Delivery of temperature sensitive items including proteins and kits will be paused on 6/19 for the Juneteenth holiday. For urgent orders please contact customer service.
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 .
Primidone is the orally active inhibitor for TRPM3 (IC50 = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for GABA receptor. Primidone can be used as the analgesic and anticonvulsant agent .
Potassium chloride, for cell culture is potassium chloride that can be used for cell culture. Potassium chloride, for cell culture increases extracellular potassium ion concentration to induce cellular depolarization, thereby activating voltage-gated calcium channels and regulating intracellular calcium signaling. Potassium chloride, for cell culture upregulates Brn-5. Potassium chloride, for cell culture inhibits the proliferation of neurons and some plant cells .
Benzocaine is an orally active local anesthetic. Benzocaine non-competitively inhibits the binding of Ca-ATPase to Ca 2+, with an IC50 of 47.1 mM. Benzocaine exerts anesthetic effects by blocking voltage-gated sodium channels. Benzocaine induces methemoglobinemia in various experimental animals .
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 .
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) .
Nisoxetine is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine is an antidepressant and local anesthetic, it can block voltage-gated sodium channels .
PF-06305591 is a potent and highly selective voltage gated sodium channelNaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile .
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 .
Benzocaine hydrochloride is an orally active local anesthetic. Benzocaine hydrochloride non-competitively inhibits the binding of Ca-ATPase to Ca 2+, with an IC50 of 47.1 mM. Benzocaine hydrochloride exerts anesthetic effects by blocking voltage-gated sodium channels. Benzocaine hydrochloride induces methemoglobinemia in various experimental animals .
Funapide (TV 45070; XEN402) is an orally active inhibitor of voltage-gated sodium channels (VGSC) in the peripheral nervous system with IC50 values ??of 84 nM and 54 nM for Nav1.5 and Nav1.7, respectively. Funapide has analgesic effects .
Proparacaine (Proxymetacaine) hydrochloride is a local anesthetic. Proparacaine hydrochloride blocks voltage-gated sodium channels on neuronal cell membranes, thereby inhibiting signal conduction and nociceptive signal transmission. Proparacaine hydrochloride blocks nociceptive signals in the eye and induces ocular muscle relaxation to reduce eye movement during surgery. Proparacaine hydrochloride is used in research related to cataracts .
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 .
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 .
SOR-C13, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 has anticancer activity .
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 .
S-Bioallethrin (D-Trans-Allethrin) 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. S-Bioallethrin also causes inhibition of lymphocyte proliferation and induces histamine release from human basophils .
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.
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 .
Ebio1 is a selective voltage-gated potassium channelKCNQ2 activator. Ebio1 activates KCNQ2 by generating an extended channelgate with greater conductance at a saturation voltage (+50 mV) .
Oxazosulfyl is a sulfyl insecticide with potent and cross-spectrum insecticidal activity. Oxazosulfyl inhibits sodium currents by binding to and stabilizing the slow-inactivated state of voltage-gated sodium channels, leading to insect paralysis. Oxazosulfyl's ability to block sodium channels is correlated with its insecticidal activity .
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 .
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 .
Phenytoin (sodium) (Standard) is the analytical standard of Phenytoin (sodium). This product is intended for research and analytical applications. 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 .
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 .
N-Desalkylflurazepam (Norfludiazepam) is a long-acting metabolite of benzodiazepine compounds, such as Flurazepam. N-Desalkylflurazepam inhibits L-type voltage-gated calcium channels with IC50 values of 55 μM and 37 μM for Cav1.2 and Cav1.3, respectively .
Primidone (Standard) is the analytical standard of Primidone. This product is intended for research and analytical applications. Primidone is the orally active inhibitor for TRPM3 (IC50 = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for GABA receptor. Primidone can be used as the analgesic and anticonvulsant agent .
KIO-301 chloride hydrochloride is an azobenzene photoswitchable compound that blocks voltage-gated ion channels, including hyperpolarization-activated cyclic nucleotide gating (HCN, during exposure to visible light) ) and voltage-gated potassium channels(voltage-gated potassium channels) .
KIO-301 chloride is an azobenzene photoswitch compound that can block voltage-gated ion channels, including hyperpolarisation-activated cyclic nucleotide-gated (HCN) and voltage-gated potassium channels during exposure to visible light .
Hymenidin is a natural antagonist of serotonergic receptor and inhibitor of voltage-gated potassium channels. Hymenidin also induces cancer cell apoptosis .
Phrixotoxin 3-NH2 TFA is a derivative of Phrixotoxin 3 TFA (HY-P1218A). 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 .
(+)-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 .
Cn2 toxin TFA (β-Mammal toxin Cn2 TFA) is a single-chain β-scorpion neurotoxic peptide that is the main toxin in scorpion venom. Cn2 toxin (TFA) specifically targets mammalian voltage-gated sodium channels (VGSC) Nav1.6 .
SOR-C13 TFA, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 TFA has anticancer activity .
Poneratoxin acetate is the acetate salt form of Poneratoxin (HY-P10234). Poneratoxin acetate is the modulator for voltage-gated sodium channel (NaV, EC50 for NaV1.6 and NaV1.7 is 97 nM and 2.3 µM), that lowers the voltage threshold for activation and inhibits the inactivation of channels, enhances the excitability of neurons, and leads to the transmission of pain signals .
Dendrotoxin-I (DTX-I) TFA is a potent K +channel blocker with IC50s of 0.13-50 nM for voltage-gated potassium channel subunits KV1.1, KV1.2 and KV1.6. Dendrotoxin-I TFA, a neurotoxin, has the potential for cancer research .
(R)-(+)-Bupivacaine hydrochloride is a voltage-gated sodium channel inhibitor. (R)-(+)-Bupivacaine hydrochloride can selectively block the voltage-gated sodium channels on nerve cell membranes, inhibit the influx of sodium ions, and thus prevent the generation and conduction of nerve impulses, exerting local anesthetic activity. (R)-(+)-Bupivacaine hydrochloride can be used in research of acute pains .
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 .
PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channelNaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile .
Licarbazepine (Standard) is the analytical standard of Licarbazepine. This product is intended for research and analytical applications. Licarbazepine (BIA 2-005; GP 47779) is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects .
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 .
Poneratoxin is the modulator for voltage-gated sodium channel (NaV, EC50 for NaV1.6 and NaV1.7 is 97 nM and 2.3 µM), that lowers the voltage threshold for activation and inhibits the inactivation of channels, enhances the excitability of neurons, and leads to the transmission of pain signals .
ztz240 is a chemical modulator of voltage-gated potassium channel Kv7 (KCNQ) (KCNQ2 and 3: EC50=6.1 μM; KCNQ4: EC50=12.2 μM). ztz240 can be used in analgesia and anti-epileptic research .
