Search Result
Results for "
Potassium Channel
" in MedChemExpress (MCE) Product Catalog:
1229
Inhibitors & Agonists
11
Biochemical Assay Reagents
157
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-P5931
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Potassium Channel toxin alpha-KTx 6.13; SPX; α-KTx6.13
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Potassium Channel
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Inflammation/Immunology
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Spinoxin isolated from the venom of scorpion Heterometrus spinifer, is a 34-residue peptide neurotoxin cross-linked by four disulfide bridges. Spinoxin is a potent inhibitor of Kv1.3 potassium channel (IC50 = 63 nM), considering to be valid molecular targets in the diagnostics and therapy of various autoimmune disorders and cancers.
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- HY-U00280
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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-P5825
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- HY-P2949
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Potassium Channel
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Cancer
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Pandinotoxin Kα, isolated from the venom of Pandinus imperator, is the inhibitor of A-type potassium channel.
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- HY-P2785
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- HY-P5177
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- HY-P2710
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Potassium Channel
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Inflammation/Immunology
Neurological Disease
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Noxiustoxin is a toxin from the venom of the Mexican scorpion Centruroides noxius which block voltage-dependent potassium channel (Kv1.3, IC50 = 360 nM), and calcium-activated potassium channel. Noxiustoxin plays an important role in neuroinflammatory disease.
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- HY-P3111
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Potassium Channel
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Others
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Slotoxin, a peptide from Centruroides noxius Hoffmann scorpion venom, blocks high conductance calcium-activated potassium channel, with Kd of 1.5 nM[1].
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- HY-P5925
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SsTx Toxin
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Potassium Channel
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Inflammation/Immunology
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Ssm Spooky Toxin from?Scolopendra mutilans, exhibits lethal toxicity in hematological and respiratory systems by potently inhibiting KCNQ (voltage-gated potassium channel family 7) channels, with IC50? of 2.8 μM, 5.26 μM and 0.1-0.3 M for Kv7.4, Kv1.3, and Shal channel, respectivily. Ssm Spooky Toxin inhibits cytokine generation by specifically acting on the KV1.3 channel in T cells. Ssm Spooky Toxin plays an essential role in the centipede’s circulatory system .
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- HY-15551
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- HY-12520B
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(±)-SKF-38393 hydrochloride; SKF-38393A hydrochloride
|
Dopamine Receptor
Potassium Channel
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Neurological Disease
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(R)-SKF 38393 ((±)-SKF-38393) hydrochloride is a potent and selective D1 dopamine receptor antagonist. (R)-SKF 38393 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channel.
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- HY-P3014
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Potassium Channel
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Others
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Hongotoxin-1, isolated from venom of Centruroides limbatus, is the inhibitor of potassium channel, with IC50 for? Kv1.1, Kv1.2, Kv1.3, and Kv1.6 of 31 pM, 170 pM, 86 pM,and 6000 pM, respectively.
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- HY-100783B
-
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(+)-Bicuculline methobromide; d-Bicuculline methobromide
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GABA Receptor
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Neurological Disease
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Bicuculline methobromide is a selective GABAA Receptor antagonist with an IC50 value of 3 μM. Bicuculline methobromide induces clonic tonic convulsions in mammals and can also be used to block Ca 2+ activated potassium channels. Bicuculline methobromide can be used in studies of epilepsy and other related psychiatric disorders.
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- HY-D0143
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Quinine
2 Publications Verification
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Flavivirus
Parasite
Potassium Channel
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Infection
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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.
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- HY-D0143B
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Parasite
Potassium Channel
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Infection
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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.
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- HY-15208
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HMR 1098
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Potassium Channel
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Neurological Disease
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Clamikalant sodium (HMR 1098) is an ATP-sensitive potassium (KATP) channel blocker. Clamikalant sodium can be used for the research of arrhythmia.
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- HY-44153
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Potassium Channel
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Neurological Disease
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KV2 channel inhibitor-1 is a selective KV2 channel inhibitor with IC50s of 0.2 μM and 0.41 μM for KV2.1 and KV2.2, respectively. KV2 channel inhibitor-1 possesses good selectivity over KV1.2 (IC50>10 μM). KV2 channel inhibitor-1 is >10-fold selective over NaV channels and other KV channels and displays weak activity on CaV channels.
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- HY-49066
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- HY-14290
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P-1134
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Potassium Channel
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Cardiovascular Disease
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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.
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- HY-U00135
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- HY-147556
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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-P5165
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Potassium Channel
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Inflammation/Immunology
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Maurotoxin is a 34-residue and four disulde-bridged toxin that can be isolated from the chactoid scorpion (Scorpio maurus). Maurotoxin inhibits the Shaker potassium channels (ShB) K + current with an IC50 of 2 nM.
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- HY-W278072
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Calcium Channel
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Neurological Disease
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Calcium Channel antagonist 1 is an antagonist of Calcium Channel Calcium Channel antagonist 1 has the potential for the research of neurology disease.
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- HY-156663
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Calcium Channel
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Cancer
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Calcium Channel antagonist 2 (Compound 154) is a calcium channel antagonist (IC50=5-20 μM). Calcium Channel antagonist 2 can be used in study of calcium channel-mediated diseases such as pain and diabetes.
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- HY-75867
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Influenza Virus
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Infection
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M2 ion channel blocker is capable of inhibiting and blocking the activity of M2 ion channel;Antiviral agent.
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- HY-100257
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- HY-146173
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Potassium Channel
Calcium Channel
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Cardiovascular Disease
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KCa1.1 channel activator-1 (compound 1E), a Quercetin hybrid derivative, is a selective vascular KCa1.1 channel channel stimulator. KCa1.1 channel activator-1 also displays CaV1.2 channel blocking activity. KCa1.1 channel activator-1 exhibits weak myorelaxant activity.
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- HY-P5182
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Potassium Channel
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Inflammation/Immunology
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HsTX1, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1, an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM inhibits TEM cell activation and attenuates inflammation in autoimmunity.
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- HY-P1281
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Potassium Channel
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Neurological Disease
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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.
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- HY-15736
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Sodium Channel
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Neurological Disease
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Sodium Channel inhibitor1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment.
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- HY-142723
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Potassium Channel
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Neurological Disease
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KCa2 channel modulator 1 (compound 2o) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 1 potentiates human KCa2.3 channels with an EC50 value of 0.19 μM and 0.99 μM on the rat KCa2.2 channel subtype.
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- HY-108069
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Potassium Channel
nAChR
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Neurological Disease
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Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist.
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- HY-139791
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XEN1101
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Potassium Channel
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Cancer
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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).
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- HY-16952A
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(±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate
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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-156664
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- HY-156669
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- HY-146174
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Potassium Channel
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Cardiovascular Disease
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KCa1.1 channel activator-2 (compound 3F), a Quercetin hybrid derivative, is a selective vascular KCa1.1 channel stimulator. KCa1.1 channel activator-2 exhibits potent myorelaxant activity.
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- HY-142735
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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-100310
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Calcium Channel
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Neurological Disease
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N-type calcium channel blocker-1 is an orally active compound which shows high affinity to functionally block N-type calcium channels with an IC50 of 0.7 μM in the IMR32 assay.
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- HY-109160
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CAD-1883
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Potassium Channel
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Neurological Disease
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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).
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- HY-P5155
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Potassium Channel
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Neurological Disease
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Stromatoxin 1 is an inhibitor of Potassium Channel, a peptide which can be isolated from tarantulas. Stromatoxin 1 selectively inhibits K(V)2.1, K(V)2.2, K(V)4.2, and K(V)2.1/9.3 channels. K(V)2.1 and K(V)2.2, but not K(V)4.2, channel subunits play a key role in opposing both myogenic and neurogenic urinary bladder smooth muscle (UBSM) contractions in rats.
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- HY-N8404
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Potassium Channel
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Inflammation/Immunology
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Chlorahololide C, a lindenane sesquiterpenoid dimer, is isolated from Chloranthus holostegius. Chlorahololide C is a potent and selective potassium channel blocker, with an IC50 of 3.6 μM.
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- HY-108586
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Potassium Channel
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Neurological Disease
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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-110011
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BRL 34915
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Potassium Channel
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Inflammation/Immunology
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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.
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- HY-126653
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- HY-41076
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Calcium Channel
CDK
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Neurological Disease
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Ca 2+ channel agonist 1 is an agonist of N-type Ca 2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
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- HY-A0176
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- HY-155058
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Sodium Channel
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Neurological Disease
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Nav1.3 channel inhibitor 1 (compound 15b) is a state-dependent voltage-gated sodium channel Nav1.3 inhibitor (IC50=20 nM). Nav1.3 channel inhibitor 1 can penetrate the blood-brain barrier and can be used in the research of nervous system diseases.
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- HY-12345
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ML365
3 Publications Verification
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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-A0148
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SKF-102886 free base; WR-171669
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Parasite
Potassium Channel
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Infection
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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-B1500
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- HY-152166
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Sodium Channel
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Neurological Disease
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NaV1.2/1.6 channel blocker-1 is a potent NaV1.2/1.6 channel blocker, with IC50s of 9.8 and 24.4 μM for rNaV1.6 and hNaV1.2, respectively. NaV1.2/1.6 channel blocker-1 can be used for the research of generalized epilepsy.
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- HY-10035
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T-Type calcium Channel inhibitor
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Calcium Channel
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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-P5180
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Sodium Channel
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Neurological Disease
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Jingzhaotoxin-V is a peptide that inhibits potassium currents in Xenopus laevis oocytes with an IC50 value of 604.2 nM. Jingzhaotoxin-V also inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 and 30.2 nM, respectively.
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- HY-B0563A
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Sodium Channel
Potassium Channel
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Neurological Disease
Cardiovascular Disease
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Ropivacaine hydrochloride monohydrate is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is widely used for regional anesthesia and neuropathic pain management in vivo.
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- HY-110358
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Sodium Channel
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Inflammation/Immunology
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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.
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- HY-110358A
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Sodium Channel
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Inflammation/Immunology
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QAQ dichloride 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 dichloride is membrane-impermeant and only infiltrates pain-sensing neurons that express endogenous import channels. QAQ dichloride dichloride acts as a light-sensitive analgesic and can be used for studying of signaling mechanisms in acute and chronic pain.
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- HY-B0563
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Sodium Channel
Potassium Channel
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Neurological Disease
Cardiovascular Disease
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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.
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- HY-B0563B
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Sodium Channel
Potassium Channel
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Neurological Disease
Cardiovascular Disease
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Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is widely used for neuropathic pain management in vivo.
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- HY-147708
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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-B0563BS
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Isotope-Labeled Compounds
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Neurological Disease
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Ropivacaine-d7 hydrochloride is a deuterium labeled Ropivacaine (hydrochloride) (HY-B0563B). Ropivacaine hydrochloride is a potent?sodium channel?blocker and blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is widely used for neuropathic pain?management in vivo.
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- HY-122697
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- HY-50707
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(Rac)-T-Type calcium Channel inhibitor
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Others
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Neurological Disease
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(Rac)-TTA-P2 is the inactive isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease.
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- HY-132201
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Potassium Channel
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Metabolic Disease
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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.
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- HY-153219A
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Potassium Channel
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Endocrinology
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P-CAB agent 2 is a potent and orally active potassium-competitive acid blocker and a gastric acid secretion inhibitor. P-CAB agent 2 inhibits H +/K +-ATPase activity with an IC50 value of <100 nM. P-CAB agent 2 inhibits the hERG potassium channel with an IC50 value of 18.69 M. P-CAB agent 2 shows no acute toxicity and inhibits histamine (HY-B1204)-induced gastric acid secretion.
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- HY-153219
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Potassium Channel
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Endocrinology
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P-CAB agent 2 hydrochloride is a potent and orally active potassium-competitive acid blocker and a gastric acid secretion inhibitor. P-CAB agent 2 hydrochloride inhibits H +/K +-ATPase activity with an IC50 value of <100 nM. P-CAB agent 2 hydrochloride inhibits the hERG potassium channel with an IC50 value of 18.69 M. P-CAB agent 2 hydrochloride shows no acute toxicity and inhibits histamine (HY-B1204)-induced gastric acid secretion.
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- HY-B0563C
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Sodium Channel
Potassium Channel
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Neurological Disease
Cardiovascular Disease
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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.
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- HY-110076
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Potassium Channel
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Others
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VU590 dihydrochloride is a potent and moderately selective ROMK (Kir1.1) inhibitor, with an IC50 of 290 nM. VU590 also inhibits Kir7.1, with an IC50 of 8 μM. VU590 dihydrochloride is not a good probe of ROMK function in the kidney.
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- HY-108595
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Potassium Channel
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Others
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VU590 is a potent and moderately selective ROMK (Kir1.1) inhibitor, with an IC50 of 290 nM. VU590 also inhibits Kir7.1, with an IC50 of 8 μM. VU590 is not a good probe of ROMK function in the kidney.
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- HY-W013727
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Potassium Channel
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Inflammation/Immunology
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UK-78282, a novel piperidine, potent and selective Kv1.3 blocker with an IC50 of 200 nM. UK-78,282 effectively suppresses human T-lymphocyte activation in vitro. UK-78,282 binds to residues at the inner surface of the channel overlapping the site of action of verapamil.
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- HY-W013712
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Potassium Channel
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Neurological Disease
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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.
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- HY-117275
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- HY-117275A
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- HY-18940A
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- HY-P1078
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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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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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FRC-8653
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Calcium Channel
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Cardiovascular Disease
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Cilnidipine is a long-acting, second-generation dihydropyridine Ca 2+-channel blocker on L and N-type Ca 2+ channel. Antihypertensive effects.
