Search Result
Results for "
excitability
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-105182
-
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LY-246708
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mAChR
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Neurological Disease
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Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .
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- HY-101897
-
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Fura-2 Acetoxymethyl ester
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Fluorescent Dye
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Others
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Fura-2 AM is a membrane permeable, intracellular, UV light-excitable and ratiometric fluorescent Ca 2+ (calcium ion) indicator. Fura-2 AM crosses cell membranes and is converted to Fura-2 (HY-D0110A) via cellular esterases. Fura-2 AM can be used to detect calcium in cells.
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- HY-Y1683
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Racementhol
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Environmental Pollutants
GABA Receptor
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Infection
Neurological Disease
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DL-Menthol (Racementhol) is an orally active, GABAaR positive allosteric modulator and UDP-glucuronosyltransferase (UGT) inhibitor that can cross the blood-brain barrier. DL-Menthol binds to GABAAR and exhibits an allosteric activation effect, enhancing GABA-mediated chloride influx and inhibiting neuronal excitability. DL-Menthol can induce surgical anesthesia in fish and inhibit the metabolic detoxification of tobacco carcinogens by human liver and intestinal UGT enzymes, resulting in reduced NNAL-N-Gluc production .
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- HY-105182A
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LY 246708 tartrate
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mAChR
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Neurological Disease
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Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia .
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- HY-100784
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EAAT
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Neurological Disease
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Dihydrokainic acid is a glutamate transporters (especially GLT1) inhibitor. Dihydrokainic acid targets GLT1 with high affinity, effectively inhibiting its transport function. Dihydrokainic acid exerts its effect by inhibiting the uptake of glutamate, leading to an increase in extracellular glutamate concentration, thereby affecting neuronal excitability and neurotransmission. Dihydrokainic acid is mainly applied in the field of neuroscience for research on glutamate-related neural functions, epilepsy, learning, and memory .
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- HY-N6789
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KT5720
4 Publications Verification
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PKA
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Neurological Disease
Cancer
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KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 + concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases .
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- HY-142240
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HSK16149
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Calcium Channel
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Neurological Disease
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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.
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- HY-148792
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PRAX-562
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Sodium Channel
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Neurological Disease
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Relutrigine (PRAX-562) is an orally active inhibitor of persistent sodium channel. Relutrigine potently and preferentially inhibits persistent INa induced by ATX-II (Nav 1.5 activator) or the SCN8A mutation N1768D with IC50 values of 141 nM and 75 nM, respectively. Relutrigine exhibits potent use-dependent block and reduces neuronal intrinsic excitability. Relutrigine has effective anticonvulsant activity .
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- HY-N5060
-
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4-Allylanisole
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Environmental Pollutants
Parasite
Apoptosis
Keap1-Nrf2
NF-κB
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Infection
Neurological Disease
Inflammation/Immunology
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Estragole (4-Allylanisole) is a relatively nontoxic volatile terpenoid ether and major component of the essential oil from many plants. Estragole significantly triggers Apoptosis, suppresses LPS-induced intracellular ROS production. Estragole activats Nrf-2 and regulates NF-κB. Estragole has anti-toxoplasma, anti-inflammatory, anti-edema, antioxidant and immunomodulatory properties. Estragole blocks DRG neuron excitability. Estragole has improves gastric ulcer activity .
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- HY-P1626
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Opioid Receptor
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Neurological Disease
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Acetyl tetrapeptide-15 is a synthetic peptide. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway. Acetyl tetrapeptide-15 is used in the cosmetics for sensitive skin .
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- HY-124467
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Ro 07-4065
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GABA Receptor
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Neurological Disease
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Difludiazepam (Ro 07-4065), a benzodiazepine derivative, is a GABAA receptor ligand with an IC50 of 4.1 nM. Difludiazepam binds to an allosteric site on the GABAA receptor to potentiate the receptor's response to GABA, reducing neuron excitability. Difludiazepam contains halogenated groups at the ortho position of its phenyl ring .
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- HY-148410A
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STK-001 sodium
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Sodium Channel
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Neurological Disease
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Zorevunersen sodium is an antisense oligonucleotide targeting the Scn1a gene based on TANGO technology. Zorevunersen sodium increases Scn1a mRNA transcripts and elevates the expression level of NaV1.1 protein. Zorevunersen sodium restores the excitability of PV interneurons, thereby reducing seizures and prolonging survival in mice. Zorevunersen sodium can be used for research on Dravet syndrome .
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- HY-D0127
-
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Fluorescent Dye
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Others
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Merocyanin 540 is a fluorescent membrane probe that selectively stains the membranes of a wide variety of electrically excitable cells, but not those of nonexcitable cells (Ex/Em: 540/580 nm) .
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- HY-108594
-
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Potassium Channel
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Metabolic Disease
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PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability .
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- HY-W013712
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Potassium Channel
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Neurological Disease
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GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect .
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- HY-143481
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Sodium Channel
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Neurological Disease
Inflammation/Immunology
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Nav1.8-IN-2 (compound 35A) is a Nav1.8 voltage-gated sodium ion inhibitor with an IC50 of 0.4 nM (HEK 293 cells). Nav1.8-IN-2 inhibits the activity of Nav1.8 voltage-gated sodium ion channels, mediates sodium ion influx in excitable cells, and is associated with the initiation and conduction of action potentials. Nav1.8-IN-2 can be used for research related to pain, cough, itching, etc .