Gonyautoxin II is a paralytic shellfish poisoning toxin. Gonyautoxin II can block of the voltage-gated sodium channels at axonal level, impeding nerve impulse propagation. Gonyautoxin II has killing activity against mouse neuroblastoma cells. Gonyautoxin II can be used for the researches of cancer and neurological disease .
Dendrotoxin-I (DTX-I) is a potent K +channels blocker with IC50s of 0.13-50 nM for voltage-gated potassium channel subunits KV1.1, KV1.2 and KV1.6, respectively. Dendrotoxin-I, a neurotoxin, has the potential for cancer research .
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 .
Licarbazepine-d4 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects .
Licarbazepine-d3 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects .
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 .
Jasmolin II is an insecticide targeting voltage-gated sodium channels in insects. Jasmolin II leads to neuronal hyperexcitation and insect paralysis. Jasmolin II is promising for research of agricultural pests .
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 .
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].
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 .
(R)-Eslicarbazepine acetate (BIA 2-059) is the R-enantiomer of Eslicarbazepine acetate (HY-B0703). Eslicarbazepine acetate is an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel .
Eslicarbazepine acetate (Standard) is the analytical standard of Eslicarbazepine acetate. This product is intended for research and analytical applications. Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
Eslicarbazepine acetate (Standard) is the analytical standard of Eslicarbazepine acetate. This product is intended for research and analytical applications. Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
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 .
Nalanthalide is a voltage-gated potassium channelKv1.3 blocker (IC50=3.9 µM) and a potential immunosuppressant. Nalanthalide can be used for research on inflammatory immune diseases, such as neuroinflammation .
Eslicarbazepine acetate-d4 is deuterated labeled Eslicarbazepine acetate (HY-B0703). Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
Eslicarbazepine Acetate-d3 is the deuterium labeled Eslicarbazepine acetate (HY-B0703). Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
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 .
Evenamide hydrochloride is an orally available voltage-gated sodium channel (VGSC) blocker (Ki=0.4 μM) for the research of schizophrenia. Evenamide hydrochloride shows efficacy in a broad spectrum of rodent models of psychosis, mania, depression, and aggressiveness .
FluoBar1 is an imaging fluorescence probe modified by a barbiturate ligand with fluorescent coumarin. FluoBar1 can monitor L-type voltage-gated calcium channels (LTCC) in living cells in real time for the study of neurological diseases .
Nisoxetine (Standard) is the analytical standard of Nisoxetine. This product is intended for research and analytical applications. Nisoxetine is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine is an antidepressant and local anesthetic, it can block voltage-gated sodium channels .
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 .
Primidone-d5 is the deuterium labeled Primidone. Primidone is the orally active inhibitor for TRPM3 (IC50 = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for GABA receptor. Primidone can be used as the analgesic and anticonvulsant agent .
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 .
UK-78282 is a selective Kv1.3 voltage-gated potassium channel inhibitor with an IC50 of 200 nM. UK-78282 also inhibit Kv1.4 potassium channel. UK-78282 can inhibit human T cell activation .
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 .
Phenytoin- 15N2, 13C is the 13C and 15N 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 .
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-Grammotoxin SIA (GrTx) is P/Q and N-type voltage-gated Calcium channels inhibitor. ω-Grammotoxin SIA is also a protein toxin that can be obtained from spider venom. ω-Grammotoxin SIA has the potential to study neurological diseases as well as cardiovascular diseases .
Nav1.8-IN-5 (Example 1) is a voltage-gated sodium channelNav1.8 inhibitor. Nav1.8-IN-5 can be used for Nav1.8-mediated diseases, such as pain and pain-related disorders, as well as cardiovascular diseases (such as atrial fibrillation) research .
DPI 201-106 (Standard) is the analytical standard of DPI 201-106. This product is intended for research and analytical applications. 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 .
Calcium Channel antagonist 6 (Compound 328) is a highly selective antagonist of voltage-gated calcium channel CaV2.2 with an IC50 value of 0.37 μM. Calcium Channel antagonist 6 inhibits of neuron depolarization-induced Ca 2+ influx. Calcium Channel antagonist 6 is promising for research of neuropathic pain .
Gonyautoxin III (GTX-III) is a paralytic shellfish poisoning toxin. Gonyautoxin III can block of the voltage-gated sodium channels at axonal level with an IC50 of 14.9 nM, impeding nerve impulse propagation. Gonyautoxin III has killing activity against mouse neuroblastoma cells. Gonyautoxin III can be used for the researches of cancer and neurological disease .
Pincainide is a calcium channel inhibitor. Pincainide inhibits voltage-gated calcium channel-mediated calcium influx in smooth muscle. Pincainide inhibits norepinephrine- and high potassium-induced contractile responses. Pincainide can be used in the research of heart diseases .
Nav1.8-IN-23 is a Nav1.8voltage-gated sodium channel inhibitor with a pIC50 of 6.1. Nav1.8-IN-23 can be used for the research of pain-related diseases .
Fotocaine is a photochromic blocker of voltage-gated ion channels. Fotocaine is readily taken up by neurons in brain slices and enables optical control of action potential firing by switching between 350 and 450 nm light. Fotocaine can be used in analgesia research .
Suzetrigine N-oxide (the third compound in P57) is a derivative of Suzetrigine (HY-148800). Suzetrigine N-oxide is an inhibitor of voltage-gated sodium channels (Nav1.8) and can be used for research on the treatment of pain, especially neuropathic pain .
Human FGF12 mRNA encodes the human fibroblast growth factor 12 (FGF12) protein, a member of the fibroblast growth factor (FGF) family. FGF12 probably involves in nervous system development and function, and the positive regulation of voltage-gated sodium channel activity.
Sodium Channel-IN-7 (Example 59) is a NaV1.7voltage-gated sodium channel inhibitor.Sodium Channel-IN-7 binds to the VSD4 binding pocket of NaV1.7, with reduced interaction with Try1537.Sodium Channel-IN-7 can be used for the research of pain .
AM-2099 (Standard) is the analytical standard of AM-2099 (HY-100727). This product is intended for research and analytical applications. AM-2099 is a potent and selective inhibitor of voltage-gated sodium channel Nav1.7 with an IC50 of 0.16 μM for human Nav1.7.
Proparacaine (Proxymetacaine) is a local anesthetic. Proparacaine blocks voltage-gated sodium channels on neuronal cell membranes, thereby inhibiting signal conduction and nociceptive signal transmission. Proparacaine blocks nociceptive signals in the eye and induces ocular muscle relaxation to reduce eye movement during surgery. Proparacaine is used in research related to cataracts .
Kv3 activator-1 is a Kv3 family voltage-gated potassium channel activator. Kv3 activator-1 reverses mechanical hyperalgesia in rat models of neuropathic and inflammatory pain, with rapid onset and long-lasting, dose-related effects. Kv3 activator-1 can be used for the research of pain .
