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Di-2-ANEPEQ is a voltagesensitive membrane potential fluorescence dye. Di-2-ANEPEQ can be used for the evaluation of voltage-sensitive fluorescence dyes for monitoring neuronal activity in the embryonic central nervous system .
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 .
DiBaC4(5) is a fluorescent voltage-sensitive dye that can be used to monitor the transmembrane potentials when Papain-dissociated retinal cells from adult zebrafish were exposed to GABAergic ligands. DiBaC4(5) is a potential-sensitive fluorescence dye .
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 .
ω-Conotoxin SO3 is a blocker of N-type voltage-sensitivecalcium channel. ω-Conotoxin SO3 is an analgesicω-conotoxin that can be isolated from the venom of C. striatus .
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 .
Carbamazepine is an orally active pressure-sensitive sodium ion channel blocker with an IC50 of 131 μM. Carbamazepine blocks voltage gated Na +, Ca 2+, and K + channels, and is also a HDAC inhibitor (IC50: 2 μM). Carbamazepine is an anticonvulsant and can be used for research of epilepsy and neuropathic pain .
Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitivecalcium channel complexes in the CNS.
Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitivesodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase .
Topiramate (McN 4853) lithium is a broad-spectrum antiepileptic agent. Topiramate lithium is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitivesodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase .
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 .
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 .
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 .
Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitivesodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase .
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 .
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 .
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 .
DiSBAC10 is a voltage-sensitive fluorescent probe used to study cell membrane electrical activity in FRET assays. In a resting polarized cell, DiSBAC10 resides on the outer leaflet of the membrane where it accepts photons from excited fluorescein-labeled proteins and re-emits the photons at a higher wavelength. Depolarization of the cell causes rapid translocation of DiSBAC10 to the inner leaflet of the membrane, thereby increasing the distance between fluorophores and reducing the FRET signal.
Mirogabalin-13C2,d1 (Mixture of Diastereomers) is a C13 and deuterium labeled Mirogabalin. 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 .
Di-4-ANEPPS is a voltage-sensitive dye in membrane potential. Di-4-ANEPPS allows reaching a time resolution better than 1 ms and exhibits changes in fluorescence of up to 10% per 100 mV. Di-4-ANEPPS is a common tool for mapping cardiac electrical activity. Di-4-ANEPPS demonstrate significant direct irreversible effect on spontaneous heart rate and ventricular impulse conduction in rabbit isolated heart model .
Sodium channels conduct sodium ions (Na+) through a cell's plasma membrane that are the source of excitatory currents for the nervous system and muscle. Na channels are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). Dysfunction in voltage-gated sodium channels correlates with neurological and cardiac diseases, including epilepsy, myopathies, pain and cardiac arrhythmias. Sodium channel blockers are used in the treatment of cardiac arrhythmia, pain and convulsion.
MCE offers a unique collection of 128 sodium channel blocker and antagonists, all of which have the identified inhibitory effect on sodium channels. MCE Sodium Channel Blocker Library can be used for neurological and cardiac diseases drug discovery and sodium channel research.
Di-2-ANEPEQ is a voltagesensitive membrane potential fluorescence dye. Di-2-ANEPEQ can be used for the evaluation of voltage-sensitive fluorescence dyes for monitoring neuronal activity in the embryonic central nervous system .
DiBaC4(5) is a fluorescent voltage-sensitive dye that can be used to monitor the transmembrane potentials when Papain-dissociated retinal cells from adult zebrafish were exposed to GABAergic ligands. DiBaC4(5) is a potential-sensitive fluorescence dye .
DiSBAC10 is a voltage-sensitive fluorescent probe used to study cell membrane electrical activity in FRET assays. In a resting polarized cell, DiSBAC10 resides on the outer leaflet of the membrane where it accepts photons from excited fluorescein-labeled proteins and re-emits the photons at a higher wavelength. Depolarization of the cell causes rapid translocation of DiSBAC10 to the inner leaflet of the membrane, thereby increasing the distance between fluorophores and reducing the FRET signal.
Di-4-ANEPPS is a voltage-sensitive dye in membrane potential. Di-4-ANEPPS allows reaching a time resolution better than 1 ms and exhibits changes in fluorescence of up to 10% per 100 mV. Di-4-ANEPPS is a common tool for mapping cardiac electrical activity. Di-4-ANEPPS demonstrate significant direct irreversible effect on spontaneous heart rate and ventricular impulse conduction in rabbit isolated heart model .
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 .
ω-Conotoxin SO3 is a blocker of N-type voltage-sensitivecalcium channel. ω-Conotoxin SO3 is an analgesicω-conotoxin that can be isolated from the venom of C. striatus .
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 .
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 .
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 .
CACNG1 Protein, a regulatory subunit of the voltage-gated calcium channel, contributes to L-type calcium currents in skeletal muscle and modulates channel inactivation kinetics. Collaborating with CACNA1S, CACNB1 or CACNB2, and CACNA2D1, CACNG1 orchestrates a balanced 1:1:1:1 ratio channel assembly, influencing the voltage-gated calcium channel's functionality in skeletal muscle. CACNG1 Protein, Mouse (Cell-Free, His) is the recombinant mouse-derived CACNG1 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of CACNG1 Protein, Mouse (Cell-Free, His) is 223 a.a., with molecular weight of 26.6 kDa.
The CACNA2D1 protein, particularly its α-2/δ subunit, plays a key role in regulating calcium current density and activation/deactivation kinetics of voltage-dependent calcium channels. It contributes to excitation-contraction coupling, coordinating cellular processes. CACNA2D1 Protein, Human (His-SUMO) is the recombinant human-derived CACNA2D1 protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag. The total length of CACNA2D1 Protein, Human (His-SUMO) is 141 a.a., with molecular weight of ~32.3 kDa.
Mirogabalin-13C2,d1 (Mixture of Diastereomers) is a C13 and deuterium labeled Mirogabalin. 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 .
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