Search Result
Results for "
Sodium Channel
" in MCE Product Catalog:
7
Biochemical Assay Reagents
157
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-100257
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- HY-15736
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- HY-108505
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- HY-101350
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- HY-B1798
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Tocainide
|
Sodium Channel
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Cardiovascular Disease
|
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Tocainide hydrochloride is an orally activesodium 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.
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- HY-B1243
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- HY-145558
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- HY-132818
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Idrevloride
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Sodium Channel
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Others
|
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Idrevloride, an epithelial sodium channel (ENaC) inhibitor (WO2016133967), can be used for the research of skin disorders.
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- HY-B0834
-
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Indoxacarb
(±)-Indoxacarb; DPX-JW062
|
Sodium Channel
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Neurological Disease
|
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Indoxacarb ((±)-Indoxacarb; DPX-JW062) is a broad-spectrum oxadiazine insecticide with high insecticidal activity and low mammalian toxicity. Indoxacarb blocks insect sodium channels (Sodium Channel) in nerve preparations and isolated neurons.
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- HY-107695
-
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Remacemide hydrochloride
FPL 12924AA
|
iGluR
Sodium Channel
|
Neurological Disease
|
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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.
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- HY-U00135
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-
- HY-147556
-
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SK3 Channel-IN-1
|
Potassium Channel
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Cancer
|
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SK3 Channel-IN-1 (compound 7a) is a potent and specific SK3 channel modulator. SK3 Channel-IN-1 has efficient effect on breast cancer MDA-MB-435 cell migration while exhibiting low cytotoxicity in other cell lines. SK3 Channel-IN-1 can modulate ion channels’activity in cancer.
|
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- HY-75867
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- HY-146173
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- HY-117714
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- HY-142723
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- HY-132133
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- HY-N6691
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Veratridine
3-Veratroylveracevine
|
Sodium Channel
|
Neurological Disease
|
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Veratridine (3-Veratroylveracevine) is a plant neurotoxin, a voltage-gated sodium channels (VGSCs) blocker. Veratridine can block the voltage-gated sodium channels (VGSC) of cell membranes. Veratridine inhibits the peak current of Nav1.7, with an IC50 of 18.39 µM.
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- HY-112472
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S3969
|
Sodium Channel
|
Metabolic Disease
|
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S3969 is a potent and reversible activator of the human epithelial sodium channel (hENaC). The apparent EC50 for S3969 activation of hENaC is 1.2 μm.
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- HY-146174
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- HY-122001
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PF-05186462
|
Sodium Channel
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Neurological Disease
|
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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.
|
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- HY-16952A
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Bepridil hydrochloride hydrate
(±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate
|
Calcium Channel
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Cardiovascular Disease
|
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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.
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- HY-142735
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KCa2 channel modulator 2
|
Potassium Channel
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Neurological Disease
|
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KCa2 channel modulator 2 (compound 2q) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 2 exhibits similar potency on the rat KCa2.2a and human KCa2.3 channel subtypes, with EC50s of 0.64 μM and 0.60 μM, respectively
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- HY-147423
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- HY-B1704A
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- HY-122376
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S-Bioallethrin
D-Trans-Allethrin; Esbiol
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Sodium Channel
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Neurological Disease
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S-Bioallethrin is a pyrethroid insecticide. S-Bioallethrin disrupts nerve function by modifying the gating kinetics of transitions between the conducting and nonconducting states of voltage-gated sodium channels.
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- HY-100310
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- HY-N3990
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- HY-B0114
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- HY-41076
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- HY-10035
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TTA-P2
T-Type calcium Channel inhibitor
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Calcium Channel
|
Neurological Disease
|
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TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease.
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- HY-P1218
-
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Phrixotoxin 3
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Sodium Channel
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Neurological Disease
|
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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.
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- HY-P1218A
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Phrixotoxin 3 TFA
|
Sodium Channel
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Neurological Disease
|
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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.
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- HY-U00280
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Potassium Channel Activator 1
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Others
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Neurological Disease
|
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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.
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- HY-100345
-
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AMTB hydrochloride
|
TRP Channel
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Cancer
Neurological Disease
|
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AMTB hydrochloride is a selective TRPM8 channel blocker. AMTB hydrochloride inhibits icilin-induced TRPM8 channel activation with a pIC50 of 6.23. AMTB hydrochloride can be used for the research of the overactive bladder and painful bladder syndrome. AMTB hydrochloride is a non-selective inhibitor of voltage-gated sodium channels (NaV).
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- HY-147708
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T-Type calcium channel inhibitor 2
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Calcium Channel
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Cancer
|
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T-Type calcium channel inhibitor 2 (compound 6g) is a potent T-type calcium channel inhibitor with IC50s of 31.0, 83.1, 69.3 µM for Cav3.1 (α1G), Cav3.2 (α1H), Cav3.3 (α1I) (α1H), respectively. T-Type calcium channel inhibitor 2 shows cytotoxicity for A549, HCT-116 cells with IC50s of 5.0, 6.4 µM, respectively.
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- HY-17612
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Evenamide
NW-3509
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Sodium Channel
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Neurological Disease
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Evenamide (NW-3509) is an orally available voltage-gated sodium channel (VGSC) blocker (Ki=0.4 µM) for the research of schizophrenia. Evenamide shows efficacy in a broad spectrum of rodent models of psychosis, mania, depression, and aggressiveness.
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- HY-11079
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A-803467
|
Sodium Channel
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Inflammation/Immunology
Neurological Disease
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A-803467 is a potent and selective tetrodotoxin-resistant Nav1.8 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.
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- HY-108506
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- HY-P2215
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Solnatide
AP 301
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Sodium Channel
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Metabolic Disease
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Solnatide (AP 301) is an inhaled synthetic peptide agent composed of 17 natural amino acids. Solnatide can directly activate the epithelial sodium channel. Solnatide can be used for the research of lung function.
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- HY-P1220
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Huwentoxin-IV
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Sodium Channel
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Neurological Disease
|
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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.
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- HY-P1220A
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Huwentoxin-IV TFA
|
Sodium Channel
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Neurological Disease
|
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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.
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- HY-147377
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- HY-119980
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Fluphenazine
|
Dopamine Receptor
Sodium Channel
SARS-CoV
|
Infection
Neurological Disease
|
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Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2.
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- HY-18940A
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- HY-P1078
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Huwentoxin XVI
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Calcium Channel
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Neurological Disease
|
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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.
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- HY-P1078A
-
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Huwentoxin XVI TFA
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Calcium Channel
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Neurological Disease
|
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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.
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- HY-17404
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- HY-N5101
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- HY-U00309
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- HY-15416
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- HY-17404S
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Cilnidipine-d7
FRC-8653-d7
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Calcium Channel
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Cardiovascular Disease
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Cilnidipine-d7 is deuterium labeled Cilnidipine. Cilnidipine is a long-acting, second-generation dihydropyridine Ca2+-channel blocker on L and N-type Ca2+ channel. Antihypertensive effects.
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- HY-B1221
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Flufenamic acid
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COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
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Inflammation/Immunology
|
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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 Ca 2+ 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.
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- HY-12949
-
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ML204
|
TRP Channel
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Neurological Disease
|
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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 Ca 2+ channels.
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- HY-P0189
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- HY-12949A
-
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ML204 hydrochloride
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TRP Channel
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Neurological Disease
|
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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 Ca 2+ channels.
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- HY-131942
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- HY-P0189A
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- HY-108592
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UCL 2077
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Potassium Channel
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Neurological Disease
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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.
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- HY-105917
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Endovion
NS3728
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Chloride Channel
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Others
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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.
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- HY-B0545S
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- HY-B1221S
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Flufenamic acid-d4
|
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
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Inflammation/Immunology
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Flufenamic acid-d4 is deuterium labeled Flufenamic acid. 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.
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- HY-17451
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- HY-126583
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Nemadipine-A
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Calcium Channel
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Cancer
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Nemadipine-A is a specific inhibitor of the EGL-19 L-type Ca 2+ channel. Nemadipine-A, a cell-permeable L-type calcium channel inhibitor, sensitizes TRAIL-resistant cancer cells to this ligand.
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- HY-P1221
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ProTx II
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Sodium Channel
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Neurological Disease
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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.
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- HY-128933
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- HY-B1221S1
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Flufenamic acid-13C6
|
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
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Inflammation/Immunology
|
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Flufenamic acid-13C6 is the 13C6 labeled Flufenamic acid. 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.
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- HY-14183
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Vernakalant Hydrochloride
RSD1235 hydrochloride
|
Potassium Channel
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Cardiovascular Disease
|
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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.
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- HY-15553B
-
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Mibefradil dihydrochloride hydrate
Ro 40-5967 dihydrochloride hydrate
|
Calcium Channel
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Cardiovascular Disease
|
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Mibefradil dihydrochloride hydrate (Ro 40-5967 dihydrochloride hydrate) is a effectively long-acting calcium channel antagonist, used as an antihypertensive agent. Mibefradil dihydrochloride hydrate acts via a higher affinity block for low-voltage-activated (T) than for high-voltage-activated (L) calcium channels.
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- HY-12796A
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- HY-12796
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- HY-12345
-
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ML365
|
Potassium Channel
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Cardiovascular Disease
|
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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.
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- HY-110153
-
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NS19504
|
Potassium Channel
|
Neurological Disease
|
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NS19504 is a Ca 2+-activated K + channel (BK channel, KCa1.1 channel) activator (EC50=11.0 µM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions.
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- HY-P1073
-
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ProTx-I
|
Calcium Channel
Sodium Channel
Potassium Channel
|
Cancer
|
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ProTx-I, a venom toxin of the tarantula Thrixopelma pruriens, is a potent, selective CaV3.1 channel blocker with IC50 values of 0.2 μM and 31.8 μM for hCaV3.1 and hCaV3.2 respectively. ProTx-I is also a potent blocker for voltage-gated Na + channels and inhibits KV 2.1 channels.
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- HY-B0545
-
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- HY-135412
-
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- HY-111325
-
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Synta66
|
CRAC Channel
|
Neurological Disease
|
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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.
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- HY-100623
-
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- HY-N2077
-
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- HY-101809
-
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- HY-B0341
-
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Nicorandil
SG-75
|
Potassium Channel
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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 (KATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases.
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- HY-P0190
-
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Iberiotoxin
|
Potassium Channel
|
Cardiovascular Disease
|
|
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels.
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- HY-101942
-
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Zegocractin
CM-4620
|
CRAC Channel
|
Neurological Disease
|
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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.
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- HY-133910
-
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Lu AE98134
|
Sodium Channel
|
Neurological Disease
|
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Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Nav1.1 channels positive modulator. Lu AE98134 also increases the activity of Nav1.2 and Nav1.5 channels but not of Nav1.4, Nav1.6 and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al.
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- HY-16915
-
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RPR-260243
|
Potassium Channel
|
Cardiovascular Disease
|
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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.
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- HY-P1424
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- HY-101674
-
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- HY-101383
-
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- HY-B0262S
-
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- HY-108584
-
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Flindokalner
BMS-204352
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Potassium Channel
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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 (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
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- HY-101360
-
-
- HY-136232
-
-
- HY-B1798A
-
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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.
|
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- HY-B0246
-
-
- HY-B0984
-
-
- HY-101621
-
-
- HY-108594
-
-
- HY-101069
-
-
- HY-N2338
-
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- HY-103371
-
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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: 0.14, 0.95, 50.72 μM, respectively). DCPIB is also a selective blocker of swelling-induced chloride current (ICl,swell), with an IC50 of 4.1 μM. DCPIB is a useful tool for investigating structure-function studies of K2P channels.
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- HY-108586
-
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NS3623
|
Potassium Channel
|
Neurological Disease
|
|
NS3623 is an activator of human ether-a-go-go-related gene (hERG1/KV11.1) 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.
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- HY-13103
-
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NS 11021
|
Potassium Channel
|
Others
|
|
NS 11021 is a potent and specific Ca 2+-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.
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- HY-A0148
-
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Halofantrine
SKF-102886 free base; WR-171669
|
Parasite
Potassium Channel
|
Infection
|
|
Halofantrine (SKF-102886 free base) is a highly lipophilic antimalarial active against Chloroquine-resistant strains of Plasmodium falciparum. Halofantrine blocks HERG potassium channels.
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- HY-136564A
-
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DAD
|
Potassium Channel
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Neurological Disease
|
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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.
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- HY-14462
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- HY-101012
-
-
- HY-105117
-
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- HY-12515A
-
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- HY-101428
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NS-638
|
Calcium Channel
|
Neurological Disease
|
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NS-638 is a small nonpeptide molecule with Ca 2+-channel blocking properties. K +-stimulated intracellular Ca 2+-elevation is blocked with an IC50 value of 3.4 μM.
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- HY-108593
-
-
- 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.