Lamotrigine-d3 is the deuterium labeled Lamotrigine . Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al .
Lamotrigine- 13C3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al .
AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channelNaV1.7 with IC50s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM .
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. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .
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 .
Diphenidol is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol is also a potent non-specific blocker of voltage-gated ion channels (Na +, K +, and Ca 2+) in neuronal cells. Diphenidol can be used in the study of antivertigo and antinausea .
KGP-25 is an inhibitor of voltage-gated sodium channel 1.8 (Nav1.8), which can be used for analgesia by targeting Nav1.8 in the peripheral nervous system (PNS). KGP-25 can also target γ-aminobutyric acid subtype A receptor (GABAA) in the central nervous system (CNS) for general anesthesia .
Benzocaine-d4 is the deuterium labeled Benzocaine (HY-Y0258). Benzocaine is an orally active local anesthetic. Benzocaine non-competitively inhibits the binding of Ca-ATPase to Ca 2+, with an IC50 of 47.1 mM. Benzocaine exerts anesthetic effects by blocking voltage-gated sodium channels. Benzocaine induces methemoglobinemia in various experimental animals .
Benzocaine-(ethyl-d5) is the deuterium labeled Benzocaine (HY-Y0258). Benzocaine is an orally active local anesthetic. Benzocaine non-competitively inhibits the binding of Ca-ATPase to Ca 2+, with an IC50 of 47.1 mM. Benzocaine exerts anesthetic effects by blocking voltage-gated sodium channels. Benzocaine induces methemoglobinemia in various experimental animals .
Proparacaine (Hydrochloride) (Standard) is the analytical standard of Proparacaine (Hydrochloride). This product is intended for research and analytical applications. Proparacaine hydrochloride is a local anesthetic. Proparacaine hydrochloride blocks voltage-gated sodium channels on neuronal cell membranes, thereby inhibiting signal conduction and nociceptive signal transmission. Proparacaine hydrochloride blocks nociceptive signals in the eye and induces ocular muscle relaxation to reduce eye movement during surgery. Proparacaine hydrochloride is used in research related to cataracts.
N-Desalkylflurazepam (Standard) is the analytical standard of N-Desalkylflurazepam. This product is intended for research and analytical applications. N-Desalkylflurazepam (Norfludiazepam) is a long-acting metabolite of benzodiazepine compounds, such as Flurazepam. N-Desalkylflurazepam inhibits L-type voltage-gated calcium channels with IC50 values of 55 μM and 37 μM for Cav1.2 and Cav1.3, respectively .
N-Desalkylflurazepam-d4 is a deuterated labeled N-Desalkylflurazepam (HY-106454). N-Desalkylflurazepam (Norfludiazepam) is a long-acting metabolite of benzodiazepine compounds, such as Flurazepam. N-Desalkylflurazepam inhibits L-type voltage-gated calcium channels with IC50 values of 55 μM and 37 μM for Cav1.2 and Cav1.3, respectively .
Zeta-Cypermethrin is a type II pyrethroid insecticide. Zeta-Cypermethrin primarily acts on voltage-gated sodium channels in nerve cells, causing delayed channel closure, persistent nerve excitation and convulsions. In Drosophila, Zeta-Cypermethrin rapidly induces extremely high metabolic resistance that can be screened, and exhibits in vitro genotoxicity to human peripheral blood lymphocytes .
Lamotrigine- 13C,d3 is the 13C- and deuterium labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al .
Benzocaine (Standard) is the analytical standard of Benzocaine (HY-Y0258). This product is intended for research and analytical applications. Benzocaine is an orally active local anesthetic. Benzocaine non-competitively inhibits the binding of Ca-ATPase to Ca 2+, with an IC50 of 47.1 mM. Benzocaine exerts anesthetic effects by blocking voltage-gated sodium channels. Benzocaine induces methemoglobinemia in various experimental animals .
Lamotrigine- 13C2, 15N is the 13C and 15N labeled Lamotrigine . Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al .
ILS-920 is a nonimmunosuppressive Rapamycin analog with reduced immunosuppressive activity and potent neuroprotective activity. ILS-920 binds selectively to the immunophilin FKBP52 and to the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 shows 200-fold selectivity for FKBP52 versus FKBP12 .
Benzocaine hydrochloride (Standard) is an analytical standard of Benzocaine hydrochloride (HY-Y0258A). This product is intended for research and analytical applications. Benzocaine hydrochloride is an orally active local anesthetic. Benzocaine hydrochloride non-competitively inhibits the binding of Ca-ATPase to Ca 2+, with a IC50 of 47.1 mM. Benzocaine hydrochloride exerts anesthetic effects by blocking voltage-gated sodium channels. Benzocaine hydrochloride induces methemoglobinemia in various experimental animals .
Nav1.7-IN-3 (Standard) is the analytical standard of Nav1.7-IN-3 (HY-101789). This product is intended for research and analytical applications. Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration .
Nav1.7-IN-22 (P58 13-2) is a selective inhibitor of voltage-gated sodium channelNav1.7. Nav1.7-IN-22 inhibits abnormal electrical signal generation and conduction in sensory neurons by blocking Nav1.7 channel activity. Nav1.7-IN-22 can be used for the study of 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 .
HV1-IN-1 hydrochloride is an inhibitor of the human voltage-gated proton channel (hHV1). HV1-IN-1 hydrochloride works by binding to the VSD of the HV1channel. The VSD is a component of the HV1channel that is responsible for detecting changes in membrane potential and triggering the opening of the channel. HV1-IN-1 hydrochloride can be used in the study of cancer, neuroinflammation and immune response .
Corza6 is a potent and selective human voltage-gated proton channel (hHv1) peptide inhibitor. Corza6 binds to the external voltage sensor domain (VSD) loop in hHv1 with a Kd of ~1 nM at the natural, hyperpolarized resting membrane potential (RMP) of mammalian cells. Corza6 allows capacitation in sperm and permits sustained reactive oxygen species (ROS) production in white blood cells (WBCs) .
DSP-2230 is the orally active inhibitor for voltage-gated sodium channel that inhibits Nav1.7-, Nav1.8-, and Nav1.9-derived sodium currents with IC50s of 7.1 μM, 11.4 μM and 6.7 μM, respectively. DSP-2230 can be used to improve neuropathic pain .
Veratridine (Standard) is the analytical standard of Veratridine. This product is intended for research and analytical applications. 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 .
Scorpion toxin Tf2 is a selective human voltage-gated sodium channelNav1.3 (hNav1.3) activator. Scorpion toxin Tf2 selectively shifts the channel's activation voltage to more negative values, enabling channel opening at resting membrane potentials. Scorpion toxin Tf2 can be used for the research of epilepsy, nociception (after spinal cord injury) .
Lamotrigine- 13C3,d3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al .
