N7395A

Cyclic ADP-ribose ammonium cADPR ammonium	Calcium Channel TRP Channel Endogenous Metabolite	Acids and Aldehydes
Cyclic ADP-ribose ammonium (cADPR ammonium) is a potent second messenger for calcium mobilization that is synthesized from NAD⁺ by an ADP-ribosyl cyclase. Cyclic ADP-ribose ammonium increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels.

HY-12546

Brevetoxin B Brevetoxin-2; PbTx-2	Sodium Channel	Natural Products
Brevetoxin B (Brevetoxin-2; PbTx-2) is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. Brevetoxin B binds to site 5 on the alpha subunit of voltage-gated sodium channels (IC₅₀=15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively.

HY-B0887

Permethrin NRDC-143	Parasite	Natural Products
Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.

HY-N6778

Paxilline	Potassium Channel Calcium Channel	Alkaloids
Paxilline is an indole alkaloid mycotoxin from Penicillium paxilli, acts as a potent BK channels inhibitor by an almost exclusively closed-channel block mechanism. Paxilline also inhibits the sarco/endoplasmic reticulum Ca²⁺ ATPase (SERCA) with IC₅₀s between 5 μM and 50 μM for differing isoforms. Paxilline possesses significant anticonvulsant activity.

HY-N0239

Bulleyaconitine A	Sodium Channel	Alkaloids
Bulleyaconitine A is an analgesic and antiinflammatory drug isolated from Aconitum plants; has several potential targets, including voltage-gated Na+ channels.

HY-W011641

(±)-Naringenin	Potassium Channel	Flavonoids
(±)-Naringenin is a naturally-occurring flavonoid. (±)-Naringenin displays vasorelaxant effect on endothelium-denuded vessels via the activation of BK_Ca channels in myocytes.

HY-B0799

Dihydroergotoxine mesylate Ergoloid mesylates	GABA Receptor	Alkaloids
Dihydroergotoxine mesylate is a complex of closely related alkaloid salts; Binds with high affinity to the GABAA receptor Cl- channel, producing an allosteric interaction with the benzodiazepine site.

HY-107301

Dehydrosoyasaponin I Soyasaponin Be; DHS-I	Potassium Channel	Saccharides and Glycosides
Dehydrosoyasaponin I (Soyasaponin Be;DHS-I), a triterpene glycoside, is a potent and reversible calcium-activated potassium (maxi-K) channels activator.

HY-N0714

Berbamine	NF-κB Autophagy	Alkaloids
Berbamine is a natural compound extracted from traditional Chinese medicine Barberry with anti-tumor, immunomodulatory and cardiovascular effects. Berbamine is a calcium channel blocker.

HY-N6708

Alamethicin	Bacterial Antibiotic	Natural Products
Alamethicin, isolated from Trichoderma viride, is a channel-forming peptide antibiotic and induces voltage-gated conductance in model and cell membranes.

HY-P0173B

Chlorotoxin TFA	Chloride Channel	Natural Products
Chlorotoxin TFA is a peptide isolated from the venom of the scorpion Leiurus quinquestriatus, acts as a chloride channel blocker. Anti-cancer activity.

HY-B1494

Picrotoxinin	Chloride Channel GABA Receptor	Natural Products
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABA_A receptor antagonist, which negatively modulates the action of GABA on GABA_A receptors.

HY-N0663

Talatisamine	Potassium Channel	Alkaloids
Talatisamine, a aconitum alkaloid, is specific K⁺ channel blocker. Talatisamine attenuates beta-amyloid oligomers induced neurotoxicity in cultured cortical neurons.

HY-101238

Agmatine sulfate	Imidazoline Receptor NO Synthase Endogenous Metabolite	Alkaloids
Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.

HY-W013093

Uridine triphosphate trisodium salt UTP triSodium salt; Uridine 5'-triphosphate triSodium salt	Others	Acids and Aldehydes
Uridine triphosphate trisodium salt is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.

HY-N3710

Dehydrocrenatidine Kumujian G; O-Methylpicrasidine I	JAK Apoptosis	Alkaloids
Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain.

HY-N8404

Chlorahololide C	Potassium Channel	Terpenoids and Glycosides
Chlorahololide C, a lindenane sesquiterpenoid dimer, is isolated from Chloranthus holostegius. Chlorahololide C is a potent and selective potassium channel blocker, with an IC₅₀ of 3.6 μM.