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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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- HY-B1221
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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
4 Publications Verification
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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-12949A
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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-105917
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Endovion; NS3728
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Chloride Channel
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Others
|
|
Endovion is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
|
-
- HY-116436
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Clathrodin is a marine alkaloid that can be isolated from sponges of the genus, Agelas. Clathrodin is a modulator of voltage-gated sodium (NaV) channels. Clathrodin is a sodium channel neurotoxin influencing sodium channel ionic conductance.
|
-
- HY-131942
-
-
- HY-P0189
-
-
- HY-101433
-
-
- HY-14256
-
-
- HY-108592
-
|
|
Potassium Channel
|
Neurological Disease
|
|
UCL 2077 is a selective slow-afterhyperpolarization (sAHP) channel blocker (IC50 = 500 nM in hippocampal neurons in culture), having minimal effects on Ca2+ channels, action potentials, input resistance and the medium after hyperpolarization. UCL 2077 is also a subtype-selective blocker of the epilepsy associated KCNQ channels.
|
-
- HY-N6691
-
|
3-Veratroylveracevine
|
Sodium Channel
|
Neurological Disease
|
|
Veratridine (3-Veratroylveracevine) is a plant neurotoxin, a voltage-gated sodium channels (VGSCs) agonist. Veratridine inhibits the peak current of Nav1.7, with an IC50 of 18.39 µM. Veratridine regulates sodium ion channels mainly by activating sodium ion channels, preventing channel inactivation and increasing sodium ion flow.
|
-
- HY-P0189A
-
-
- HY-B1221S1
-
|
|
Isotope-Labeled Compounds
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
|
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 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.
|
-
- HY-P5869
-
|
|
Sodium Channel
Calcium Channel
|
Neurological Disease
|
|
Kurtoxin is a selective Cav3 (T-type) voltage-gated Ca 2+ channel gating inhibitor with a Kd of 15 nM for Cav3.1 (α1G T-type) Ca 2+ channel. Kurtoxin can interact with high affinity with native neuronal high-threshold L-type, N-type, and P-type Ca 2+ channels in central and peripheral neurons. Kurtoxin also shows cross-reactivity with voltage-gated Na + channel.
|
-
- HY-B1221S
-
|
|
Isotope-Labeled Compounds
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
|
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 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.
|
-
- HY-B0545S
-
|
|
TRP Channel
Bacterial
HIV
|
Metabolic Disease
|
|
Probenecid-d14 is the deuterium labeled Probenecid. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels[1][2].
|
-
- HY-P0190A
-
|
|
Potassium Channel
|
Others
|
|
Iberiotoxin (TFA) is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin (TFA) does not block other types of voltage-dependent ion channels.
|
-
- HY-126583
-
|
|
Calcium Channel
|
Cancer
|
|
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.
|
-
- HY-P1221
-
|
|
Sodium Channel
|
Neurological Disease
|
|
ProTx II is a selective blocker of Nav1.7 sodium channels with an IC50 of 0.3 nM, and is at least 100-fold selective for Nav1.7 over other sodium channel subtypes. ProTx-II inhibits sodium channels by decreasing channel conductance and shifting activation to more positive potentials and blocks action potential propagation in nociceptors.
|
-
- HY-17451
-
-
- HY-14183
-
|
RSD1235 hydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na + and atria-preferred K + channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channel wt, Kv1.5 channel I508F, Kv1.5 channel T479A, respectively.
|
-
- HY-P1221A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
ProTx II TFA is a selective blocker of Nav1.7 sodium channels with an IC50 of 0.3 nM, and is at least 100-fold selective for Nav1.7 over other sodium channel subtypes. ProTx-II inhibits sodium channels by decreasing channel conductance and shifting activation to more positive potentials and blocks action potential propagation in nociceptors.
|
-
- HY-15553B
-
|
Ro 40-5967 dihydrochloride hydrate
|
Calcium Channel
|
Cardiovascular Disease
|
|
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.
|
-
- HY-128933
-
|
Adenylyl-imidodiphosphate tetralithium
|
Potassium Channel
|
Metabolic Disease
|
|
AMP-PNP tetralithium (Adenylyl-imidodiphosphate tetralithium) is a non-hydrolysable analogue of ATP and inhibits KATP channels.
|
-
- HY-110153
-
|
|
Potassium Channel
|
Neurological Disease
|
|
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.
|
-
- HY-P1073
-
|
|
Calcium Channel
Sodium Channel
Potassium Channel
|
Cancer
|
|
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.
|
-
- HY-D1368
-
|
|
Fluorescent Dye
|
Others
|
|
BDP FL amine hydrochloride is a borondipyrromethene dye with good water solubility. BDP FL amine hydrochloride can be read on the FAM channel.
|
-
- HY-P2786A
-
-
- HY-12796A
-
|
Vixotrigine hydrochloride; GSK-1014802 hydrochloride; CNV1014802 hydrochloride
|
Sodium Channel
|
Neurological Disease
|
|
Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
|
-
- HY-P10025
-
-
- HY-12796
-
|
Vixotrigine; GSK-1014802; CNV1014802
|
Sodium Channel
|
Neurological Disease
|
|
Raxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
|
-
- HY-119335
-
|
S-2703
|
Sodium Channel
|
Others
|
|
Cyphenothrin (S-2703) is a pyrethroid pesticide. Cyphenothrin acts on the neuromuscular system of insects, intervening in the gating mechanism of sodium channels.
|
-
- HY-135478
-
|
NCC1048
|
Calcium Channel
Sodium Channel
|
Neurological Disease
|
|
LY393615 (NCC1048) is a novel neuronal Ca 2+ (calcium channel) and Na + channel (sodium channel) blocker with IC50s of 1.9 μΜ and 5.2 μΜ for α1A and α1B calcium channel subunits. LY393615 has good brain penetration and neuroprotective effects in models of in cerebral ischemia that can be used for neurological disease research.
|
-
- HY-B0545
-
-
- HY-135412
-
|
|
Sodium Channel
|
Neurological Disease
|
|
N-Methyl Duloxetine hydrochloride is an analgesic. N-Methyl Duloxetine (hydrochloride) elicits both tonic and use-dependent block of neuronal Na + channels.
|
-
- HY-111325
-
Synta66
3 Publications Verification
|
CRAC Channel
|
Neurological Disease
|
|
Synta66 is an inhibitor of store-operated calcium entry channel Orai, which forms the pore of the CRAC channel, and used for the research of neurological disease.
|
-
- HY-100623
-
-
- HY-133910
-
|
|
Sodium Channel
|
Neurological Disease
|
|
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.
|
-
- HY-P5179
-
|
HWTX-I
|
Sodium Channel
Calcium Channel
|
Neurological Disease
|
|
Huwentoxin I (HWTX-I) is a peptide toxin that inhibits voltage-gated sodium channels and N-type calcium channels. Huwentoxin I inhibits sodium channels in rat hippocampus and cockroach dorsal unpaired median (DUM) neurons with IC50 values of 66.1 and 4.80 nM, respectively.
|
-
- HY-B0341
-
|
SG-75
|
Potassium Channel
|
Cardiovascular Disease
|
|
Nicorandil (SG-75) is a potent potassium channel activator and targets vascular nucleoside diphosphate-dependent K + channels and cardiac ATP-sensitive K + channels (KATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases.
|
-
- HY-P0190
-
|
|
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.
|
-
- HY-101942
-
|
CM-4620
|
CRAC Channel
|
Neurological Disease
|
|
Zegocractin (CM-4620) is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC50s of 119 nM and 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.
|
-
- HY-N2077
-
|
|
Calcium Channel
|
Metabolic Disease
|
|
Heteroclitin D is a lignin from Kadsura medicinal plants with anti-liqid peroxidation. Heteroclitin D inhibits L-type calcium channels.
|
-
- HY-101809A
-
|
|
iGluR
|
Cardiovascular Disease
|
|
CNS-5161 is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
|
-
- HY-106439
-
|
ABIO-08/01
|
Chloride Channel
|
Neurological Disease
|
|
BTG 1640 (ABIO-08/01) is a potent anxiolytic isoxazoline. BTG 1640 is a selective inhibitor of GABA- and glutamate-gated chloride channels.
|
-
- HY-101809
-
|
CNS 5161A
|
iGluR
|
Cardiovascular Disease
|
|
CNS-5161 hydrochloride is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
|
-
- HY-P1424
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Lei-Dab7 is a potent and selective SK2 (KCa2.2) channels blocker with a Kd of 3.8 nM. Lei-Dab7 shows low or no activity on KCa1, KCa3, Kv and Kir2.1 channels.
|
-
- HY-147691
-
|
|
Glutathione Peroxidase
Potassium Channel
|
Inflammation/Immunology
|
|
MPO-IN-5 (compound 1) is a potent, irreversible MPO (myeloperoxidase) inhibitor. MPO-IN-5 inhibits MPO peroxidation and hERG binding, with IC50 values of 0.22 and 2.8 μM, respectively. MPO-IN-5 shows rapid kinetics of inhibition, with enzyme inactivation rate (kinact/Ki) of 23000 M −1s −1.
|
-
- HY-121520
-
-
- HY-100345
-
|
|
TRP Channel
|
Cancer
Neurological Disease
|
|
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).
|
-
- HY-P1219
-
|
β-TRTX-Cj1α
|
Sodium Channel
|
Neurological Disease
|
|
Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype.
|
-
- HY-108584
-
|
BMS-204352
|
Potassium Channel
|
Neurological Disease
|
|
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
|
-
- HY-101383
-
|
|
Sodium Channel
|
Neurological Disease
|
|
PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.
|
-
- HY-118387
-
|
|
Potassium Channel
|
Neurological Disease
|
|
AVE-0118 is a nonselective Kv1.5 blocker with an IC50 of 1.1 μM. AVE-0118 is a multichannel inhibitor with weak, micromolar activity against Kv1.5 and other ion channels. It is inactive against IKs, IKATP, and L-type Ca+ channels.
|
-
- HY-151891
-
|
|
Potassium Channel
|
Cancer
|
|
TASK-1-IN-1 is a potent and selective TASK-1 (Potassium Channel) inhibitor with an IC50 of 148 nM. TASK-1-IN-1 shows a reduced inhibition of TASK-3 channels (IC50 of 1750 nM) and not a significant effect on other K+ channels. TASK-1-IN-1 has anticancer effects.
|
-
- HY-P5154
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Tamapin is a venom peptide, targeting to small conductance Ca(2+)-activated K(+) (SK) channels. Tamapin is a selctive blocker of SK2 (Potassium Channel). Tamapin inhibits SK channel-mediated currents in pyramidal neurons of the hippocampus. Tamapin can be isolated from the Indian red scorpion (Mesobuthus tamulus).
|
-
- HY-N1847
-
|
|
Sodium Channel
|
Neurological Disease
|
|
3'-Methoxydaidzein is a isoflavone and a Sodium Channel inhibitor. 3'-Methoxydaidzein inhibits subtypes NaV1.7, NaV1.8 and NaV1.3 with IC50 of 181 nM, 397 nM, and 505 nM, respectively. 3'-Methoxydaidzein exerts analgesic activity by inhibiting voltage-gated sodium channels.
|
-
- HY-101360
-
|
1-Ethyl-2-benzimidazolinone
|
Potassium Channel
|
Neurological Disease
|
|
1-EBIO is an activator of Ca 2+ sensitive K + channels. 1-EBIO is used to study the role of K + channels in diverse physiological functions.
|
-
- HY-B1704
-
-
- HY-B1704A
-
|
|
Monoamine Transporter
Sodium Channel
|
Neurological Disease
|
|
Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.
|
-
- HY-136232
-
|
|
Others
|
Neurological Disease
|
|
PSEM 308 hydrochloride is a pharmacologically selective actuator module (PSAM) agonist. PSEM 308 Activates PSAML141F-GlyR chimeric ion channels.
|
-
- HY-122376
-
|
D-Trans-Allethrin; Esbiol
|
Sodium Channel
|
Neurological Disease
|
|
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.
|
-
- HY-B0262S
-
|
|
Sodium Channel
|
Metabolic Disease
|
|
Methocarbamol-d5 is deuterium labeled Methocarbamol. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel[1].
|
-
- HY-B1798A
-
|
|
Sodium Channel
|
Inflammation/Immunology
|
|
Tocainide hydrochloride is a sodium channel blocker, it blocks the sodium channels in the pain-producing foci in the nerve membranes. Tocainide hydrochloride is a primary amine analog of lidocaine, can be used for the treatment of tinnitus.
|
-
- HY-101674
-
-
- HY-103371
-
DCPIB
4 Publications Verification
|
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.
|
-
- HY-108594
-
|
|
Potassium Channel
|
Metabolic Disease
|
|
PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability.
|
-
- HY-101069
-
-
- HY-P2270
-
|
|
Fluorescent Dye
Arp2/3 Complex
|
Others
|
|
Phalloidin-TRITC is a fluorescein derivative of Phalloidin, which can specifically label myof lin and display red fluorescence when labeled and can be observed using Tesred channels.
|
-
- HY-N2338
-
|
Cholesteryl myristate; Cholesteryl tetradecanoate
|
nAChR
GABA Receptor
Potassium Channel
Endogenous Metabolite
|
Cancer
|
|
Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.
|
-
- HY-13103
-
|
|
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.
|
-
- HY-136564A
-
|
|
Potassium Channel
|
Neurological Disease
|
|
DAD is a type of ion channel blocker that blocks voltage-gated potassium channels. DAD is a third-generation photoswitch that responds to visible light. DAD has the potential for restoring visual function.
|
-
- HY-P5871
-
|
JzTx-XII
|
Potassium Channel
|
Others
|
|
Jingzhaotoxin-XII (JzTx-XII) is a specific Kv4.1 channel inhibitor with an IC50 of 0.363 μM. Jingzhaotoxin-XII interacts with the channels by modifying the gating behavior.
|
-
- HY-B1798
-
|
|
Sodium Channel
|
Cardiovascular Disease
|
|
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.
|
-
- HY-14462
-
|
39-1B4
|
Calcium Channel
|
Cardiovascular Disease
|
|
NP118809 is a potent N-type calcium channel blocker, with an IC50 of 0.11 μM; also less potently inhibits L-type calcium channel with an IC50 of 12.2 μM.
|
-
- HY-P5172
-
|
|
Sodium Channel
|
Neurological Disease
|
|
MitTx-alpha is a subunit of MitTx. MitTx is a potent, persistent, and selective agonist for acid-sensing ion channels (ASICs). MitTx is highly selective for the ASIC1 subtype at neutral pH; under more acidic conditions (pH<6.5), MitTx massively potentiates (>100-fold) proton-evoked activation of ASIC2a channels.
|
-
- HY-P5154A
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Tamapin TFA is a venom peptide, targeting to small conductance Ca(2+)-activated K(+) (SK) channels. Tamapin TFA is a selctive blocker of SK2 (Potassium Channel). Tamapin TFA inhibits SK channel-mediated currents in pyramidal neurons of the hippocampus. Tamapin TFA can be isolated from the Indian red scorpion (Mesobuthus tamulus).
|
-
- HY-18662
-
|
|
TRP Channel
|
Cancer
Neurological Disease
|
|
RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels.
|
-
- HY-P5771
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Jingzhaotoxin-IX, a C-terminally amidated peptide composed of 35 amino acid residues, is a neurotoxin. Jingzhaotoxin-IX inhibits voltage-gated sodium channels (both tetrodotoxin-resistant and tetrodotoxin-sensitive isoforms) and Kv2.1 channel. Jingzhaotoxin-IX has no effect on delayed rectifier potassium channel Kv1.1, 1.2 and 1.3.
|
-
- HY-B0246
-
-
- HY-B0984
-
-
- HY-101621
-
-
- HY-143202
-
|
|
Biochemical Assay Reagents
|
Others
|
|
DPhPC is a phospholipid used to synthesize bilayer vesicles. DPhPC bilayers do not permit ions to leak in the absence of a pore/ion channel, which can be used for studies on channel proteins.
|
-
- HY-12515A
-
|
YC-93
|
Calcium Channel
Autophagy
|
Neurological Disease
Cancer
|
|
Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.
|
-
- HY-101428
-
|
|
Calcium Channel
|
Neurological Disease
|
|
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.
|
-
- HY-108593
-
|
BMS-A
|
Potassium Channel
|
Neurological Disease
|
|
BMS 191011 (BMS-A) is a potent BKCa channel opener (large-conductance Ca 2+-activated potassium channel). BMS-191011 shows neuroprotective activities in rodent models of stroke.
|
-
- HY-P5140
-
|
|
Calcium Channel
|
Metabolic Disease
|
|
ω-Tbo-IT1 is a peptide toxin that can be isolated from the venom of Tibellus oblongus.ω-Tbo-IT1 is an inhibitor of insect calcium channel.
