Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
28 Results for "
hyperexcitability
" in MedChemExpress (MCE) Product Catalog:
Products (28)
28 Results for "hyperexcitability" in MCE Product Catalog:
39
39 Publications Verification
Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis . Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
39
39 Publications Verification
Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis . Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
4
4 Cited Publications
Synonyms: EMA401; PD-126055; (S)-EMA400
Target:
Research Areas:
Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons .
3
3 Cited Publications
Synonyms: YH25448; GNS-1480
Target:
Research Areas:
Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
3
3 Cited Publications
Cat. No.: HY-109061B
CAS No.: 2247995-37-3
Synonyms: YH25448 mesylate; GNS-1480 mesylate
Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
1
1 Cited Publications
Synonyms: NBI-921352; XEN901
Target:
Research Areas:
Zandatrigine (NBI-921352; XEN901) is a selective, orally active, voltage-gated sodium channel NaV1.6/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 .
1
1 Cited Publications
Target:
Research Areas:
NS309 is a potent and selective activator of the Ca 2+-activated SK/IK potassium channels, but displays no activity at BK channels .
Cat. No.: HY-A0042
CAS No.: 106308-44-5
Synonyms: CGP 33101; E 2080; RUF 331
Target:
Research Areas:
Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome .
Cat. No.: HY-W011602
CAS No.: 77-93-0
Research Areas:
Triethyl citrate is an orally active citrate compound. Triethyl citrate induces acute toxic effects, including weakness, depression, ataxia, hyperexcitability, restlessness, dripping urine, and irregular, labored breathing. Triethyl citrate can be used in research on plasticizers for food packaging materials .
Target:
Research Areas:
QO 58 is a potent modulator of K(v)7 channels. QO-58 increases the current amplitudes, shifts the voltage-dependent activation curve in a more negative direction and slows the deactivation of K(v)7.2/K(v)7.3 currents. QO-58 has the potential for the research of diseases associated with neuronal hyperexcitability .
Target:
Research Areas:
RL648_81 is a specific KQT-like subfamily 2/3 (KCNQ2/3) activator with an EC50 of 190 nM. RL648_81 robustly shifts the V1/2 of KCNQ2/3 channels towards hyperpolarized potentials.RL648_81 does not shift the V1/2 of either KCNQ4 or KCNQ5.RL648_81 has?the?potential?for?neurologic disorders associated with neuronal hyperexcitability research .
Cat. No.: HY-179215
CAS No.: 2093928-29-9
Target:
Research Areas:
OV329 hydrochloride is a potent GABA aminotransferase inactivator. OV329 hydrochloride is a Vigabatrin (HY-15399) analogue. OV329 hydrochloride can increase brain GABA levels and block abnormal intracerebral hyperexcitability. OV329 hydrochloride exhibits anticonvulsant and antiepileptic activities. OV329 hydrochloride can be used for the research of neurological disease, such as seizure .
Cat. No.: HY-179215A
CAS No.: 2093928-28-8
Target:
Research Areas:
OV329 is a potent GABA aminotransferase inactivator. OV329 is a Vigabatrin (HY-15399) analogue. OV329 can increase brain GABA levels and block abnormal intracerebral hyperexcitability. OV329 exhibits anticonvulsant and antiepileptic activities. OV329 can be used for the research of neurological disease, such as seizure .
Cat. No.: HY-W011602R
CAS No.: 77-93-0
Research Areas:
Triethyl citrate (Standard) is the analytical standard of Triethyl citrate (HY-W011602). This product is intended for research and analytical applications. Triethyl citrate is an orally active citrate compound. Triethyl citrate induces acute toxic effects, including weakness, depression, ataxia, hyperexcitability, restlessness, dripping urine, and irregular, labored breathing. Triethyl citrate can be used in research on plasticizers for food packaging materials .
Cat. No.: HY-P5183
Target:
Research Areas:
Cat. No.: HY-13106A
CAS No.: 1316755-17-5
Synonyms: EMA401 sodium; PD-126055 sodium
Target:
Research Areas:
Olodanrigan (EMA401) sodium is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. Olodanrigan sodium is under development as a neuropathic pain therapeutic agent. Olodanrigan sodium analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons .
Cat. No.: HY-B0828
CAS No.: 24017-47-8
Target:
Research Areas:
Triazophos, a non-systemic insecticide and acaricide that acts as an acetylcholinesterase (AChE) inhibitor, covalently and irreversibly binds to the acetylcholine binding site, thus blocking the hydrolysis of acetylcholine and leading to hyperexcitability; it is effective against a variety of soil insects and mites, including aphids, thrips, midges, beetles, Lepidoptera larvae, cutworms, and spider mites in crops such as ornamentals, cotton, rice, maize, soybeans, oil palms, olives, and coffee.
Cat. No.: HY-120484
CAS No.: 1219624-62-0
Target:
Research Areas:
A-1048400 is an orally active and selective calcium channel inhibitor with an IC50 value of 1.4 μM for N-type channels, 1.2 μM for T-type channel. A-1048400 inhibits neurotransmitter release and reduces membrane hyperexcitability, exerting potent analgesic activity. A-1048400 is promising for research of neuropathic pain (e.g., pain induced by spinal nerve ligation and chronic constriction injury) .
Cat. No.: HY-174146
CAS No.: 2410053-15-3
Target:
Research Areas:
5-HT1A agonist 1 (Compound Ex.37) is a highly selective 5-HT1a receptor agonist (EC50=0.18 nM). 5-HT1A agonist 1 mimicks serotonin binding to the receptor, promotes postsynaptic membrane hyperpolarization, inhibits neuronal hyperexcitability, and reduces the release of anxiety-related neurotransmitters. 5-HT1A agonist 1 is promising for research of neuropsychiatric diseases .
Cat. No.: HY-A0042R
CAS No.: 106308-44-5
Synonyms: CGP 33101 (Standard); E 2080 (Standard); RUF 331 (Standard)
Target:
Research Areas:
Rufinamide (Standard) is the analytical standard of Rufinamide (HY-A0042). This product is intended for research and analytical applications. Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome .
- 1
- 2
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