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- HY-16126
-
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- HY-135407S
-
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- HY-U00218
-
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- HY-B0768A
-
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- HY-B0567
-
-
- HY-101740
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- HY-B0419
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- HY-U00201
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- 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-P1281
-
|
Kaliotoxin
|
Potassium Channel
|
Neurological Disease
|
|
Kaliotoxin is a peptidyl inhibitor of neuronal BK-Type. Kaliotoxin can specific inhibit Kv channels and calcium-activated potassium channels. Kaliotoxin can be used for the research of the regulation of membrane potential and neuron excitability.
|
-
- 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-P1080
-
|
ω-Agatoxin IVA
|
Calcium Channel
|
Neurological Disease
|
|
ω-Agatoxin IVA is a potent, selective P/Q type Ca 2+ (Cav2.1) channel blocker with IC50s of 2 nM and 90 nM for P-type and Q-type Ca 2+ 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-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 (KATP). 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 Nav and Kv 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
-
-
- HY-W011509
-
-
- HY-14255
-
-
- HY-U00173
-
-
- HY-14290A
-
-
- HY-103315
-
-
- HY-101843
-
-
- HY-108582
-
|
Y-27152
|
Potassium Channel
|
Cardiovascular Disease
|
|
Y-27152, a prodrug of the KATP (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-14290
-
|
Pinacidil
P-1134
|
Potassium Channel
|
Cardiovascular Disease
|
|
Pinacidil is a potent activator of potassium channel. Pinacidil is an antihypertensive agent which hyperpolarises vascular smooth muscle by opening K +-channels. Pinacidil significantly improves the reperfusion function and cardiac compliance. Pinacidil has direct cardioprotective efficacy.
|
-
- 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-P1410
-
|
GsMTx4
|
TRP Channel
Piezo Channel
|
Inflammation/Immunology
Neurological Disease
Cardiovascular Disease
|
|
GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.
|
-
- HY-124702
-
|
ICA-105574
|
Potassium Channel
|
Cardiovascular Disease
|
|
ICA-105574 is a potent and efficacious hERG channel activator. The primary mechanism by which ICA-105574 potentiates hERG channel activity is by removing hERG channel inactivation. ICA-105574 steeply potentiates current amplitudes more than 10-fold with an EC50 value of 0.5 +/- 0.1 μM and a Hill slope (n(H)) of 3.3 +/- 0.2.
|
-
- HY-110105
-
|
NS8593 hydrochloride
|
Potassium Channel
|
Neurological Disease
|
|
NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-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-N3729
-
|
(-)-Denudatin B
Denudatin B
|
Calcium Channel
|
Cardiovascular Disease
|
|
(-)-Denudatin B is an antiplatelet agent. (-)-Denudatin B relaxed vascular smooth muscle by inhibiting the Ca2+ influx through voltage-gated and receptor-operated Ca2+ channels. And (-)-Denudatin B has nonspecific antiplatelet action
|
-
- HY-B0405
-
-
- HY-B0405A
-
-
- HY-Z1897S
-
-
- HY-116448
-
-
- HY-B0401
-
-
- HY-B1109
-
-
- HY-B2136
-
-
- HY-100572
-
-
- HY-14256
-
-
- HY-U00236
-
-
- HY-N2164
-
-
- HY-15553A
-
-
- HY-B0285
-
-
- HY-B0285A
-
-
- HY-B0480A
-
-
- 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 Ca 2+ channel blocker. ω-Agatoxin TK inhibits the high K + depolarisation-induced rise in internal Ca 2+ 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
|
mGluR
Phosphodiesterase (PDE)
Apoptosis
Calmodulin
|
Inflammation/Immunology
|
|
CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-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-B0480
-
-
- HY-P1410A
-
|
GsMTx4 TFA
|
TRP Channel
Piezo Channel
|
Inflammation/Immunology
Neurological Disease
Cardiovascular Disease
|
|
GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology.
|
-
- 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 Ca 2+ channels displaying IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively.
|
-
- HY-109160
-
|
Rimtuzalcap
CAD-1883
|
Potassium Channel
|
Neurological Disease
|
|
Rimtuzalcap (CAD-1883) is a first-in-class selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels). Rimtuzalcap can be used for the research of movement disorders including essential tremor (ET) and spinocerebellar ataxia (SCA).
|
-
- 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
-
-
- HY-N3463
-
-
- HY-P0191
-
-
- HY-P0163
-
-
- HY-109077
-
-
- HY-U00044
-
-
- HY-12778
-
-
- HY-14284
-
-
- HY-14656
-
-
- HY-B1448
-
-
- 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
-
-
- HY-W032013
-
-
- HY-12596
-
|
JNJ-26489112
|
Calcium Channel
Sodium Channel
Potassium Channel
|
Neurological Disease
|
|
JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na + channels and N-type Ca 2+ channels, and is effective as a K + channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC50=35 μM) and CA-I (18 μM).
|
-
- HY-108573
-
|
P-1075
|
Potassium Channel
|
Cardiovascular Disease
|
|
P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 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
|
mGluR
Phosphodiesterase (PDE)
Apoptosis
Calmodulin
|
Inflammation/Immunology
|
|
CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-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-10588
-
|
Bay K 8644
(±)-Bay K 8644
|
Calcium Channel
|
Neurological Disease
Cardiovascular Disease
|
|
Bay K 8644 ((±)-Bay K 8644) is a racemate consisting of two isomers (R)-(+)-Bay-K-8644 and (S)-(-)-Bay-K-8644. Bay K 8644 is a L-type Ca 2+ channel agonist with an EC50 of 17.3 nM. Bay K 8644 increases Ca 2+ influx through sarcolemmal Ca 2+ channels by increasing the open time of the channel. Bay K 8644 has vasoconstrictive effects.
|
-
- 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-B0317C
-
|
Amlodipine mesylate
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine mesylate, 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 mesylate can be used for the research of high blood pressure and cancer.
|
-
- HY-12515B
-
|
(S)-Nicardipine
(S)-YC-93 free base
|
Calcium Channel
|
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-B0166G
-
-
- 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
-
-
- HY-D1528
-
-
- HY-B1090S
-
-
- HY-B0612D
-
-
- HY-14657
-
-
- HY-B0552A
-
-
- HY-14187
-
-
- HY-U00086
-
-
- HY-U00026
-
-
- HY-P0191A
-
-
- HY-B0552
-
-
- HY-113147B
-
-
- HY-15707
-
|
NS6180
|
Potassium Channel
|
Inflammation/Immunology
|
|
NS6180 is a new orally active KCa3.1 channel inhibitor. NS6180 inhibits cloned human KCa3.1 channels with an IC50value of 9 nM. NS6180 can be used for the research of inflammatory bowel disease (IBD) .
|
-
- 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 KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (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-P1427
-
|
Guangxitoxin 1E
|
Potassium Channel
|
Neurological Disease
|
|
Guangxitoxin 1E is a potent and selective blocker of KV2.1 and KV2.2 channels. Guangxitoxin 1E inhibits KV2 with an IC50 of 1-3 nM. KV2 channels underlie delayed-rectifier potassium currents in various neurons.
|
-
- HY-B0433A
-
|
Quinine hydrochloride dihydrate
|
Parasite
Potassium Channel
|
Infection
|
|
Quinine hydrochloride dihydrate (Qualaquin) is an orally active and can be used in anti-malarial studies. Quinine hydrochloride dihydrate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM.
|
-
- 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 (KCa5.1) 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
-
-
- HY-B0612E
-
-
- HY-B0284
-
-
- HY-107319
-
-
- HY-U00212
-
-
- HY-16723
-
-
- HY-N9404
-
-
- HY-N1378
-
-
- HY-B0023S
-
-
- HY-B0405S
-
-
- HY-12515C
-
|
(R)-Nicardipine
(R)-YC-93 free base
|
Calcium Channel
|
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
-
-
- 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 Ca 2+ levels by activating Ca 2+-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-D0143A
-
|
Quinine dihydrochloride
|
Parasite
Potassium Channel
|
Infection
|
|
Quinine dihydrochloride is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine dihydrochloride is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM.
|
-
- HY-P3467
-
-
- HY-14462S
-
|
NP118809-d8
|
Calcium Channel
|
Cardiovascular Disease
|
|
NP118809-d8 is the deuterium labeled NP118809. 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-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 (KCa5.1) channel currents evoked by voltage pulses to +100 mV, with an IC50 of 169 μM.
|
-
- HY-107031
-
|
Metapramine
19560 RP
|
iGluR
Others
|
Others
|
|
Metapramine (19560 RP) is an antidepressant agent, belonging to the class of tricyclic compounds. Metapramine inhibits norepinephrine reuptake, without affecting the reuptake of serotonin or dopamine. Metapramine is a low-affinity antagonist of the N-methyl-D-aspartic acid (NMDA) receptor complex channel.
|
-
- HY-12343
-
|
ML277
CID-53347902
|
Potassium Channel
|
Cardiovascular Disease
|
|
ML277 (CID-53347902) is a potent and selective activator of K(v)7.1 (KCNQ1) potassium channel activator (EC50=270 nM), rescues function of pathophysiologically important mutant channel complexes in human induced pluripotent stem cell-derived cardiomyocytes.
|
-
- 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-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-N0172
-
-
- HY-B0023
-
-
- HY-12502B
-
-
- HY-12502
-
-
- HY-101096
-
-
- HY-15376
-
-
- HY-19721
-
-
- HY-17001A
-
-
- HY-101616
-
-
- HY-142240
-
-
- 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
-
-
- HY-136909
-
|
SR33805
|
Calcium Channel
|
Cardiovascular Disease
|
|
SR33805 is a potent Ca 2+ 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 Ca 2+ channels. SR33805 can be used for the research of acute or chronic failing hearts.
|
-
- HY-P2324
-
|
Gramicidin A
|
Bacterial
HIF/HIF Prolyl-Hydroxylase
Antibiotic
|
Cancer
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-110184
-
|
PK-THPP
|
Potassium Channel
|
Neurological Disease
|
|
PK-THPP is a potent TWIK-related acid-sensitive K(+) ion channel (TASK-3 ion channel) blocker (IC50s are 35 nM and 300 nM for TASK-3 and TASK-1, respectively). PK-THPP increases breathing rate and induces respiratory alkalosis in rats.
|
-
- 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
-
-
- 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 Ca 2+ 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-B0682
-
|
Mitiglinide
KAD-1229 free acid anhydrous; S21403 free acid anhydrous
|
Potassium Channel
|
Metabolic Disease
|
|
Mitiglinide (KAD-1229), an insulinotropic agent, is an ATP-sensitive K + (KATP) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide can be used for the research of type 2 diabetes.
|
-
- 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-139904
-
-
- 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
-
-
- HY-N0601
-
-
- HY-112279
-
-
- HY-N7511
-
-
- HY-W016498
-
-
- HY-133715
-
-
- HY-12082A
-
-
- HY-103309A
-
|
ML218 hydrochloride
|
Calcium Channel
|
Neurological Disease
|
|
ML218 hydrochloride is a potent, selective and orally active T-type Ca 2+ 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, KATP 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 Ca 2+ 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, KATP 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
3β-Hydroxy-5-pregnen-20-one monosulfate Sodium
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium 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 can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium 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 + (KATP) channel antagonist. Mitiglinide calcium hydrate is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP 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-B0317AS
-
|
Amlodipine-d4 maleate
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine-d4 maleate is the deuterium labeled Amlodipine maleate. 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-50694
-
|
Senicapoc
ICA-17043
|
Potassium Channel
|
Others
|
|
Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca 2+-activated K + channel; KCa3.1) blocker with an IC50 of 11 nM. Senicapoc blocks Ca 2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
|
-
- HY-10955
-
|
TTA-P1
|
Calcium Channel
|
Neurological Disease
|
|
TTA-P1 is a potent state-independent compound inhibiting human T-type calcium channel. T-type calcium channels play a role in diverse physiological responses including neuronal burst firing, hormone secretion, and cell growth. TTA-P1 has the potential for the research of absence epilepsy.
|
-
- HY-113147AS
-
-
- HY-101245
-
-
- HY-18996
-
-
- HY-B0419S1
-
-
- HY-15208
-
-
- HY-B0419S2
-
-
- HY-15551
-
-
- HY-107349
-
-
- 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
-
-
- HY-108451
-
-
- HY-17403
-
-
- HY-12502A
-
-
- HY-B0151S1
-
|
Pregnenolone-13C2,d2
3β-Hydroxy-5-pregnen-20-one-13C2,d2
|
TRP Channel
Endogenous Metabolite
Cannabinoid Receptor
Autophagy
|
Neurological Disease
|
|
Pregnenolone-13C2,d2 is the deuterium and 13C labeled Pregnenolone (HY-B0151). Pregnenolone 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-B0151S
-
|
Pregnenolone-d4
3β-Hydroxy-5-pregnen-20-one-d4
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone-d4 is the deuterium labeled Pregnenolone. 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-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 + (KATP) channel antagonist. Mitiglinide Calcium is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide Calcium can be used for the research of type 2 diabetes.
|
-
- HY-N7395A
-
-
- 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-B0433B
-
|
Quinine sulfate (2:1)
|
Parasite
Potassium Channel
|
Infection
|
|
Quinine sulfate (2:1) (Qualaquin) is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine sulfate (2:1) is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM.
|
-
- HY-150539
-
-
- HY-101396
-
-
- HY-101346
-
-
- HY-A0093
-
-
- HY-B0401S
-
-
- HY-120546
-
-
- HY-B0284S
-
-
- 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-B0246S1
-
-
- HY-116448S
-
-
- 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-B0317S
-
|
Amlodipine-1,1,2,2-d4 maleate
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine-1,1,2,2-d4 maleate is the deuterium labeled Amlodipine. 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-W013712
-
|
GI-530159
|
Potassium Channel
|
Neurological Disease
|
|
GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect.