MK-5661 is an orally potent NaV1.8voltage-gated sodium channel inhibitor with an EC50 of 4.3 nM. MK-5661 selectively inhibits peripheral nociceptive signaling mediators. MK-5661 reduces capsaicin-induced spontaneous nociceptive behaviors in humanized rats and attenuates capsaicin-induced skin flushing responses in rhesus monkeys. MK-5661 is applicable for pain-related research .
Guangxitoxin 1E TFA is the TFA salt form of Guangxitoxin 1E (HY-P1427). Guangxitoxin 1E TFA is a peptide toxin and a selective inhibitor for voltage-gated potassium channelKV2.1 and KV2.2 with IC50 of 1-3 nM. Guangxitoxin 1E TFA enhances glucose-stimulated intracellular calcium ion oscillations and increases insulin secretion in a glucose-dependent manner .
VGSCs-IN-1 (compound 14), a 2-piperazine analog of Riluzole (HY-B0211), is a human voltage-gated sodium channels (VGSCs) inhibitor. VGSCs-IN-1 shows great Nav1.4 blocking activity. VGSCs-IN-1 has a pKa of 7.6 and a cLog P of 2.4. VGSCs-IN-1 can be used for cell excitability disorders research .
Nisoldipine (BAY-k 5552; Sular) is an orally active and blood-brain barrier-penetrating dihydropyridine calcium antagonist, with greater vascular selectivity than other calcium channel antagonists. Nisoldipine inhibits calcium influx and blocks voltage-gated calcium channels. Nisoldipine dilates coronary and systemic arteries. Nisoldipine has antihypertensive and anti-anginal activity. Nisoldipine also displays neuroprotective and antiviral activity .
Corza6 TFA is a potent and selective human voltage-gated proton channel (hHv1) peptide inhibitor. Corza6 TFA binds to the external voltage sensor domain (VSD) loop in hHv1 with a Kd of ~1 nM at the natural, hyperpolarized resting membrane potential (RMP) of mammalian cells. Corza6 TFA allows capacitation in sperm and permits sustained reactive oxygen species (ROS) production in white blood cells (WBCs) .
ProTx-III is a selective and potent inhibitor of voltage-gated sodium channelNav1.7, with an IC50 of 2.1 nM. ProTx-III is a spider venom peptide isolated from the venom of the Peruvian green velvet tarantella. ProTx-III has a typical inhibitor cystine knot motif (ICK). ProTx-III is able to reverse the pain response. ProTx-III can be used to study diseases such as chronic pain, epilepsy, and arrhythmia .
Flumethrin (FCR 2769) is a pyrethroid insecticide and acaricide . Flumethrin targets voltage-gated sodium channels and estrogen receptor α (ERα). Flumethrin induces cytotoxicity, apoptosis, genotoxicity and DNA damage in breast cancer cells by regulating the expression of BCL2, BAX, TP53 and P21 genes. Flumethrin is applicable to relevant studies on ectoparasite infections (tick and flea burdens) in dogs and cats, as well as breast cancer .
Diphenidol (hydrochloride) (Standard) is the analytical standard of Diphenidol (hydrochloride). This product is intended for research and analytical applications. Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na+, K+, and Ca2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea [4] .
Nav1.8-IN-20 (Compound I) is an orally active and potent voltage-gated sodium channel Nav1.8 inhibitor with an IC50 value of 14 nM. Nav1.8-IN-20 blocks the generation and conduction of action potentials in peripheral nociceptive neurons, exerting analgesic effects. Nav1.8-IN-20 is promising for research of various pain types such as acute pain, chronic pain, inflammatory pain, and neuropathic pain .
QO-83, Retigabine analogue, is a voltage-gated potassium channel KCNQ2 (Kv7.2) activator with an EC50 of 0.56 μM. QO-83 binds to a single hydrophobic pocket of KCNQ2-CaM complex in closed conformation. QO-83 induces a negative shift in the voltage-dependent activation curve of KCNQ2 channels, increasing the channel's voltage sensitivity. QO-83 can be used for the research of epilepsies .
Vinpocetine-d5 is the deuterium labeled Vinpocetine. Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na+ channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders .
(S)-(+)-Docosahexaenyl-2'-hydroxy-1'-propylamide (N-Docosahexacnoylethanolamide(22:6)) is a DHEA homolog. (S)-(+)-Docosahexaenyl-2'-hydroxy-1'-propylamide blocks the Shaker-related voltage-gated potassium channels. (S)-(+)-Docosahexaenyl-2'-hydroxy-1'-propylamide can inhibit the Kv1.2 K+ currents with an IC50 of 1.5 μM .
Diphenidol-d10 (hydrochloride) (Difenidol hydrochloride-d10) is deuterium labeled Diphenidol (hydrochloride). 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. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .
HV1-IN-2 (Compound 14c) is a human voltage-gated proton channel (HV1) inhibitor with an IC50 of 2.14 μM. HV1-IN-2 has a potent anticancer activity with significant antiproliferative effects against THP-1 and MCF-7 cells. HV1-IN-2 can be used for cancers research, such as colorectal tumours, leukaemia, and breast cancer .
Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
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 .
Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
Articaine (Standard) is the analytical standard of Articaine. This product is intended for research and analytical applications. Articaine (Hoe-045 free base) is an amide agent that can suppress or relieve pain. containing an ester group, reversibly binding to the α-subunit of the voltage-gated sodium channels within the inner cavity of the nerve, can provide effective pain relief. Articaine ameliorates LPS-induced acute kidney injury via inhibition of NF-κB activation and the NLRP3 inflammasome pathway .
Nav1.8-IN-24 is a voltage-gated sodium channelNav1.8 inhibitor with pIC50 values of 7.4 (resting state) and 7.5 (inactivated state), and it exhibits high selectivity for NaV1.1-1.7 subtypes. Nav1.8-IN-24 possesses in vitro safety and drug interaction profiles. Nav1.8-IN-24 can be used for the research of acute pain and chronic neuropathic pain .
Insecticidal agent 21 (Compound 6) is an insecticide that is effective against Culex pipiens larvae (LC50: 0.4 μg/mL). Insecticidal agent 21 achieves multi-target neurotoxicity by inhibiting acetylcholinesterase (AChE) and simultaneously targeting other neural receptors (nicotinic acetylcholine receptors (nAChR), voltage-gated sodium channels (VGSC), and γ-aminobutyric acid receptors (GABAAR)). Insecticidal agent 21 has a strong insecticidal effect and can be used in the development of new insecticides to address the problem of mosquito resistance to traditional insecticides .
Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.
Flumethrin (Standard) (FCR 2769 (Standard)) is the analytical standard of Flumethrin (HY-107835). This product is intended for research and analytical applications. Flumethrin (FCR 2769) is a pyrethroid insecticide and acaricide. Flumethrin targets voltage-gated sodium channels and estrogen receptor α (ERα). Flumethrin induces cytotoxicity, apoptosis, genotoxicity and DNA damage in breast cancer cells by regulating the expression of BCL2, BAX, TP53 and P21 genes. Flumethrin is applicable to relevant studies on ectoparasite infections (tick and flea burdens) in dogs and cats, as well as breast cancer.