HY-B1671

(+)-Kavain	GABA Receptor Sodium Channel Calcium Channel	Flavonoids
(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na⁺ and Ca²⁺ channels. (+)-Kavain is shown to bind at the α4β2δ GABA_A receptor and potentiate GABA efficacy. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied.

HY-N2060

Evocarpine	Apoptosis Bacterial	Alkaloids
Evocarpine, a quinolone alkaloid that could be isolated from Evodiae fructus, inhibitss Ca²⁺ influx through voltage-dependent calcium channels. Antimycobacterial activity.

HY-135013

Umbellulone	TRP Channel	Natural Products
Umbellulone is an active constituent of the leaves of Umbellularia californica. Umbellulone stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism.

HY-N0252

Catharanthine (+)-3,4-Didehydrocoronaridine	Calcium Channel	Alkaloids
Catharanthine is an alkaloid isolated from Madagascar periwinkle, inhibits voltage-operated L-type Ca²⁺ channel, with anti-cancer and blood pressure-lowering activity.

HY-N5006

Guanfu base G	Potassium Channel	Alkaloids
Guanfu base G is an antiarrhythmic alkaloid isolated from Aconitum coreanum. Guanfu base G inhibits HERG channel current with an IC₅₀ of 17.9 μM.

HY-N1469

Kaurenoic acid	Others	Terpenoids and Glycosides
Kaurenoic acid is a diterpene from Sphagneticola trilobata, inhibits Inflammatory Pain by the inhibition of cytokine production and activation of the NO–cyclic GMP–PKG–ATP-sensitive potassium channel signaling pathway.

HY-N0252A

Catharanthine Tartrate (+)-3,4-Didehydrocoronaridine Tartrate	Calcium Channel	Alkaloids
Catharanthine Tartrate is an alkaloid isolated from Madagascar periwinkle, inhibits voltage-operated L-type Ca²⁺ channel, with anti-cancer and blood pressure-lowering activity.

HY-107372

Uridine triphosphate UTP; Uridine 5'-triphosphate	Endogenous Metabolite	Acids and Aldehydes
Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.

HY-N6691

Veratridine 3-Veratroylveracevine	Sodium Channel	Natural Products
Veratridine (3-Veratroylveracevine), a alkaloid derived from plants in the family Liliaceae, is a sodium channel agonist. Veratridine inhibits the peak current of Nav1.7, with an IC₅₀ of 18.39 µM.

HY-N2197

Hirsuteine	Others	Alkaloids
Hirsuteine is an indole alkaloid extracted from Uncaria genus. Hirsuteine non-competitively antagonizes nicotine-mediated dopamine release by blocking ion permeation through nicotinic receptor channel complexes.

HY-N1584

Halofuginone RU-19110	DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel	Alkaloids
Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

HY-N2412

Irisolidone	Chloride Channel	Flavonoids
Irisolidone is a major isoflavone found in Pueraria lobata flowers. Irisolidone exhibits potent hepatoprotective activity. Irisolidone shows the high efficacy for *volume-regulated anion channels* (VRAC)** blockade.

HY-B1500

2,2,2-Trichloroethanol	Potassium Channel	Natural Products
2,2,2-Trichloroethanol, the active form of the sedative hypnotic drug chloral hydrate, is an agonist for the nonclassical K_2P channels TREK-1 (KCNK2) and TRAAK (KCNK4).

HY-N1584A

Halofuginone hydrobromide RU-19110 hydrobromide	DNA/RNA Synthesis TGF-beta/Smad Parasite Sodium Channel Calcium Channel	Alkaloids
Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

HY-N6868

Dimethyl lithospermate B dmLSB	Sodium Channel	Natural Products
Dimethyl lithospermate B (dmLSB) is a selective Na⁺ channel agonist. Dimethyl lithospermate B slows inactivation of sodium current (INa), leading to increased inward current during the early phases of the action potential (AP).

HY-N0252B

Catharanthine Sulfate (+)-3,4-Didehydrocoronaridine Sulfate	Calcium Channel	Natural Products
Catharanthine Sulfate ((+)-3,4-Didehydrocoronaridine Sulfate) is an alkaloid isolated from Madagascar periwinkle, inhibits voltage-operated L-type Ca²⁺ channel, with anti-cancer and blood pressure-lowering activities.

HY-N0042

Ginsenoside Rc Panaxoside Rc	GABA Receptor TNF Receptor Interleukin Related	Saccharides and Glycosides Terpenoids and Glycosides
Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptor_A (GABA_A)-mediated ion channel currents (I_GABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.