|
-
- 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 Ca 2+ 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-103308
-
|
TRAM-39
|
Potassium Channel
|
Neurological Disease
|
|
TRAM-39 is a selective blocker of intermediate conductance Ca2+-activated K+ (IKCa) channels. TRAM-39 inhibits KCa3.1 channel with an IC50 value of 60 nM. TRAM-39 can be used for the research of ataxia, epilepsy, memory disorders, schizophrenia and Parkinson’s disease.
|
-
- HY-18723
-
|
Yoda 1
|
Piezo Channel
Akt
ERK
Potassium Channel
|
Cardiovascular Disease
|
|
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca 2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation.
|
-
- HY-110189S1
-
|
Pregnenolone monosulfate-d4 sodium
3β-Hydroxy-5-pregnen-20-one monosulfate-d4 Sodium
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
|
|
Pregnenolone monosulfate-d4 (sodium) is the deuterium labeled Pregnenolone monosulfate. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium 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 can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
|
-
- HY-103309S
-
|
ML218-d9
|
Calcium Channel
|
Neurological Disease
|
|
ML218-d9 is the deuterium labeled ML218. ML218 is a potent, selective and orally active T-type Ca 2+ 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, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier.
|
-
- HY-N0239
-
-
- HY-109077S
-
-
- HY-16916
-
-
- HY-14284S
-
-
- HY-B0267
-
-
- 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
-
-
- HY-147909
-
-
- HY-100244
-
-
- HY-U00137
-
-
- HY-131261
-
-
- HY-U00250
-
-
- HY-B0419S
-
-
- HY-103318
-
-
- HY-13519
-
-
- HY-19366
-
-
- HY-B0682S2
-
|
Mitiglinide-d5 calcium
|
Potassium Channel
|
Metabolic Disease
|
|
Mitiglinide-d5 (calcium) is deuterium labeled Mitiglinide. Mitiglinide (KAD-1229), an insulinotropic agent, is an ATP-sensitive K+ (KATP) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide can be used for the research of type 2 diabetes.
|
-
- 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-117639
-
|
AUT1
|
Potassium Channel
|
Neurological Disease
|
|
AUT1 is a recombinant human Kv3 channel modulator. AUT1 modulates Kv3.1b and Kv3.2a channels in human recombinant with pEC50 values of 5.33 and 5.31 μM, respectively. AUT1 can be used for the research of disorders associated with dysfunction of inhibitory feedback in corticolimbic circuits, such as schizophrenia.
|
-
- HY-B0262S2
-
|
Methocarbamol-13C,d3
|
Sodium Channel
|
Neurological Disease
|
|
Methocarbamol-13C,d3 is the 13C- and 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-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-W011641
-
-
- HY-B0799
-
-
- 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
-
-
- HY-B0575
-
-
- HY-101362
-
-
- HY-15763
-
|
Erastin
|
Ferroptosis
VDAC
|
Cancer
|
|
Erastin is a ferroptosis inducer. Erastin binds and inhibits voltage-dependent anion channels (VDAC2/VDAC3).
|
-
- HY-135356
-
-
- HY-B0246S2
-
-
- HY-19664
-
-
- 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
-
-
- HY-103307
-
-
- 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
-
-
- 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-B0402S
-
|
Amantadine-d15
1-Adamantanamine-d15; 1-Aminoadamantane-d15
|
Influenza Virus
Orthopoxvirus
SARS-CoV
Apoptosis
|
Cancer
Infection
Neurological Disease
|
|
Amantadine-d15 (1-Adamantanamine-d15) is the deuterium labeled Amantadine. Amantadine (1-Adamantanamine) is an antiviral agent with activity against influenza A viruses. Amantadine blocks the proton flow through the M2 ion channel (M2 proton channel of influenza A) and thus prevents the release of viral RNA into the cytoplasm of the infected cells. Amantadine is an antiparkinsonian agent.
|
-
- 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-B0682S1
-
|
(2R)-Mitiglinide-d5 calcium
|
Potassium Channel
|
Metabolic Disease
|
|
(2R)-Mitiglinide-d5 (calcium) is deuterium labeled Mitiglinide. Mitiglinide (KAD-1229), an insulinotropic agent, is an ATP-sensitive K+ (KATP) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide can be used for the research of type 2 diabetes.
|
-
- HY-151451
-
|
Cav 3.2 inhibitor 2
|
Calcium Channel
|
Neurological Disease
|
|
Cav 3.2 inhibitor 2 is a Cav3.2 T-type Ca 2+ channels inhibitor with an IC50 of 0.09339 μM under -80mV holding potential. Cav 3.2 inhibitor 2 potently suppresses T-channel-dependent somatic and visceral pain in mice. Cav 3.2 inhibitor 2 can be used for the research of intractable pain.
|
-
- HY-B0563
-
|
Ropivacaine
|
Sodium Channel
Potassium Channel
|
Neurological Disease
Cardiovascular Disease
|
|
Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (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 neuropathic pain management.
|
-
- HY-B0563B
-
-
- HY-B0317BS
-
|
Amlodipine-d4 besylate
Amlodipine benzenesulfonate-d4 besylate
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine-d4 (Amlodipine (benzenesulfonate)-d4) besylate is the deuterium labeled Amlodipine besylate. 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-B0517A
-
-
- HY-126653
-
-
- 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
-
-
- HY-B0211
-
-
- HY-B0401S1
-
-
- 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
-
-
- HY-B0612DS
-
-
- HY-17436
-
-
- HY-10388
-
-
- HY-108590
-
-
- HY-131283
-
-
- HY-131899
-
-
- HY-B1793
-
-
- HY-19062
-
-
- HY-B1140S
-
-
- HY-A0176
-
-
- HY-P3656
-
-
- 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
-
-
- HY-108577
-
-
- HY-12498
-
|
GV-58
|
Calcium Channel
|
Neurological Disease
|
|
GV-58 is a novel N- and P/Q-type calcium (Ca 2+) channel agonist with EC50s of 7.21 and 8.81 μM, respectively. GV-58 slows the deactivation of channels, resulting in a large increase in presynaptic Ca 2+ entry during activity. GV-58 can be used in lambert-eaton myasthenic syndrome (LEMS) research.
|
-
- 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 IC50s 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-B0402A
-
|
Amantadine hydrochloride
1-Adamantanamine hydrochloride; 1-Adamantylamine hydrochloride; 1-Aminoadamantane hydrochloride
|
Influenza Virus
Orthopoxvirus
SARS-CoV
Apoptosis
Bcl-2 Family
CDK
|
Cancer
Infection
Neurological Disease
|
|
Amantadine (1-Adamantanamine) hydrochloride is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine hydrochloride inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine hydrochloride also has anti-orthopoxvirus and anticancer activity. Amantadine hydrochloride can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.
|
-
- HY-B0402
-
|
Amantadine
1-Adamantanamine; 1-Aminoadamantane
|
Influenza Virus
Orthopoxvirus
SARS-CoV
Apoptosis
CDK
Bcl-2 Family
|
Cancer
Infection
Neurological Disease
|
|
Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.
|
-
- HY-B0563A
-
-
- HY-14656S
-
-
- 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 Ki of 300 nM.
|
-
- HY-N0663
-
-
- HY-B1378
-
-
- HY-100750
-
-
- HY-B0246S
-
-
- HY-108504
-
-
- HY-103623
-
-
- HY-B0575S
-
-
- 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-17402
-
-
- HY-100230A
-
-
- HY-100611
-
-
- HY-N0714
-
|
Berbamine
|
NF-κB
Autophagy
|
Cancer
|
|
Berbamine is a natural compound extracted from traditional Chinese medicine Phellodendron amurense Rupr. with anti-tumor, immunomodulatory and cardiovascular effects. Berbamine is a calcium channel blocker.
|
-
- HY-135328
-
-
- HY-115681
-
|
(2R/S)-6-PNG
6-Prenylnaringenin
|
Calcium Channel
|
Neurological Disease
|
|
(2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Cav3.2 T-type Ca 2+ 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-B0347
-
|
Lacidipine
|
Calcium Channel
Reactive Oxygen Species
Caspase
Apoptosis
|
Cardiovascular Disease
|
|
Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI).
|
-
- HY-P1075
-
|
CALP3
|
Calcium Channel
|
Cancer
Neurological Disease
|
|
CALP3, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ 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-136190
-
|
TRPC6-PAM-C20
|
TRP Channel
|
Neurological Disease
|
|
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 Ca 2+ concentrations ([Ca 2+]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-B0151S2
-
|
Pregnenolone-d4-1
3β-Hydroxy-5-pregnen-20-one-d4-1
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone-d4-1 (3β-Hydroxy-5-pregnen-20-one-d4-1) is the deuterium labeled Pregnenolone. 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-110189S
-
|
Pregnenolone monosulfate sodium-13C2,d2
3β-Hydroxy-5-pregnen-20-one monosulfate Sodium-13C2,d2
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone monosulfate sodium-13C2,d2 is the 13C- and deuterium labeled Pregnenolone monosulfate sodium. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) 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-14187S
-
-
- HY-150541
-
-
- 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-W016498S
-
-
- HY-101238
-
-
- HY-101437A
-
-
- HY-132813
-
-
- HY-112729
-
|
HC-056456
3,4-Bis(2-thienoyl)-1,2,5-oxadiazole-N-oxide
|
Calcium Channel
|
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-101323
-
|
Olvanil
NE-19550; N-Vanillyloleamide
|
TRP Channel
|
Neurological Disease
|
|
Olvanil (NE-19550) is an analgesic and an agonist of transient receptor potential vanilloid type 1 (TRPV1) channels with an EC50 of 0.7 nM.
|
-
- HY-W013093
-
-
- 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
-
-
- 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
-
-
- 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
-
-
- HY-14656S1
-
-
- HY-145126
-
|
CP-628006
|
CFTR
|
Others
|
|
CP-628006, a small molecule CFTR potentiator, restores ATP-dependent channel gating to the cystic fibrosis mutant G551D-CFTR.
|
-
- HY-B0563S1
-
|
Ropivacaine-d7
|
Sodium Channel
Potassium Channel
|
Neurological Disease
Cardiovascular Disease
|
|
Ropivacaine-d7 is deuterium labeled Ropivacaine. Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (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 neuropathic pain management.
|
-
- HY-P3316
-
|
OSK-1
|
Potassium Channel
|
Inflammation/Immunology
Neurological Disease
|
|
OSK-1 is a potent Kv channel blocker with IC50s of of 0.6 nM, 5.4 nM, 0.014 nM for Kv1.1, Kv1.2 and Kv1.3, respectively. OSK1 is a moderate blocker of Ca 2+-activated KCa3.1 channel with an IC50 of 225 nM. OSK-1 belongs to α-KTx3 toxins and is used as a immunosuppressive drug.
|
-
- HY-W009724S
-
|
2-Aminoethyl diphenylborinate-d10
2-APB-d10
|
Calcium Channel
TRP Channel
|
Others
|
|
2-Aminoethyl diphenylborinate-d10 (2-APB-d10) is the deuterium labeled 2-Aminoethyl diphenylborinate. 2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R. 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca 2+ (SOC) channel and activates some TRP channels (V1, V2 and V3).
|
-
- 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 Ca 2+ channels. (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied.
|
-
- HY-120597
-
|
SAK3
|
Calcium Channel
|
Neurological Disease
|
|
SAK3 is a potent T-type voltage-gated Ca 2+ channels (T-VGCCs) enhancer. SAK3 enhances Cav3.1 and Cav3.3 T-type Ca 2+ channel currents. Acute SAK3 administration improves memory deficits in olfactory-bulbectomized mice. SAK3 inhibits amyloid β plaque formation in APP-KI mice by activating the proteasome activity.
|
-
- HY-P1075A
-
|
CALP3 TFA
|
Calcium Channel
|
Cancer
Neurological Disease
|
|
CALP3 TFA, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 TFA can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
|
-
- 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 + (KATP) channel antagonist. Mitiglinide calcium hydrate is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell KATP channel). Mitiglinide Calcium hydrate can be used for the research of type 2 diabetes.
|
-
- HY-B1482A
-
|
Mesoridazine
TPS-23
|
Potassium Channel
|
Neurological Disease
|
|
Mesoridazine (TPS-23) , a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC50 of 550 nM (at 0 mV) in human embryonic kidney 293 cells.Mesoridazine can be used for the research of schizophrenia, as well as certain other psychiatric disorders.
|
-
- 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-B0402B
-
|
Amantadine sulfate
1-Adamantanamine sulfate; 1-Aminoadamantane sulfate
|
Influenza Virus
Orthopoxvirus
SARS-CoV
Apoptosis
CDK
Bcl-2 Family
|
Cancer
Infection
Neurological Disease
|
|
Amantadine (1-Adamantanamine) sulfate is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine sulfate inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine sulfate also has anti-orthopoxvirus and anticancer activity. Amantadine sulfate can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.
|
-
- HY-B1482
-
|
Mesoridazine benzenesulfonate
TPS-23 benzenesulfonate
|
Potassium Channel
|
Neurological Disease
|
|
Mesoridazine (TPS-23) benzenesulfonate, a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine benzenesulfonate is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC50 of 550 nM (at 0 mV) in human embryonic kidney 293 cells.Mesoridazine benzenesulfonate can be used for the research of schizophrenia, as well as certain other psychiatric disorders.