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- HY-W014504
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Endogenous Metabolite
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Metabolic Disease
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DL-Kynurenine is a key metabolite in the tryptophan metabolic pathway and can cross the blood-brain barrier. DL-Kynurenine has a bidirectional regulatory effect on neural excitability. DL-Kynurenine can enhance the convulsive and lethal effects caused by strychnine. DL-Kynurenine is the precursor of Kynurenic acid (HY-100806), which is an antagonist at the glycine site of NMDA receptors and can counteract excitatory toxins. DL-Kynurenine can be used for research on neurotoxicity .
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- HY-N3711
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JNK
ERK
Apoptosis
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Neurological Disease
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Dehydrocrenatidine, a β-carboline alkaloid that can be isolated from Picrasma quassioides. Dehydrocrenatidine induces cell apoptosis by activates ERK and JNK. Dehydrocrenatidine inhibits invasion and migration of cancer cells, it also suppresses neuronal excitability to exert analgesic effects .
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- HY-N5060S
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4-Allylanisole-d4
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Parasite
Isotope-Labeled Compounds
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Neurological Disease
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Estragole-d4 is deuterated labeled Estragole (HY-N5060). Estragole (4-Allylanisole) is a relatively nontoxic volatile terpenoid ether and major component of the essential oil from many plants. Estragole significantly triggers Apoptosis, suppresses LPS-induced intracellular ROS production. Estragole activats Nrf-2 and regulates NF-κB. Estragole has anti-toxoplasma, anti-inflammatory, anti-edema, antioxidant and immunomodulatory properties. Estragole blocks DRG neuron excitability. Estragole has improves gastric ulcer activity [10] .
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- HY-P1073
-
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Calcium Channel
Potassium Channel
Sodium Channel
TRP Channel
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Neurological Disease
Cancer
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ProTx-I is a toxin derived from Thrixopelma pruriens and a peptide inhibitor targeting TTX-resistant sodium channels. ProTx-I interacts with voltage sensors of multiple domains such as NaV1.7, reduces neuronal excitability through allosteric modulation of channel gating and alteration of voltage dependence. The IC50 values of ProTx-I against human NaV1.7, NaV1.2, NaV1.6, and NaV1.5 are 95 nM, 104 nM, 21 nM, and 358 nM, respectively; ProTx-I also potently inhibits Ba 2+ currents of hCav3.1, while its inhibitory potency against hCav3.2 is approximately 160-fold lower. ProTx-I is applicable to the research of chronic pain .
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- HY-D1702
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Fluorescent Dye
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Others
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Mag-Fura-2 tetrapotassium is a cell-impermeant UV excitable rational fluorescent Mg 2+/Ca 2+ indicator (Ex=334-360 nm, Em=510 nm). Mag-Fura-2 tetrapotassium can be used for the determination of Mg 2+ and Ca 2+ concentrations .
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- HY-113316A
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Endogenous Metabolite
Opioid Receptor
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Neurological Disease
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(±)-Salsolinol hydrochloride is the hydrochloride form of (±)-Salsolinol (HY-113316). (±)-Salsolinol hydrochloride is a Dopamine (HY-B0451)-derived endogenous metabolite. (±)-Salsolinol hydrochloride activates μ-opioid receptors (MORs), reduces GABAergic transmission, increases the excitability of dopamine (DA) neurons, and thus accelerates the sustained firing of neurons in the posterior ventral tegmental area (pVTA) .
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- HY-148410
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STK-001
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Sodium Channel
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Neurological Disease
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Zorevunersen is an antisense oligonucleotide targeting the Scn1a gene based on TANGO technology. Zorevunersen increases Scn1a mRNA transcripts and elevates the expression level of NaV1.1 protein. Zorevunersen restores the excitability of PV interneurons, thereby reducing seizures and prolonging survival in mice. Zorevunersen can be used for research on Dravet syndrome .
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- HY-A0236
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Sodium Channel
Potassium Channel
Calcium Channel
Calmodulin
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Cardiovascular Disease
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Aprindine is an Ib-class anti-arrhythmic agent. Aprindine mainly exerts its effect by blocking sodium channels (INa), thereby reducing the excitability and conduction velocity of cardiac muscle cells. Aprindine significantly inhibits delayed potassium currents, which helps to prolong the atrial effective refractory period (AERP) and inhibit the occurrence of atrial fibrillation. Aprindine can also regulate intracellular calcium ion concentration by inhibiting Na +/Ca 2+ exchange current (INCX), thereby further stabilizing cardiac electrical activity. Aprindine can be used for the study of atrial fibrillation (AF) and ventricular arrhythmias .
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- HY-N16525
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Na+/Ca2+ Exchanger
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Neurological Disease
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Muramine is an alkaloid. Muramine can be isolated from the bulbs of Corydalis decumbens. Muramine inhibits spontaneous Ca 2+ oscillations. Muramine inhibits neuronal excitability with an IC50 value of 13.5 μM .
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- HY-P10234A
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Sodium Channel
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Neurological Disease
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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 .
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- HY-105182S1
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LY-246708-d3
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Isotope-Labeled Compounds
mAChR
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Neurological Disease
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Xanomeline-d3 (LY-246708-d3) is deuterium labeled Xanomeline. Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .
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- HY-135000
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DcSTX; DecarbamoylSTX
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Endogenous Metabolite
Drug Metabolite
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Neurological Disease
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Decarbamoylsaxitoxin is a sodium channel inhibitor that blocks the influx of sodium ions through the membranes of excitable nerves and skeletal muscle cells, thereby preventing the formation of action potentials. Decarbamoylsaxitoxin is an acidic hydrolysis product of saxitoxin, and its toxic effects on mice are identical to those of saxitoxin. Decarbamoylsaxitoxin inhibits veratridine- and ouabain-induced swelling and lysis of mouse neuroblastoma cells by blocking Na + channels. Decarbamoylsaxitoxin can be used in studies related to paralytic shellfish poisoning .
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- HY-135809
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Potassium Channel
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Neurological Disease
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A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K + channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception .
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- HY-A0236A
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Sodium Channel
Potassium Channel
Calcium Channel
Calmodulin
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Cardiovascular Disease
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Aprindine hydrochloride is an Ib-class anti-arrhythmic agent. Aprindine hydrochloride mainly exerts its effect by blocking sodium channels (INa), thereby reducing the excitability and conduction velocity of cardiac muscle cells. Aprindine hydrochloride significantly inhibits delayed potassium currents, which helps to prolong the atrial effective refractory period (AERP) and inhibit the occurrence of atrial fibrillation. Aprindine hydrochloride can also regulate intracellular calcium ion concentration by inhibiting Na +/Ca 2+ exchange current (INCX), thereby further stabilizing cardiac electrical activity. Aprindine hydrochloride can be used for the study of atrial fibrillation (AF) and ventricular arrhythmias .
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- HY-W127781
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Fluorescent Dye
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Others
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Rhod-2 triammonium is a cell impermeant, red fluorescent calcium indicator. Rhod-2 triammonium exhibits a significant shift in fluorescence intensity upon calcium binding (ex max=549 nm; calcium-free v. ex/em max=552/581 nm; calcium-bound). Unlike the UV-excitable indicators Fura-2 and Indo-1 (HY-D0121), there is no accompanying spectral shift .
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- HY-D0114
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- HY-105182AR
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LY 246708 tartrate (Standard)
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Reference Standards
mAChR
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Neurological Disease
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Xanomeline (tartrate) (Standard) is the analytical standard of Xanomeline (tartrate). This product is intended for research and analytical applications. Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia .
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- HY-P10234
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Sodium Channel
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Neurological Disease
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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 .
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- HY-N5060R
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4-Allylanisole (Standard)
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Parasite
Reference Standards
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Neurological Disease
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Estragole (Standard) is the analytical standard of Estragole. This product is intended for research and analytical applications. Estragole (4-Allylanisole), a relatively nontoxic volatile terpenoid ether, is a major component of the essential oil of many plants. Estragole dose-dependently blocks nerve excitability . Estragole displays anti-toxoplasma activity .
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- HY-W480392
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Adenosine Receptor
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1,9-Dimethylxanthine is an adenosine receptor antagonist that has the activity of blocking the effects of adenosine on the central nervous system. 1,9-Dimethylxanthine enhances nerve excitability by regulating the adenosine system. 1,9-Dimethylxanthine is used as a pharmacological tool in research to help explore physiological and pathological processes related to adenosine.
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- HY-176248
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Histamine Receptor
Serotonin Transporter
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Neurological Disease
Inflammation/Immunology
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Dimephosphon is an anti-inflammatory agent with antihistamine and antiserotonin activities. Dimephosphon helps maintain the conduction function of the spinal cord and reduces the excitability of spinal motor neurons in the area surrounding the lesion. Dimephosphon directly activates lymphatic vessel movement and improves lymphatic circulation. Dimephosphon can be used for the study of inflammatory edema, acute spinal cord injury and lymphatic circulation disorders .
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- HY-W031620
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Sodium Channel
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Neurological Disease
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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 .
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- HY-P1426
-
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Potassium Channel
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Neurological Disease
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AmmTX3 is a peptide toxin identified from the venom of the scorpion Androctonus mauretanicus. AmmTX3 is a highly specific blocker of Kv4 channels, which selectively and almost completely blocks transient A-type K + currents with a Ki of 131 nM. AmmTX3 induces epileptiform behaviors and causes death in mice receiving intracerebroventricular injection. AmmTX3 increases the excitability of dentate gyrus granule cells, reduces GABAergic inhibition, enhances and stabilizes the EPSP-spike component of long-term potentiation, and impairs reference memory. AmmTX3 can be used in research related to pain, epilepsy, and autism spectrum disorder .
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- HY-171807
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nAChR
STAT
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Neurological Disease
Inflammation/Immunology
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TC-2559 free base is a α4β2 nicotinic acetylcholine receptor (nAChR) agonists with an EC50 of 0.18 μM. TC-2559 free base shows much weaker potencies on the group of b4-containing nAChR subtypes, α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. TC-2559 free base can increase the discharge of dopamine cells in the ventral tegmental area (VTA) of rats in vitro, enhancing the excitability and aggressive behavior of VTA dopamine neurons. TC-2559 free base inhibits STAT3 to exert anti-inflammatory properties and relieves mice mechanical allodynia and improve rats cognitive deficits. TC-2559 free base can be used for the study of nerve pain .