HY-N1072

Wilforgine	Others	Terpenoids and Glycosides
Wilforgine is a bioactive sesquiterpene alkaloid in Tripterygium wilfordii Hook. F. Wilforgine can induce microstructural and ultrastructural changes in the muscles of Mythimna separata larvae, and the sites of action are proposed to be calcium receptors or channels in the muscular system.

HY-N7126

Citronellal	Others	Acids and Aldehydes
Citronellal is a monoterpenea from the essential oils in various aromatic species of plants, with depressant, hypnotic, and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K^⁺ channel pathway.

HY-N1462

Atractyloside potassium salt	Others	Saccharides and Glycosides Terpenoids and Glycosides
Atractyloside potassium salt is a toxic diterpenoid glycoside that can be isolated from the fruits of Xanthium sibiricum. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart.

HY-N4097

Incensole	Others	Terpenoids and Glycosides
Incensole, a 14-membered diterpenoid, is isolated from both essential oils and resins of frankincense. Incensole has shown anti-inflammatory and anti-depression activities due to their ability to activate ion channels in the brain to alleviate anxiety or depression.

HY-N6688

Verruculogen	Potassium Channel Bacterial Antibiotic	Natural Products
Verruculogen is a toxin produced mainly by Penicillium and Aspergillus spp. and causes severe tremors in affected animals. Verruculogen inhibits Ca²⁺-activated K⁺ channels. Verruculogen is an M phase inhibitor of the mammalian cell cycle.

HY-B1167

Ajmaline Cardiorythmine; (+)-Ajmaline	Sodium Channel	Alkaloids
Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC₅₀ of 1 μM in HEK cells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia.

HY-N6016

Bacopaside II	Apoptosis	Saccharides and Glycosides Terpenoids and Glycosides
Bacopaside II, an extract from the medicinal herb Bacopa monnieri, blocks the Aquaporin-1 (AQP1) water channel and impairs migration of cells that express AQP1. Bacopaside II induces cell cycle arrest and apoptosis.

HY-75161

(-)-Menthol	TRP Channel Endogenous Metabolite	Terpenoids and Glycosides
(-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca²⁺-permeable nonselective cation channel, to increase [Ca²⁺]_i. Antitumor activity.

HY-N1934

Dihydroberberine	Potassium Channel HSP	Natural Products
Dihydroberberine inhibits human ether-a-go-go-related gene (hERG) channels and remarkably reduces heat shock protein 90 (Hsp90) expression and its interaction with hERG. Dihydroberberine has anti-inflammatory, anti-atherosclerotic, hypolipidemic and antitumor activities.

HY-N0219

Bicuculline (+)-Bicuculline; d-Bicuculline	GABA Receptor	Alkaloids
Bicuculline ((+)-Bicuculline; d-Bicuculline), as a convulsant alkaloid, is a competitive neurotransmitter GABA_A receptor antagonist (IC₅₀=2 μM). Bicuculline also blocks Ca²⁺-activated potassium (SK) channels and subsequently blocks the slow afterhyperpolarization (slow AHP) .

HY-B0166A

L-Ascorbic acid sodium salt Sodium L-ascorbate; Vitamin C Sodium salt	Calcium Channel Reactive Oxygen Species Apoptosis	Natural Products
L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively Ca_v3.2 channels with an IC₅₀ of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.

HY-133168

Englerin A	TRP Channel	Terpenoids and Glycosides
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC₅₀s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca²⁺ influx and Ca²⁺ cell overload.

HY-B0778

Milbemycin oxime	Parasite Antibiotic	Natural Products
Milbemycin oxime is a macrocyclic lactone and has broad-spectrum anti-parasitic activity. Milbemycin oxime is composed of milbemycins A4 and A3. Milbemycin oxime binds glutamate-gated chloride channels. Milbemycin oxime is against intestinal nematodes, pulmonary and cardiac helminths.

HY-12361

PF 1022A	Parasite	Natural Products
PF 1022A is a cyclooctadepsipeptide with broadspectrum anthelmintic properties produced by fermentation of the fungus Mycelia sterilia. PF 1022A is a channel-forming ionophore. PF 1022A showes strong anthelmintic activities against *Ascaridia galli* in chickens. PF 1022A also can be used for angiostrongyliasis research.

HY-P1346

APETx2	Sodium Channel	Natural Products
APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC₅₀ of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain.