5-HT2C-agonist-14 is a 5-HT2C receptor agonist with an EC50 of 2.9 μM against human receptors. It also acts as a voltage-gated sodium channel inhibitor with blood-brain barrier permeable. 5-HT2C-agonist-14 elevates seizure threshold, suppresses seizure progression and alleviates pain-related behaviors. It can be used in the research of epilepsy and pain-related diseases .
6-FAM-AEEAc-Stichodactyla helianthus Neurotoxin (ShK) TFA (6-FAM-AEEAC-SHK TFA) is a peptide neurotoxin conjugated with a fluorescent marker. 6-FAM-AEEAc-Stichodactyla helianthus Neurotoxin (ShK) TFA can block voltage-gated potassium channels (kv1.1 and kv1.2) to prolong the duration of action potentials, thereby affecting the conduction of neural signals. 6-FAM-AEEAc-Stichodactyla helianthus Neurotoxin (ShK) TFA can be used in neuroscience research .
Ssm Spooky Toxin TFA is found in Scolopendra mutilans that potently inhibits KCNQ (voltage-gated potassium channel family 7) channels, with IC50s 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 TFA inhibits cytokine generation by specifically acting on the KV1.3 channel in T cells. Ssm Spooky Toxin TFA plays an essential role in the centipede’s circulatory system .
Lubeluzole is the S-isomer of benzothiazole derivative. Lubeluzole can inhibit glutamate release, glutamate-activated NO synthesis and block voltage-gated Sodium Channel and Calcium Channel. Lubeluzole exhibits anti-ischemic and neuroprotective effects. Lubeluzole also shows anti-bacterial and anti-diarrheal potential. Lubeluzole can inhibit cardiac sodium channel and prolong cardiac action potential. Lubeluzole can inhibit cancer cells proliferation and invasion and shows chemosensitizing effect. Lubeluzole can be used for the researches of cancer, infection, neurological and cardiovascular disease such as stroke, infectious diarrhea and ovarian .
Flumethrin-d5 (FCR 2769-d5) is the deuterium labeled Flumethrin (HY-107835). Flumethrin (FCR 2769) is a pyrethroid insecticide and acaricide . Flumethrin targets voltage-gated sodium channels and estrogen receptor α (ERα). Flumethrin induces cytotoxicity, apoptosis, genotoxicity and DNA damage in breast cancer cells by regulating the expression of BCL2, BAX, TP53 and P21 genes. Flumethrin is applicable to relevant studies on ectoparasite infections (tick and flea burdens) in dogs and cats, as well as breast cancer .
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 .
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 .
Ssm Spooky Toxin is found in Scolopendra mutilans that potently inhibits KCNQ (voltage-gated potassium channel family 7) channels, with IC50s 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 .
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 .
Fluphenazine-d6 (hydrochloride) is deuterium labeled Fluphenazine (hydrochloride). Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
Fluphenazine dimaleate is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dimaleate blocks neuronal voltage-gated sodium channels. Fluphenazine dimaleate acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dimaleate can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dimaleate can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
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 .
Di-4-ANEPPS is a voltage-sensitive dye that acts on voltage-gated ion channels (such as sodium channels) and inhibits sodium current, significantly reducing sodium current density, although specific values like IC50 remain unclear. It mainly binds to the voltage-sensitive regions on the cell membrane, changing its fluorescence properties to reflect membrane potential changes and thus affecting the function of ion channels to exert its activity. This substance can be used in cardiovascular research, such as the electrophysiology of cardiomyocytes, myocardial ischemia, and the effects of drugs on cardiomyocytes. It is of great value in evaluating drug cardiotoxicity and exploring the mechanisms of arrhythmias .
Fluphenazine (dihydrochloride) (Standard) is the analytical standard of Fluphenazine (dihydrochloride). This product is intended for research and analytical applications. Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
C-HBrO-GGT is a sequence-activated two-photon fluorescent probe. C-HBrO-GGT exhibits sequential fluorescence activation properties: it generates fluorescence in response to hypobromous acid only after being hydrolytically activated by γ-glutamyl transpeptidase. C-HBrO-GGT enables verification of the voltage-gated chloride channel (CLC-1)-HBrO-catalase (CAT)-GGT signaling pathway at the cellular level. C-HBrO-GGT can serve as a tool to indicate the precise location of mature atherosclerotic plaques and provide early warning of plaque formation. C-HBrO-GGT is applicable to relevant research on atherosclerosis .
Ceratotoxin-1 (CcoTx1), a peptide toxin, is an voltage-gated sodium channel subtypes inhibitor. Ceratotoxin-1 inhibits Nav1.1/β1, Nav1.2/β1, Nav1.4/β1, and Nav1.5/β1 with IC50 of 523 nM, 3 nM, 888 nM, and 323 nM, respectively. Ceratotoxin-1 also inhibits Nav1.8/β1 .
Lubeluzole dihydrochloride is the dihydrochloride salt of Lubeluzole (HY-105084). Lubeluzole dihydrochloride is the S-isomer of benzothiazole derivative. Lubeluzole dihydrochloride can inhibit glutamate release, glutamate-activated NO synthesis and block voltage-gated Sodium Channel and Calcium Channel. Lubeluzole dihydrochloride exhibits anti-ischemic and neuroprotective effects. Lubeluzole dihydrochloride also shows anti-bacterial and anti-diarrheal potential. Lubeluzole dihydrochloride can inhibit cardiac sodium channel and prolong cardiac action potential. Lubeluzole dihydrochloride can inhibit cancer cells proliferation and invasion and shows chemosensitizing effect. Lubeluzole dihydrochloride can be used for the researches of cancer, infection, neurological and cardiovascular disease such as stroke, infectious diarrhea and ovarian .
Crisugabalin is an orally active, selective ligand for the α2δ subunit of voltage-gated calcium channels, with a target IC50 of 3.96 nM in rats. Crisugabalin inhibits the binding of [ 3H]gabapentin to the α2δ subunit, reduces calcium influx, decreases neuronal excitability, and impairs nociceptive transmission. Crisugabalin alleviates mechanical allodynia, neuropathic pain and inflammatory pain in rats, and reduces phase II pain behaviors. Crisugabalin can be used in research related to chronic pain, neuropathic pain, diabetic neuropathy, fibromyalgia, inflammatory pain, diabetic peripheral neuropathy and postherpetic neuralgia.
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).