|
-
- HY-100727
-
-
- HY-116790A
-
-
- 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
-
-
- HY-10388A
-
-
- HY-B1445
-
-
- 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-124687
-
-
- HY-15125
-
-
- HY-147005
-
-
- HY-20587
-
-
- HY-N2060
-
-
- 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-B0369AS
-
-
- HY-N0252
-
-
- 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 Ca 2+ influx.
|
-
- HY-N5006
-
-
- HY-N1469
-
-
- HY-136189
-
-
- HY-A0093S1
-
-
- HY-B0887S1
-
|
Permethrin-d9
|
Parasite
|
Infection
|
|
Permethrin-d9 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-112723
-
-
- 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
-
-
- HY-107372
-
-
- HY-103310
-
-
- HY-147391
-
-
- HY-101621S
-
-
- HY-B0612A
-
-
- HY-130074
-
-
- HY-B0612
-
-
- 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-120026
-
|
KB130015
KB015
|
Thyroid Hormone Receptor
|
Neurological Disease
|
|
KB130015 (KB015) is an orally active and potent ThRα and ThRβ (Thyroid Hormone Receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 has antiarrhythmic properties. KB130015 markedly slows the kinetics of inactivation of Na + channels. KB130015 opens large-conductance Ca 2+-activated K + channels and relaxes vascular smooth muscle.
|
-
- 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-121166
-
|
Levobetaxolol
(S)-Betaxolol
|
Adrenergic Receptor
|
Others
|
|
Levobetaxolol is a potent and high affinity β-adrenergic antagonist with IC50 values of 33.2, 2970, 709 nM for guinea pig atrial β1, tracheal β2 and rat colonic β3 receptors, respectively. Levobetaxolol reduces IOP (intraocular pressure). Levobetaxolol exhibits a micromolar affinity for L-type Ca21-channels. Levobetaxolol decreases the effects of ischaemia/reperfusion injury in rats. Levobetaxolol has the potential for the research of glaucoma.
|
-
- HY-B0267AS
-
-
- HY-P0062
-
-
- HY-B0772A
-
-
- HY-18600A
-
-
- HY-133614
-
|
Dihydroisopimaric acid
|
Potassium Channel
|
Others
|
|
Dihydroisopimaric acid activates large conductance Ca 2+ activated K + (BK) channels alphabeta1 in the direct measurement of BKalphabeta1 opening under whole-cell voltage clamp.
|
-
- HY-P1282
-
-
- HY-D1543
-
|
Pyronin B
|
DNA Stain
Others
|
Infection
|
|
Pyronin B is an organic cationic dye used for the staining of bacteria, mycobacteria and ribonucleic acids. Pyronin B is also used as a small hydrophobic (SH) protein channel inhibitor.
|
-
- HY-137986
-
-
- HY-114301
-
-
- HY-A0148A
-
|
Halofantrine hydrochloride
SKF-102886; WR-171669 hydrochloride
|
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-B1657A
-
|
Fosphenytoin disodium
|
Sodium Channel
|
Neurological Disease
|
|
Fosphenytoin sodium is a phenytoin prodrug with similar anticonvulsant properties. Its main mechanism is to block frequency-dependent, use-dependent and voltage-dependent neuronal sodium channels, and therefore limit repetitive firing of action potentials.
|
-
- HY-18600
-
-
- HY-P0062B
-
-
- HY-B1500
-
-
- 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-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 Ca 2+ channel antagonist and has the potential for Alzheimer’s disease research.
|
-
- HY-15124
-
-
- HY-118048
-
-
- HY-114608
-
-
- HY-66010A
-
|
Cinepazide
|
Calcium Channel
|
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
-
-
- HY-B0448A
-
-
- HY-110011
-
|
Cromakalim
BRL 34915
|
Potassium Channel
|
Inflammation/Immunology
|
|
Cromakalim is a potassium channel opener. Cromakalim can be used as a bronchodilator in asthma. Cromakalim inhibits the spontaneous tone of human isolated bronchi in a concentration-related manner being nearly as effective as isoprenaline or theophylline.
|
-
- HY-114301A
-
-
- HY-N2197
-
|
Hirsuteine
|
nAChR
|
Neurological Disease
|
|
Hirsuteine is an indole alkaloid extracted from Uncaria rhynchophylla. Hirsuteine non-competitively antagonizes nicotine-mediated dopamine release by blocking ion permeation through nicotinic receptor channel complexes.
|
-
- HY-P3655
-
|
Agelenin
|
Calcium Channel
|
Others
|
|
Agelenin is a polypeptide composed of 35 amino acids. Agelenin could be isolated from the Agelenidae spider Agelena opulenta. Agelenin has structural similarity to insect-specific calcium channel inhibitor.
|
-
- HY-Y0258S
-
|
Benzocaine-d4
|
Sodium Channel
|
Neurological Disease
|
|
Benzocaine-d4 is the deuterium labeled Benzocaine. 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-P1282A
-
-
- HY-B0448
-
-
- HY-B0551
-
-
- HY-P0188
-
-
- HY-123825
-
-
- HY-B0551A
-
-
- HY-N1584
-
-
- HY-Y0258S1
-
-
- HY-100783A
-
|
(-)-Bicuculline methochloride
l-Bicuculline methochloride
|
GABA Receptor
|
Neurological Disease
|
|
(-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
|
-
- HY-A0176S
-
-
- HY-146334
-
|
DFBTA
|
Chloride Channel
|
Inflammation/Immunology
|
|
DFBTA is an orally active, potent and little brain penetrated ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain.
|
-
- HY-P0188A
-
-
- HY-B1243S
-
|
Propoxycaine-d4 hydrochloride
|
Sodium Channel
|
Neurological Disease
|
|
Propoxycaine-d4 hydrochloride is the deuterium labeled Propoxycaine hydrochloride. 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-33350
-
-
- HY-P3089
-
|
Dendrotoxin K
|
Potassium Channel
|
Others
|
|
Dendrotoxin K is a Kv1.1 channel blocker. Dendrotoxin K determines glutamate release in CA3 neurons in a time-dependent manner through the control of the presynaptic spike waveform.
|
-
- HY-B0284S1
-
-
- HY-144802
-
-
- HY-100783
-
|
(-)-Bicuculline methobromide
l-Bicuculline methobromide
|
GABA Receptor
|
Neurological Disease
|
|
(-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-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
-
-
- HY-101789
-
-
- HY-145992
-
-
- HY-136589
-
-
- 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-108506S2
-
|
Licarbazepine-d4-1
BIA 2-005-d4-1; GP 47779-d4-1
|
Sodium Channel
|
Neurological Disease
|
|
Licarbazepine-d4-1 is deuterium labeled Licarbazepine. Licarbazepine (BIA 2-005; GP 47779) is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects.
|
-
- HY-N4323
-
-
- HY-N0322A
-
|
Cholesterol (Water Soluble)
|
Others
|
Others
|
|
Cholesterol Water Soluble can be used for the research of the effects of cholesterol on the potassium currents in inner hair cells (IHCs). Cholesterol is an integral component of the cell membrane and regulates the activity of ion channels in the lipid bilayer.
|
-
- 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 Kd value of 1.45 µM. Halazone protects sodium channels from inactivation. Halazone is widely used for disinfection of drinking water.
|
-
- HY-122135
-
-
- HY-69359
-
|
Nipecotic acid
(±)-β-Homoproline; Hexahydronicotinic acid; 3-Carboxypiperidine
|
GABA Receptor
|
Neurological Disease
|
|
Nipecotic acid ((±)-β-Homoproline) is a potent inhibitor of neuronal and glial-aminobutyric acid (GABA) uptake in vitro. Nipecotic acid can also directly activate GABAA-like chloride channels, with an EC50 of approximately 300 μM.
|
-
- 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
-
-
- HY-B0632
-
|
Diltiazem
|
Calcium Channel
|
Cardiovascular Disease
|
|
Diltiazem is an orally active L-type Ca 2+ channel blocker. Diltiazem shows antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris.
|
-
- HY-B0432B
-
-
- HY-P0062A
-
-
- HY-100712
-
|
DPO-1
|
Potassium Channel
|
Cardiovascular Disease
|
|
DPO-1 is a potent inhibitor of the voltage-gated potassium channel subtype Kv1.5 and a blocker of ultrarapid delayed rectifier potassium current. DPO-1 prevents atrial arrhythmia.
|
-
- HY-B1378S1
-
|
Ethosuximide-d5
|
Calcium Channel
|
Neurological Disease
|
|
Ethosuximide-d5 is 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-13812
-
-
- 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
-
-
- HY-N7126
-
|
Citronellal
|
Potassium Channel
|
Neurological Disease
|
|
Citronellal is a monoterpenea from the essential oils in various aromatic species of plants, with depressant, and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K ⁺ channel pathway.
|
-
- 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
-
-
- 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 Ca 2+ channel, with anti-cancer and blood pressure-lowering activities.
|
-
- HY-B1551
-
|
Benzonatate
Benzononatine
|
Sodium Channel
|
Neurological Disease
|
|
Benzonatate (Benzononatine) is a peripheral oral antitussive that dampens the activity of cough stretch receptors. Benzonatate has sodium channel-blocking properties and local anesthetic effects on the respiratory stretch receptors due to a tetracaine-like metabolite.
|
-
- HY-N0042
-
-
- HY-17436S1
-
|
Clevidipine-d7
|
Calcium Channel
|
Cardiovascular Disease
|
|
Clevidipine-d7 is the deuterium labeled Clevidipine. 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-P0256
-
-
- HY-N1072
-
|
Wilforgine
|
Calcium Channel
|
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
-
-
- HY-100831
-
|
YM-58483
BTP2
|
CRAC Channel
|
Inflammation/Immunology
|
|
YM-58483 (BTP2) is the first selective and potent inhibitor of CRAC channels and subsequent Ca 2+ signals. YM-584832 is a blocker of store-operated Ca 2+ entry (SOCE).
|
-
- HY-108506S1
-
-
- HY-14744S
-
|
Levamlodipine-d4
(S)-Amlodipine-d4; Levoamlodipine-d4
|
Calcium Channel
|
Others
|
|
Levamlodipine-d4 ((S)-Amlodipine-d4) is the deuterium labeled Levamlodipine. Levamlodipine ((S)-Amlodipine) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina.
|
-
- HY-17436S
-
|
Clevidipine-d5
|
Calcium Channel
|
Cardiovascular Disease
|
|
Clevidipine-d5 is the deuterium labeled Clevidipine. 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-123481
-
-
- HY-17360S1
-
|
Tiotropium-d6 bromide
BA679 BR-d6
|
mAChR
|
Neurological Disease
|
|
Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). 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-100641
-
-
- HY-101253
-
|
AM-92016 hydrochloride
|
Potassium Channel
|
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 IKr 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
-
-
- HY-136615
-
-
- HY-B1837
-
|
Cyfluthrin
|
Sodium Channel
|
Infection
|
|
Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product.
|
-
- HY-108069
-
-
- HY-101436
-
|
Sematilide
CK-1752
|
Potassium Channel
|
Cardiovascular Disease
|
|
Sematilide (CK-1752) is a selective IKr 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-108506S
-
-
- HY-111996
-
-
- 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-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 Ki 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-110230
-
-
- HY-19408
-
|
Pyr10
|
TRP Channel
|
Others
|
|
Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca 2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca 2+ 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 (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
-
- HY-151450
-
-
- 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-B0358
-
-
- HY-146380
-
|
S1427
|
Histone Demethylase
|
Cancer
|
|
S1427 is a tranylcypromine-derived LSD1 inhibitor with the IC50 of 390 nM and Ki of 80 nM. S1427 exhibits desirable hERG channel inhibition and microsomal stability profiles. Inhibition of LSD1 partially reduces the proliferation of cancer cells.
|
-
- 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
-
-
- HY-B0612DS1
-
-
- HY-19666
-
|
DPI 201-106
SDZ 201106
|
Sodium Channel
|
Cardiovascular Disease
|
|
DPI 201-106 (SDZ 201106) is a cardiotonic agent with a synergistic sarcolemmal and intracellular mechanism of action. DPI 201-106 shows cardioselective modulation of voltage-gated sodium channels (VGSCs) resulting in a positive inotropic effect.
|
-
- HY-B0493S1
-
-
- HY-N1462
-
|
Atractyloside potassium salt
|
Chloride Channel
|
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
-
-
- HY-108575
-
-
- 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-B0339S
-
|
Primidone-d5
|
Sodium Channel
|
Neurological Disease
|
|
Primidone-d5 is the deuterium labeled Primidone. 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-135328S
-
-
- 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-W040265
-
|
Fenamic acid
N-Phenylanthranilic acid
|
Chloride Channel
|
Inflammation/Immunology
|
|
Fenamic acid (N-Phenylanthranilic acid, NPAA) is an orally active chloride channel blocker. Fenamic acid is the basic constituent of non-steroidal anti-inflammatory agents (NSAIA), and derives into mefenamic, tofenacin, flufenac acid and melofenac acid. Fenamic acid also acts as antibacterial and analgesic agent -.
|
-
- 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 Ca 2+-activated K + channels. Verruculogen is an M phase inhibitor of the mammalian cell cycle.