HY-N6776

Penitrem A	Potassium Channel	Alkaloids
Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals.

HY-135897

Urolithin C	Calcium Channel Reactive Oxygen Species Apoptosis Endogenous Metabolite	Phenols
Urolithin C, a gut-microbial metabolite of Ellagic acid, is a glucose-dependent activator of insulin secretion. Urolithin C is a L-type Ca²⁺ channel opener and enhances Ca²⁺ influx. Urolithin C induces cell apoptosis through a mitochondria-mediated pathway and also stimulates reactive oxygen species (ROS) formation.

HY-N0747

Oxypeucedanin	Potassium Channel	Phenylpropanoids
Oxypeucedanin is a furocoumarin derivative isolated from Angelica dahurica. Oxypeucedanin is a selective open-channel blocker, inhibits the hKv1.5 current with an IC₅₀ value of 76 nM. Oxypeucedanin prolongs cardiac action potential duration (APD), is a potential antiarrhythmic agent for atrial fibrillation. Oxypeucedanin induces cell apoptosis through inhibition of cancer cell migration.

HY-N7503

Psoralenoside	Histamine Receptor CaMK Calcium Channel	Saccharides and Glycosides
Psoralenoside is a benzofuran glycoside from Psoralea corylifolia. Psoralenoside exhibits high binding affinities against histaminergic H₁, calmodulin, and voltage-gated L-type calcium channels (E-value≥-6.5 Kcal/mol). Psoralenoside shows estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.

HY-13295

Vinpocetine Ethyl apovincaminate	Sodium Channel IKK Phosphodiesterase (PDE)	Alkaloids
Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na⁺ channels. The IC₅₀ value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.

HY-N1500

Pulegone	TRP Channel Endogenous Metabolite	Natural Products
Pulegone, the major chemical constituent of Calamintha nepeta (L.) Savi essential oil which is an aromatic herb with a mint-oregano flavor, is one of avian repellents. The molecular target for the repellent action of Pulegone in avian species is nociceptive TRP ankyrin 1 (TRPA1). Pulegone stimulates both TRPM8 and TRPA1 channel in chicken sensory neurons and suppresses the former but not the latter at high concentrations.

HY-N0603

20(S)-Ginsenoside Rg3 20(S)-Propanaxadiol; S-ginsenoside Rg3	Sodium Channel Potassium Channel NF-κB COX Amyloid-β Endogenous Metabolite	Saccharides and Glycosides Terpenoids and Glycosides
20(S)-Ginsenoside Rg3 is the main component of Red ginseng. Ginsenoside Rg3 inhibits Na⁺ and hKv1.4 channel with IC₅₀s of 32.2±4.5 and 32.6±2.2 μM, respectively. 20(S)-Ginsenoside Rg3 also inhibits Aβ levels, NF-κB activity, and COX-2 expression.

HY-B0166

L-Ascorbic acid L-Ascorbate; Vitamin C	Reactive Oxygen Species Calcium Channel Apoptosis Endogenous Metabolite	Natural Products
L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Ca_v3.2 channels with an IC₅₀ of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells.

HY-N0822

Shikonin C.I. 75535; Isoarnebin 4	Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV	Quinones
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC₅₀ of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.

HY-N1483

Guanfu base A	Potassium Channel	Alkaloids
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a K_i of 1.20 μM in human liver microsomes (HLMs) and a K_i of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (K_i of 0.38 μM) and dog (K_i of 2.4 μM) microsomes. Guanfu base A also inhibits HERG channel current.

HY-N0215

L-Phenylalanine (S)-2-Amino-3-phenylpropionic acid	Calcium Channel iGluR Endogenous Metabolite	Alkaloids Acids and Aldehydes
L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca⁺ channels antagonist with a K_i of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (K_B of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.

HY-N4267

Yangambin	Calcium Channel	Phenylpropanoids
Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca²⁺ influx through voltage-gated Ca²⁺ channels, leading to the reduction in [Ca²⁺]i in vascular smooth muscle cells and consequent peripheral vasodilation. Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC₅₀ of 33.8 μM and for anti-inflammatory activity with an IC₅₀ of 37.4 μM.