|
-
- HY-16126
-
|
L-651582; CAI
|
Calcium Channel
|
Cancer
Inflammation/Immunology
|
|
Carboxyamidotriazole (L-651582) is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole shows anti-tumor, anti-inflammatory and antiangiogenic effects.
|
-
- HY-14834A
-
-
- HY-101012
-
-
- HY-105117
-
-
- HY-12545
-
|
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
-
|
|
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-U00201
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
KRN4884 is a K + channel opener. In the presence of intracellular ATP (1 mM), KRN4884 (0.1-3 μM) activates KATP channels in a concentration-dependent manner (EC50=0.55 μM).
|
-
- HY-136564
-
|
|
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-B0834
-
|
(±)-Indoxacarb; DPX-JW062
|
Sodium Channel
|
Neurological Disease
|
|
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.
|
-
- HY-135407S
-
|
|
Drug Metabolite
|
Neurological Disease
|
|
N-Desethyl Oxybutynin-d5 (hydrochloride) is deuterium labeled N-Desethyl Oxybutynin hydrochloride. N-Desethyl Oxybutynin is the the active metabolite Oxybutynin. Oxybutynin is an anticholinergic agent that inhibits voltage-dependent K+ channels[1].
|
-
- HY-12515
-
|
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-B0341S
-
|
|
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[1][2][3].
|
-
- HY-152103
-
|
|
Fluorescent Dye
|
Others
|
|
CB2-H is a dual-channel fluorescent probe for the simultaneous detection of HOCl and ONOO -. CB2-H enables the concurrent detection of HOCl and ONOO - at two independent channels without spectral cross-interference and can be applied for dual-channel fluorescence imaging of endogenously produced HOCl and ONOO - in living cells and zebrafish under different stimulants.
|
-
- HY-112075
-
|
|
Potassium Channel
Calcium Channel
|
Cardiovascular Disease
|
|
Lidoflazine is a high affinity blocker of the HERG (human ether-a-go-go-related gene) K + channel. Lidoflazine is an antianginal calcium channel blocker that carries a significant risk of QT interval prolongation and ventricular arrhythmia.
|
-
- HY-P3269
-
|
|
Calcium Channel
|
Others
|
|
Calciseptine, a natural?neurotoxin?isolated from the black mamba Dendroaspis p. polylepis venom. Calciseptine consists of 60 amino acids with four disulfide bonds. Calciseptine specifically blocks L-type?calcium channel[1].
|
-
- HY-B0545R
-
|
|
TRP Channel
Bacterial
HIV
|
Metabolic Disease
Cancer
|
|
Probenecid (Standard) is the analytical standard of Probenecid. This product is intended for research and analytical applications. Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels.
|
-
- HY-N7875
-
|
|
Others
|
Others
|
|
Celangulin is an insecticidal component isolated from Celastrus angulatus. Celangulin activates the calcium channel on the plasma membrane with increasing the intracellular Ca 2+ after influx from the external. Celangulin activates the calcium channel in the ER.
|
-
- HY-P5917
-
|
Vaejovis mexicanus peptide 24
|
Potassium Channel
|
Others
|
|
Vm24-toxin is a toxin peptide that can be isolated from the Mexican scorpion Vaejovis mexicanus smithy. Vm24-toxin is an inhibitor of Kv1.3 potassium channel.
|
-
- HY-W011509
-
|
|
Potassium Channel
|
Neurological Disease
|
|
CyPPA is a positive modulator of hSK3 and hSK2, with EC50 values of 14 μM and 5.6 μM, repectively. CyPPA is inactive on both hSK1 and hIK channels[1]
|
-
- HY-P5142
-
|
ω-ACTX-Hv1; ω-Atracotoxin-HV1
|
Calcium Channel
|
Neurological Disease
|
|
ω-Hexatoxin-Hv1a is a neurotoxin that can be isolated from the venom spider (Hadronyche versuta).ω-Hexatoxin-Hv1a blocks voltage-gated calcium channels.
|
-
- HY-112705
-
|
|
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
-
|
|
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
-
|
|
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-U00218
-
-
- HY-B0768A
-
-
- HY-B0567
-
-
- HY-101740
-
-
- HY-B0419
-
-
- HY-16915
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivation of hERG1 channels. RPR260243-modified HERG currents are inhibited by Dofetilide (IC50=58 nM). RPR260243 displays no activator-like effects on other voltage-dependent ion channels, including the closely related ERG3 K+ channel. RPR-260243 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-110105
-
|
|
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-P1080A
-
|
|
Calcium Channel
|
Neurological Disease
|
|
ω-Agatoxin IVA TFA 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 TFA (IC50, 30-225 nM) inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA TFA also blocks the high potassium-induced release of serotonin and norepinephrine. ω-Agatoxin IVA TFA has no effect on L-type or N-type calcium channels.
|
-
- HY-101843
-
-
- HY-108582
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
Y-27152, a proagent 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
-
|
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-B1378S
-
|
|
Isotope-Labeled Compounds
Calcium Channel
|
Neurological Disease
|
|
Ethosuximide-d3 is the deuterium labeled Ethosuximide. Ethosuximide, a widely prescribed anti-epileptic agent, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel[1][2].
|
-
- HY-N3729
-
|
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-W415121
-
|
|
iGluR
Sodium Channel
Calcium Channel
Potassium Channel
|
Cancer
Neurological Disease
|
|
Bupivacaine hydrochloride monohydrate is a NMDA receptor inhibitor. Bupivacaine hydrochloride monohydrate can block sodium, L-calcium, and potassium channels. Bupivacaine hydrochloride monohydrate potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine hydrochloride monohydrate can be used for the research of chronic pain.
|
-
- HY-P5793
-
-
- HY-14255
-
-
- HY-U00173
-
-
- HY-14290A
-
|
P-1134 monohydrate
|
Potassium Channel
|
Others
|
|
Pinacidil (P-1134) monohydrate, an antihypertensive agent, is a potassium channel activator.
|
-
- HY-103315
-
-
- HY-P3065
-
|
|
Calcium Channel
|
Neurological Disease
|
|
Calcicludine is a protein toxin from the venom of the green mamba Dendroaspis angusticeps that inhibits high-voltage-activated calcium channel, especially L-type calcium channel with the IC50 of 88 nM. Calcicludine has role in excitatory synaptic transmission.
|
-
- HY-15553A
-
|
Ro 40-5967 dihydrochloride
|
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Mibefradil dihydrochloride (Ro 40-5967 dihydrochloride) is a calcium channel blocker with moderate selectivity for T-type Ca 2+ channels (IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively).
|
-
- HY-P3055
-
|
DTX-I
|
Potassium Channel
|
Cancer
Neurological Disease
|
|
Dendrotoxin-I is a potent K + channels blocker and targets voltage-gated potassium channel subunits KV1.1 and KV1.2. Dendrotoxin-I is a neurotoxin isolated from thevenom of Dendroaspis snakes.
|
-
- HY-B0285
-
-
- HY-B0285A
-
-
- HY-B0480A
-
-
- HY-P1079
-
|
|
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
-
|
|
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
-
|
(±)-Brompheniramine maleate
|
Histamine Receptor
mAChR
Potassium Channel
Sodium Channel
Calcium Channel
|
Endocrinology
Inflammation/Immunology
Neurological Disease
|
|
Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research.
|
-
- HY-P1410A
-
|
|
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-P5804
-
|
|
Calcium Channel
|
Neurological Disease
|
|
ω-Conotoxin CVIF is a selective Cav2.2 channel inhibitor with an IC50 of 34.3 nM in rat isolated DRG neurons. ω-Conotoxin CVIF block of Cav2.2 channels is weakly reversible.
|
-
- HY-15553
-
|
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-N2433
-
|
|
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-12596
-
|
|
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
-
|
|
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
-
|
|
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
|
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-116448
-
-
- HY-P5943
-
-
- HY-B0401
-
-
- HY-P5942
-
-
- HY-B1109
-
-
- HY-B2136
-
-
- HY-100572
-
-
- HY-U00236
-
-
- HY-N2164
-
-
- HY-P5184
-
|
HNTX-IV
|
Sodium Channel
|
Neurological Disease
|
|
Hainantoxin-IV is a specific antagonist of Sodium Channel, targeting to tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels. His28 and Lys32 are the key resiudes of Hainantoxin-IV for binding with target, while Hainantoxin-IV adopts an inhibitor cystine knot motif.
|
-
- HY-113147A
-
|
|
Potassium Channel
Endogenous Metabolite
|
Metabolic Disease
Cardiovascular Disease
|
|
L-Palmitoylcarnitine chloride, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia. L-Palmitoylcarnitine chloride inhibits KATP channel activity, without affecting the single channel conductance, through interaction with Kir6.2.
|
-
- HY-W032013
-
-
- HY-B0317
-
|
|
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
-
|
|
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)-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
-
-
- HY-P5788
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Hemitoxin, a scorpion-venom peptide, is a K + channel blocker. Hemitoxin blocks rat Kv1.1, Kv1.2 and Kv1.3 channels expressed in Xenopus oocytes with IC50 values of 13 nM, 16 nM and 2 nM, respectively.
|
-
- HY-B0285B
-
|
MK-870 hydrochloride dihydrate
|
Sodium Channel
Apoptosis
TRP Channel
|
Metabolic Disease
Cardiovascular Disease
|
|
Amiloride hydrochloride dihydrate (MK-870 hydrochloride dihydrate) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride dihydrate is a blocker of polycystin-2 (PC2; TRPP2) channel.
|
-
- HY-12515AS
-
|
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[1].
|
-
- HY-107756
-
-
- HY-12507
-
-
- HY-N3463
-
-
- HY-P0191
-
-
- HY-P0163
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Gramicidin is an antimicrobial peptide assembling as channels in membranes and increasing their permeability towards cations.
|
-
- HY-109077
-
-
- HY-U00044
-
-
- HY-12778
-
-
- HY-14284
-
-
- HY-14656
-
-
- HY-B1448
-
-
- HY-113147B
-
|
|
Endogenous Metabolite
Potassium Channel
|
Metabolic Disease
Cardiovascular Disease
|
|
L-Palmitoylcarnitine TFA, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia. L-Palmitoylcarnitine TFA inhibits KATP channel activity, without affecting the single channel conductance, through interaction with Kir6.2.
|
-
- HY-15707
-
|
|
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
-
|
|
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
-
|
|
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-149944
-
|
|
Sodium Channel
|
Inflammation/Immunology
|
|
Analgesic agent-2 is a selective and orally active NaV1.8 Channel inhibitor, with an IC50 of 50.18 nM in HEK293 cells stably expressing human NaV1.8 channel. Analgesic agent-2 has analgesic activity.
|
-
- HY-P5160
-
|
PhlTx1
|
Sodium Channel
|
Inflammation/Immunology
|
|
Phlotoxin-1 (PhlTx1) is a 34-amino acid and 3-disulfide bridge peptide. Phlotoxin-1 can be isolated from Phlogiellus genus spider. Phlotoxin-1 is an antinociceptive agent by inhibiting NaV1.7 channel.
|
-
- HY-P1427
-
|
|
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
-
|
|
Flavivirus
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-B0262
-
|
|
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-D1528
-
-
- HY-N12093
-
-
- HY-B0612D
-
-
- HY-14657
-
-
- HY-B0552A
-
|
Cinchocaine hydrochloride
|
Sodium Channel
|
Neurological Disease
|
|
Dibucaine hydrochloride (Cinchocaine hydrochloride) is a sodium channel inhibitor. Dibucaine hydrochloride is a potent SChE inhibitor.
|
-
- HY-108505
-
-
- HY-B0612C
-
|
|
Calcium Channel
|
Others
|
|
(R)-Lercanidipine is the R-enantiomer of Lercanidipine. (R)-lercanidipine is a calcium channel blocker.
|
-
- HY-14187
-
-
- HY-156335
-
|
VU245
|
Others
|
Others
|
|
VU0531245 is a SLACK channel inhibitor (IC50: 2.1 μM).
|
-
- HY-U00086
-
-
- HY-U00026
-
-
- HY-P0191A
-
-
- HY-B0552
-
-
- HY-B0405S
-
-
- HY-12515C
-
|
(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
-
|
ACA
|
Phospholipase
TRP Channel
|
Cardiovascular Disease
|
|
N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker. N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia.
|
-
- HY-B0317B
-
|
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-116838
-
|
|
Bacterial
|
Infection
|
|
TAM-16 is a potent and orally active polyketide synthase 13 (Pks13) inhibitor with an IC50 value of 0.32 μM. TAM-16 has promising activity against Mycobacterium tuberculosis. TAM-16 inhibits hERG cardiac ion channel.
|
-
- HY-B0151
-
|
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
-
|
|
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-D0143A
-
|
|
Flavivirus
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-107031
-
|
19560 RP
|
iGluR
|
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
-
|
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-B1090S
-
-
- HY-B1140
-
-
- HY-B0612E
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
(S)-Lercanidipine hydrochloride is the S-enantiomer of Lercanidipine hydrochloride. (S)-lercanidipine hydrochloride is a potent calcium channel blocker.
|
-
- HY-B0284
-
-
- HY-P5887
-
-
- HY-107319
-
-
- HY-U00212
-
-
- HY-B0284S
-
-
- HY-16723
-
-
- HY-137148
-
|
|
Others
|
Cancer
|
|
DIOA is a potent acid-sensitive outwardly rectifying (ASOR) anion channel antagonist.
|
-
- HY-101350
-
-
- HY-N1378
-
-
- HY-B0246S1
-
-
- HY-145558
-
-
- HY-P1440A
-
|
|
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-P5868
-
|
|
Sodium Channel
|
Neurological Disease
|
|
mHuwentoxin-IV is a naturally modified Huwentoxin-IV (HY-P1220). mHuwentoxin-IV inhibits tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels of dorsal root ganglion neurons with an IC50 of 54.16 nM. mHuwentoxin-IV inhibition of tetrodotoxin-sensitive sodium channels is not reversed by strong depolarization voltages.
|
-
- HY-W009724
-
|
2-APB
|
Calcium Channel
TRP Channel
|
Others
|
|
2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R. 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca 2+ (SOC) channel and activates some TRP channels (V1, V2 and V3).
|
-
- HY-136909
-
|
|
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
-
|
|
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
-
|
|
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
-
|
|
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-B0285AR
-
|
MK-870 hydrochloride (Standard)
|
Sodium Channel
TRP Channel
Apoptosis
|
Metabolic Disease
Cardiovascular Disease
|
|
Amiloride (hydrochloride) (Standard) is the analytical standard of Amiloride (hydrochloride). This product is intended for research and analytical applications. Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride is a blocker of polycystin-2 (PC2; TRPP2) channel.
|
-
- HY-B0433B
-
|
|
Flavivirus
Parasite
Potassium Channel
|
Infection
|
|
Quinine hemisulfate is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine hemisulfate 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-16125
-
|
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
-
|
|
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
-
|
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
-
|
|
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-103309A
-
|
|
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
-
|
|
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
-
|
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
-
|
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-N0172
-
-
- HY-148800
-
-
- HY-B0023
-
-
- HY-12502B
-
-
- HY-12502
-
-
- HY-101096
-
-
- HY-15376
-
|
HP 749 free base
|
Adrenergic Receptor
|
Neurological Disease
|
|
Besipirdine is a non-receptor-dependent cholinomimetic agent with noradrenergic activity. Besipirdine inhibits voltage-dependent sodium and potassium channels.