|
-
- 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-122504
-
-
- HY-B1445S
-
|
Minoxidil sulfate-d10
|
Potassium Channel
|
Metabolic Disease
|
|
Minoxidil sulfate-d10 is the deuterium labeled Minoxidil sulfate. 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-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-151452
-
-
- HY-P3064
-
|
Scyllatoxin
Leiurotoxin I
|
Potassium Channel
|
Neurological Disease
|
|
Scyllatoxin (Leiurotoxin I) is a peptide toxin, it can be isolated from the venom of the scorpion (Leiurus quinquestriatus hebraeus). Scyllatoxin is a blocker of small-conductance KCa (SK) channel. Scyllatoxin enhances both norepinephrine (NE) and epinephrine (Epi) release in vivo.
|
-
- 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
-
-
- HY-30234A
-
-
- HY-B1751B
-
-
- 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-A0057
-
|
Gabapentin
|
Calcium Channel
|
Neurological Disease
Cancer
|
|
Gabapentin is a potent, orally active P/Q type Ca 2+ channel blocker. Gabapentin inhibits neuronal Ca 2+ influx and reduction of neurotransmitter release. Gabapentin is a GABA analog that can be used to relieve neuropathic pain.
|
-
- 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-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 (IC50=9.8 μM).
|
-
- HY-B0632S1
-
|
Diltiazem-d4 hydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
Diltiazem-d4 hydrochloride is the deuterium labeled Diltiazem. Diltiazem is an orally active L-type Ca 2+ channel blocker, with antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris.
|
-
- HY-A0057A
-
|
Gabapentin hydrochloride
|
Calcium Channel
|
Neurological Disease
Cancer
|
|
Gabapentin hydrochloride is a potent, orally active P/Q type Ca 2+ channel blocker. Gabapentin hydrochloride inhibits neuronal Ca 2+ influx and reduction of neurotransmitter release. Gabapentin hydrochloride is a GABA analog that can be used to relieve neuropathic pain.
|
-
- 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
-
-
- HY-30234
-
-
- HY-B0517S
-
|
Mepivacaine-d3
|
Sodium Channel
|
Neurological Disease
|
|
Mepivacaine-d3 is the deuterium labeled Mepivacaine. 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-B1558
-
|
Bifemelane
MCI-2016 free base
|
Calcium Channel
|
Neurological Disease
|
|
Bifemelane is a nootropic compound. Bifemelan causes the first peak by stimulating release from intracellular Ca 2+ stores and the second by capacitive entry through store–operated Ca 2+ channels. Bifemelane will be provided as a pharmacological tool for basic studies on astrocytes.
|
-
- 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 Ca 2+-permeable nonselective cation channel, to increase [Ca 2+]i. Antitumor activity.
|
-
- HY-B0632S
-
|
Diltiazem-d6
|
Calcium Channel
|
Cardiovascular Disease
|
|
Diltiazem-d6 is the deuterium labeled Diltiazem. Diltiazem is an orally active L-type Ca 2+ channel blocker, with antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris.
|
-
- HY-122605
-
-
- 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 (Ki 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 Kd 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-B1657AS
-
|
Fosphenytoin-d10 disodium
|
Sodium Channel
|
Neurological Disease
|
|
Fosphenytoin-d10 (disodium) is deuterium labeled Fosphenytoin (disodium). Fosphenytoin sodium is a phenytoin prodrug with similar anticonvulsant properties. Its main mechanism is to block frequency-dependent, use-dependent and voltage-dependent neuronal sodium channels, and therefore limit repetitive firing of action potentials.
|
-
- HY-B0112
-
-
- 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-108585
-
|
VU591 hydrochloride
|
Potassium Channel
|
Neurological Disease
|
|
VU591 hydrochloride is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM. VU591 hydrochloride can be used for neurological research with HY-108585A (the equivalent of VU591 hydrochloride).
|
-
- HY-P3507
-
|
Dalazatide
ShK-186
|
Potassium Channel
|
Inflammation/Immunology
|
|
Dalazatide (ShK-186) is a Kv1. 3 potassium channel peptide inhibitor. Dalazatide can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease.
|
-
- HY-B0495A
-
|
Lamotrigine hydrate
LTG hydrate; BW430C hydrate
|
Sodium Channel
Autophagy
|
Neurological Disease
|
|
Lamotrigine hydrate is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine hydrate selectively blocks voltage-gated Na + channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine hydrate can be used for the research of epilepsy, focal seizure, et al.
|
-
- HY-119934
-
-
- HY-108589
-
|
PNU 37883 hydrochloride
PNU 37883A
|
Potassium Channel
|
Neurological Disease
|
|
PNU 37883 hydrochloride (PNU 37883A) is a selective vascular ATP-sensitive potassium (Kir6, KATP) 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-108585A
-
|
VU591
|
Potassium Channel
|
Neurological Disease
|
|
VU591 is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM. VU591 can be used for neurological research with HY-108585 (the equivalent of VU591 hydrochloride).
|
-
- HY-N1934
-
-
- HY-108235A
-
|
Lanicemine dihydrochloride
AZD6765 dihydrochloride; ARL 15896AR
|
iGluR
|
Neurological Disease
|
|
Lanicemine (AZD6765) dihydrochloride is a low-trapping NMDA channel blocker (Ki 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-B0166A
-
-
- HY-131614
-
|
TPC2-A1-N
|
Calcium Channel
|
Others
|
|
TPC2-A1-N is a powerful and Ca 2+-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 Ca 2+ 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-101346S
-
|
ZD 7288-d3
ICI D7288-d3
|
HCN Channel
|
Neurological Disease
|
|
ZD 7288-d3 (ICI D7288-d3) is the deuterium labeled ZD7288. ZD7288 (ICI D7288) is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.
|
-
- HY-141796
-
|
MS67
|
Histone Methyltransferase
PROTACs
|
Cancer
|
|
MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects.
|
-
- HY-108974
-
|
Drotaverine hydrochloride
|
Phosphodiesterase (PDE)
Calcium Channel
|
|
|
Drotaverine (hydrochloride) is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.
|
-
- HY-B1751C
-
-
- 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
-
-
- HY-N0219
-
|
Bicuculline
(+)-Bicuculline; d-Bicuculline
|
GABA Receptor
|
Neurological Disease
|
|
Bicuculline ((+)-Bicuculline; d-Bicuculline), as a convulsant alkaloid, is a competitive neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+-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 CaV2.3 channel blocker with an IC50 of 30 nM. SNX-482 has antinociceptive effect.
|
-
- HY-122697
-
-
- 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 IC50s 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 Ki 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-17402S
-
-
- HY-120033
-
|
RY796
|
Sodium Channel
|
Neurological Disease
|
|
RY796 is a potent and selective voltage-gated potassium (KV2) channel inhibitor with IC50s of 0.25 μM and 0.09 μM for KV2.1 and KV2.2. RY796 has analgesic activity.
|
-
- HY-16973S
-
|
Fluralaner-13C2,15N,d3
A1443-13C2,15N,d3; AH252723-13C2,15N,d3
|
Parasite
|
Infection
|
|
Fluralaner-13C2,15N,d3 is the deuterium, 13C-, and 15-labeled Fluralaner. Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
|
-
- HY-B1494
-
|
Picrotoxinin
|
Chloride Channel
GABA Receptor
|
Neurological Disease
|
|
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM.
|
-
- HY-B1751F
-
-
- HY-147383
-
|
NS-8
|
Potassium Channel
|
Endocrinology
|
|
NS-8, a pyrrole derivative, activates the Ca 2+-sensitive k +-channel. NS-8 can suppress the micturition reflex by decreasing afferent pelvic nerve activity. NS-8 can be used in the research of urinary frequency and incontinence.
|
-
- HY-B0612AS1
-
|
Lercanidipine-13C,d3-1 hydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
Lercanidipine-13C,d3-1 (hydrochloride) is deuterium labeled Lercanidipine (hydrochloride). 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-17360S
-
|
Tiotropium-d3 bromide
BA679 BR-d3
|
mAChR
|
Neurological Disease
|
|
Tiotropium-d3 (bromide) (BA679 BR-d3) is the deuterium labeled Tiotropium (Bromide). 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-W016498S1
-
-
- 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 Kd 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 Ca 2+ 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-130353S
-
|
Desethyl Amiodarone-d4 hydrochloride
|
Potassium Channel
Autophagy
|
Cardiovascular Disease
|
|
Desethyl Amiodarone-d4 hydrochloride is the deuterium labeled Desethylamiodarone hydrochloride. 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-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-B1751
-
-
- 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-B1448A
-
|
Benidipine
KW-3049 free base
|
Apoptosis
Calcium Channel
|
Cardiovascular Disease
|
|
Benidipine is a potent and orally active calcium channel antagonist. Benidipine shows anti-apoptosis effects in ischaemic/reperfused myocardial cells. Benidipine increases the activity of endothelial cell-type nitric oxide synthase and improves coronary circulation in hypertensive rats.
|
-
- HY-B0166S6
-
-
- HY-143315
-
-
- 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-100714
-
-
- HY-P1249A
-
-
- 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 Ca 2+ influx and Ca 2+ 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-118170
-
|
T16A(inh)-C01
|
Chloride Channel
|
Others
|
|
T16A(inh)-C01 is an inhibitor of TMEM16A (ANO1). T16A(inh)-C01 blocks chloride channel mediated by ANO1 with an IC50 of 8.4 μM, without interfering with calcium signaling.
|
-
- 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-HT2B receptor antagonist with a pKi 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-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 Ca 2+) in neuronal cells.
|
-
- HY-17402S1
-
-
- 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-148304
-
-
- 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-132932
-
-
- HY-107212
-
|
Selamectin
|
Parasite
Chloride Channel
P-glycoprotein
Bacterial
|
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
-
-
- HY-15419A
-
|
RS-127445
|
5-HT Receptor
|
Neurological Disease
|
|
RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
|
-
- HY-108583
-
|
Psora-4
5-(4-Phenylbutoxy)psoralen
|
Potassium Channel
|
Inflammation/Immunology
|
|
Psora-4 is a potent and selective inhibitor of Kv1.3 (voltage-gated potassium channels) with an EC50 of 3 nM. Psora-4 has immunosuppressive activity and inhibits proliferation of human and rat myelin-specific effector memory T cells in vitro.
|
-
- HY-17437A
-
-
- HY-146320
-
|
ANO1-IN-1
|
Chloride Channel
|
Cancer
|
|
ANO1-IN-1 (Compound 9c) is a selective ANO1 channel blocker with an IC50 of 2.56 μM and 15.43 μM against ANO1 and ANO2, respectively. ANO1-IN-1 suppresses strongly proliferation of glioblastoma cells.
|
-
- 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-14186
-
|
KVI-020
WYE-160020
|
Potassium Channel
|
Cardiovascular Disease
|
|
KVI-020 is an orally active, potent and selective blocker of the atrial potassium channel Kv1.5, with an IC50 of 480 nM. KVI-020 can inhibits hERG, with an IC50 of 15100 nM. KVI-020 is a potent antiarrhythmic agent, and can be used for atrial fibrillation (AF) research.
|
-
- HY-146321
-
|
ANO1-IN-2
|
Chloride Channel
|
Cancer
|
|
ANO1-IN-2 (Compound 10q) is a selective ANO1 channel blocker with an IC50 of 1.75 μM and 7.43 μM against ANO1 and ANO2, respectively. ANO1-IN-2 suppresses strongly proliferation of glioblastoma cells.
|
-
- HY-15065
-
-
- HY-18600AS
-
|
Azimilide-d8 dihydrochloride
NE-10064-d8 dihydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
Azimilide-d8 (NE-10064-d8) dihydrochloride is the deuterium labeled Azimilide dihydrochloride. 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-P1651
-
|
SOR-C13
|
Calcium Channel
|
Cancer
|
|
SOR-C13, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 has anticancer activity.
|
-
- HY-B0162
-
|
Ivabradine
|
HCN Channel
|
Cardiovascular Disease
|
|
Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity.
|
-
- 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 Kd 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-B0114S1
-
|
Oxcarbazepine-d4-1
GP 47680-d4-1
|
Sodium Channel
Apoptosis
|
Cancer
Neurological Disease
|
|
Oxcarbazepine-d4-1 is 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-B1751A
-
-
- HY-B1751E
-
-
- 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-120514
-
|
JNc-440
|
TRP Channel
Potassium Channel
|
Cardiovascular Disease
|
|
JNc-440 is a potent antihypertensive agent. JNc-440 can enhance the interaction of TRPV4 and Ca 2+-activated potassium channel 3 (KCa2.3) in endothelial cells. JNc-440 can also enhance vasodilation, and exerted antihypertensive effects 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-B0162A
-
|
Ivabradine hydrochloride
|
HCN Channel
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity.
|
-
- HY-100973A
-
-
- HY-12521
-
|
GSK-5498A
|
CRAC Channel
|
Inflammation/Immunology
|
|
GSK-5498A is a selective CARC channel inhibitor (IC50: 1 μM). GSK-5498A inhibits mediators release from mast cells and pro-inflammatory cytokines release from T cells. GSK-5498A can be used in the research of inflammatory disorders.