Cat. No.	Product Name	Species	Source

HY-P7840

CLIC1 Protein, Human (His) rHuChloride intracellular Channel protein 1/CLIC1, His; Chloride Intracellular Channel Protein 1; Chloride Channel ABP; Nuclear Chloride Ion Channel 27; NCC27; Regulatory Nuclear Chloride Ion Channel Protein; hRNCC; CLIC1; G6; NCC27	Human	E. coli

HY-P70120

*Chloride intracellular channel* protein 4/CLIC4 Protein, Human (His)** rHuChloride intracellular Channel protein 4/CLIC4, His; Chloride Intracellular Channel Protein 4; Intracellular Chloride Ion Channel Protein p64H1; CLIC4	Human	E. coli

HY-P7857

CLIC3 Protein, Human (His)
rHuChloride intracellular Channel protein 3/CLIC3, His; Chloride intracellular Channel protein 3; CLIC3
Human E. coli
HY-P70113

CLIC5 Protein, Human (His)
rHuChloride intracellular Channel protein 5/CLIC5, His; Chloride Intracellular Channel Protein 5; CLIC5
Human E. coli
HY-P7843

CLIC2/XAP121 Protein, Human (His)
rHuChloride intracellular Channel protein 2/CLIC2, His; Chloride Intracellular Channel Protein 2; XAP121; CLIC2
Human E. coli

Cat. No.	Product Name

HY-B0545S

Probenecid-d14
Probenecid-d14 is the deuterium labeled Probenecid. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels.

HY-B0262S

Methocarbamol D5

Methocarbamol D5 is deuterium labeled Methocarbamol. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel.

HY-135407S

N-Desethyl Oxybutynin D5 hydrochloride
N-Desethyl Oxybutynin D5 hydrochloride is deuterium labeled N-Desethyl Oxybutynin hydrochloride. N-Desethyl Oxybutynin is the the active metabolite Oxybutynin. Oxybutynin is an anticholinergic agent that inhibits voltage-dependent K⁺ channels.

HY-B0341S

Nicorandil-d4
Nicorandil-d4 (SG-75-d4) is the deuterium labeled Nicorandil. Nicorandil (SG-75) is a potent potassium channel activator and targets vascular nucleoside diphosphate-dependent K⁺ channels and cardiac ATP-sensitive K⁺ channels (K_ATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases.

HY-B1378S

Ethosuximide-d3
Ethosuximide-d3 is the deuterium labeled Ethosuximide. Ethosuximide, a widely prescribed anti-epileptic drug, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.

HY-Z1897S

N-Methyl duloxetine-d7
N-Methyl duloxetine-d7 is the deuterium labeled N-Methyl Duloxetine. N-Methyl Duloxetine is an analgesic. N-Methyl Duloxetine elicits both tonic and use-dependent block of neuronal Na⁺ channels.

HY-12515AS

Nicardipine D3 hydrochloride
Nicardipine D3 hydrochloride (YC-93 D3) is the deuterium labeled Nicardipine hydrochloride. Nicardipine hydrochloride is a calcium channel blocker with an IC₅₀ of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.

HY-B1090S

Cinnarizine D8

Cinnarizine D8 is a deuterium labeled Cinnarizine. Cinnarizine is an antihistamine and a calcium channel blocker.
HY-B0023S

Azelnidipine D7

Azelnidipine D7 is deuterium labeled Azelnidipine, which is a L-type calcium channel blocker.

HY-B0262S1

Methocarbamol-d3
Methocarbamol-d3 is the deuterium labeled Methocarbamol. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research.

HY-B0284S

Nifedipine D6

Nifedipine D6 (BAY-a-1040 D6) is deuterium labeled nifedipine, and nifedipine is a potent calcium channel blocker.
HY-B0419S

Manidipine-d4

Manidipine-d4 is the deuterium labeled Manidipine. Manidipine is a calcium channel blocker that is used clinically as an antihypertensive.
HY-B0347S

Lacidipine-d10

Lacidipine-d10 is the deuterium labeled Lacidipine. Lacidipine (Lacipil, Motens) is a L-type calcium channel blocker.

HY-B0612DS

(R)-Lercanidipine D3 hydrochloride
(R)-lercanidipine D3 (hydrochloride) is a deuterium labeled (R)-Lercanidipine hydrochloride. (R)-Lercanidipine D3 (hydrochloride), the R-enantiomer of Lercanidipine, is a calcium channel blocker.

HY-B0246S

Carbamazepine-D10

Carbamazepine-D10 (CBZ-D10) is the deuterium labeled Carbamazepine. Carbamazepine (CBZ), a sodium channel blocker, is an anticonvulsant agent.
HY-B0575S

Triamterene D5

Triamterene D5 is deuterium labeled Triamterene, which can block epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic.