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- HY-W424017A
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Endogenous Metabolite
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Neurological Disease
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Lophophine hydrochloride is the drug intermediate of anhalonine and Lophophorine (HY-119478), and can be found in Lophophora diffusa. Anhalonine causes slight sleepiness in frog. Lophophorine causes long-lasting convulsions, reflex excitability, muscle stiffness, and paralysis in rabbit and frog model .
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- HY-170908
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5-HT Receptor
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Neurological Disease
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Pellotine is an alkaloid that can be isolated from Lophophora. Pellotine is the inverse agonist for 5-HT7 receptor with an EC50 of 291 nM. Pellotine exhibits good affinity to 5-HT1DR and 5-HT6R with Ki of 117 nM and 170 nM. Pellotine reduces intracellular cAMP levels, thereby reducing neuronal excitability and neurotransmitter release .
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- HY-105182R
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LY-246708 (Standard)
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Reference Standards
mAChR
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Neurological Disease
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Xanomeline (Standard) is the analytical standard of Xanomeline. This product is intended for research and analytical applications. Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .
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- HY-P1281
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Potassium Channel
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Neurological Disease
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Kaliotoxin is a peptidyl inhibitor of neuronal BK-Type. Kaliotoxin can specific inhibit Kv channels and calcium-activated potassium channels. Kaliotoxin can be used for the research of the regulation of membrane potential and neuron excitability .
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- HY-135131
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iGluR
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Neurological Disease
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Synthalin hydrochloride is a K+ channel blocker with neuronal excitability modulating activity. Synthalin hydrochloride has an effect on NMDA-mediated depolarization, possibly through receptor-mediated modulation of L-glutamate and serotonin (5-HT). The use of Synthalin hydrochloride can enhance the understanding of changes in membrane potential of different neurons and help study the role of polyamines in neuronal excitability .
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- HY-146129
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Aldose Reductase
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Metabolic Disease
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As an aldose reductase (ALR2) inhibitor, the compound is used to enhance the combination of inhibitory excitability and antioxidant capacity to delay the progress of diabetes complications.
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- HY-121789
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Cytochrome P450
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Others
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Proadifen is a compound that inhibits cytochrome P450 activity, which can change the excitability of catecholamine-secreting neurons in the brain and have different effects on neurons in different brain regions.
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- HY-100842A
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GABA Receptor
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Neurological Disease
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(S)-3C4HPG is a metabotropic glutamate receptor antagonist, demonstrating significant potential in modulating neuronal excitability and influencing synaptic transmission.
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- HY-149863
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Epigenetic Reader Domain
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Neurological Disease
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DDO-8926 is a potent and selective BET inhibitor that can significantly reduce mechanical hypersensitivity by inhibiting the expression of pro-inflammatory cytokines and reducing excitability for neuropathic pain research .
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- HY-19465
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iGluR
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Neurological Disease
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Dasolampanel is a kainate receptor antagonist that helps regulate the excitability of the nervous system by blocking kainate receptors and reducing glutamate-mediated excitatory transmission. Dasolampanel can be used in the study of diseases such as overexcitement and sleep disorders .
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- HY-111245
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- HY-14856
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PD 0200390
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GABA Receptor
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Neurological Disease
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Atagabalin (PD 0200390) is a selective GABA (gamma-aminobutyric acid) receptor agonist with antianxiety and sedative effects. Atagabalin enhances the activity of the GABA receptor by binding to the α2δ subunit of the GABA receptor, thereby increasing the GABA mediated inhibition. This enhancement results in reduced excitability of neurons, helping to reduce anxiety and improve sleep. Atagabalin can be used to study neuropsychiatric disorders, anxiety or sleep disorders .
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- HY-W013353
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Endogenous Metabolite
Opioid Receptor
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Neurological Disease
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(RS)-Salsolinol hydrobromide is the hydrobromide form of (±)-Salsolinol (HY-113316). (RS)-Salsolinol hydrobromide is a Dopamine (HY-B0451)-derived endogenous metabolite. (RS)-Salsolinol hydrobromide activates μ-opioid receptors (MORs), reduces GABAergic transmission, increases the excitability of dopamine (DA) neurons, and thus accelerates the sustained firing of neurons in the posterior ventral tegmental area (pVTA) .
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- HY-108578
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Potassium Channel
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Neurological Disease
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RuBi-4AP, a derivative of 4-aminopyridine (4AP; HY-B0604), is a caged Kv channel blocker. RuBi-4AP contains a photolabile protecting group, allowing its effect to be controlled precisely in both space and time with light. RuBi-4AP can be used for the research of neuronal excitability, synaptic transmission, and signal propagation .
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- HY-136784A
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Fluorescent Dye
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Others
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Rhod-2 sodium is a cell impermeant, red fluorescent calcium indicator. Rhod-2 sodium exhibits a significant shift in fluorescence intensity upon calcium binding (ex max=549 nm; calcium-free v. ex/em max=552/581 nm; calcium-bound). Unlike the UV-excitable indicators Fura-2 and Indo-1 (HY-D0121), there is no accompanying spectral shift .