|
-
- HY-B0122
-
-
- HY-B0448S
-
|
Phenytoin-d10
5,5-Diphenylhydantoin-d10
|
Sodium Channel
Virus Protease
|
Neurological Disease
|
|
Phenytoin-d10 (5,5-Diphenylhydantoin-d10) is the deuterium labeled Phenytoin. 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-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
|
Chloride Channel
|
Neurological Disease
|
|
GaTx2 is a seletive and a high affinity inhibitor of ClC-2 channels with a voltage-dependent apparent KD 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-B0122A
-
-
- HY-16935
-
|
Mavatrep
JNJ-39439335
|
TRP Channel
|
Neurological Disease
|
|
Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain.
|
-
- HY-147638
-
-
- 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 (Ki 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-114029
-
|
Ep vinyl quinidine
3-Epiquinine; Epivinylquinidine
|
Parasite
|
Infection
Cardiovascular Disease
|
|
Ep vinyl quinidine (3-Epiquinine) is an epi-vinyl stereoisomer of Quinidine. Quinidine is an antiarrhythmic agent. Quinidine is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine is also a K+ channel blocker with an IC50 of 19.9 μM. Quinidine can be used for malaria research.
|
-
- HY-B0166S7
-
-
- 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-100547
-
|
IEM-1754
|
iGluR
|
Neurological Disease
|
|
IEM-1754, a dicationic adamantane derivative, is a potent blocker of open channels of native ionotropic glutamate receptors including quisqualate-sensitive receptors in insect muscles, NMDAR in cultured rat cortical neurons, and AMPAR in freshly isolated hippocampal cells. IEM-1754 shows anticonvulsant potency in vivo.
|
-
- HY-100080S
-
|
A-887826-d8
|
Sodium Channel
|
Neurological Disease
|
|
A-887826-d8 is the deuterium labeled A-887826. 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-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
-
-
- HY-17437
-
-
- HY-111613S
-
|
Pinaverium bromide-d4
|
Calcium Channel
|
Others
|
|
Pinaverium bromide-d4 is deuterium labeled Pinaverium bromide. 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-B0166S5
-
-
- HY-B0252
-
-
- HY-19765
-
|
GSK2798745
|
TRP Channel
|
Cardiovascular Disease
|
|
GSK2798745 is a potent, selective, and 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 can be used in cardiac and respiratory diseases research.
|
-
- HY-12533A
-
|
Disopyramide phosphate
Dicorantil phosphate; SC-7031 phosphate
|
Potassium Channel
Sodium Channel
|
Cardiovascular Disease
|
|
Disopyramide phosphate is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide phosphate blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide phosphate inhibits HERG encoded potassium channels. Disopyramide phosphate also exhibits complex protein binding, and has a potent negative inotropic action.
|
-
- HY-B0166S2
-
-
- 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-P1422
-
|
Spadin
|
Potassium Channel
5-HT Receptor
|
Neurological Disease
|
|
Spadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC50 value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research.
|
-
- HY-144801A
-
|
DDO-02005
|
Potassium Channel
|
Cardiovascular Disease
|
|
DDO-02005 is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine.
|
-
- 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 KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2.
|
-
- HY-B0166S4
-
-
- HY-111191A
-
|
(R)-ONO-2952
|
Others
|
Neurological Disease
|
|
(R)-ONO-2952 is a R-enantiomer of ONO-2952. ONO-2952 is a potent, selective and orally active TSPO antagonist with Kis 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.
|
-
- HY-134494
-
|
MS48107
|
GPR68
|
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-B0166S3
-
-
- HY-B0424S
-
|
Nitrendipine-d5
AY-E-5009-d5
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Nitrendipine-d5 (AY-E-5009-d5) is the deuterium labeled Nitrendipine. Nitrendipine (BAY-E-5009), an analogue of Nifedipine (HY-B0284), is a dihydropyridine calcium channel blocker with vasodilator action. Nitrendipine has antihypertensive effect.
|
-
- 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 Na 2+ 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-W111226
-
|
Fmoc-His(3-Me)-OH
|
Amyloid-β
Others
|
Cardiovascular Disease
|
|
Fmoc-His(3-Me)OH derives Histidine-associating compounds with biological activity. Fmoc-His(3-Me)OH, with Fmoc-citrulline-OH, Fmoc-His(1-Me)-OH together, forms tri-peptides and shows vasodilating effect with EC50s of 2.7-4.7 mM in 1.0 mM Phenylephrine (PE)-contracted aorta rings. Fmoc-His(3-Me)OH (resin) also makes Methyl-His-Gly-Lys (His(3-Me)-Gly-Lys), thus acts as an [Ca 2+]i inhibitor. Fmoc-His(3-Me)OH methylates NAHIS02, making it unable to block the Alzheimer's Aβ channel.
|
-
- HY-108587
-
-
- 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 (Ki 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-B0309S
-
|
Felodipine-d8
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Felodipine-d8 is the deuterium labeled Felodipine. 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-13044
-
-
- HY-B1751D
-
-
- HY-146155
-
-
- HY-147639
-
-
- HY-135897
-
-
- 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 +/Ca 2+ 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-B0309S1
-
|
Felodipine-d5
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Felodipine-d5 is deuterium labeled Felodipine. 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-101422
-
|
GAL-021
|
Potassium Channel
|
Inflammation/Immunology
|
|
GAL-021 is a potent BKCa-channel blocker. GAL-021 inhibits KCa1.1 in GH3 cells. GAL-021 is a novel breathing control modulator that is based on selective modification of the almitrine pharmacophore. GAL-021 increases minute ventilation in rats and non-human primates.
|
-
- HY-B1193
-
-
- HY-N8472
-
|
Chrodrimanin B
|
GABA Receptor
|
Infection
|
|
Chrodrimanin B, a metabolite of a fungal, is a potent, non-open-channel-blocking antagonist on B. mori GABAR RDL with an IC50 of 1.13 nM. Chrodrimanin B attenuates the peak current amplitude of the GABA response of RDL with an IC50 of 1.66 nM. Chrodrimanin B, a meroterpenoid, shows insecticidal activity.
|
-
- 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 (KATP) 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-B0309S2
-
|
Felodipine-d3
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Felodipine-d3 is the deuterium labeled Felodipine. 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-W396714
-
|
Succinic acid sodium
Wormwood acid Sodium
|
Potassium Channel
|
Neurological Disease
|
|
Succinic acid sodium is a potent and orally active anxiolytic agent. Succinic acid sodium shows inhibitory effects on colonic epithelial cell proliferation in vivo. Succinic acid sodium can down-regulate the expression of KCNMB1 (potassium channel subunit β1) and TET1 (ten‑eleven translocation 1). Succinic acid sodium can be used for gestational hypertension research.
|
-
- HY-P1422A
-
|
Spadin TFA
|
Potassium Channel
5-HT Receptor
|
Neurological Disease
|
|
Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC50 value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research.
|
-
- HY-B0185B
-
|
Lidocaine hydrochloride hydrate
Lignocaine hydrochloride hydrate
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Lidocaine (Lignocaine) hydrochloride hydrate inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate 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 hydrate is an amide derivative and has potential for the research of ventricular arrhythmia.
|
-
- 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-B0516
-
|
Articaine hydrochloride
Hoe-045
|
Sodium Channel
NF-κB
NOD-like Receptor (NLR)
|
Neurological Disease
|
|
Articaine hydrochloride (Hoe-045) is an amide anaesthetic containing an ester group, reversibly binding to the α-subunit of the voltage-gated sodium channels within the inner cavity of the nerve, can provide effective pain relief. Articaine hydrochloride ameliorates LPS-induced acute kidney injury via inhibition of NF-ĸB activation and the NLRP3 inflammasome pathway.
|
-
- HY-100641S
-
|
4-Hydroxytolbutamide-d9
Hydroxytolbutamide-d9
|
Potassium Channel
Autophagy
|
Cancer
Metabolic Disease
|
|
4-Hydroxytolbutamide-d9 (Hydroxytolbutamide-d9) is the deuterium labeled 4-Hydroxytolbutamide. 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-133596
-
|
12,14-Dichlorodehydroabietic acid
|
Potassium Channel
GABA Receptor
|
Neurological Disease
|
|
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca 2+-activated K + (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca 2+ and stimulates transmitter release.
|
-
- HY-144801
-
|
DDO-02005 free base
|
Potassium Channel
|
Cardiovascular Disease
|
|
DDO-02005 (free base) is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 (free base) has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine.
|
-
- HY-14336
-
|
SB 271046
|
5-HT Receptor
|
Neurological Disease
|
|
SB 271046 is a potent, selective and orally active 5-HT6 receptor antagonist with a pKi of 8.92-9.09. SB 271046 show >200-fold selective for the 5-HT6 receptor over other receptors, binding sites and ion channels. SB 271046 has anticonvulsant activity.
|
-
- 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 and has potential for the research of ventricular arrhythmia.
|
-
- HY-108974S
-
|
Drotaverine-d10 hydrochloride
|
Phosphodiesterase (PDE)
Calcium Channel
|
|
|
Drotaverine-d10 hydrochloride is the deuterium labeled Drotaverine hydrochloride. Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine hydrochloride exhibits in vivo antispasmodic efficacy without anticholinergic effects.
|
-
- HY-16952
-
|
Bepridil
(±)-Bepridil; Org 5730
|
Calcium Channel
Sodium Channel
SARS-CoV
|
Infection
Cardiovascular Disease
|
|
Bepridil ((±)-Bepridil) is a calcium channel blocking agent used as antiarrhythmic agent. Bepridil inhibits both calcium and sodium currents, has research potential in certain ischemia-induced ventricular arrhythmias. Bepridil also has strong inhibition of SARS-CoV-2 from entry and replication inside Vero E6 and A549 cells.
|
-
- HY-103137
-
|
Zacopride hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Zacopride hydrochloride is a highly potent 5-HT3 receptor antagonist with Kis of 0.38 and 373 nM for 5-HT3 and 5-HT4 receptor, respectively. Zacopride hydrochloride is also a moderate IK1 channel agonist. Zacopride hydrochloride exerts significant antiarrhythmic and cardiac protective effects.
|
-
- HY-101840
-
-
- HY-101840A
-
-
- HY-17429S
-
|
Flecainide-d4 acetate
R-818-d4
|
Sodium Channel
|
Cardiovascular Disease
|
|
Flecainide-d4 acetate (R-818-d4) is the deuterium labeled Flecainide acetate. 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-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 INa. 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-109545
-
|
Isopropyl unoprostone
Unoprostone isopropyl ester; UF-021
|
Potassium Channel
|
Others
|
|
Isopropyl unoprostone (Unoprostone isopropyl ester), an analogue of a prostaglandin metabolite, is a potent large conductance Ca 2+-activated K + (BK) channels activator. Isopropyl unoprostone has antiglaucoma effects, lowering intraocular pressure (IOP) by increasing aqueous humour outflow. Isopropyl unoprostone can improve retinal sensitivity and the protection of central retinal sensitivity.
|
-
- HY-108512
-
|
PD 144418
|
Sigma Receptor
|
Neurological Disease
|
|
PD 144418 is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki 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-103337
-
|
N-Arachidonoylserotonin
Arachidonyl serotonin; AA-5-HT
|
FAAH
TRP Channel
|
Neurological Disease
|
|
N-Arachidonoylserotonin (Arachidonyl serotonin; AA-5-HT) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 value of 1~12 µM. N-Arachidonoylserotonin acts also as an antagonist of transient receptor potential vanilloid-type 1 (TRPV1) channels (IC50=70~100 nM). N-Arachidonoylserotonin is analgesic in rodents .
|
-
- HY-108460
-
|
A-784168
|
TRP Channel
|
Neurological Disease
|
|
A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration.
|
-
- HY-147357
-
|
TRPC3/6-IN-1
|
TRP Channel
|
Cardiovascular Disease
|
|
TRPC3/6-IN-1 is a potent selectivity blocker of the canonical transient receptor channels (TRPC3/6), has block potency for hTRPC3 and hTRPC6 with IC50 values of 1260 nM and 500 nM, respectively. TRPC3/6-IN-1 can be used for the research of chronic models of heart failure.
|
-
- HY-108235S
-
|
Lanicemine-d5
AZD6765-d5
|
iGluR
|
Neurological Disease
|
|
Lanicemine-d5 (AZD6765-d5) is the deuterium labeled Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (Ki 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-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 and a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
|
-
- HY-135746
-
-
- HY-131897
-
-
- HY-118472
-
|
Benazeprilat
CGS 14831
|
Endogenous Metabolite
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Benazeprilat is an orally active and the active metabolite of benazepril, a carboxyl-containing ACE inhibitor with antihypertensive activity. Benazepril is a well-established antihypertensive agent, both in monotherapy and in combination with other classes of drugs including thiazide diuretics and calcium channel blockers. Benazepril is a first-line treatment in reducing various pathologies associated with CV risk and secondary end-organ damage.
|
-
- HY-14946
-
|
Amifampridine
3,4-Diaminopyridine
|
Potassium Channel
|
Neurological Disease
|
|
Amifampridine (3,4-Diaminopyridine) is an orally active, potent and cell permeable voltage-gated potassium (Kv) channel blocker (PCB). Amifampridine is efficacy in the reversal of BoNT/A (HY-P79153) intoxication. Amifampridine increases transmitter release from neuromuscular junctions (NMJs). Amifampridine can be used for Lambert-Eaton myasthenic syndrome (LEMS) research.