|
-
- HY-19721
-
-
- HY-17001A
-
-
- HY-B0023S
-
-
- HY-101616
-
-
- HY-17412A
-
-
- HY-17412
-
-
- HY-P1441
-
|
|
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
-
|
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
-
|
|
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[1][2][3].
|
-
- HY-B0317AS
-
|
|
Isotope-Labeled Compounds
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[1][2][3].
|
-
- HY-50694
-
|
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
-
|
|
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-P5862
-
|
Mu-Conotoxin BuIIIB
|
Sodium Channel
|
Neurological Disease
|
|
μ-Conotoxin BuIIIB (Mu-Conotoxin BuIIIB) is a mammalian neuronal voltage-gated sodium channel (VGSC) blocker. μ-Conotoxin BuIIIB can be obtained from the venom of Cone snails and is a probe for ion channel function research. μ-Conotoxin BuIIIB can be used in the study of neurological diseases such as pain.
|
-
- HY-113147AS
-
|
|
Potassium Channel
Endogenous Metabolite
|
Metabolic Disease
Cardiovascular Disease
|
|
L-Palmitoylcarnitine-d3 (hydrochloride) is the deuterium labeled L-Palmitoylcarnitine hydrochloride. L-Palmitoylcarnitine hydrochloride, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia. L-Palmitoylcarnitine hydrochloride inhibits KATP channel activity, without affecting the single channel conductance, through interaction with Kir6.2[1].
|
-
- HY-139904
-
|
|
TRP Channel
|
Others
|
|
TRPA1 Antagonist 3 is a photoswitchable TRPA1 agonist that enables optical control of the TRPA1 channel.
|
-
- HY-16973
-
|
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-P5336
-
-
- HY-17436
-
-
- HY-N7511
-
-
- HY-W016498
-
-
- HY-133715
-
|
SUN 1165 free base; Pilzicainide
|
Sodium Channel
|
Cardiovascular Disease
|
|
Pilsicainide (SUN 1165 free acid) is a potent sodium channel blocker and potent class Ic antiarrhythmic agent.
|
-
- HY-128696
-
|
Amlodipine aspartate
|
Drug Metabolite
|
Cardiovascular Disease
|
|
Amlodipine aspartic acid impurity is the impurity of Amlodipine aspartic acid. Amlodipine aspartic acid is a calcium channel blocker with antihypertensive and antianginal properties.
|
-
- HY-12082A
-
|
|
Potassium Channel
Parasite
|
Infection
|
|
GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization with an IC50 of 7.5 μM.
|
-
- HY-132818
-
|
|
Sodium Channel
|
Others
|
|
Idrevloride, an epithelial sodium channel (ENaC) inhibitor (WO2016133967), can be used for the research of skin disorders.
|
-
- HY-142240
-
-
- HY-B0151S1
-
|
3β-Hydroxy-5-pregnen-20-one-13C2,d2
|
Isotope-Labeled Compounds
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[1][2][3][4].
|
-
- HY-B0151S
-
|
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[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
|
-
- HY-10035A
-
|
|
Others
|
Neurological Disease
|
|
(R)-TTA-P2 is the inactive isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease.
|
-
- HY-B0151S2
-
|
3β-Hydroxy-5-pregnen-20-one-d4-1
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone-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[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
|
-
- HY-B0402S
-
|
1-Adamantanamine-d15; 1-Aminoadamantane-d15
|
Influenza Virus
Orthopoxvirus
SARS-CoV
Apoptosis
|
Cancer
Infection
Neurological Disease
|
|
Amantadine-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[1][2].
|
-
- HY-B0285AS
-
|
MK-870-15N3 hydrochloride
|
Apoptosis
TRP Channel
Sodium Channel
|
|
|
Amiloride- 15N3 (hydrochloride) is the 15N labeled Amiloride hydrochloride[1]. Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC[2]) and urokinase-type plasminogen activator receptor (uTPA[3]). Amiloride hydrochloride is a blocker of polycystin-2 (PC2;TRPP2[4]) channel.
|
-
- HY-17398
-
|
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-P5802
-
|
|
Calcium Channel
|
Neurological Disease
|
|
ω-Conotoxin FVIA is an N-type Ca 2+channel (Ca v 2.2)
inhibitor. ω-Conotoxin FVIA reduces mechanical and thermal pain abnormalities
in a rat model of caudal nerve injury. ω-Conotoxin FVIA can be used in the
study of highly effective pain relievers with low side effects
.
|
-
- HY-N7395A
-
-
- HY-17611
-
|
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-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-B0317S1
-
|
|
Isotope-Labeled Compounds
|
Cancer
|
|
Amlodipine-d4 is a deuterium labeled Amlodipine (HY-B0317). 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-101245
-
|
SUN-1165; Pilzicainide(hydrochloride)
|
Sodium Channel
|
Cardiovascular Disease
|
|
Pilsicainide hydrochloride (SUN-1165) is an orally active sodium channel blocker and potent class Ic antiarrhythmic agent.
|
-
- HY-12542A
-
|
Dantrolene sodium hydrate
|
Calcium Channel
Autophagy
|
Others
|
|
Dantrolene sodium salt hydrate is a calcium channel protein inhibitor that inhibits the release of calcium ions from the sarcoplasm. Dantrolene sodium salt hydrate is a skeletal muscle relaxant.
|
-
- HY-18996
-
-
- HY-P5821
-
-
- HY-118172
-
-
- HY-101621S
-
-
- HY-12693A
-
|
(Rac)-IAA-94
|
Others
|
Others
|
|
(Rac)-Methylindazone ((Rac)-IAA-94) is the racemate of Methylindazone. Methylindazone is a potent CLIC1 channel blocker.
|
-
- HY-107349
-
-
- HY-P0173A
-
|
|
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
-
|
NZ-105 hydrochloride monoethanolate
|
Calcium Channel
|
Cardiovascular Disease
|
|
Efonidipine hydrochloride monoethanolate (NZ-105 hydrochloride monoethanolate) is a dual T-type and L-type calcium channel blocker (CCB).
|
-
- HY-110189S1
-
|
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[1][2]. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
|
-
- HY-103309S
-
|
|
Calcium Channel
|
Neurological Disease
|
|
ML218-d9 is the deuterium labeled ML218. ML218 is a potent, selective and orally active T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier[1].
|
-
- HY-P5174
-
|
|
Sodium Channel
|
Neurological Disease
|
|
MitTx is a complex formed by MitTx-α and MitTx-β. MitTx is an ASIC1 channel activator with EC50 values of 9.4 and 23 nM for ASIC1a and ASIC1b isoforms, respectively. MitTx is highly selective for ASIC1 isoforms at neutral pH. Under acidic conditions, MitTx greatly enhances proton-evoked ASIC2a channel activation.
|
-
- HY-108425A
-
|
|
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-W032013S
-
|
Octanol-d17
|
Calcium Channel
Endogenous Metabolite
|
|
|
1-Octanol-d17 is the deuterium labeled 1-Octanol[1]. 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents[2]. 1-Octanol is a highly attractive biofuel with diesel-like properties[3].
|
-
- HY-B0317S
-
|
|
Isotope-Labeled Compounds
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[1][2][3].
|
-
- HY-W010668
-
|
|
Flavivirus
Parasite
Potassium Channel
|
Others
|
|
Quinine sulfate hydrate (2:1:4) is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine sulfate hydrate (2:1:4) 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-N6778
-
|
|
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-111013
-
|
|
Others
|
Cardiovascular Disease
|
|
VK-II-86 is a Carvedilol (HY-B0006) analogue lacking antagonist activity at β-adrenoceptors, in hypokalaemia. VK-II-86 prevents hypokalaemia-induced ventricular arrhythmia through multi-channel effects. VK-II-86 prevents all hypokalaemia-induced changes in ion channel activity and oxidative stress.
|
-
- HY-111747
-
|
|
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-W032013S1
-
|
Octanol-d2
|
Calcium Channel
Endogenous Metabolite
|
|
|
1-Octanol-d2 is the deuterium labeled 1-Octanol[1]. 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents[2]. 1-Octanol is a highly attractive biofuel with diesel-like properties[3].
|
-
- HY-130354
-
|
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
-
|
|
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
-
|
|
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-B0317BS
-
|
Amlodipine benzenesulfonate-d4 besylate
|
Isotope-Labeled Compounds
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Amlodipine-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[1][2][3].
|
-
- HY-N8264
-
|
|
TRP Channel
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
Moringin is a potent and selective TRPA1 ion channel natural agonist with an EC50 of 3.14 μM. Moringin does not activate or activates very weakly the vanilloids somatosensory channels TRPV1, TRPV2, TRPV3 and TRPV4, and the melastatin cooling receptor TRPM8. Moringin has hypoglycemic, antimicrobial, anti-inflammatory, anticancer and neuroprotection activities.
|
-
- HY-150539
-
-
- HY-101346
-
-
- HY-A0093
-
|
KOE-1173 hydrochloride
|
Sodium Channel
|
Cardiovascular Disease
|
|
Mexiletine hydrochloride (KOE-1173 hydrochloride), a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker.
|
-
- HY-B0246S
-
-
- HY-B0401S
-
-
- HY-120546
-
|
Z944
|
Calcium Channel
|
Neurological Disease
|
|
Ulixacaltamide (Z944) is an orally active T-type calcium channel antagonist that rescues impairments in crossmodal and visual recognition memory.
|
-
- HY-B0887
-
|
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-P5805
-
-
- HY-116448S
-
-
- HY-147423
-
-
- HY-B0682S2
-
|
|
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[1][2].
|
-
- HY-122560A
-
|
|
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
-
|
|
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
-
|
|
Isotope-Labeled Compounds
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[1][2][3].
|
-
- HY-15292
-
S107
1 Publications Verification
|
Others
|
Cardiovascular Disease
|
|
S107 is an orally available, blood brain barrier-permeable compound, which stabilizes RyR2 channels by enhancing the binding of calstabin 2 to the mutant Ryr2-R2474S channel. S107 inhibits Ca 2+ leakage from the sarcoplasmic reticulum (SR) and prevents cardiac arrhythmias and raises the seizure threshold.
|
-
- HY-102070
-
|
|
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
-
|
|
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-N0239
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Bulleyaconitine A is an analgesic and antiinflammatory drug isolated from Aconitum plants; has several potential targets, including voltage-gated Na+ channels.
|
-
- HY-109077S
-
-
- HY-N3990
-
|
(-)-Hardwikiic acid
|
Sodium Channel
|
Infection
Neurological Disease
|
|
Hardwickiic acid ((-)-Hardwikiic acid) is an antinociceptive compound that blocks Tetrodotoxin-sensitive voltage-dependent sodium channels. Hardwickiic acid shows insecticidal activity.
|
-
- HY-B0401S1
-
-
- HY-14284S
-
-
- HY-14744
-
|
(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-156596A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Aneratrigine (hydrochloride) is a sodium channel protein type 9 subunit alpha blocker. Aneratrigine (hydrochloride) can be used for neuropathic pain diseases research.
|
-
- HY-P1403
-
|
|
Potassium Channel
|
Others
|
|
Tertiapin LQ is a specific and reversible renal outer medullary potassium ROMK1 (Kir1.1) channel inhibitor.
|
-
- HY-147909
-
-
- HY-100244
-
-
- HY-U00137
-
-
- HY-152847
-
|
QLS-101
|
Potassium Channel
|
Neurological Disease
|
|
Foslevcromakalim (QLS-101) is a ATP-sensitive potassium channel opener. Foslevcromakalim is the proagent used for ocular hypotensive effect.
|
-
- HY-131261
-
|
|
Others
|
Inflammation/Immunology
|
|
Ibuprofen alcohol, a nonsteroidal antiinflammatory agent (NSAID), exhibits very little activity for acid-sensing ion channels (ASICs).
|
-
- HY-U00250
-
-
- HY-B0419S
-
-
- HY-101256
-
|
|
Potassium Channel
|
Others
|
|
ZM226600 is an ATP-sensitive potassium channel opener (EC50: 500 nM). ZM226600 inhibits bladder spontaneous activity.
|
-
- HY-103318
-
-
- HY-13519
-
-
- HY-19366
-
-
- HY-156596
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Aneratrigine is a sodium channel protein type 9 subunit alpha blocker. Aneratrigine can be used for neuropathic pain diseases research.
|
-
- HY-P5144
-
-
- HY-101507
-
|
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
-
|
|
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[1][2].
|
-
- HY-151451
-
|
|
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-148802
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Taplucainium chloride is a Sodium Channel blocker. Taplucainium chloride exhibits 70-95% inhibition at 10μM. Taplucainium chloride can be used as an analgesic agent.
|
-
- HY-A0257
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Prenylamine is a calcium channel blocker of the amphetamine chemical class. Prenylamine can be used as a vasodilator and can be used for the research of angina pectoris.
|
-
- HY-W011641
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
(±)-Naringenin is a naturally-occurring flavonoid. (±)-Naringenin displays vasorelaxant effect on endothelium-denuded vessels via the activation of BKCa channels in myocytes.
|
-
- HY-B0799
-
|
Ergoloid mesylates
|
GABA Receptor
|
Neurological Disease
|
|
Dihydroergotoxine mesylate is a complex of closely related alkaloid salts; Binds with high affinity to the GABAA receptor Cl- channel, producing an allosteric interaction with the benzodiazepine site.
|
-
- HY-101547
-
|
|
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-108506
-
|
BIA 2-005; GP 47779
|
Sodium Channel
|
Neurological Disease
|
|
Licarbazepine (BIA 2-005; GP 47779) is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects.
|
-
- HY-135356
-
|
|
Drug Metabolite
|
Cardiovascular Disease
|
|
m-Nifedipine is an impurity of Nifedipine (BAY-a-1040). Nifedipine is a potent calcium channel blocker and agent of choice for cardiac insufficiencies.
|
-
- HY-B0246S2
-
-
- HY-19664
-
-
- HY-131281
-
|
|
Drug Metabolite
|
Others
|
|
Ivabradine impurity 1 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
|
-
- HY-106895
-
-
- HY-106855
-
|
H 234/09
|
Potassium Channel
|
Cardiovascular Disease
|
|
Almokalant is a class III antiarrhythmic agent, acts as a potassium channel blocker, and inhibits a specific component (Ikr) of the time-dependent delayed rectifier K + current.
|
-
- HY-103307
-
-
- HY-131282
-
|
|
Drug Metabolite
|
Others
|
|
Ivabradine impurity 2 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
|
-
- HY-108690
-
|
|
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-149536
-
|
|
Potassium Channel
|
Neurological Disease
|
|
TWIK-1/TREK-1-IN-1 (compound 2a) is an inhibitor of the TWIK-related potassium channel (Potassium Channel) TREK-1. TREK-1 contains a two-pore domain potassium (K2p) channel that dimerizes into TREK-1 homodimer and TWIK-1/TREK-1 heterodimer, and is an important antidepressant target. TWIK-1/TREK-1-IN-3 targets TREK-1 homodimer and TWIK-1/TREK-1 heterodimer with IC50s of 9.36 μM and 14.6 μM, respectively, and has antidepressant-like effects.