γ-Cyhalothrin is an orally active, blood-brain barrier permeable Type II synthetic pyrethroid insecticide. γ-Cyhalothrin is the insecticidally active enantiomer of λ-Cyhalothrin (HY-B0836). γ-Cyhalothrin disrupts voltage-gated sodium channels, induces salivation and reduces spontaneous activity in rats. γ-Cyhalothrin exerts toxic effects on aquatic invertebrates and fish, triggers community-level effects in aquatic ecosystems, and inhibits host-seeking Ixodes scapularis nymphs in residential lawn ecotones. γ-Cyhalothrin is applicable to insecticidal-related research .
Mirogabalin besylate (Standard) is the analytical standard of Mirogabalin besylate (HY-108006). This product is intended for research and analytical applications. Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.
Articaine (Hoe-045) hydrochloride is a selective inhibitor of voltage-gated sodium channels (such as rNav1.4, hNav1.7, and rNav1.8), with an IC50of 15.8 μM for open-state Na +channels, and IC50of 40.6 μM and 378 μM for inactivated and resting-state Na +channels, respectively. Articaine hydrochloride exerts local anesthetic activity by inhibiting Na + influx to block nerve impulse conduction, and can also inhibit NF-κB activation and NLRP3 inflammasome pathways, exhibiting anti-inflammatory function. Articaine hydrochloride can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury) .
Articaine (Hoe-045) is a selective inhibitor of voltage-gated sodium channels (such as rNav1.4, hNav1.7, and rNav1.8), with an IC50of 15.8 μM for open-state Na +channels, and IC50of 40.6 μM and 378 μM for inactivated and resting-state Na +channels, respectively. Articaine exerts local anesthetic activity by inhibiting Na + influx to block nerve impulse conduction, and can also inhibit NF-κB activation and NLRP3 inflammasome pathways, exhibiting anti-inflammatory function. Articaine can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury) .
LTGO-33 is a potent and selective voltage-gated sodium channelNaV1.8 inhibitor. LTGO-33 inhibits NaV1.8 in the nM potency range and exhibits over 600-fold selectivity against human NaV1.1-NaV1.7 and NaV1.9. LTGO-33 exhibits state-independent inhibition with similar potencies on channels in the closed and inactivated conformations. LTGO-33 inhibits native TTX-R NaV1.8 currents in non-human primate and human DRG neurons, where it reduces action potential firing. LTGO-33 can be used for pain disorders research .
Articaine (Hoe-045) hydrochloride (Standard) is the analytical standard of Articaine hydrochloride (HY-B0516). This product is intended for research and analytical applications. Articaine (Hoe-045) hydrochloride is a selective inhibitor of voltage-gated sodium channels (such as rNav1.4, hNav1.7, and rNav1.8), with an IC50of 15.8 μM for open-state Na +channels, and IC50of 40.6 μM and 378 μM for inactivated and resting-state Na +channels, respectively. Articaine hydrochloride exerts local anesthetic activity by inhibiting Na + influx to block nerve impulse conduction, and can also inhibit NF-κB activation and NLRP3 inflammasome pathways, exhibiting anti-inflammatory function. Articaine hydrochloride can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury) .
Articaine (Standard) is the analytical standard of Articaine (HY-B0516A). This product is intended for research and analytical applications. Articaine (Hoe-045) hydrochloride is a selective inhibitor of voltage-gated sodium channels (such as rNav1.4, hNav1.7, and rNav1.8), with an IC50of 15.8 μM for open-state Na +channels, and IC50of 40.6 μM and 378 μM for inactivated and resting-state Na +channels, respectively. Articaine hydrochloride exerts local anesthetic activity by inhibiting Na + influx to block nerve impulse conduction, and can also inhibit NF-κB activation and NLRP3 inflammasome pathways, exhibiting anti-inflammatory function. Articaine hydrochloride can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury) .
Cavα2δ1&NET-IN-2 (Compound 45CS) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-2 inhibits Cavα2δ-1 with a Ki of 454 nM. Cavα2δ1&NET-IN-2 inhibits NET with a Ki of 59 nM and IC50 of 7 nM. Cavα2δ1&NET-IN-2 can be used for research of pain .
Cavα2δ1&NET-IN-1 (Compound 59S) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-1 inhibits Cavα2δ-1 with a Ki of 112 nM. Cavα2δ1&NET-IN-1 inhibits NET with a Ki of 383 nM and IC50 of 67 nM. Cavα2δ1&NET-IN-1 can be used for research of pain .
Zandatrigine (NBI-921352; XEN901) is a selective, orally active, voltage-gated sodium channelNaV1.6/SCN8A inhibitor that can penetrate the blood-brain barrier. Zandatrigine inhibits sodium influx by non-covalently binding to the VSD4 structure of NaV1.6, blocking the persistent and resuscitative currents under pathological conditions. Zandatrigine can reduce neuronal hyperexcitability and reduce epileptic seizures. Zandatrigine is 134-756-fold selective for other isoforms such as NaV1.1 and NaV1.2, and has minimal effect on NaV1.1 expressed by inhibitory interneurons. Zandatrigine can be used to study NaV1.6-mediated neuroexcitability diseases such as SCN8A-related developmental epileptic encephalopathy (SCN8A-DEE) and adult focal epilepsy .
5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2.
UORSY New Generation Screening Library contains about 1,900,000 compounds. The library is a revolutionary collection of lead-like molecules with outstanding structural quality and diversity—New Generation Screening Library (NGSL). Its core is decorated with interesting building blocks, including important medicinal fragments such as peptide bonds, amino groups and hydroxyl groups. and designed for discovery of new Voltage-gated calcium channel blockers.
Potassium channels are the most widely distributed type of ion channel and are found in virtually all living organisms. There are four major classes of K channels: voltage-gated potassium channel, calcium-activated potassium channel, inwardly rectifying potassium channel and tandem pore domain potassium channel. There is growing evidence that dysfunction in potassium channels correlates with several diseases, such as chronic hypertension, diabetes, hypercholesterolemia and atherosclerosis, etc.
MCE Potassium Channel Compound Library consists of 313 potassium channel inhibitor and activators, which is a useful tool to discover drugs for cardiovascular diseases and potassium channel research.
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 187 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-4-ANEPPS is a voltage-sensitive dye that acts on voltage-gated ion channels (such as sodium channels) and inhibits sodium current, significantly reducing sodium current density, although specific values like IC50 remain unclear. It mainly binds to the voltage-sensitive regions on the cell membrane, changing its fluorescence properties to reflect membrane potential changes and thus affecting the function of ion channels to exert its activity. This substance can be used in cardiovascular research, such as the electrophysiology of cardiomyocytes, myocardial ischemia, and the effects of drugs on cardiomyocytes. It is of great value in evaluating drug cardiotoxicity and exploring the mechanisms of arrhythmias .
FluoBar1 is an imaging fluorescence probe modified by a barbiturate ligand with fluorescent coumarin. FluoBar1 can monitor L-type voltage-gated calcium channels (LTCC) in living cells in real time for the study of neurological diseases .