|
-
- HY-108512A
-
|
PD 144418 oxalate
|
Sigma Receptor
|
Neurological Disease
|
|
PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki 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-108591
-
|
L-364,373
R-L3
|
Potassium Channel
|
Cardiovascular Disease
|
|
L-364,373 (R-L3) is a voltage-gated Kv7.1 (KCNQ1)/mink channels activator. L-364,373 activates Iks (slow delayed rectifier potassium current) and shortens action potential duration in guinea pig cardiac myocytes, and suppresses early afterdepolarizations in rabbit ventricular myocytes.
|
-
- 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 Ki 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-101422A
-
|
GAL-021 sulfate
|
Potassium Channel
|
Inflammation/Immunology
|
|
GAL-021 sulfate is a potent BKCa-channel blocker. GAL-021 sulfate inhibits KCa1.1 in GH3 cells. GAL-021 sulfate is a novel breathing control modulator that is based on selective modification of the almitrine pharmacophore. GAL-021 sulfate increases minute ventilation in rats and non-human primates.
|
-
- HY-139426
-
-
- HY-110234
-
-
- HY-A0064S
-
|
Verapamil-d3 hydrochloride
(±)-Verapamil-d3 hydrochloride; CP-16533-1-d3 hydrochloride
|
Calcium Channel
P-glycoprotein
Cytochrome P450
|
Cardiovascular Disease
|
|
Verapamil-d3 ((±)-Verapamil-d3) hydrochloride is the deuterium labeled Verapamil hydrochloride. 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-12496
-
|
NS-1619
|
Potassium Channel
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
NS-1619 is an opener of large conductance Ca 2+-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-D1571
-
|
CellTracker Blue CMF2HC Dye
|
DNA Stain
Others
|
Others
|
|
CellTracker Blue CMF2HC Dye is a blue dye, can be used in two-channel nuclei acid sequencing, with blue and purple excitation light (450-460 nm/400-405nm or 415-450 nm/480-525nm). CellTracker Blue CMF2HC Dye can be used to rapid determination of antibiotic sensitivity of microorganisms.
|
-
- HY-B1546
-
|
Benzamil
Benzylamiloride
|
Na+/Ca2+ Exchanger
Sodium Channel
|
Neurological Disease
|
|
Benzamil (Benzylamiloride), an Amiloride analogue, is a Na +/Ca 2+ 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 Ca 2+-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-N1500
-
|
Pulegone
|
TRP Channel
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Pulegone, the major chemical constituent of Nepeta catariaessential oil which is an aromatic herb, 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-N0747
-
|
Oxypeucedanin
|
Potassium Channel
Apoptosis
|
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 +/Ca 2+ 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 Ca 2+-activated currents, with an IC50 of 1.1 μM.
|
-
- HY-113469A
-
|
Cyclic GMP sodium
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Cyclic GMP sodium (cGMP) is an important regulator of short-term changes in smooth muscle tone and longer-term responses to chronic drug treatment or proliferative signals, it is in response to atrial natriuretic peptide (ANP) or nitric oxide (NO). Cyclic GMP sodium interacts with cation channels to regulate ion transport or activate the cyclic GMP-dependent protein kinase to result in protein phosphorylation.
|
-
- HY-23196S
-
|
Minoxidil-d10
|
Potassium Channel
|
|
|
Minoxidil-d10 (U10858-d10) is the deuterium labeled Minoxidil. Minoxidil (U10858) is an ATP-sensitive potassium (KATP) 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-B0516A
-
|
Articaine
Hoe-045 free base
|
NF-κB
NOD-like Receptor (NLR)
Sodium Channel
|
Inflammation/Immunology
|
|
Articaine (Hoe-045 free base) is an amide anaesthetic containing an ester group, reversibly binding to the α-subunit of the voltage-gated sodium channels within the inner cavity of the nerve, can provide effective pain relief. Articaine ameliorates LPS-induced acute kidney injury via inhibition of NF-ĸB activation and the NLRP3 inflammasome pathway.
|
-
- HY-14946A
-
|
Amifampridine phosphate
3,4-Diaminopyridine phosphate
|
Potassium Channel
|
Neurological Disease
|
|
Amifampridine (3,4-Diaminopyridine) phosphate is an orally active, potent and cell permeable voltage-gated potassium (Kv) channel blocker (PCB). Amifampridine phosphate is efficacy in the reversal of BoNT/A (HY-P79153) intoxication. Amifampridine phosphate increases transmitter release from neuromuscular junctions (NMJs). Amifampridine phosphate can be used for Lambert-Eaton myasthenic syndrome (LEMS) research.
|
-
- HY-110162
-
|
QO 58
|
Potassium Channel
|
Neurological Disease
|
|
QO 58 is a potent modulator of K(v)7 channels. QO-58 increases the current amplitudes, shifts the voltage-dependent activation curve in a more negative direction and slows the deactivation of K(v)7.2/K(v)7.3 currents. QO-58 has the potential for the research of diseases associated with neuronal hyperexcitability.
|
-
- HY-B0495S4
-
|
Lamotrigine-13C3
LTG-13C3; BW430C-13C3
|
Sodium Channel
Autophagy
|
Neurological Disease
|
|
Lamotrigine-13C3 is the 13C-labeled Lamotrigine. 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-120348
-
-
- HY-132670S
-
|
(R)-(-)-Felodipine-d5
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
(R)-(-)-Felodipine-d5 is the deuterium labeled (R)-(-)-Felodipine. (R)-(-)-Felodipine is the S enantiomer of Felodipine. 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-B0254S
-
|
Glipizide-d11
|
Potassium Channel
|
Metabolic Disease
|
|
Glipizide-d11 is the deuterium labeled Glipizide. 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 (KATP) channels among β cells of pancreatic islets of Langerhans.
|
-
- HY-14600
-
-
- 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 Ca 2+-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-139791
-
|
KCNQ2/3 activator-1
|
Potassium Channel
|
Cancer
|
|
KCNQ2/3 activator-1 is an activator of Kv7.2/Kv7.3 (KCNQ2/3) potassium channel. KCNQ2/3 activator-1 has the potential in relieving pain (the main problem from medical treatment) (extracted from patent WO2021113757A1, compound A).
|
-
- HY-12532S
-
|
Astemizole-d3
|
Histamine Receptor
Potassium Channel
|
Inflammation/Immunology
Endocrinology
|
|
Astemizole-d3 is the deuterium labeled Astemizole. 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-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
|
Piezo Channel
|
Cardiovascular Disease
|
|
Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel. Dooku1 inhibited 2 μM Yoda1-induced Ca 2+-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
Calcium Channel
Calmodulin
|
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-B0495S1
-
|
Lamotrigine-13C,d3
LTG-13C,d3; BW430C-13C,d3
|
Sodium Channel
Autophagy
|
Neurological Disease
|
|
Lamotrigine-13C,d3 is the 13C- and deuterium labeled Lamotrigine. 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-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 Ca 2+ influx through both voltage-gated Ca 2+ channels and NMDA receptors and increases neuroD expression. ISX-9 also induces cardiomyogenic differentiation of Notch-activated epicardium-derived cells (NECs).
|
-
- HY-B1588S
-
|
Carbenoxolone-d4
|
Amyloid-β
HIV
11β-HSD
|
Infection
Inflammation/Immunology
Neurological Disease
|
|
Carbenoxolone-d4 is deuterium labeled Carbenoxolone. Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties.
Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the treatment of chronic liver disease.
Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD.
Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop.
Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form.
Carbenoxolone has antiviral activity against DENV infection targeting the virus itself.
|
-
- HY-106577
-
|
Cibenzoline
Cifenline; Ro 22-7796
|
Potassium Channel
|
Cardiovascular Disease
|
|
Cibenzoline is a potent inhibitor of KATP channel with directly affecting the pore-forming Kir6.2 subunit rather than the SUR1 subunit. Cibenzoline is a class Ia antiarrhythmic drug. Cibenzoline has little anticholinergic activity. Cibenzoline markedly attenuate LVPG which has a close relationship with myocardial contractility decreasing. Cibenzoline has the potential for the research of hypertrophic obstructive cardiomyopathy.
|
-
- HY-111655
-
|
SKA-31
|
Potassium Channel
|
Cardiovascular Disease
|
|
SKA-31 is a potent potassium channel activator with EC50s 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-100168
-
|
BAPTA
|
Phospholipase
|
Others
|
|
BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators.
|
-
- HY-13295
-
-
- HY-148129
-
|
TRPC6-IN-3
|
TRP Channel
|
Cardiovascular Disease
|
|
TRPC6-IN-3 (compound 17) is a potent, orally active transient receptor potential C6 ion channel (TRPC6) inhibitor. TRPC6-IN-3 modulates not only intracellular calcium concentration, but also membrane potential by modulating the flux of cations including calcium and sodium ions. TRPC6-IN-3 can be used in research of respiratory system.
|
-
- HY-107370
-
|
Atomoxetine
Tomoxetine; (R)-Tomoxetine
|
Serotonin Transporter
Sodium Channel
|
Neurological Disease
|
|
Atomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with Ki values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DAEX and NEEX in the PFC and enhances catecholaminergic neurotransmission. Atomoxetine (Tomoxetine) is a potent Na + channels (VGSCs) blocker. Atomoxetine (Tomoxetine) can be used for attention-deficit hyperactivity disorder (ADHD) research.
|
-
- HY-B0252S
-
|
Hydrochlorothiazid-d2
HCTZ-d2
|
TGF-beta/Smad
Potassium Channel
|
Metabolic Disease
Cardiovascular Disease
|
|
Hydrochlorothiazid-d2 (HCTZ-d2) is the deuterium labeled Hydrochlorothiazide. 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-B0185S1
-
|
Lidocaine-d10
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Lidocaine-d10 is the deuterium labeled Lidocaine. 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 and has potential for the research of ventricular arrhythmia.
|
-
- HY-103550
-
|
A-841720
|
mGluR
|
Neurological Disease
|
|
A-841720 is a potent, non-competitive and selective mGlu1 receptor antagonist with an IC50 of 10 nM for human mGlu1 receptor. A-841720 displays 34-fold selectivity over mGlu5 (IC50 of 342 nM), and no significant activity at a range of other neurotransmitter receptors, ion channels, and transporters. A-841720 has the potential for chronic pain research.
|
-
- HY-W037817
-
|
Dimethyl L-glutamate
Dimethyl glutamate
|
Potassium Channel
Bacterial
|
Infection
Metabolic Disease
|
|
Dimethyl L-glutamate (Dimethyl glutamate), a membrane-permeable analog of Glutamate, can stimulate insulin release induced by Glucose. Dimethyl L-glutamate suppresses the KATP channel activities. Dimethyl L-glutamate inhibits E. gracilis growth and causes abnormal cell division. Dimethyl L-glutamate can be used in the research of diabetes, glucose transport, phosphorylation, and further metabolism.
|
-
- HY-118689
-
|
RA-2
|
Potassium Channel
|
Inflammation/Immunology
Neurological Disease
Cardiovascular Disease
|
|
RA-2 is a negative-gating modulator of KCa2/3 channels with an IC50 of 17 nM. RA-2 inhibits bradykinin-induced endothelium-derived hyperpolarization (EDH)-type relaxation in U46619-precontracted rings. RA-2 can help to define the physiologic and pathomechanistic roles of KCa2/3 in the vasculature, central nervous system, and during inflammation.
|
-
- HY-B1193S1
-
-
- 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 Ca 2+ 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-B0267A
-
|
Oxybutynin chloride
|
mAChR
Potassium Channel
|
Neurological Disease
|
|
Oxybutynin chloride is an oral active and competitive mAChR antagonist with Kis of 14.3 and 5.55 nM for specific [ 3H]NMS binding in the mouse bladder and cerebral cortex, respectively. Oxybutynin chloride inhibits vascular Kv channels in a manner independent of anticholinergic effect, with an IC50 value of 11.51 μM. Oxybutynin chloride reduces muscle spasm in the bladder and urinary tract, can be used in study of overactive bladder syndrome (OAB).
|
-
- HY-B0185AS1
-
|
Lidocaine-d6 hydrochloride
Lignocaine-d6 hydrochloride
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Lidocaine-d6 (hydrochloride) is 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 and a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
|
-
- HY-B0166
-
-
- HY-B0185S
-
|
Lidocaine-d10 N-Oxide
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Lidocaine-d10 N-Oxide is the deuterium labeled Lidocaine. 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 and has potential for the research of ventricular arrhythmia.
|
-
- HY-N0361
-
-
- HY-124304
-
|
Pinokalant
LOE-908
|
TRP Channel
SARS-CoV
|
Neurological Disease
|
|
Pinokalant is a broad-spectrum and non-selectivecation channel inhibitor. Pinokalant significantly reduces cortical infarct volume. Pinokalant o improves the metabolic and electrophysiologic status of the ischemic penumbra. Pinokalant reduces lesion size on magnetic resonance images in the acute phase following middle cerebral artery occlusion in rats. Pinokalant has the potential for the research of stroke. Pinokalant also shows anti-SARS-CoV-2 activity.
|
-
- HY-113066
-
|
Guanosine 5'-diphosphate
GDP
|
Endogenous Metabolite
Potassium Channel
|
Inflammation/Immunology
|
|
Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
|
-
- HY-B1193S
-
-
- HY-113066C
-
|
Guanosine 5'-diphosphate sodium
GDP Sodium
|
Endogenous Metabolite
Potassium Channel
|
Inflammation/Immunology
|
|
Guanosine 5'-diphosphate (GDP) sodium is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate sodium is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate sodium can be used in the research of inflammation, such as anemia of inflammation (AI).