|
-
- HY-149538
-
|
|
Potassium Channel
|
Neurological Disease
|
|
TWIK-1/TREK-1-IN-3 (compound 2h) is an inhibitor of TWIK-related potassium channel (Potassium Channel) TREK-1. TREK-1 contains a two-pore domain potassium (K2p) channel that dimerizes into TREK-1 homodimer and TWIK-1/TREK-1 heterodimer, and is an important antidepressant target. TWIK-1/TREK-1-IN-3 targets TREK-1 homodimer and TWIK-1/TREK-1 heterodimer with IC50s of 9.74 μM and 16.5 μM, respectively, and has antidepressant-like effects.
|
-
- HY-110189S
-
|
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[1][2]. Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
|
-
- HY-108577
-
|
|
Potassium Channel
|
Neurological Disease
|
|
XE991 dihydrochloride, a Kv7 (KCNQ) channels blocker, potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current with IC50s of 0.75 µM, 0.71 µM, 0.6 μM, and 0.98 µM, respectively.
|
-
- HY-12498
-
|
|
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-18063
-
|
|
Potassium Channel
Cytochrome P450
|
Neurological Disease
|
|
ML252 is a selective inhibitor of potassium channel, targeting to KCNQ2 channel (Kv7.2) (IC50=69 nM). ML252 also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively.
|
-
- HY-P1604
-
|
|
Sodium Channel
|
Inflammation/Immunology
|
|
ATX-II is a specific Na + channel Modulator toxin that can be isolated from the venom of sea anemone (Anemonia sulcata). ATX-II causes delayed inactivation of the Na +channel in cell cultures. ATX-II sensitizes skeletal muscle to Halothane (HY-B1010), Caffeine, and Ryanodine (HY-103306). ATX-II also induces pulmonary vein arrhythmogenesis and atrial fibrillation.
|
-
- HY-108425
-
|
|
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-108577A
-
|
|
Potassium Channel
|
Neurological Disease
|
|
XE 991 dihydrochloride, a Kv7 (KCNQ) channels blocker, potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current with IC50s of 0.75 μM, 0.71 μM, 0.6 μM, and 0.98 μM, respectively.
|
-
- HY-B0402A
-
|
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
-
|
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-B0517A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Mepivacaine hydrochloride binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.
|
-
- HY-15082
-
|
BIIR 561
|
Sodium Channel
iGluR
|
Neurological Disease
|
|
Irampanel (BIIR 561) is an AMPA receptor and voltage-dependent sodium channel blocker. Irampanel inhibits kainate-induced currents in rat cortical neurons.
|
-
- HY-N6708
-
|
|
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-B1243
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Propoxycaine hydrochloride inhibits voltage-gated sodium channels, and thereby inhibits the ionic flux required for the initiation and conduction of impulses. Propoxycaine hydrochloride application can lead to a loss of sensation.
|
-
- HY-118328
-
|
|
5-HT Receptor
Potassium Channel
|
Cancer
|
|
Hymenidin is a natural antagonist of serotonergic receptor and inhibitor of voltage-gated potassium channels. Hymenidin also induces cancer cell apoptosis.
|
-
- HY-P0173B
-
|
|
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-B0284S1
-
-
- HY-10388
-
-
- HY-108590
-
-
- HY-131283
-
|
|
Drug Metabolite
|
Endocrinology
|
|
8-Demethyl Ivabradine is a metabolite of Ivabradine. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker.
|
-
- HY-148752
-
|
|
TRP Channel
|
Metabolic Disease
|
|
TRPV1 activator-2 (compound 9), a capsaicin head analog, makes specific interactions with channel residues at the lipid-water.
|
-
- HY-131899
-
|
|
Potassium Channel
Sodium Channel
|
Others
|
|
N-Bromoacetamide can irreversibly remove sodium channel inactivation in the cytoplasmic face of the membrane, also decreasing K current rapid inactivation.
|
-
- HY-B1793
-
|
|
Potassium Channel
|
Cancer
Neurological Disease
|
|
Tetraethylammonium chloride is a non-selective potassium channel blocker. Tetraethylammonium chloride is a good substrate for organic cation transporter (OCTN1). Tetraethylammonium chloride antitumor properties.
|
-
- HY-19062
-
-
- HY-B1140S
-
-
- HY-P5818
-
-
- HY-P3656
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
Kaliotoxin (1-37) is a toxin from the scorpion Artdroctonus mauretanicus mauretanicus. Kaliotoxin (1-37) is a potent calcium-dependent potassium channel blocker.
|
-
- HY-14744A
-
|
(S)-Amlodipine besylate; Levoamlodipine besylate
|
Calcium Channel
|
Cardiovascular Disease
|
|
Levamlodipine besylate ((S)-Amlodipine besylate) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina.
|
-
- HY-P1084
-
|
β-PMTX
|
Sodium Channel
|
Neurological Disease
|
|
β-Pompilidotoxin (β-PMTX), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells.
|
-
- HY-136190
-
|
|
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-115681
-
|
6-Prenylnaringenin; (±)-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
-
|
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
-
|
|
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-122001
-
|
|
Sodium Channel
|
Neurological Disease
|
|
PF-05186462 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channel, with an IC50 of 21 nM. PF-05186462 shows significant selectivity for Nav1.7 versus other sodium channels (Nav 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, and 1.8). PF-05186462 can be used for the research of acute or chronic pain.
|
-
- HY-P1075
-
CALP3
1 Publications Verification
|
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
-
|
|
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-134559
-
-
- HY-14656S
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Diltiazem-d3 (hydrochloride) is the deuterium labeled Diltiazem hydrochloride. Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist)[1][2].
|
-
- HY-16671
-
|
|
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
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Talatisamine, a aconitum alkaloid, is specific K + channel blocker. Talatisamine attenuates beta-amyloid oligomers induced neurotoxicity in cultured cortical neurons.
|
-
- HY-B1378
-
|
|
Calcium Channel
|
Neurological Disease
Cancer
|
|
Ethosuximide, a widely prescribed anti-epileptic agent, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.
|
-
- HY-100750
-
-
- HY-108504
-
|
V 102862
|
Sodium Channel
|
Neurological Disease
|
|
Co 102862 (V 102862) is a potent, broad-spectrum, state-dependent Na + channel blocker. Co 102862 is also an orally active anticonvulsant.
|
-
- HY-103623
-
-
- HY-17360
-
|
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-B0612DS
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
(R)-lercanidipine D3 (hydrochloride) is a deuterium labeled (R)-Lercanidipine hydrochloride. (R)-Lercanidipine-d3 (hydrochloride), the R-enantiomer of Lercanidipine, is a calcium channel blocker[1].
|
-
- HY-112472
-
|
|
Sodium Channel
|
Metabolic Disease
|
|
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.
|
-
- HY-100230A
-
|
|
Potassium Channel
|
Others
|
|
ML133 hydrochloride is a selective Kir2 family channels inhibitor, with an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5.
|
-
- HY-P5899
-
-
- HY-100611
-
-
- HY-129088
-
-
- HY-N0714
-
|
|
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-B0563S1
-
|
|
Isotope-Labeled Compounds
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[1][2]. 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[3]. Ropivacaine is used for the research of neuropathic pain management[1].
|
-
- HY-P3316
-
|
|
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 agent.
|
-
- HY-B1671
-
|
|
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
-
|
|
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-P1604A
-
|
|
Sodium Channel
|
Inflammation/Immunology
|
|
ATX-II TFA is a specific Na + channel Modulator toxin that can be isolated from the venom of sea anemone (Anemonia sulcata). ATX-II TFA causes delayed inactivation of the Na +channel in cell cultures. ATX-II TFA sensitizes skeletal muscle to Halothane (HY-B1010), Caffeine, and Ryanodine (HY-103306). ATX-II TFA also induces pulmonary vein arrhythmogenesis and atrial fibrillation.
|
-
- HY-P1075A
-
|
|
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
-
|
|
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[1][2].
|
-
- HY-B1482A
-
|
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
-
|
|
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
-
|
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
-
|
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-14187S
-
|
|
Potassium Channel
Autophagy
|
Cardiovascular Disease
|
|
Amiodarone-d10 (hydrochloride) is the deuterium labeled Amiodarone. Amiodarone hydrochloride is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM[1][2].
|
-
- HY-150541
-
-
- HY-19960
-
BCTC
2 Publications Verification
|
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-139786
-
|
ION-827359
|
Sodium Channel
|
Others
|
|
Cofirasersen is designed to reduce the expression of ENaC in the lung. ENaC is a sodium transport channel and believed to be hyperactive in cystic fibrosis, which is caused by mutations in the cystic fibrosis transmembrane regulator gene.
|
-
- HY-W016498S
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
Paraxanthine-d6 is the deuterium labeled Paraxanthine. Paraxanthine, a caffeine metabolite, provides protection against Dopaminergic cell death via stimulation of Ryanodine Receptor Channels.
|
-
- HY-101238
-
-
- HY-101437A
-
|
FCE-26742A mesylate
|
Sodium Channel
|
Neurological Disease
|
|
Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na + channel blocker derived from α-aminoamide, with function of suppressing pain.
|
-
- HY-112729
-
|
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-B0575S
-
|
|
Sodium Channel
|
Metabolic Disease
|
|
Triamterene-d5 is deuterium labeled Triamterene, which can block epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic.
|
-
- HY-101323
-
|
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
-
|
UTP trisodium salt; Uridine 5'-triphosphate trisodium salt
|
Endogenous Metabolite
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Uridine triphosphate trisodium salt is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
|
-
- HY-N3710
-
|
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
-
|
|
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-109987
-
|
|
Parasite
|
Infection
|
|
ISPA-28 is a specific plasmodial surface anion channel (PSAC) antagonist. ISPA-28 binds directly and reversibly to CLAG3.
|
-
- HY-131012
-
|
|
Potassium Channel
|
Others
|
|
GoSlo-SR-5-69 is a potent activator of large conductance Ca 2+-activated K + (BK) channels, with an EC50 of 251 nM.
|
-
- HY-139786A
-
|
ION-827359 sodium
|
|
Others
|
|
Cofirasersen sodium is designed to reduce the expression of ENaC in the lung. ENaC is a sodium transport channel and believed to be hyperactive in cystic fibrosis, which is caused by mutations in the cystic fibrosis transmembrane regulator gene.
|
-
- HY-124925
-
|
(-)-Isoeburnamine; (-)-epi-Eburnamine
|
Sodium Channel
|
Neurological Disease
|
|
Vincanol ((-)-Isoeburnamine) is a blocker of voltage-gated Na+ channels. Vincanol blocks Na + currents with an IC50 value of 40 μM. Vincanol has neuroprotective effect.
|
-
- HY-110270
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
RN-9893 is a potent and selective TRPV4 receptor antagonist with IC50 values of 320, 420 and 660 nM for mouse, human and rat channels, respectively.
|
-
- HY-B1655
-
|
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 agent used for schizophrenia.
|
-
- HY-P5145
-
-
- HY-P1084A
-
|
β-PMTX TFA
|
Sodium Channel
|
Neurological Disease
|
|
β-Pompilidotoxin TFA (β-PMTX TFA), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells.
|
-
- HY-14656S1
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Diltiazem-(acetoxy-d3) (hydrochloride) is the deuterium labeled Diltiazem hydrochloride. Diltiazem hydrochloride is a Ca2+ influx inhibitor (slow channel blocker or calcium antagonist)[1][2].
|
-
- HY-145126
-
|
|
CFTR
|
Others
|
|
CP-628006, a small molecule CFTR potentiator, restores ATP-dependent channel gating to the cystic fibrosis mutant G551D-CFTR.
|
-
- HY-100727
-
-
- HY-116790A
-
-
- HY-B1288
-
|
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-108506S1
-
-
- HY-10388A
-
|
|
Calcium Channel
|
Others
|
|
TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca 2+ channel antagonist.
|
-
- HY-B1445
-
|
|
Potassium Channel
|
Metabolic Disease
|
|
Minoxidil sulfate, a potent and ATP-sensitive K + channel opener, is the sulfated metabolite of minoxidil. Minoxidil sulfate is considered as a vasodilator to promote hair growth in vivo.
|
-
- HY-A0084
-
|
|
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
-
|
|
CRAC Channel
|
Cardiovascular Disease
|
|
piCRAC-1 is a potent, photoinducible Ca 2+ release-activated Ca 2+ (CRAC) channel inhibitor. piCRAC-1 alleviates thrombocytopenia and hemorrhage.
|
-
- HY-20587
-
|
|
CRAC Channel
|
Inflammation/Immunology
|
|
CRAC intermediate 1 is a key intermediate in the chemical synthesis of a series of CRAC channel inhibitors, detailed information can be found in Patent WO 2010122089 A1, intermediate 9.
|
-
- HY-108506S
-
|
BIA 2-005-d3; GP 47779-d3
|
Sodium Channel
|
Neurological Disease
|
|
Licarbazepine-d3 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects[1][2].
|
-
- HY-N2060
-
-
- HY-A0093S
-
|
KOE-1173-d6 (hydrochloride)
|
Sodium Channel
|
Cardiovascular Disease
|
|
Mexiletine-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[1].
|
-
- HY-135013
-
|
|
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
-
|
|
iGluR
|
Neurological Disease
|
|
Orphenadrine-d3 (citrate) is the deuterium labeled Orphenadrine citrate. Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.
|
-
- HY-155236
-
-
- HY-N0252
-
|
(+)-3,4-Didehydrocoronaridine
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Catharanthine is an alkaloid isolated from Catharanthus roseus, inhibits voltage-operated L-type Ca 2+ channel, with anti-cancer and blood pressure-lowering activity.
|
-
- HY-108465
-
|
|
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-P1218
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
|
-
- HY-13422A
-
|
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-157131
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPV2-selective blocker 1 (compound IV2-1) is a selective TRPV2 channel blocker with an IC50 of 6.3 μM. TRPV2-selective blocker 1 does not affect TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 also inhibits TRPV2-mediated Ca 2+ influx in macrophages, and inhibits macrophage phagocytosis.
|
-
- HY-B0402S1
-
|
1-Adamantanamine-d6; 1-Aminoadamantane-d6
|
Apoptosis
CDK
SARS-CoV
Bcl-2 Family
Influenza Virus
Orthopoxvirus
|
|
|
Amantadine-d6 is the deuterium labeled Amantadine[1]. 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[2][3][4][5][6][7].
|
-
- HY-P3071
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
ShK toxin blocks voltage-dependent potassium channel (Kv1.3 channel). ShK toxin can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin suppresses K+ currents in cultured rat dorsal root ganglion neurons. ShK toxin also inhibits T lymphocyte proliferation.
|
-
- HY-P5870
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
KTX-Sp2 is a potassium channel toxin. KTX-Sp2 effectively blocks three types of exogenous voltage-gated potassium channels: Kv1.1, Kv1.2 and Kv1.3. Ktx-Sp2 inhibits endogenous Kv1.3 and suppresses Ca 2+ signaling in Jurkat T cells. Ktx-Sp2 inhibits IL-2 secretion from activated Jurkat T cells.