C-HBrO-GGT is a sequence-activated two-photon fluorescent probe. C-HBrO-GGT exhibits sequential fluorescence activation properties: it generates fluorescence in response to hypobromous acid only after being hydrolytically activated by γ-glutamyl transpeptidase. C-HBrO-GGT enables verification of the voltage-gated chloride channel (CLC-1)-HBrO-catalase (CAT)-GGT signaling pathway at the cellular level. C-HBrO-GGT can serve as a tool to indicate the precise location of mature atherosclerotic plaques and provide early warning of plaque formation. C-HBrO-GGT is applicable to relevant research on atherosclerosis .
Potassium chloride, for cell culture is potassium chloride that can be used for cell culture. Potassium chloride, for cell culture increases extracellular potassium ion concentration to induce cellular depolarization, thereby activating voltage-gated calcium channels and regulating intracellular calcium signaling. Potassium chloride, for cell culture upregulates Brn-5. Potassium chloride, for cell culture inhibits the proliferation of neurons and some plant cells .
SOR-C13, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 has anticancer activity .
Corza6 is a potent and selective human voltage-gated proton channel (hHv1) peptide inhibitor. Corza6 binds to the external voltage sensor domain (VSD) loop in hHv1 with a Kd of ~1 nM at the natural, hyperpolarized resting membrane potential (RMP) of mammalian cells. Corza6 allows capacitation in sperm and permits sustained reactive oxygen species (ROS) production in white blood cells (WBCs) .
Corza6 TFA is a potent and selective human voltage-gated proton channel (hHv1) peptide inhibitor. Corza6 TFA binds to the external voltage sensor domain (VSD) loop in hHv1 with a Kd of ~1 nM at the natural, hyperpolarized resting membrane potential (RMP) of mammalian cells. Corza6 TFA allows capacitation in sperm and permits sustained reactive oxygen species (ROS) production in white blood cells (WBCs) .
Phrixotoxin 3-NH2 TFA is a derivative of Phrixotoxin 3 TFA (HY-P1218A). 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 .
Cn2 toxin TFA (β-Mammal toxin Cn2 TFA) is a single-chain β-scorpion neurotoxic peptide that is the main toxin in scorpion venom. Cn2 toxin (TFA) specifically targets mammalian voltage-gated sodium channels (VGSC) Nav1.6 .
SOR-C13 TFA, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 TFA has anticancer activity .
Poneratoxin acetate is the acetate salt form of Poneratoxin (HY-P10234). Poneratoxin acetate is the modulator for voltage-gated sodium channel (NaV, EC50 for NaV1.6 and NaV1.7 is 97 nM and 2.3 µM), that lowers the voltage threshold for activation and inhibits the inactivation of channels, enhances the excitability of neurons, and leads to the transmission of pain signals .
Dendrotoxin-I (DTX-I) TFA is a potent K +channel blocker with IC50s of 0.13-50 nM for voltage-gated potassium channel subunits KV1.1, KV1.2 and KV1.6. Dendrotoxin-I TFA, a neurotoxin, has the potential for cancer research .
Scorpion toxin Tf2 is a selective human voltage-gated sodium channelNav1.3 (hNav1.3) activator. Scorpion toxin Tf2 selectively shifts the channel's activation voltage to more negative values, enabling channel opening at resting membrane potentials. Scorpion toxin Tf2 can be used for the research of epilepsy, nociception (after spinal cord injury) .
Guangxitoxin 1E TFA is the TFA salt form of Guangxitoxin 1E (HY-P1427). Guangxitoxin 1E TFA is a peptide toxin and a selective inhibitor for voltage-gated potassium channelKV2.1 and KV2.2 with IC50 of 1-3 nM. Guangxitoxin 1E TFA enhances glucose-stimulated intracellular calcium ion oscillations and increases insulin secretion in a glucose-dependent manner .
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 .
Ssm Spooky Toxin TFA is found in Scolopendra mutilans that potently inhibits KCNQ (voltage-gated potassium channel family 7) channels, with IC50s 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 TFA inhibits cytokine generation by specifically acting on the KV1.3 channel in T cells. Ssm Spooky Toxin TFA plays an essential role in the centipede’s circulatory system .
Poneratoxin is the modulator for voltage-gated sodium channel (NaV, EC50 for NaV1.6 and NaV1.7 is 97 nM and 2.3 µM), that lowers the voltage threshold for activation and inhibits the inactivation of channels, enhances the excitability of neurons, and leads to the transmission of pain signals .
Dendrotoxin-I (DTX-I) is a potent K +channels blocker with IC50s of 0.13-50 nM for voltage-gated potassium channel subunits KV1.1, KV1.2 and KV1.6, respectively. Dendrotoxin-I, a neurotoxin, has the potential for cancer research .
Ssm Spooky Toxin is found in Scolopendra mutilans that potently inhibits KCNQ (voltage-gated potassium channel family 7) channels, with IC50s 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 .
Ceratotoxin-1 (CcoTx1), a peptide toxin, is an voltage-gated sodium channel subtypes inhibitor. Ceratotoxin-1 inhibits Nav1.1/β1, Nav1.2/β1, Nav1.4/β1, and Nav1.5/β1 with IC50 of 523 nM, 3 nM, 888 nM, and 323 nM, respectively. Ceratotoxin-1 also inhibits Nav1.8/β1 .
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 .
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 .
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 .
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 .
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-Grammotoxin SIA (GrTx) is P/Q and N-type voltage-gated Calcium channels inhibitor. ω-Grammotoxin SIA is also a protein toxin that can be obtained from spider venom. ω-Grammotoxin SIA has the potential to study neurological diseases as well as cardiovascular diseases .
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 .
ProTx-III is a selective and potent inhibitor of voltage-gated sodium channelNav1.7, with an IC50 of 2.1 nM. ProTx-III is a spider venom peptide isolated from the venom of the Peruvian green velvet tarantella. ProTx-III has a typical inhibitor cystine knot motif (ICK). ProTx-III is able to reverse the pain response. ProTx-III can be used to study diseases such as chronic pain, epilepsy, and arrhythmia .
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 .
6-FAM-AEEAc-Stichodactyla helianthus Neurotoxin (ShK) TFA (6-FAM-AEEAC-SHK TFA) is a peptide neurotoxin conjugated with a fluorescent marker. 6-FAM-AEEAc-Stichodactyla helianthus Neurotoxin (ShK) TFA can block voltage-gated potassium channels (kv1.1 and kv1.2) to prolong the duration of action potentials, thereby affecting the conduction of neural signals. 6-FAM-AEEAc-Stichodactyla helianthus Neurotoxin (ShK) TFA can be used in neuroscience research .
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 .
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 .
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 .
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 .
Hymenidin is a natural antagonist of serotonergic receptor and inhibitor of voltage-gated potassium channels. Hymenidin also induces cancer cell apoptosis .