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- HY-136784
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Fluorescent Dye
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Others
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Rhod-2 potassium is a cell impermeant, red fluorescent calcium indicator. Rhod-2 potassium exhibits a significant shift in fluorescence intensity upon calcium binding (ex max=549 nm; calcium-free v. ex/em max=552/581 nm; calcium-bound). Unlike the UV-excitable indicators Fura-2 and Indo-1 (HY-D0121), there is no accompanying spectral shift .
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- HY-W014504S1
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Isotope-Labeled Compounds
Endogenous Metabolite
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Metabolic Disease
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DL-Kynurenine-d7 is the deuterium labeled DL-Kynurenine. DL-Kynurenine is a key metabolite in the tryptophan metabolic pathway and can cross the blood-brain barrier. DL-Kynurenine has a bidirectional regulatory effect on neural excitability. DL-Kynurenine can enhance the convulsive and lethal effects caused by strychnine. DL-Kynurenine is the precursor of Kynurenic acid (HY-100806), which is an antagonist at the glycine site of NMDA receptors and can counteract excitatory toxins. DL-Kynurenine can be used for research on neurotoxicity.
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-
- HY-127004
-
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RGH-5002
|
Sodium Channel
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Others
|
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Silperisone hydrochloride is an organosilicone compound similar to tolperisone that has centrally acting muscle relaxant properties. Silperisone (hydrochloride) is a sodium channel protein type 2 alpha channel blocker that blocks sodium and calcium channels in cells, reduces muscle cell excitability and contraction, reduces peripheral tone, and acts as a muscle relaxant and peripheral vascular dilator. Silperisone (hydrochloride) is used to study recurrent painful myoclonus due to spinal cord injury, abnormal hypertonia due to cerebrovascular disease, myotonia symptoms, pyramidal tonia syndrome, multiple sclerosis myospasm, and myelitis .
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-
- HY-W014504R
-
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Reference Standards
Endogenous Metabolite
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Metabolic Disease
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DL-Kynurenine (Standard) is the analytical standard of DL-Kynurenine. This product is intended for research and analytical applications. DL-Kynurenine is a key metabolite in the tryptophan metabolic pathway and can cross the blood-brain barrier. DL-Kynurenine has a bidirectional regulatory effect on neural excitability. DL-Kynurenine can enhance the convulsive and lethal effects caused by strychnine. DL-Kynurenine is the precursor of Kynurenic acid (HY-100806), which is an antagonist at the glycine site of NMDA receptors and can counteract excitatory toxins. DL-Kynurenine can be used for research on neurotoxicity.
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-
- HY-P10290
-
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Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide Y (human) free acid is the deamidated form of Neuropeptide Y (human, rat, mouse) (HY-P0198). The amidation of Neuropeptide Y C-terminal tyrosine is critical for its function. Non-amidated Neuropeptide Y fails to elicit G protein signaling .
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- HY-168166
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Endogenous Metabolite
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Neurological Disease
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CHET3 is a sex-selective activator with potent analgesic activity. CHET3 was discovered to be a highly selective omnidirectional modulator of TASK-3-containing K2P channels, including TASK-3 homologues and TASK-3/TASK-1 heterologues. CHET3 exhibited significant analgesic effects in multiple acute and chronic pain models in mice, which could be abolished by pharmacological means or genetic knockout of TASK-3. CHET3 is able to functionally modulate the membrane excitability of specific small sensory neurons, which supports its analgesic effects on thermal hypersensitivity and mechanical hyperalgesia in chronic pain .
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- HY-P1426A
-
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Potassium Channel
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Neurological Disease
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AmmTX3 TFA is a peptide toxin identified from the venom of the scorpion Androctonus mauretanicus. AmmTX3 TFA is a highly specific blocker of Kv4 channels, which selectively and almost completely blocks transient A-type K + currents with a Ki of 131 nM. AmmTX3 TFA induces epileptiform behaviors and causes death in mice receiving intracerebroventricular injection. AmmTX3 TFA increases the excitability of dentate gyrus granule cells, reduces GABAergic inhibition, enhances and stabilizes the EPSP-spike component of long-term potentiation, and impairs reference memory. AmmTX3 TFA can be used in research related to pain, epilepsy, and autism spectrum disorder .
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- HY-121183
-
|
RP 52891
|
Potassium Channel
|
Cardiovascular Disease
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Aprikalim (RP 52891), a potassium channel opener (KCO), activates ATP-sensitive K+ (KATP) channels in guinea pig ventricular myocytes. Using patch-clamp techniques, it was found that aprikalim enhances KATP channel activity more effectively in Mg-NDP solution compared to standard solutions. In Mg-NDP solution, aprikalim reduced the sensitivity of KATP channels to ATP, increasing the concentration of ATP required to inhibit channel activity by half (K1) from 56 μM to 180 μM. However, this effect diminished over time. Aprikalim's ability to activate KATP channels in Mg-NDP solution suggests potential therapeutic implications in modulating cardiac excitability and may relate to changes in channel protein enzymatic activity under experimental conditions .
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-
- HY-108594R
-
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|
Reference Standards
Potassium Channel
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Metabolic Disease
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PD-118057 (Standard) is the analytical standard of PD-118057 (HY-108594). This product is intended for research and analytical applications. PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability .
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- HY-129947
-
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Endogenous Metabolite
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Neurological Disease
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(-)-Carveol is a natural unsaturated monocyclic monoterpene alcohol with the activity of regulating neural excitability. (-)-Carveol can activate or inhibit neural excitability by changing its chemical structure, which has potential significance for the design of targeted compounds. (-)-Carveol can also be used as a fragrance in cosmetics and a flavor additive in the food industry .