|
-
- HY-117825
-
|
|
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). RU-TRAAK-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-120026
-
|
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
-
|
|
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
-
|
(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-N5006
-
-
- HY-N1469
-
-
- HY-136189
-
|
|
Calcium Channel
|
Neurological Disease
|
|
UK-59811 hydrochloride, a Br-dihydropyridine derivative, is a potent bacterial homotetrameric model voltage-gated Ca 2+ (CaV) channel CaVAb inhibitor with an IC50 of 194 nM.
|
-
- HY-A0093S1
-
|
KOE-1173-d3 hydrochloride
|
Isotope-Labeled Compounds
Sodium Channel
|
Cardiovascular Disease
|
|
Mexiletine-d3 (hydrochloride) is deuterium labeled Mexiletine (hydrochloride). Mexiletine hydrochloride (KOE-1173 hydrochloride), a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker[1][2].
|
-
- HY-B0887S1
-
|
NRDC-143-d9
|
Isotope-Labeled Compounds
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-16723A
-
|
(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
-
|
(+)-3,4-Didehydrocoronaridine Tartrate
|
Calcium Channel
|
Cancer
Cardiovascular Disease
|
|
Catharanthine Tartrate is an alkaloid isolated from Catharanthus roseus, inhibits voltage-operated L-type Ca 2+ channel, with anti-cancer and blood pressure-lowering activity.
|
-
- HY-107372
-
-
- HY-P5835
-
|
|
Potassium Channel
|
Neurological Disease
|
|
δ-Dendrotoxin is a K + channel blocker that can be obtained from the venom of the black mamba snake. δ-Dendrotoxin can be used in the study of neurological diseases.
|
-
- HY-147391
-
|
|
Sodium Channel
|
Neurological Disease
|
|
ASIC-IN-1 is a potent acid sensing ion channel inhibitor with an IC50 value of < 10 µM. ASIC-IN-1 causes a dose- dependent reduction of the pain intensity.
|
-
- HY-B0612A
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Lercanidipine hydrochloride is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine hydrochloride has long lasting antihypertensive action and reno-protective effect.
|
-
- HY-130074
-
|
|
TRP Channel
|
Neurological Disease
|
|
FEMA 4809 is a TRPM8 receptor agonist (EC50=0.2 nM) for use as a cooling agent. TRPM8 is the ion channel responsible for the cool perception.
|
-
- HY-B0612
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Lercanidipine is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine has long lasting antihypertensive action and reno-protective effect.
|
-
- HY-B0267AS
-
-
- HY-107349S
-
|
Spasmopriv-d8
|
Calcium Channel
|
Neurological Disease
|
|
Fenoverine-d8 is the deuterium labeled Fenoverine[1]. Fenoverine (Spasmopriv) is an antispasmodic agent and inhibits calcium channel currents[2]. Fenoverine induces rhabdomyolysis[3].
|
-
- HY-P0062
-
-
- HY-B0772A
-
|
MS-551
|
Potassium Channel
|
Cardiovascular Disease
|
|
Nifekalant hydrochloride (MS-551), a class III antiarrhythmic agent, is a IKr potassium channel blocker with an IC50 of 10 µM. Nifekalant hydrochloride can be used for refractory ventricular tachyarrhythmias research.
|
-
- HY-14744S
-
|
(S)-Amlodipine-d4; Levoamlodipine-d4
|
Isotope-Labeled Compounds
Calcium Channel
|
Others
|
|
Levamlodipine-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[1].
|
-
- HY-18600A
-
|
NE-10064 dihydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
Azimilide (NE-10064) dihydrochloride is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
|
-
- HY-133614
-
|
|
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
-
|
|
DNA Stain
|
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
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
LUF7244 is a selective allosteric modulator of Kv11.1 channels. LUF7244 inhibits early afterdepolarizations. LUF7244 can be used for anti-arrhythmia research.
|
-
- HY-112723
-
|
ACT-709478
|
Calcium Channel
|
Neurological Disease
|
|
Apinocaltamide (ACT-709478) is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies.
|
-
- HY-114301
-
|
|
Sodium Channel
|
Neurological Disease
|
|
PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile.
|
-
- HY-A0148A
-
|
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-N3573
-
|
|
Potassium Channel
|
Others
|
|
Chlorahololide D is a potent and selective Potassium Channel blocker with an IC50 value of 2.7 μM. Chlorahololide D is a nature product that could be isolated from the whole plant of Chloranthus holostegius.
|
-
- HY-B1657A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Fosphenytoin sodium is a phenytoin proagent 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
-
|
NE-10064
|
Potassium Channel
|
Cardiovascular Disease
|
|
Azimilide(NE-10064) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
|
-
- HY-P5873
-
|
JZTX-X
|
Potassium Channel
|
Neurological Disease
|
|
Jingzhaotoxin-X (JZTX-X) is a selective Kv4.2 and Kv4.3 potassium channels inhibitor. Jingzhaotoxin-X causes long-lasting mechanical hyperalgesia.
|
-
- HY-P0062B
-
-
- HY-B0339
-
|
|
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-113643
-
|
|
Calcium Channel
5-HT Receptor
|
Neurological Disease
|
|
Levemopamil hydrochloride is a blood-brain barrier penetrable calcium channel blocker and a 5-HT2 antagonist. Levemopamil hydrochloride can be used for temporary occlusion and neurological disease research.
|
-
- HY-P5162
-
|
|
Sodium Channel
|
Inflammation/Immunology
|
|
Dc1a potently promotes opening of the German cockroach Nav channel (BgNav1). Dc1a is a toxin can be isolated from the desert bush spider Diguetia canities.
|
-
- HY-108461
-
-
- HY-121604
-
|
|
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-D1431
-
|
|
Fluorescent Dye
|
Cancer
|
|
ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206), highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining cells after fixation.
|
-
- HY-D1297
-
|
|
Fluorescent Dye
|
Others
|
|
ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206), highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining cells after fixation.
|
-
- HY-P1218A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
|
-
- HY-N1584
-
|
RU-19110
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Cancer
Infection
Inflammation/Immunology
Cardiovascular Disease
|
|
Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
|
-
- HY-B0347S1
-
|
|
Apoptosis
Caspase
Calcium Channel
Reactive Oxygen Species
|
Cardiovascular Disease
|
|
Lacidipine- 13C8 is the deuterium labeled Lacidipine[1]. 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)[2][3].
|
-
- HY-D1429
-
|
|
Fluorescent Dye
|
Others
|
|
ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206), highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining cells after fixation.
|
-
- HY-15124
-
-
- HY-118048
-
|
|
Sodium Channel
|
Neurological Disease
|
|
NAV 26 (compound 26) is a selective voltage-gated sodium channel Nav1.7 blocker with an IC50 of 0.37 μM. NAV 26 can be used for pain research.
|
-
- HY-114608
-
|
|
Sodium Channel
|
Neurological Disease
|
|
RY785 is a potent and selective voltage-gated potassium (KV2) channel inhibitor with an IC50 of 0.05 μM for KV2.2. RY785 has analgesic activity.
|
-
- HY-66010A
-
|
|
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-107697
-
|
|
iGluR
|
Neurological Disease
|
|
N20C hydrochloride is a selective and noncompetitive open NMDA receptor open channel blocker, with micromolar affinity, fast on-off blockade kinetics, and strong voltage dependence. Neuroprotective activity.
|
-
- HY-B0517
-
|
|
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
-
|
|
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
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Methyl homoveratrate, a metabolite of RWJ-26240 in vivo, can be identified in plasma, urine and faecal extract. McN5691 (RWJ-26240) is a voltage-sensitive calcium channel blocker.
|
-
- HY-B0448A
-
|
5,5-Diphenylhydantoin sodium salt
|
Sodium Channel
Virus Protease
|
Neurological Disease
Cancer
|
|
Phenytoin sodium (5,5-Diphenylhydantoin sodium salt) is a potent Voltage-gated Na + channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice.
|
-
- HY-P5854
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Aa1 toxin, a neurotoxic peptide that can be obtained from the venom of Androctonus australis Garzoni, is a specific potassium channel blocker. Aa1 toxin can be used in the study of neurological diseases.
|
-
- HY-114301A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile.
|
-
- HY-N2197
-
|
|
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
-
|
|
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
-
|
|
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
-
|
|
Calcium Channel
|
Neurological Disease
|
|
ω-Conotoxin MVIIC is a N- and P/Q-type Ca 2+ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release.
|
-
- HY-123825
-
-
- HY-B0551A
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Doxapram hydrochloride hydrate inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.
|
-
- HY-Y0258S1
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Benzocaine-(ethyl-d5) 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-100783A
-
|
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-P5855
-
|
|
Sodium Channel
|
Neurological Disease
|
|
μ-Conotoxin SxIIIC is an irreversible NaV channel inhibitor that can be obtained from the Conus striolatus. μ-Conotoxin SxIIIC can be used in the study of neurological diseases such as chronic pain.
|
-
- HY-146334
-
|
|
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
-
|
|
Calcium Channel
|
Neurological Disease
|
|
ω-Conotoxin MVIIC TFA is a N- and P/Q-type Ca 2+ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release.
|
-
- HY-N2940
-
|
BAA
|
TRP Channel
|
Inflammation/Immunology
|
|
Bisandrographolide A (BAA) activates TRPV4 channel with an EC50 of 790-950 nM. Bisandrographolide A can bind to CD81 and suppress its function. Bisandrographolide A is an anti-inflammatory, immunostimulant, and antihypertensive compound.
|
-
- HY-33350
-
-
- HY-P3089
-
|
|
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-144802
-
-
- HY-100783
-
|
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
-
|
|
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
-
|
BAY-E-5009
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Nitrendipine (BAY-E-5009), an analogue of Nifedipine (HY-B0284), is a dihydropyridine calcium channel blocker with vasodilator action. Nitrendipine has antihypertensive effect.
|
-
- HY-101789
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration.
|
-
- HY-145992
-
-
- HY-136589
-
-
- HY-107754
-
|
|
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-B0493S1
-
-
- HY-108506S2
-
-
- HY-N4323
-
-
- HY-148866
-
|
|
Calcium Channel
|
Endocrinology
Neurological Disease
|
|
Cavα2δ1&NET-IN-3 (example 216) is an inhibitor of the subunit α2δ of voltage-gated calcium channels (VGCC) and noradrenaline transporter (NET). Cavα2δ1&NET-IN-3 has Kis of 100-500 nM for human α2δ-1 subunit of Cav2.2 calcium channel and NET, respectively.
|
-
- HY-116330
-
|
|
Calcium Channel
TRP Channel
|
Inflammation/Immunology
Neurological Disease
|
|
Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model.
|
-
- HY-111828
-
|
|
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
-
|
RU-19110 hydrobromide
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Cancer
Infection
Inflammation/Immunology
Cardiovascular Disease
|
|
Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.
|
-
- HY-N0322A
-
|
|
Liposome
|
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
-
|
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-135328S
-
-
- HY-B1386
-
|
|
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
-
|
|
Sodium Channel
|
Neurological Disease
|
|
A-317567 is a potent acid-sensing ion channel 3 (ASIC-3) inhibitor with an IC50 of 1.025 μM. A-317567 has antidepressant and antinociception effects.
|
-
- HY-120751
-
-
- HY-69359
-
|
(±)-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-135328AS
-
|
(±)-Norverapamil-d7 (hydrochloride); D591-d7 (hydrochloride)
|
Calcium Channel
|
Cardiovascular Disease
|
|
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[1][2].
|
-
- HY-17429
-
|
R-818
|
Sodium Channel
|
Cardiovascular Disease
|
|
Flecainide acetate (R-818) is a class 1C antiarrhythmic agent 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-B0632
-
|
|
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
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
-
|
(S)-SA-79
|
Sodium Channel
|
Cardiovascular Disease
|
|
(S)-Propafenone ((S)-SA-79) is the S-enantiomer of Propafenone. (S)-Propafenone ((S)-SA-79) exerts beta-blocking action and the sodium channel-dependent antiarrhythmic class 1 activity.
|
-
- HY-P0062A
-
-
- HY-116759
-
-
- HY-100712
-
|
|
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-121539
-
|
|
TRP Channel
|
Neurological Disease
|
|
Supercinnamaldehyde is a potent transient receptor potential ankyrin 1 (TRPA1) activator with an EC50 value of 0.8 μM. Supercinnamaldehyde activates TRPA1 ion channels through covalent modification of cysteines.
|
-
- HY-17402S
-
-
- HY-117714
-
|
|
Sodium Channel
|
Neurological Disease
|
|
AZD-3161 is a potent and selective blocker of NaV1.7 channel, with a pIC50 of 7.1. AZD-3161 can be used for the research of neuropathic and inflammatory pain.
|
-
- HY-148410
-
|
STK-001
|
Sodium Channel
|
Others
|
|
Zorevunersen (STK-001) is an antisense oligonucleotide that is intended to increase the level of productive SCN1A mRNA and consequently increase the expression of the sodium channel Nav1.1 protein. Zorevunersen is used for the study of Dravet syndrome.
|
-
- HY-B1378S1
-
-
- HY-13812
-
-
- HY-N7126
-
|
|
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-14834
-
-
- HY-100080
-
|
|
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
-
|
dmLSB
|
Sodium Channel
|
Cardiovascular Disease
|
|
Dimethyl lithospermate B (dmLSB) is a selective Na + channel agonist. Dimethyl lithospermate B slows inactivation of sodium current (INa), leading to increased inward current during the early phases of the action potential (AP).
|
-
- HY-P5796
-
|
|
Calcium Channel
|
Neurological Disease
|
|
FS-2 is a potent and specific L-type CaV channel inhibitor. FS-2 inhibits high K + or glucose induced L-type Ca 2+ influx in RIN beta cells.
|
-
- HY-B0493S
-
|
|
Chloride Channel
|
Inflammation/Immunology
|
|
Niflumic Acid-d5 is the deuterium labeled Niflumic acid. Niflumic acid, a Ca2+-activated Cl- channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis[1][2].
|
-
- HY-14182
-
|
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
-
|
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-P3089A
-
|
|
Potassium Channel
|
Others
|
|
Dendrotoxin K TFA is a Kv1.1 channel blocker. Dendrotoxin K TFA determines glutamate release in CA3 neurons in a time-dependent manner through the control of the presynaptic spike waveform.
|
-
- HY-N0252B
-
|
(+)-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-B0575R
-
|
|
Sodium Channel
G protein-coupled Bile Acid Receptor 1
|
Metabolic Disease
|
|
Triamterene (Standard) is the analytical standard of Triamterene. This product is intended for research and analytical applications. Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic. Triamterene as an inhibitor of the TGR5 receptor.
|
-
- HY-D1362
-
|
|
Fluorescent Dye
|
Others
|
|
BDP 630/650 maleimide is a fluorophore which can be read on the Cyanine5 channel. BDP 630/650 maleimide is useful for fluorescence lifetime related measurements because of the long life time of the excited state.
|
-
- HY-W009356A
-
|
|
Biochemical Assay Reagents
|
Others
|
|
L-Cystine hydrochloride is an amino acid. L-Cystine is converted to L-Cysteine in the body. Moreover, L-Cystine/L-Cysteine conversion system is a channel on the cell membrane, which can maintain the internal REDOX homeostasis of E. coli.
|
-
- HY-B1551
-
|
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-116330A
-
|
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 also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model.