Dendrotoxin-I (DTX-I) is a potent K +channels blocker with IC50s of 0.13-50 nM for voltage-gated potassium channel subunits KV1.1, KV1.2 and KV1.6, respectively. Dendrotoxin-I, a neurotoxin, has the potential for cancer research .
Veratridine (Standard) is the analytical standard of Veratridine. This product is intended for research and analytical applications. 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 .
Jasmolin II is an insecticide targeting voltage-gated sodium channels in insects. Jasmolin II leads to neuronal hyperexcitation and insect paralysis. Jasmolin II is promising for research of agricultural pests .
Eslicarbazepine acetate (Standard) is the analytical standard of Eslicarbazepine acetate. This product is intended for research and analytical applications. Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
Nalanthalide is a voltage-gated potassium channelKv1.3 blocker (IC50=3.9 µM) and a potential immunosuppressant. Nalanthalide can be used for research on inflammatory immune diseases, such as neuroinflammation .
Articaine (Standard) is the analytical standard of Articaine. This product is intended for research and analytical applications. Articaine (Hoe-045 free base) is an amide agent that can suppress or relieve pain. containing an ester group, reversibly binding to the α-subunit of the voltage-gated sodium channels within the inner cavity of the nerve, can provide effective pain relief. Articaine ameliorates LPS-induced acute kidney injury via inhibition of NF-κB activation and the NLRP3 inflammasome pathway .
The CACNA1C protein is the alpha-1C subunit of voltage-gated calcium channels that generate L-type calcium currents that are critical for calcium influx and sarcoplasmic release. Its role in excitation-contraction coupling is critical for cardiac development, rhythm regulation, and smooth muscle cell contraction. CACNA1C Protein, Pig (Cell-Free, His) is the recombinant pig-derived CACNA1C protein, expressed by E. coli Cell-free , with N-10*His labeled tag.
The hERG protein is the α subunit of voltage-gated potassium channels and is critical for mediating cardiac delayed rectifier potassium current (IKr). It lacks individual channel activity but dynamically affects properties by forming heterotetramers with other isoforms. hERG Protein, Human (HEK293, GFP, His) is the recombinant human-derived hERG protein, expressed by HEK293 , with C-10*His, C-GFP labeled tag.
The hERG protein is the α subunit of voltage-gated potassium channels and is critical for mediating cardiac delayed rectifier potassium current (IKr). It lacks individual channel activity but dynamically affects properties by forming heterotetramers with other isoforms. hERG Protein, Human (HEK293) is the recombinant human-derived hERG protein, expressed by HEK293, with tag free.
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.
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 .
Lamotrigine- 13C3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al .
Lamotrigine-d3 is the deuterium labeled Lamotrigine . Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al .
Lamotrigine- 13C2, 15N is the 13C and 15N labeled Lamotrigine . Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al .
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
Lamotrigine- 13C,d3 is the 13C- and deuterium labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al .
Licarbazepine-d4 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects .
Licarbazepine-d3 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects .
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 .
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].
Eslicarbazepine acetate-d4 is deuterated labeled Eslicarbazepine acetate (HY-B0703). Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
Eslicarbazepine Acetate-d3 is the deuterium labeled Eslicarbazepine acetate (HY-B0703). Eslicarbazepine acetate (BIA 2-093), an antiepileptic agent, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
Primidone-d5 is the deuterium labeled Primidone. Primidone is the orally active inhibitor for TRPM3 (IC50 = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for GABA receptor. Primidone can be used as the analgesic and anticonvulsant agent .
Phenytoin- 15N2, 13C is the 13C and 15N 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 .
Benzocaine-d4 is the deuterium labeled Benzocaine (HY-Y0258). Benzocaine is an orally active local anesthetic. Benzocaine non-competitively inhibits the binding of Ca-ATPase to Ca 2+, with an IC50 of 47.1 mM. Benzocaine exerts anesthetic effects by blocking voltage-gated sodium channels. Benzocaine induces methemoglobinemia in various experimental animals .
Benzocaine-(ethyl-d5) is the deuterium labeled Benzocaine (HY-Y0258). Benzocaine is an orally active local anesthetic. Benzocaine non-competitively inhibits the binding of Ca-ATPase to Ca 2+, with an IC50 of 47.1 mM. Benzocaine exerts anesthetic effects by blocking voltage-gated sodium channels. Benzocaine induces methemoglobinemia in various experimental animals .
N-Desalkylflurazepam-d4 is a deuterated labeled N-Desalkylflurazepam (HY-106454). N-Desalkylflurazepam (Norfludiazepam) is a long-acting metabolite of benzodiazepine compounds, such as Flurazepam. N-Desalkylflurazepam inhibits L-type voltage-gated calcium channels with IC50 values of 55 μM and 37 μM for Cav1.2 and Cav1.3, respectively .
Lamotrigine- 13C3,d3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al .
Vinpocetine-d5 is the deuterium labeled Vinpocetine. Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na+ channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders .
Diphenidol-d10 (hydrochloride) (Difenidol hydrochloride-d10) is deuterium labeled Diphenidol (hydrochloride). 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. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea .
Fluphenazine-d6 (hydrochloride) is deuterium labeled Fluphenazine (hydrochloride). Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
Flumethrin-d5 (FCR 2769-d5) is the deuterium labeled Flumethrin (HY-107835). Flumethrin (FCR 2769) is a pyrethroid insecticide and acaricide . Flumethrin targets voltage-gated sodium channels and estrogen receptor α (ERα). Flumethrin induces cytotoxicity, apoptosis, genotoxicity and DNA damage in breast cancer cells by regulating the expression of BCL2, BAX, TP53 and P21 genes. Flumethrin is applicable to relevant studies on ectoparasite infections (tick and flea burdens) in dogs and cats, as well as breast cancer .
Elsunersen is an antisense oligonucleotide that selectively decreases expression of the gene for the voltage-gated sodium channel Nav1.2 (SCN2A). It is used for the study of SCN2A developmental and epileptic encephalopathy (SCN2A-DEE). SCN2A-DEE is a debi
Elsunersen sodium is an antisense oligonucleotide that selectively decreases expression of the gene for the voltage-gated sodium channel Nav1.2 (SCN2A). It is used for the study of SCN2A developmental and epileptic encephalopathy (SCN2A-DEE). SCN2A-DEE is
Human FGF12 mRNA encodes the human fibroblast growth factor 12 (FGF12) protein, a member of the fibroblast growth factor (FGF) family. FGF12 probably involves in nervous system development and function, and the positive regulation of voltage-gated sodium channel activity.
Inquiry Online
Your information is safe with us. * Required Fields.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedChemExpress values your privacy and your trust is important to us. We use cookies to enhance your website experience. Some cookies are necessary to run the website.
Privacy and Cookie Policy