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-
- HY-174899
-
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iGluR
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Neurological Disease
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AMPA-IN-2 is an orally active AMPA inhibitor that can cross the blood-brain barrier. AMPA-IN-2 improves epileptic seizures by inhibiting the intrinsic excitability of neurons and inhibiting the excitability of glutamatergic transmission. AMPA-IN-2 exerts anti-epileptic effects in the pentylenetetrazol (PTZ) model and can be used as a promising candidates with high broad-spectrum anti-epileptic potential .
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-
- HY-19185
-
|
|
Potassium Channel
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Endocrinology
|
|
ZD-2767 is a selective ATP-sensitive potassium channel agonist. ZD-276 reduces cell membrane excitability and contractility by activating KATP channels in bladder smooth muscle. ZD-2767 is promising for research of overactive bladder .
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-
- HY-105203
-
|
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Others
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Neurological Disease
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MS-322 is an orally active centrally acting muscle relaxant. MS-322 can dose-dependently inhibit spinal reflex potentials, reduce neuronal excitability and muscle afferent discharges, and so on in rats. In addition, MS-322 has relatively weak inhibitory effects on other central nervous system pathways and no effect on the neuromuscular junction .
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-
- HY-DY1101
-
|
Fura-2 Acetoxymethyl ester (solution)
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Fluorescent Dye
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Others
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Fura-2 AM (solution) (Fura-2 Acetoxymethyl ester (solution)) is a membrane permeable, intracellular, UV light-excitable and ratiometric fluorescent Ca 2+ (calcium ion) indicator. Fura-2 AM crosses cell membranes and is converted to Fura-2 (HY-D0110A) via cellular esterases. Fura-2 AM can be used to detect calcium in cells. Solvent and concentration: DMSO: 1 mM
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-
- HY-183857
-
|
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TRP Channel
|
Neurological Disease
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DD-161515 is a TRPV1/VR1 inhibitor with an IC50 of 0.7 μM in rats. DD-161515 binds to an allosteric site of TRPV1 distinct from that of capsaicin, blocks channel opening, inhibits receptor-mediated calcium ion influx, reduces the excitability of peripheral sensory nerve fibers, and thereby inhibits nociception induced by heat and transmission of chemically induced pain signals. DD-161515 can be used in studies related to inflammatory pain .
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-
- HY-A0236AR
-
|
|
Reference Standards
Sodium Channel
Potassium Channel
Calcium Channel
Calmodulin
|
Cardiovascular Disease
|
|
Aprindine hydrochloride (Standard) is the analytical reference standard of Aprindine hydrochloride (HY-A0236A). This product is used for research and analytical applications. Aprindine hydrochloride is an Ib-class anti-arrhythmic agent. Aprindine hydrochloride mainly exerts its effect by blocking sodium channels (INa), thereby reducing the excitability and conduction velocity of cardiac muscle cells. Aprindine hydrochloride significantly inhibits delayed potassium currents, which helps to prolong the atrial effective refractory period (AERP) and inhibit the occurrence of atrial fibrillation. Aprindine hydrochloride can also regulate intracellular calcium ion concentration by inhibiting Na +/Ca 2+ exchange current (INCX), thereby further stabilizing cardiac electrical activity. Aprindine hydrochloride can be used for the study of atrial fibrillation (AF) and ventricular arrhythmias.
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-
- HY-133240
-
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DNA Alkylator/Crosslinker
Calcium Channel
Potassium Channel
Sodium Channel
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Infection
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|
trans-AzoTAB is a photoresponsive potassium/sodium/calcium channel modulator and DNA-binding agent. trans-AzoTAB undergoes trans-cis isomerization driven by light, with variable polarity and DNA affinity. trans-AzoTAB also enhances voltage-gated potassium currents and inhibits sodium and calcium currents in cardiomyocytes, thereby reducing spontaneous electrical activity and excitation conduction velocity. In addition, trans-AzoTAB induces compaction and frozen conformation of λ-phage DNA, and non-sequence-dependently inhibits transcription and translation processes in the dark; its activity can be reversed and restored by visible light after activation with ultraviolet irradiation. trans-AzoTAB can serve as a probe for two-photon optical regulation of myocardial excitability, and is used to construct photoresponsive interfacial polymer structures .
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-
- HY-182517
-
|
|
TRP Channel
|
Inflammation/Immunology
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|
AG1529 is a TRPV1 inhibitor and capsaicinoid-based soft agent with a human TRPV1 IC50 of 0.9-0.93 μM. AG1529 reversibly blocks capsaicin-evoked TRPV1 activation, binds to the TRPV1 capsaicin binding site, moderately affects pH-induced TRPV1 gating, and does not alter voltage- or heat-mediated TRPV1 responses. AG1529 suppresses TRPV1-mediated neuronal excitability, reduces capsaicin- and pH-evoked neuronal firing, abolishes histaminergic and inflammation-mediated TRPV1 sensitization. AG1529 exhibits anti-nociceptive and antipruritic effects, attenuates in vivo hyperalgesia and pruritus, dose-dependently reduces acute histaminergic itch in rodents, and mildly blocks hTRPA1 and hTRPM8 channel activity. AG1529 undergoes hydrolysis and dermal deactivation, minimizes TRPV1-associated side reactions, does not evoke capsaicin-like burning sensation, and does not disrupt physiological thermal regulation. AG1529 can be used for the research of inflammatory cutaneous nociception and acute histaminergic pruritus .
