427 Results for "

gate

" in MedChemExpress (MCE) Product Catalog:
Products (427)

427 Results for "gate" in MCE Product Catalog:

6
6 Cited Publications
Cat. No.: HY-108006
CAS No.: 1138245-21-2
Purity:  99.57%
Synonyms: DS 5565 besylate
Target:  

Calcium Channel

Research Areas:  

Neurological Disease

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.
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4
4 Cited Publications
Cat. No.: HY-N6691
CAS No.: 71-62-5
Synonyms: 3-Veratroylveracevine
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 .
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4
4 Cited Publications
Cat. No.: HY-N6789
CAS No.: 108068-98-0
Target:  

PKA

Research Areas:  

Neurological Disease Cancer

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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4
4 Cited Publications
Cat. No.: HY-16787
CAS No.: 313254-51-2
Target:  

Sodium Channel

Research Areas:  

Cardiovascular Disease

ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM).
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3
3 Cited Publications
Cat. No.: HY-130777A
Purity:  ≥94.0%
Synonyms: Adenylyl imidodiphosphate lithium hydrate
AMP-PNP (Adenylyl imidodiphosphate) lithium hydrate is a non-hydrolyzable ATP analog. AMP-PNP lithium hydrate binds to ATP binding sites competely but is not hydrolyzed by enzymes, providing stable experimental conditions for studying ATP-dependent processes. AMP-PNP lithium hydrate can also be used to study enzyme activity, kinase regulation, DNA/RNA metabolism, ion channel function, and protein complex assembly .
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3
3 Cited Publications
Cat. No.: HY-108690
CAS No.: 928783-29-3
Purity:  99.45%
Research Areas:  

Others

Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
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3
3 Cited Publications
Cat. No.: HY-B0883
CAS No.: 1811-28-5
3,6-Diaminoacridine hemisulfate is a multifunctional acridine compound. 3,6-Diaminoacridine hemisulfate is an acridine dye and also a DNA inserter. 3,6-Diaminoacridine hemisulfate is a potent broad-spectrum antibacterial agent. Its mechanism is to insert into bacterial DNA, interfering with replication and transcription, leading to bacterial lysis. 3,6-Diaminoacridine hemisulfate is a Kir3.2 potassium channel blocker and can be used to study the neurological phenotype of Down syndrome. 3,6-Diaminoacridine hemisulfate can penetrate the stratum corneum of the skin and accumulate in the cell nucleus. Long-term exposure may induce skin cancer or other malignant tumors .
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3
3 Cited Publications
Cat. No.: HY-B0162
CAS No.: 155974-00-8
Target:  

HCN Channel

Research Areas:  

Cardiovascular Disease Cancer

Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity .
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3
3 Cited Publications
Cat. No.: HY-B0162A
CAS No.: 148849-67-6
Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity .
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3
3 Cited Publications
Cat. No.: HY-66012
CAS No.: 5875-06-9
Synonyms: Proxymetacaine hydrochloride
Target:  

Sodium Channel

Research Areas:  

Neurological Disease

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 .
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3
3 Cited Publications
Cat. No.: HY-P10234A
Target:  

Sodium Channel

Research Areas:  

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 .
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3
3 Cited Publications
Cat. No.: HY-119980
CAS No.: 69-23-8
Purity:  98.70%
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 .
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3
3 Cited Publications
Cat. No.: HY-A0081
CAS No.: 146-56-5
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 .
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3
3 Cited Publications
Cat. No.: HY-103430A
CAS No.: 99295-33-7
Purity:  99.82%
SKF-83566 is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a Ki value of approximately 0.4-0.56 nM. SKF-83566 modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway. SKF-83566 acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2). SKF-83566 competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation. SKF-83566 is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect") .
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2
2 Cited Publications
Cat. No.: HY-100345
CAS No.: 926023-82-7
Purity:  99.18%
Target:  

TRP Channel

Research Areas:  

Neurological Disease Cancer

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) .
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2
2 Cited Publications
Cat. No.: HY-B1704
CAS No.: 53179-07-0
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 .
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2
2 Cited Publications
Cat. No.: HY-B1704A
CAS No.: 57754-86-6
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 .
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2
2 Cited Publications
Cat. No.: HY-B0339
CAS No.: 125-33-7
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 .
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2
2 Cited Publications
Cat. No.: HY-120033
CAS No.: 1393441-53-6
Purity:  98.59%
Target:  

Sodium Channel

Research Areas:  

Neurological Disease

RY796 is a potent and selective voltage-gated potassium (KV2) channel inhibitor with IC50s of 0.25 μM and 0.09 μM for KV2.1 and KV2.2. RY796 has analgesic activity .
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2
2 Cited Publications
Cat. No.: HY-N6708
CAS No.: 27061-78-5
Alamethicin is a linear 20-amino acid antibiotic, which can induce voltage-gated conductance in model and cell membranes. Alamethicin exhibits antimicrobial activity against Gram-positive bacteria, but not Gram-negative bacteria. Alamethicin can form an amphipathic α-helical structure in biological membranes .
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