|
-
- HY-19408
-
Pyr10
3 Publications Verification
|
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
-
|
|
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-17436S1
-
|
|
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[1][2].
|
-
- HY-108502
-
|
|
Sodium Channel
|
Cardiovascular Disease
|
|
KC 12291 hydrochloride is an orally active blocker of voltage-gated sodium channel (VGSC). KC 12291 hydrochloride reduces the amplitude of sustained Na + current to exert antiischemic activity. KC 12291 hydrochloride has significant cardioprotective effect in vitro and in vivo.
|
-
- HY-P0256
-
Apamin
1 Publications Verification
Apamine
|
Potassium Channel
|
Inflammation/Immunology
Neurological Disease
|
|
Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca 2+-activated K + (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.
|
-
- HY-N1072
-
|
|
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
-
|
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-P5816
-
|
|
Sodium Channel
|
Neurological Disease
|
|
BmK-M1 is a scorpion toxin, and is composed of 64 amino acids cross-linked by four disulfide bridges. BmK-M1 inhibits Na + channel and can be considered both as a cardiotoxin and a neurotoxin.
|
-
- HY-P3037
-
|
|
Calcium Channel
|
|
|
Imperatoxin A, a peptide toxin derived from the venom of the African scorpion Pandinus imperator, activator of Ca 2+-release channels/ryanodine receptors (RyRs)? enhances the influx of Ca 2+ from the sarcoplasmatic reticulum into the cell.
|
-
- HY-17360S
-
|
BA679 BR-d3
|
mAChR
|
Neurological Disease
|
|
Tiotropium-d3 (bromide) 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-123481
-
|
|
P2X Receptor
|
Metabolic Disease
|
|
JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pKi values of 9.1 and 7.9 for rat and human P2X7 channels, respectively.
|
-
- HY-17360S1
-
|
BA679 BR-d6
|
Isotope-Labeled Compounds
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
-
|
Hydroxytolbutamide
|
Potassium Channel
Autophagy
|
Cancer
Metabolic Disease
|
|
4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic.
|
-
- HY-101253
-
|
|
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
-
|
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
-
|
|
5-HT Receptor
Dopamine Receptor
|
|
|
5-HT6/7 antagonist 1 is a multifunctional ligand that antagonizes 5-HT6/7/2A and D2 receptors, without interacting with M1 receptors and hERG channels.
|
-
- HY-136615
-
|
|
Potassium Channel
|
Neurological Disease
|
|
5-Hydroxydecanoate sodium is a selective ATP-sensitive K + (KATP) channel blocker (IC50 of ~30 μM). 5-Hydroxydecanoate sodium is a substrate for mitochondrial outer membrane acyl-CoA synthetase and has antioxidant activity.
|
-
- HY-B1837
-
|
|
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-101436
-
|
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-111996
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
Kv3 modulator 1 is a Kv3 voltage-gated potassium channel modulator extracted from patent WO2018020263A1, Compound X. Kv3 modulator 1 has the potential for inflammatory pain treatment.
|
-
- HY-14848
-
|
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
-
|
D 9998-d4 hydrochloride
|
Potassium Channel
iGluR
|
Neurological Disease
|
|
Flupirtine-d4 (D 9998-d4) hydrochloride is the deuterium labeled Flupirtine. Flupirtine(D 9998) hydrochloride is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties.
|
-
- HY-12693
-
|
R(+)-IAA-94
|
Chloride Channel
|
Others
|
|
R(+)-Methylindazone (R(+)-IAA-94) is a potent indanyloxyacetic acid blocker of epithelial chloride channels. R(+)-Methylindazone inhibits Nef-sdAb19 (single-domain antibody) interaction and binds to negative factor (Nef).
|
-
- HY-151450
-
-
- HY-132133
-
-
- HY-110237
-
|
|
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-W016498S1
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
Paraxanthine- 13C4, 15N3 is the 13C-labeled and 15N-labeled Paraxanthine. Paraxanthine, a caffeine metabolite, provides protection against Dopaminergic cell death via stimulation of Ryanodine Receptor Channels.
|
-
- HY-146380
-
|
|
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-P1426
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
AmmTX3 is a peptide toxin that can be isolated from the venom of the scorpion Androctonus mauretanicus. AmmTX3 is specific blocker of Kv4 channel. AmmTX3 inhibits the A-type K + current (Ki: 131 nM).
|
-
- HY-22044
-
|
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-P5143
-
|
|
Calcium Channel
|
Inflammation/Immunology
|
|
ω-Conotoxin SO3 is a blocker of N-type voltage-sensitive calcium channel. ω-Conotoxin SO3 is an analgesicω-conotoxin that can be isolated from the venom of C. striatus.
|
-
- HY-16696
-
SN 2
3 Publications Verification
|
TRP Channel
Flavivirus
|
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-B0632A
-
|
MK 793
|
Calcium Channel
|
Cardiovascular Disease
|
|
Diltiazem malate is a potent and orally active L-type calcium channel inhibitor. Diltiazem malate shows antihypertensive and antiarrhythmic effects. Diltiazem malate can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris.
|
-
- HY-B0612DS1
-
|
|
Isotope-Labeled Compounds
Calcium Channel
|
Cardiovascular Disease
|
|
Lercanidipine-d3 (hydrochloride) is the deuterium labeled Lercanidipine. Lercanidipine is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine has long lasting antihypertensive action and reno-protective effect[1][2][3].
|
-
- HY-19666
-
|
SDZ 201106
|
Sodium Channel
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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.
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- HY-N1462
-
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Chloride Channel
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Cardiovascular Disease
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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.
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- HY-128829
-
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Potassium Channel
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Inflammation/Immunology
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Kv3 modulator 2 (formula (I)) is a potent Kv3 channels modulator extracted from patent WO2018109484A1, compound formula (I) , has analgesic activity and is used in the prophylaxis or treatment of related disorders.
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- HY-P1441A
-
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Sodium Channel
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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.
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- HY-108575
-
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Potassium Channel
CFTR
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Cardiovascular Disease
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Chromanol 293B is a selective blocker of the slow delayed rectifier K + current (IKs) with IC50 of 1-10 μM and a weak inhibitor of KATP channel. Chromanol 293B also blocks the CFTR chloride current with an IC50 of 19 μM.
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- HY-18779
-
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TRP Channel
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Inflammation/Immunology
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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.
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- HY-B0339S
-
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Sodium Channel
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Neurological Disease
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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[1].
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- HY-N4097
-
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Others
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Neurological Disease
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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.
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- HY-W040265
-
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N-Phenylanthranilic acid
|
Chloride Channel
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Inflammation/Immunology
|
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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 -.
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- HY-153746
-
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Potassium Channel
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Inflammation/Immunology
|
|
Kv3 modulator 5 (Example 5) is a Kv3 channel modulator. Kv3 modulator 5 increases the Kv3.2 current. Kv3 modulator 5 can be used for research of hearing disorders.
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- HY-N6688
-
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Potassium Channel
Bacterial
Antibiotic
|
Infection
|
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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.
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- HY-18600AS
-
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NE-10064-dd8 (dihydrochloride)
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Potassium Channel
|
Cardiovascular Disease
|
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Azimilide-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.
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- HY-122504
-
|
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Potassium Channel
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Neurological Disease
|
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Linoleoyl glycine is a modified polyunsaturated fatty acid. Linoleoyl glycine has activating effects on human KCNQ1/KCNE1 (hKCNQ1/hKCNE1) channels expressed in Xenopus oocytes.
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- HY-P1952A
-
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Sodium Channel
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Neurological Disease
|
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µ-Conotoxin-CnIIIC acetate, a 22-residue conopeptide, is a potent antagonist of the voltage-gated NaV1.4 sodium channel with an IC50 of 1.3 nM acting at the neuromuscular junction. µ-Conotoxin-CnIIIC acetate has myorelaxant and analgesic effects.
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- HY-106916
-
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Potassium Channel
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Neurological Disease
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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.
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- HY-151452
-
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Calcium Channel
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Neurological Disease
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Cav 3.2 inhibitor 3 (Compound 4) is a potent Cav3.2 T-type Ca 2+ channel inhibitor with an IC50 of 0.1534 μM, and has little binding affinity to D2 receptors.
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-
- HY-P3064
-
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Leiurotoxin I
|
Potassium Channel
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Neurological Disease
|
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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.
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- HY-111613
-
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Calcium Channel
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Others
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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.
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- HY-P0256A
-
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Apamine TFA
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Potassium Channel
|
Inflammation/Immunology
Neurological Disease
|
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Apamin TFA (Apamine TFA) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca 2+-activated K + (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.
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- HY-B0114
-
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GP 47680
|
Sodium Channel
Apoptosis
|
Cancer
Neurological Disease
|
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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.
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-
- HY-30234A
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- HY-16973S
-
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A1443-13C2,15N,d3; AH252723-13C2,15N,d3
|
Isotope-Labeled Compounds
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.
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- HY-A0057
-
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Calcium Channel
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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.
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-
- HY-17612
-
|
NW-3509
|
Sodium Channel
|
Neurological Disease
|
|
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-122464A
-
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(-)-Jasmonic acid
|
Molecular Glues
|
Others
|
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Jasmonic acid ((-)-Jasmonic acid) is a plant growth regulator and a derivative of α-Linolenic acid (HY-N0728). Jasmonic acid signaling can also induce the MAP kinase cascade pathway, calcium channel, and many processes that interact with signaling molecules.
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- HY-B1167
-
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Cardiorythmine; (+)-Ajmaline
|
Sodium Channel
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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.
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- HY-N2412
-
|
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Chloride Channel
|
Cancer
Neurological Disease
|
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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).
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-
- HY-A0057A
-
|
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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.
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- HY-122015
-
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Potassium Channel
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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.
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-
- HY-153850
-
|
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Others
|
Others
|
|
RNA Aptamer Peach Ⅰ (sodium) has an exceptionally high affinity to TO3-Biotin (TO3-B, red channel, ex: 637 nm, em: 658 nm), and can be used to visualize RNA expression or localization in live cells.
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- HY-19282A
-
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Sodium Channel
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Neurological Disease
|
|
(5R)-BW-4030W92 is the R enantiomer of BW-4030W92. BW-4030W92 is a non-selective, voltage-, and use-dependent sodium channel antagonist.
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-
- HY-30234
-
-
- HY-B0517S
-
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|
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[1][2].
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-
- HY-153851
-
|
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Others
|
Others
|
|
RNA Aptamer Peach Ⅱ (sodium) has an exceptionally high affinity to TO3-Biotin (TO3-B, red channel, ex: 637 nm, em: 658 nm), and can be used to visualize RNA expression or localization in live cells.
|
-
- HY-B1558
-
|
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
-
|
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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.
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- HY-75161
-
|
|
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.
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-
- HY-B0448S
-
|
5,5-Diphenylhydantoin-d10
|
Sodium Channel
Virus Protease
|
Neurological Disease
|
|
Phenytoin-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[1][2].
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- HY-B0632S
-
|
|
Isotope-Labeled Compounds
Calcium Channel
|
Cardiovascular Disease
|
|
Diltiazem-d6 is the deuterium labeled Diltiazem. Diltiazem is an orally active L-type Ca2+ channel blocker, with antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris[1][2][3].
|
-
- HY-126985
-
|
Anhydroepitetrodotoxin
|
Sodium Channel
|
Neurological Disease
|
|
4,9-Anhydrotetrodotoxin is a selective voltage-gated sodium channel (VGSC) inhibitor that blocks Nav1.1 and Nav1.6 in human brain and induces a hyperpolarizing shift in the voltage dependence of inactivated Nav1.6.
|
-
- HY-122605
-
|
CBA
|
TRP Channel
|
Cancer
Cardiovascular Disease
|
|
TRPM4-IN-1 (CBA) is a potent and selective inhibitor of the cation channel TRPM4, with an IC50 of 1.5 μM. TRPM4-IN-1 can be used for the research of cardiac diseases and prostate cancer.
|
-
- HY-129677
-
|
|
Others
|
Others
|
|
ORC-13661 hydrochloride is a hair cell protector. ORC-13661 hydrochloride protects sensory hair cells from aminoglycoside and Cisplatin (HY-17394) ototoxicity. ORC-13661 hydrochloride is a reversibly mechanoelectrical transducer (MET) channel permeant blocker.
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-
- HY-131614
-
|
|
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-102052
-
|
|
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
-
|
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-D1816
-
|
|
Fluorescent Dye
|
Others
|
|
Vari Fluor 555-Phalloidin is a fluorescent derivative of Phalloidin that specifically labels myofilament proteins and exhibits red fluorescence when labeled, allowing for fluorescence imaging using the PE channel (Ex/Em=550 nm/561 nm).
|
-
- HY-111036
-
|
|
TRP Channel
|
Others
|
|
AMG0347 is a transient receptor potential type V1 receptor antagonist. AMG0347 inhibits activation of the rat TRPV1 channel by heat (IC50 = 0.2 nm), protons (IC50= 0.8 nm), or capsaicin (IC50 = 0.7 nm).
|
-
- HY-108235
-
|
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-P1426A
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
AmmTX3 TFA is a peptide toxin that can be isolated from the venom of the scorpion Androctonus mauretanicus. AmmTX3 TFA is specific blocker of Kv4 channel. AmmTX3 TFA inhibits the A-type K + current (Ki: 131 nM).
|
-
- HY-N2941
-
|
|
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-P3156
-
|
|
Fungal
|
Infection
|
|
Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasma membrane. Syringomycin E causes K + efflux, Ca 2+ influx, and changes in membrane potential, and is related to channel formation.
|
-
- HY-D0877
-
|
|
Biochemical Assay Reagents
|
Others
|
|
TAPS is a biological buffer, remain lysozyme native structure intact and prevents thermal denaturation against high temperatures. TAPS exhibits pKa value of 8.1, while the half-maximum values of connexin channel activity is 8.5 (pH).
|
-
- HY-131868
-
|
|
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
-
|
|
Isotope-Labeled Compounds
Sodium Channel
|
Neurological Disease
|
|
Fosphenytoin-d10 (disodium) is deuterium labeled Fosphenytoin (disodium). Fosphenytoin sodium is a phenytoin proagent 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
-
|
U10858
|
Potassium Channel
Endogenous Metabolite
|
Cardiovascular Disease
Cancer
|
|
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-B0887S
-
|
NRDC-143-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[1][2].
|
-
- HY-108585
-
|
|
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-B0495A
-
|
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-120294
-
|
|
CGRP Receptor
TRP Channel
|
Neurological Disease
|
|
Chrysin 6-C-glucoside 8-C-arabinoside can inhibit the CGRP releasing and the activation of TRPV1 channel. Chrysin 6-C-glucoside 8-C-arabinoside can be used for anti-migraine research.
|
-
- HY-119934
-
|
|
Sodium Channel
|
Neurological Disease
|
|
NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium channel (NaV) 1.7 inhibitor with an IC50 of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5.
|
-
- HY-108589
-
|
PNU 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
-
|
|
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-D1817
-
|
|
Fluorescent Dye
|
Others
|
|
Vari Fluor 488-Phalloidin is a fluorescent derivative of Phalloidin that specifically labels myofilament proteins and exhibits green fluorescence when labeled, allowing for fluorescence imaging using FITC channels (Ex/Em=488 nm/513 nm).