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-
- HY-182023
-
|
|
Reactive Oxygen Species (ROS)
GABA Receptor
|
Neurological Disease
|
|
Anticonvulsant agent 11 (Compound 8b) is an anticonvulsant agent. Anticonvulsant agent 11 exerts neuroprotective effects by enhancing cell viability and reducing ROS levels. Anticonvulsant agent 11 induces the expression of GABAA α1, resulting in neuronal hyperpolarization. Anticonvulsant agent 11 increases the number of neurite-bearing cells and the length of neurites. Anticonvulsant agent 11 exhibits dose-dependent anticonvulsant effects in mice. Anticonvulsant agent 11 can be used for the research of epilepsy .
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-
| Cat. No. |
Product Name |
Type |
-
- HY-101897
-
|
Fura-2 Acetoxymethyl ester
|
Fluorescent Dye
|
|
Fura-2 AM is a membrane permeable, intracellular, UV light-excitable and ratiometric fluorescent Ca 2+ (calcium ion) indicator. Fura-2 AM crosses cell membranes and is converted to Fura-2 (HY-D0110A) via cellular esterases. Fura-2 AM can be used to detect calcium in cells.
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-
- HY-D0127
-
|
|
Fluorescent Dye
|
|
Merocyanin 540 is a fluorescent membrane probe that selectively stains the membranes of a wide variety of electrically excitable cells, but not those of nonexcitable cells (Ex/Em: 540/580 nm) .
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-
- HY-D1702
-
|
|
Fluorescent Dye
|
|
Mag-Fura-2 tetrapotassium is a cell-impermeant UV excitable rational fluorescent Mg 2+/Ca 2+ indicator (Ex=334-360 nm, Em=510 nm). Mag-Fura-2 tetrapotassium can be used for the determination of Mg 2+ and Ca 2+ concentrations .
|
-
- HY-D0114
-
|
|
Fluorescent Dye
|
|
3-Carboxy-7-Hydroxycoumarin is a UV-light excitable fluorescent dye .
|
-
- HY-136784A
-
|
|
Fluorescent Dye
|
|
Rhod-2 sodium is a cell impermeant, red fluorescent calcium indicator. Rhod-2 sodium exhibits a significant shift in fluorescence intensity upon calcium binding (ex max=549 nm; calcium-free v. ex/em max=552/581 nm; calcium-bound). Unlike the UV-excitable indicators Fura-2 and Indo-1 (HY-D0121), there is no accompanying spectral shift .
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-
- HY-136784
-
|
|
Fluorescent Dye
|
|
Rhod-2 potassium is a cell impermeant, red fluorescent calcium indicator. Rhod-2 potassium exhibits a significant shift in fluorescence intensity upon calcium binding (ex max=549 nm; calcium-free v. ex/em max=552/581 nm; calcium-bound). Unlike the UV-excitable indicators Fura-2 and Indo-1 (HY-D0121), there is no accompanying spectral shift .
|
-
- HY-DY1101
-
|
Fura-2 Acetoxymethyl ester (solution)
|
Fluorescent Dye
|
Fura-2 AM (solution) (Fura-2 Acetoxymethyl ester (solution)) is a membrane permeable, intracellular, UV light-excitable and ratiometric fluorescent Ca 2+ (calcium ion) indicator. Fura-2 AM crosses cell membranes and is converted to Fura-2 (HY-D0110A) via cellular esterases. Fura-2 AM can be used to detect calcium in cells. Solvent and concentration: DMSO: 1 mM
|
| Cat. No. |
Product Name |
Type |
-
- HY-W127781
-
|
|
Biochemical Assay Reagents
|
|
Rhod-2 triammonium is a cell impermeant, red fluorescent calcium indicator. Rhod-2 triammonium exhibits a significant shift in fluorescence intensity upon calcium binding (ex max=549 nm; calcium-free v. ex/em max=552/581 nm; calcium-bound). Unlike the UV-excitable indicators Fura-2 and Indo-1 (HY-D0121), there is no accompanying spectral shift .
|
-
- HY-W480392
-
|
|
Biochemical Assay Reagents
|
|
1,9-Dimethylxanthine is an adenosine receptor antagonist that has the activity of blocking the effects of adenosine on the central nervous system. 1,9-Dimethylxanthine enhances nerve excitability by regulating the adenosine system. 1,9-Dimethylxanthine is used as a pharmacological tool in research to help explore physiological and pathological processes related to adenosine.