|
-
- HY-B0252S1
-
|
Hydrochlorothiazid-13C,d2
HCTZ-13C,d2
|
TGF-beta/Smad
Potassium Channel
|
Metabolic Disease
Cardiovascular Disease
|
|
Hydrochlorothiazid-13C,d2 is the 13C- and deuterium labeled Hydrochlorothiazide. 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-N0603
-
-
- HY-10341
-
|
Fasudil Hydrochloride
HA-1077 Hydrochloride; AT-877 Hydrochloride
|
ROCK
Calcium Channel
Autophagy
PKA
PKC
HIV
|
Cancer
|
|
Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki 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 Ca 2+ channel antagonist and vasodilator.
|
-
- 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 K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane.
|
-
- HY-151198
-
|
CHF-6366
|
mAChR
Adrenergic Receptor
Calcium Channel
|
Endocrinology
Inflammation/Immunology
|
|
CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs. CHF-6366 can be used to research chronic obstructive pulmonary disease (COPD).
|
-
- 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, an amide derivative, has the potential for the research of the ventricular arrhythmia.
|
-
- 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 pKi 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-B1640
-
|
Ethacrynic acid
Etacrynic acid
|
Gutathione S-transferase
NF-κB
Calcium Channel
|
Cancer
Inflammation/Immunology
|
|
Ethacrynic acid (Etacrynic 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-100168A
-
|
BAPTA tetrasodium
|
Phospholipase
|
Others
|
|
BAPTA tetrasodium is a selective chelator for calcium. BAPTA tetrasodium, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrasodium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA tetrasodium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators.
|
-
- HY-10341C
-
|
Fasudil dihydrochloride
HA-1077 dihydrochloride; AT-877 dihydrochloride
|
Calcium Channel
ROCK
PKA
PKC
Autophagy
HIV
|
Cancer
|
|
Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki 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 dihydrochloride is also a potent Ca 2+ channel antagonist and vasodilator.
|
-
- HY-100168B
-
|
BAPTA tetrapotassium
|
Phospholipase
|
Others
|
|
BAPTA tetrapotassium is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrapotassium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators.
|
-
- 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 Ki 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 Ca 2+ channel antagonist and vasodilator.
|
-
- 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-144341
-
|
DprE1-IN-1
|
Bacterial
|
Infection
|
|
DprE1-IN-1 is a potent, orally active DprE1 inhibitor with favorable hepatocyte stability, low cytotoxicity and low hERG channel inhibition. DprE1-IN-1 displays potent activity against both drug-susceptible and clinically isolated drug-resistant Tuberculosis strains with MICs<0.1 μg/mL, as well as good intracellular antimycobacterial activity with a 1.29 log10 CFU reduction in macrophages.
|
-
- HY-148418
-
|
TUG-499
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes.
|
-
- 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-113066A
-
|
Guanosine 5'-diphosphate disodium salt
GDP diSodium salt
|
Endogenous Metabolite
Potassium Channel
|
Inflammation/Immunology
|
|
Guanosine 5'-diphosphate (GDP) disodium salt is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate disodium salt is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate disodium salt can be used in the research of inflammation, such as anemia of inflammation (AI).
|
-
- HY-15206
-
|
Glibenclamide
Glyburide
|
Potassium Channel
Mitochondrial Metabolism
Autophagy
CFTR
P-glycoprotein
|
Metabolic Disease
|
|
Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) 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 KATP 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-B1906
-
|
Streptomycin
Agrept; Agrimycin; Streptomycin A
|
Antibiotic
Bacterial
|
Infection
Neurological Disease
|
|
Streptomycin (Agrept) is an effective antibiotic against M. tuberculosis, is used for the research of tuberculosis (TB). Streptomycin also is a bacteriocidal agent that can be used for the research of a number of bacterial infections. Streptomycin can bind strongly to nucleic acids, interferes and blocks protein synthesis while permitting continued RNA and DNA synthesis. Streptomycin, as a common antibiotic used in culture media, also is a blocker of stretch-activated and mechanosensitive ion channels in neurons and cardiac myocytes .
|
-
- 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 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=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-10341B
-
|
Fasudil hydrochloride semihydrate
HA-1077 hydrochloride semihydrate; AT877 hydrochloride semihydrate
|
ROCK
Calcium Channel
Autophagy
HIV
PKA
PKC
|
Cancer
|
|
Fasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki 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 semihydrate is also a potent Ca 2+ channel antagonist and vasodilator.
|
-
- HY-13295S
-
-
- HY-121119
-
-
- HY-119101
-
|
AZD-5672
|
CCR
Potassium Channel
P-glycoprotein
|
Inflammation/Immunology
|
|
AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis.
|
-
- HY-103112A
-
|
SB 243213 dihydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C 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
|
Adrenergic Receptor
|
Neurological Disease
|
|
ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki 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-P1411
-
|
Psalmotoxin 1
PcTx1; Psalmopoeus cambridgei toxin-1
|
Sodium Channel
Apoptosis
|
Cancer
Neurological Disease
|
|
Psalmotoxin 1 (PcTx1) is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a). Psalmotoxin 1 is a potent and slective ASIC1a inhibitor (IC50: 0.9 nM) by increasing the apparent affinity for H + of ASIC1a. Psalmotoxin 1 can induce cell apoptosis, also inhibits cell migration, proferliration and invasion of cancer cells. Psalmotoxin 1 can be used in the research of cancers, or neurological disease.
|
-
- HY-103112B
-
|
SB 243213
|
5-HT Receptor
|
Neurological Disease
|
|
SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C 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-146468
-
-
- HY-107625A
-
|
SNAP 94847 hydrochloride
|
MCHR1 (GPR24)
|
Neurological Disease
|
|
SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=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-A0095S1
-
|
Flibanserin-d4-1
BIMT-17-d4-1; BIMT-17BS-d4-1
|
5-HT Receptor
|
Neurological Disease
|
|
Flibanserin-d4-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=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-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 Kds 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 (Ki= 2.2 nM, Kd=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-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C 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-B0432
-
|
Propafenone
SA-79
|
Sodium Channel
Adrenergic Receptor
Potassium Channel
|
Cancer
Cardiovascular Disease
|
|
Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC50=32 nM). Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC50 values of 4.9 μm and 8.6 μm, respectively. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis.
|
-
- 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-15206S
-
|
Glyburide-d11
|
Potassium Channel
Mitochondrial Metabolism
Autophagy
CFTR
P-glycoprotein
|
Metabolic Disease
|
|
Glyburide-d11 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) 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 KATP 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-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 Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes. Guanfu base A also inhibits HERG channel current.
|
-
- HY-100001
-
-
- 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 Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB 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-B0822
-
|
Fipronil
|
GABA Receptor
Cytochrome P450
Apoptosis
|
Neurological Disease
|
|
Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes.
|
-
- HY-B0495S
-
|
Lamotrigine-13C3,d3
LTG-13C3,d3; BW430C-13C3,d3
|
Sodium Channel
Autophagy
|
Neurological Disease
|
|
Lamotrigine-13C3,d3 (LTG-13C3,d3) is the 13C-labeled Lamotrigine. 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-B0653
-
|
Levobupivacaine
(S)-(-)-Bupivacaine
|
Sodium Channel
Ferroptosis
|
Cancer
Neurological Disease
|
|
Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local anaesthetic. Levobupivacaine exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer.
|
-
- HY-123264
-
|
RL648_81
|
Potassium Channel
|
Neurological Disease
|
|
RL648_81 is a specific KQT-like subfamily 2/3 (KCNQ2/3) activator with an EC50 of 190 nM. RL648_81 robustly shifts the V1/2 of KCNQ2/3 channels towards hyperpolarized potentials.RL648_81 does not shift the V1/2 of either KCNQ4 or KCNQ5.RL648_81 has the potential for neurologic disorders associated with neuronal hyperexcitability research.
|
-
- HY-15589
-
|
GW9508
|
Free Fatty Acid Receptor
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 (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.
|
-
- HY-146158
-
|
WX-081
|
Bacterial
Potassium Channel
Antibiotic
|
Infection
|
|
WX-081, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity. WX-081 exhibits potent activity with MIC50s of 0.083 and 0.11 μg/mL for drug susceptible tuberculosis (DS-TB) and multidrug resistant tuberculosis (MDR-TB) strains. WX-081 also inhibits hERG channel with the IC50 of 1.89 μM.
|
-
- 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-B0653A
-
|
Levobupivacaine hydrochloride
(S)-(-)-Bupivacaine monohydrochloride
|
Sodium Channel
Ferroptosis
|
Neurological Disease
Cancer
|
|
Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local anaesthetic. Levobupivacaine hydrochloride exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer.
|
-
- HY-B0824
-
|
Bifenthrin
|
Sodium Channel
|
Neurological Disease
|
|
Bifenthrin is a synthetic pyrethroid insecticide. Bifenthrin prolongs the opening time of Nav1.8 sodium channels, leading to membrane depolarization and conductance block in the insect nervous system, thereby disrupting neural function. Bifenthrin was effective in inhibiting A. gambiae (LD50=0.15 ng/mg) and C. quinquefasciatus (LD50=0.16 ng/mg). Bifenthrin has good lethality against susceptible and resistant mosquitoes and is very effective in inhibiting blood sucking and can be developed as a mosquito-removal netting material.
|
-
- HY-13750
-
-
- HY-15206S1
-
|
Glyburide-d3
Glyburide-d3
|
Potassium Channel
Mitochondrial Metabolism
Autophagy
CFTR
P-glycoprotein
|
Metabolic Disease
|
|
Glyburide-d3 (Glyburide-d3) is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) 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 KATP 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-12501A
-
|
ITI-214
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki 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 Kis 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 Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka 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 CaV1.3 L-type calcium channel (LTCC) antagonist with an IC50 of 1.7 μM. CaV1.3 antagonist-1 inhibits CaV1.3 LTCC >600-fold more potently than CaV1.2 LTCC. CaV1.3 antagonist-1, a cyclopentyl derivative, has the potential for Parkinson's disease research.
|
-
- HY-131897S
-
-
- 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 Ca 2+ transport with an IC50 of 140 nM in a Ca 2+ 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 KCa2.2 (SK2) channel blocker (Kd=3.8 nM). Lei-Dab7 TFA exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, Kv 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-B0166S1
-
-
- HY-12501
-
|
ITI-214 free base
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki 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 Kis 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 pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki 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-N6789
-
|
KT5720
|
PKA
|
Cancer
Neurological Disease
|
|
KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 µM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 + concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases.
|
-
- HY-107405
-
|
TC-N 1752
|
Sodium Channel
|
Neurological Disease
|
|
TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain.
|
-
- HY-119980A
-
|
Fluphenazine dimaleate
|
Dopamine Receptor
Sodium Channel
SARS-CoV
|
Infection
Neurological Disease
|
|
Fluphenazine dimaleate is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dimaleate blocks neuronal voltage-gated sodium channels. Fluphenazine dimaleate acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dimaleate can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dimaleate can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2.
|
-
- HY-119980S
-
|
Fluphenazine-d8
|
Sodium Channel
Dopamine Receptor
SARS-CoV
|
Others
|
|
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2.
|
-
- HY-B1371A
-
-
- 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-B0166S
-
-
- 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-N0215S12
-
|
L-Phenylalanine-d5
|
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine-d5 is the deuterium labeled L-Phenylalanine. 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 Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.
|
-
- 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 (pHi) 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-N0215S6
-
|
DL-Phenylalanine-d5 hydrochloride
2-Amino-3-phenylpropionic acid-d5 hydrochloride
|
Calcium Channel
iGluR
Endogenous Metabolite
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Metabolic Disease
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DL-Phenylalanine-d5 (2-Amino-3-phenylpropionic acid-d5) hydrochloride is the deuterium labeled DL-Phenylalanine hydrochloride. L-Phenylalanine hydrochloride is an essential amino acid isolated from Escherichia coli. L-Phenylalanine hydrochloride is a α2δ subunit of voltage-dependent Ca + channels antagonist with a Ki of 980 nM. L-phenylalanine hydrochloride is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine hydrochloride is widely used in the production of food flavors and pharmaceuticals.
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- HY-117734
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PYD-106
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iGluR
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Neurological Disease
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PYD-106 is a stereoselective pyrrolidinone (PYD) positive allosteric modulator for GluN2C-containing NMDA receptors. PYD-106 increases opening frequency and open time of single channel currents activated by maximally effective concentrations of agonist but only has modest effects on glutamate and glycine EC50. PYD-106 selectively enhances the responses of diheteromeric GluN1/GluN2C receptors but not triheteromeric GluN1/GluN2A/GluN2C receptors.
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- HY-B1033S
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Metergoline-d5
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5-HT Receptor
Dopamine Receptor
Sodium Channel
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Neurological Disease
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Metergoline-d5 is the deuterium labeled Metergoline. Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki 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.
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- HY-12946
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BI 653048
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Glucocorticoid Receptor
Cytochrome P450
HCV Protease
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Infection
Inflammation/Immunology
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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.
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- HY-105285
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- HY-70057S1
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Safinamide-d4-1
FCE 26743-d4-1; EMD 1195686-d4-1
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Monoamine Oxidase
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Neurological Disease
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Safinamide-d4-1 is 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.
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- HY-12946A
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