|
-
- HY-B0424S
-
|
AY-E-5009-d5
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
|
|
Nitrendipine-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[1][2][3][4].
|
-
- HY-108235A
-
|
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
-
|
Sodium ascorbate; Sodium L-ascorbate; Vitamin C sodium salt; Vitamine C sodium salt
|
Calcium Channel
Reactive Oxygen Species
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
L-Ascorbic acid sodium salt (Sodium ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt selectively inhibits Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.
|
-
- HY-141796
-
|
|
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
-
|
|
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-107695
-
|
FPL 12924AA
|
iGluR
Sodium Channel
|
Neurological Disease
|
|
Remacemide hydrochloride (FPL 12924AA), a moderate inhibitor of the Na + channel, is a weak uncompetitive NMDA receptor antagonist with IC50s of 68 μM and 76 μM for MK-801 binding and NMDA currents, respectively. Remacemide hydrochloride is an anticonvulsant agent.
|
-
- HY-P1410B
-
-
- HY-P5858
-
|
|
Sodium Channel
|
Neurological Disease
|
|
μ-Conotoxin SIIIA is a tetrodotoxin (TTX)-resistant sodium channel blocker. μ-Conotoxin SIIIA is a toxic peptide that can be obtained from the venom of Conus snails. μ-Conotoxin SIIIA can be used in the study of neurological diseases, such as neuropathic pain.
|
-
- HY-107757
-
|
|
Sodium Channel
|
Neurological Disease
|
|
GMQ is a ASIC (acid-sensing ion) channel activator with an EC50 value of 1.83 mM for ASIC3 at pH 7.4. GMQ opens only ASIC3 but no other ASICs at pH 7.4. GMQ can be used for neurological disease research.
|
-
- HY-B0612AS1
-
|
|
Isotope-Labeled Compounds
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[1][2][3].
|
-
- HY-155635
-
|
|
Sodium Channel
|
Infection
|
|
Nav1.8-IN-4 (compound 9a) is a Nav1.8 channel inhibitor (IC50=0.014 μM). Nav1.8-IN-4 can be used for research on pain-related diseases.
|
-
- HY-B1751C
-
|
|
Parasite
Cytochrome P450
Potassium Channel
|
Infection
|
|
Quinidine hydrobromide is an antiarrhythmic agent. Quinidine is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine hydrobromide is also a K + channel blocker with an IC50 of 19.9 μM. Quinidine hydrobromide can be used for malaria research.
|
-
- HY-109177
-
|
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; 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-P5865
-
|
Theraphotoxin-Tap1a; TRTX-Tap1a; µ/ω-TRTX-Tap1a
|
Sodium Channel
|
Neurological Disease
|
|
Tap1a (Theraphotoxin-Tap1a) is a spider venom peptide that inhibits sodium channels with IC50s of 80 nM and 301 nM against Nav1.7 and Nav1.1, respectively. Tap1a shows analgesic effects.
|
-
- HY-142050
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
(R)-IDHP is an isomer of IDHP, a salvia metabolite that exerts vasorelaxant effects by inhibiting Ca 2+ release and Ca 2+ inward flow in voltage-dependent and receptor-operated calcium channels in vascular smooth muscle cells. IDHP is used in studies of cardiovascular disease.
|
-
- HY-W357818
-
|
GX
|
NF-κB
MEK
ERK
Sodium Channel
|
Cancer
|
|
Glycinexylidide (GX) is the active metabolite of Lidocaine. Lidocaine is a local anesthetic that inhibits sodium channels involving complex voltage and dependence. Lidocaine also reduces the growth, migration and invasion of gastric cancer cells. Glycinexylidide has research potential for use in anesthesia, cancer, and cardiovascular disease.
|
-
- HY-P1074
-
|
|
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-B0562
-
|
|
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 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-120033
-
|
|
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-B1494
-
|
|
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-10015
-
|
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-B1751F
-
-
- HY-147383
-
|
|
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-15084B
-
|
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; CP-16533-1
|
Calcium Channel
P-glycoprotein
Cytochrome P450
|
Metabolic Disease
Cancer
|
|
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
-
|
|
Isotope-Labeled Compounds
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[1][2][3].
|
-
- HY-155017
-
|
|
Sodium Channel
|
Cancer
Neurological Disease
|
|
6-Iodoamiloride is a potent acid-sensing ion channel 1 (ASIC1) inhibitor with an IC50 of 88 nM. 6-Iodoamiloride inhibits ASIC3-mediated currents from rat dorsal root ganglion neurons with an IC50 of 230 nM.
|
-
- HY-14828
-
|
SMP-986
|
mAChR
|
Metabolic Disease
|
|
Afacifenacin (SMP-986) is a potent and orally active muscarinic receptor antagonist. Afacifenacin inhibits the bladder afferent pathway through the sodium-channel blockade, increasing volume, and reducing the frequency of urination and incontinence. Afacifenacin has the potential for the research of overactive bladder (OAB).
|
-
- HY-A0064
-
|
(±)-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-125982
-
|
|
Others
|
Others
|
|
VUAA1 is an insect odorant co-receptor (Orco) agonist. VUAA1 activates both heteromeric and homomeric Orco-containing channels. VUAA1 can disrupt the destructive behaviors of nuisance insects. VUAA1 can be used for insect olfactory research.
|
-
- HY-152107
-
|
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes.
|
-
- HY-P5863
-
|
Mamb-2
|
Sodium Channel
|
Neurological Disease
|
|
Mambalgin-2 (Mamb-2) is an acid-sensitive ion channels (ASICs) inhibitor and a venom peptide. Mambalgin-2 can be obtained from the venom of the African black mamba. Mambalgin-2 can be used in the study of pain and neurological diseases.
|
-
- HY-132268
-
|
|
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-B1751B
-
-
- HY-B0233
-
|
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-P5159
-
|
|
Sodium Channel
|
Inflammation/Immunology
|
|
Crotamine is a Na + channel modulator. Crotamine is a 42 amino acid toxin cross-linked by three disulfide bridges. Crotamine has analgesic activity. Crotamine also interacts with lipid membranes and shows myonecrotic activity. Crotamine can be isolated from Crotalus durissus terrificus venom.
|
-
- HY-P5772
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Jingzhaotoxin-II, a 32 amino acid residues including two acidic and two basic residues, is a neurotoxin. Jingzhaotoxin-II inhibits voltage-gated sodium channels (VGSC) that significantly slows rapid inactivation of TTX-resistant (TTX-R) VGSC on cardiac myocytes with the IC50 of 0.26 μM.
|
-
- HY-B0309
-
|
|
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
-
|
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-D1756
-
|
|
Fluorescent Dye
|
Others
|
|
ROX NHS ester, 6-isomer is a highly fluorescent, and photostable rhodamine dye for various applications. ROX labeled oligonucleotide probes are often used in qPCR, and qPCR instruments have ROX channel. This is reactive dye for the labeling of amino-groups in peptides, proteins, and amino-oligonucleotides. Pure single isomer.
|
-
- HY-B0166S6
-
-
- HY-17436S3
-
|
|
Calcium Channel
|
|
|
(R)-Clevidipine- 13C,d3 is the deuterium and 13C labeled Clevidipine[1]. Clevidipine is a short-acting dihydropyridine calcium channel antagonist (IC50= 7.1 nM, V(H) = -40 mV ) under development for treatment of perioperative hypertension[2].
|
-
- HY-143315
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Protease-Activated Receptor-1 antagonist 3 is a potent protease-activated receptor-1 antagonist with an IC50 value of 7 nM. Protease-Activated Receptor-1 antagonist 3 shows binding affinity for hERG K + channel with an IC50 value of 9 µM.
|
-
- HY-154832
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Cav 3.2 inhibitor 4 (compound 21) is a potent, peripherally restricted, selective T-type calcium channel (Cav3.2) inhibitor, with an IC50 of 0.6 μM. Cav 3.2 inhibitor 4 can be used for the research of atrial fibrillation.
|
-
- HY-B0211S
-
|
PK 26124-13C,15N2
|
GABA Receptor
Sodium Channel
|
|
|
Riluzole- 13C, 15N2 is the 13C and 15N labeled Riluzole[1]. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM[2][3].
|
-
- HY-113673
-
|
|
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-B0267
-
|
|
mAChR
Potassium Channel
|
Neurological Disease
|
|
Oxybutynin is an anticholinergic agent, which inhibits vascular Kv channels in a concentration-dependent manner, with an IC50 of 11.51 μM. Oxybutynin is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P5810
-
|
CcoTx2; β-TRTX-cm1b
|
Sodium Channel
|
Neurological Disease
|
|
Ceratotoxin-2 (CcoTx2) is a voltage-gated sodium channel blocker with IC50s of 8 nM and 88 nM against Nav1.2/β1 and Nav1.3/β1, respectively.
|
-
- HY-P3507
-
|
ShK-186
|
Potassium Channel
|
Metabolic Disease
Inflammation/Immunology
|
|
Dalazatide (ShK-186) is a specific 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-B0495
-
|
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
-
|
2-APV; DL-2-Amino-5-phosphonovaleric acid
|
iGluR
|
Inflammation/Immunology
Neurological Disease
|
|
DL-AP5 (2-APV) is a competitive NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 shows significantly antinociceptive activity. DL-AP5 specifically blocks on channels in the rabbit retina.
|
-
- HY-P1249A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide SF (mouse,rat) TFA 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 TFA increases the amplitude of the sustained current of heterologously expressed acid sensing ion channel 3 (ASIC3) .
|
-
- HY-137563
-
|
|
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
-
|
|
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-114354
-
|
BOD FL alkyne
|
Fluorescent Dye
|
Others
|
|
BODIPY FL alkyne (BOD FL alkyne) is a green-fluorescent dye (Ex=503 nm; Em=512 nm), a bright and photostable fluorophore which emits in fluorescein (FAM) channel. BODIPY FL alkyne can be conjugated with a number of azide-containing molecules by copper-catalyzed Click Chemistry.
|
-
- HY-P5864
-
|
|
Sodium Channel
|
Neurological Disease
|
|
μ-Conotoxin BuIIIA (Mu-Conotoxin BuIIIA) is a voltage-gated sodium channel (VGSC) blocker. μ-Conotoxin BuIIIA is a toxic peptide that can be obtained from the venom of Cone snails. μ-Conotoxin BuIIIA can be used in the study of neurological diseases.
|
-
- HY-132222
-
|
|
TRP Channel
|
Cancer
|
|
SET2 is a selective TRPV2 antagonist (IC50=0.46 μM). SET2 blocks the TRP channel and suppresses prostate cancer cells migration. SET2 reduces the lysophosphatidic acid (LPA, a TRPV2 activator)-induced cytoplasmic calcium increases.
|
-
- HY-147377
-
-
- HY-154831
-
|
N-Behenoyl-D-erythro-sphingosine; Cer d18:1/22:0
|
Others
|
Metabolic Disease
|
|
C22-Ceramide (Cer d18:1/22:0) is an endogenous bioactive sphingolipid. C22-Ceramide reduces the propensity of C16-ceramide channel formation in isolated rat liver mitochondria and in liposomes.
|
-
- HY-B0422
-
|
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
-
|
|
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
-
|
|
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
-
|
|
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
-
|
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-P1410C
-
-
- HY-17402S1
-
-
- HY-12361
-
|
|
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
-
|
|
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-17429S
-
|
R-818-d4
|
Sodium Channel
|
Cardiovascular Disease
|
|
Flecainide-d4 (acetate) is the deuterium labeled Flecainide acetate. Flecainide acetate (R-818) is a class 1C antiarrhythmic agent 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[1][2].
|
-
- HY-119961
-
|
Dexivacaine; (S)-Mepivacaine
|
Others
|
Cardiovascular Disease
|
|
(+)-Mepivacaine is a racemic isomer of Mepivacaine (HY-B0517), which has analgesic and vasoconstrictive activity. Mepivacaine is an amide type agent that temporarily causes local loss of consciousness. Mepivacaine binds to specific voltage-gated sodium channels on neuronal cell membranes, inhibiting sodium influx and membrane depolarization.
|
-
- HY-P5817
-
|
|
Sodium Channel
|
Neurological Disease
|
|
ω-Conotoxin CVIB is a non-selective N- and P/Q-type voltage-gated calcium channels (VGCCs) antagonist. ω-Conotoxin CVIB inhibits depolarization-activated whole-cell VGCC currents in dorsal root ganglion (DRG) neurons with a pIC50 of 7.64.
|
-
- HY-107212
-
|
|
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-B1751
-
-
- HY-17402S2
-
-
- HY-15419A
-
|
|
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-12650
-
|
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-122331
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Norbormide shows vasoconstrictor activity by blocking calcium channel. The activity of Norbormide is species- and tissue-specific, endothelium independent, and is restricted to the peripheral arteries of rat. Norbormide is also a toxicant, and the oral LD50s in mouse, hamster, guinea pig and rabbit are 2250, 140, 620, and 1000 mg/kg.
|
-
- HY-148304A
-
-
- HY-108583
-
|
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-P1952
-
|
|
Sodium Channel
|
Inflammation/Immunology
|
|
μ-Conotoxin-CnIIIC is a 22-residue conopeptide that can be isolated from Conus consors. μ-Conotoxin-CnIIIC is a potent and persistent blocker of NaV1.4 channel. μ-Conotoxin-CnIIIC has analgesic, anaesthetic and myorelaxant properties.
|
-
- HY-17437A
-
-
- HY-B0612AS
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Lercanidipine- 13C,d3 (hydrochloride) is the deuterium and 13C labeled Lercanidipine hydrochloride[1]. Lercanidipine hydrochloride is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine hydrochloride has long lasting antihypertensive action and reno-protective effect[2][3][4].
|
-
- HY-P5853
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
Aam-KTX is a Kv channel inhibitor with IC50 values of 1.1 nM and >750 nM for Kv1.3 and Kv1.1, respectively. Aam-KTX is a toxic peptide obtained from the venom of the scorpion Mesobuthus eupeus. Aam-KTX has potential in autoimmune diseases research.
|
-
- HY-146320
-
|
|
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
-
|
|
Sodium Channel
|
Inflammation/Immunology
Neurological Disease
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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.
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- HY-14186
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WYE-160020
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Potassium Channel
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Cardiovascular Disease
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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.
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- HY-B0166S5
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- HY-146321
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Chloride Channel
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Cancer
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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.
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- HY-15065
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- HY-B0166S2
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- HY-A0236A
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Potassium Channel
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Cardiovascular Disease
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Aprindine hydrochloride is a class I-b anti-arrhythmic agent and a hERG channel blocker with an IC50 of 0.23 μM. Aprindine hydrochloride has inhibitory effects on Na+/Ca2+ exchanger currents, which is partly responsible for their antiarrhythmic and cardioprotective effects. Aprindine hydrochloride is widely used for trial and ventricular tachyarrhythmias research research.
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- HY-12550
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Potassium Channel
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Neurological Disease
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GW542573X is a potent and selective Ca 2+-activated K + 2 (SK2) channels activator. GW542573X induces the Ca 2+-response curve of hSK1 that left-shifted from an EC50 (Ca 2+) value of 410 nM to 240 nM.
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- HY-B0166S4