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1626
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Acetyl tetrapeptide-15 is a synthetic peptide. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway. Acetyl tetrapeptide-15 is used in the cosmetics for sensitive skin .
|
-
- HY-P1073
-
|
|
Calcium Channel
Potassium Channel
Sodium Channel
TRP Channel
|
Neurological Disease
Cancer
|
ProTx-I is a toxin derived from Thrixopelma pruriens and a peptide inhibitor targeting TTX-resistant sodium channels. ProTx-I interacts with voltage sensors of multiple domains such as NaV1.7, reduces neuronal excitability through allosteric modulation of channel gating and alteration of voltage dependence. The IC50 values of ProTx-I against human NaV1.7, NaV1.2, NaV1.6, and NaV1.5 are 95 nM, 104 nM, 21 nM, and 358 nM, respectively; ProTx-I also potently inhibits Ba 2+ currents of hCav3.1, while its inhibitory potency against hCav3.2 is approximately 160-fold lower. ProTx-I is applicable to the research of chronic pain .
|
-
- HY-P10234A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
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 .
|
-
- HY-P10234
-
|
|
Sodium Channel
|
Neurological Disease
|
|
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 .
|
-
- HY-P1426
-
|
|
Potassium Channel
|
Neurological Disease
|
|
AmmTX3 is a peptide toxin identified from the venom of the scorpion Androctonus mauretanicus. AmmTX3 is a highly specific blocker of Kv4 channels, which selectively and almost completely blocks transient A-type K + currents with a Ki of 131 nM. AmmTX3 induces epileptiform behaviors and causes death in mice receiving intracerebroventricular injection. AmmTX3 increases the excitability of dentate gyrus granule cells, reduces GABAergic inhibition, enhances and stabilizes the EPSP-spike component of long-term potentiation, and impairs reference memory. AmmTX3 can be used in research related to pain, epilepsy, and autism spectrum disorder .
|
-
- HY-P1281
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Kaliotoxin is a peptidyl inhibitor of neuronal BK-Type. Kaliotoxin can specific inhibit Kv channels and calcium-activated potassium channels. Kaliotoxin can be used for the research of the regulation of membrane potential and neuron excitability .
|
-
- HY-P2590
-
|
|
Peptides
|
Others
|
|
Tnrnflrfamide is a neuropeptide that modulates the receptor muscles of the lobster abdominal stretch receptors and their exoskeletal muscle homologues. Tnrnflrfamide enhances motor performance, including the amplitude of excitatory postsynaptic potentials and the development of nerve-evoked tension .
|
-
- HY-P10290
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide Y (human) free acid is the deamidated form of Neuropeptide Y (human, rat, mouse) (HY-P0198). The amidation of Neuropeptide Y C-terminal tyrosine is critical for its function. Non-amidated Neuropeptide Y fails to elicit G protein signaling .
|
-
- HY-P1426A
-
|
|
Potassium Channel
|
Neurological Disease
|
|
AmmTX3 TFA is a peptide toxin identified from the venom of the scorpion Androctonus mauretanicus. AmmTX3 TFA is a highly specific blocker of Kv4 channels, which selectively and almost completely blocks transient A-type K + currents with a Ki of 131 nM. AmmTX3 TFA induces epileptiform behaviors and causes death in mice receiving intracerebroventricular injection. AmmTX3 TFA increases the excitability of dentate gyrus granule cells, reduces GABAergic inhibition, enhances and stabilizes the EPSP-spike component of long-term potentiation, and impairs reference memory. AmmTX3 TFA can be used in research related to pain, epilepsy, and autism spectrum disorder .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-N5060S
-
|
|
|
Estragole-d4 is deuterated labeled Estragole (HY-N5060). Estragole (4-Allylanisole) is a relatively nontoxic volatile terpenoid ether and major component of the essential oil from many plants. Estragole significantly triggers Apoptosis, suppresses LPS-induced intracellular ROS production. Estragole activats Nrf-2 and regulates NF-κB. Estragole has anti-toxoplasma, anti-inflammatory, anti-edema, antioxidant and immunomodulatory properties. Estragole blocks DRG neuron excitability. Estragole has improves gastric ulcer activity [10] .
|
-
-
- HY-105182S1
-
|
|
|
Xanomeline-d3 (LY-246708-d3) is deuterium labeled Xanomeline. Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .
|
-
-
- HY-W014504S1
-
|
|
|
DL-Kynurenine-d7 is the deuterium labeled DL-Kynurenine. DL-Kynurenine is a key metabolite in the tryptophan metabolic pathway and can cross the blood-brain barrier. DL-Kynurenine has a bidirectional regulatory effect on neural excitability. DL-Kynurenine can enhance the convulsive and lethal effects caused by strychnine. DL-Kynurenine is the precursor of Kynurenic acid (HY-100806), which is an antagonist at the glycine site of NMDA receptors and can counteract excitatory toxins. DL-Kynurenine can be used for research on neurotoxicity.
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-148410A
-
|
STK-001 sodium
|
|
Antisense Oligonucleotides
|
|
Zorevunersen sodium is an antisense oligonucleotide targeting the Scn1a gene based on TANGO technology. Zorevunersen sodium increases Scn1a mRNA transcripts and elevates the expression level of NaV1.1 protein. Zorevunersen sodium restores the excitability of PV interneurons, thereby reducing seizures and prolonging survival in mice. Zorevunersen sodium can be used for research on Dravet syndrome .
|
-
- HY-148410
-
|
STK-001
|
|
Antisense Oligonucleotides
|
|
Zorevunersen is an antisense oligonucleotide targeting the Scn1a gene based on TANGO technology. Zorevunersen increases Scn1a mRNA transcripts and elevates the expression level of NaV1.1 protein. Zorevunersen restores the excitability of PV interneurons, thereby reducing seizures and prolonging survival in mice. Zorevunersen can be used for research on Dravet syndrome .
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