HY-14187S

Amiodarone-d10 hydrochloride
Amiodarone-d10 hydrochloride is the deuterium labeled Amiodarone. Amiodarone hydrochloride is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with an IC₅₀ of 19.1 μM.

HY-101621S

Teludipine-d6

Teludipine-d6 (GR53992B-d6) is the deuterium labeled Teludipine hydrochloride. Teludipine is a lipophilic calcium channel blocker.

HY-A0176S

Glisoxepid-d4
Glisoxepid-d4 is the deuterium labeled Glisoxepide. Glisoxepide, a sulphonamide derivative, is an orally available nonselective K(ATP) channel blocker, with antihyperglycemic activity and cardiovascular regulation effect.

HY-135328S

Norverapamil D7
Norverapamil D7 is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

HY-A0093S

Mexiletine D6 hydrochloride
Mexiletine D6 hydrochloride (KOE-1173 D6 hydrochloride) is a deuterium labeled Mexiletine hydrochloride (KOE-1173 hydrochloride). Mexiletine hydrochloride, a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker.

HY-B0493S

Niflumic Acid-d5
Niflumic Acid-d5 is the deuterium labeled Niflumic acid. Niflumic acid, a Ca²⁺-activated Cl^- channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.

HY-135328AS

Norverapamil D7 hydrochloride
Norverapamil D7 ((±)-Norverapamil D7) hydrochloride is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

HY-B0612DS1

Lercanidipine-d3 hydrochloride
Lercanidipine-d3 hydrochloride is the deuterium labeled Lercanidipine. Lercanidipine is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine has long lasting antihypertensive action and reno-protective effect.

HY-B0887S

Permethrin-d5
Permethrin-d5 (NRDC-143-d5) is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.

HY-17402S1

Nisoldipine-d4
Nisoldipine-d4 (BAY-k 5552-d4) is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC₅₀ of 10 nM.

HY-17402S2

Nisoldipine-d7
Nisoldipine-d7 (BAY-k 5552-d7) is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC₅₀ of 10 nM.

HY-B0422S

Nateglinide D5
Nateglinide D5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K⁺ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.

HY-B0114S

Oxcarbazepine-D4
Oxcarbazepine-D4 (GP 47680-D4) is the deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines. Anti-cancer and anticonvulsant effects.

HY-23196S

Minoxidil-d10
Minoxidil-d10 (U10858-d10) is the deuterium labeled Minoxidil. Minoxidil (U10858) is an ATP-sensitive potassium (K_ATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. Minoxidil is also a potent inhibitor of soybean lipoxygenaseare with an IC₅₀ of 20 μM.

HY-B0233S

Isradipine-d3
Isradipine-d3 (PN 200-110-d3) is the deuterium labeled Isradipine. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease.

HY-B1193S

Terfenadine-d3

Terfenadine-d3 ((±)-Terfenadine-d3) is the deuterium labeled Terfenadine. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC₅₀ of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca²⁺ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.

HY-12533S

Disopyramide-d14 tosylate salt

Disopyramide-d14 (Dicorantil-d14) tosylate salt is the deuterium labeled Disopyramide. Disopyramide (Dicorantil) is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action.

HY-B0185AS

Lidocaine-d10 hydrochloride

Lidocaine-d10 (Lignocaine-d10) hydrochloride is the deuterium labeled Lidocaine hydrochloride. Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative commonly used to anesthetize. hydrochloride is a a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.

HY-103399S

Trovafloxacin-d4 mesylate

Trovafloxacin-d4 mesylate is the deuterium labeled Trovafloxacin mesylate. Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC₅₀ of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1.

HY-70057S

Safinamide-d4

Safinamide-d4 (FCE 26743-d4) is the deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC₅₀=0.098 µM) over MAO-A (IC₅₀=580 µM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC₅₀=8 µM) than at resting (IC₅₀=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.

HY-19545AS

SCH-23390-d3 hydrochloride

SCH-23390-d3 (R-(+)-SCH-23390-d3) hydrochloride is the deuterium labeled SCH-23390 hydrochloride. SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D₁-like receptor antagonist with K_is of 0.2 nM and 0.3 nM for the D₁ and D₅ receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT_2C receptor agonist with a K_i of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT₂ and 5-HT_1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC₅₀ of 268 nM.

Sodium Channel

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

NaturalProducts

Recombinant Proteins

Isotope-Labeled Compounds

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