11 Results for "

state-dependent block

" in MedChemExpress (MCE) Product Catalog:
Products (11)

11 Results for "state-dependent block" in MCE Product Catalog:

1
1 Cited Publications
Cat. No.: HY-W052508
CAS No.: 5747-48-8
Synonyms: N-Desalkylquetiapine
Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-W040555
CAS No.: 111974-74-4
Synonyms: N-Desalkylquetiapine dihydrochloride
Norquetiapine ( N-Desalkylauetiapine) dihydrochloride, a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine dihydrochloride selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine dihydrochloride blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine dihydrochloride shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine dihydrochloride can be used for the study of depression and inflammation .
loading...
    loading...
Cat. No.: HY-12796
CAS No.: 934240-30-9
Purity:  99.85%
Synonyms: Vixotrigine; GSK-1014802; CNV1014802
Target:  

Sodium Channel

Research Areas:  

Neurological Disease

Raxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
loading...
    loading...
Cat. No.: HY-12796A
CAS No.: 934240-31-0
Purity:  98.94%
Synonyms: Vixotrigine hydrochloride; GSK-1014802 hydrochloride; CNV1014802 hydrochloride
Target:  

Sodium Channel

Research Areas:  

Neurological Disease

Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
loading...
    loading...
Cat. No.: HY-120751
CAS No.: 1309601-26-0
Target:  

Calcium Channel

Research Areas:  

Neurological Disease

TROX-1 is a selective, orally active and brain-penetrant N-type calcium channel (Cav2.2) inhibitor with an IC50 value of 0.11 μM. TROX-1 exerts state-dependent and use-dependent inhibition, preferentially targets open/inactivated channels, blocks depolarization-associated calcium influx, and fully blocks calcium influx in rat dorsal root ganglion neurons. TROX-1 reverses inflammatory-induced hyperalgesia, nerve injury-induced allodynia. TROX-1 can be used for the research of pain .
loading...
    loading...
Cat. No.: HY-W158030
CAS No.: 5418-95-1
Synonyms: 2GBI
2-Guanidinobezimidazole (2GBI) is a NLRP3 agonist with a KD of 1.29 μM and a selective state-dependent HVCN1 blocker. 2-Guanidinobezimidazole directly binds NLRP3’s LRR domain, enhances NLRP3-ASC and NLRP3-NEK7 interactions, and drives NLRP3 inflammasome activation. 2-Guanidinobezimidazole can be used for the research of LLC lung carcinoma, B16F10 melanoma and ischemic stroke .
loading...
    loading...
Cat. No.: HY-108504
CAS No.: 181144-66-1
Purity:  99.90%
Synonyms: V 102862
Target:  

Sodium Channel

Research Areas:  

Neurological Disease

Co 102862 (V 102862) is a potent, broad-spectrum, state-dependent Na + channel blocker. Co 102862 is also an orally active anticonvulsant .
loading...
    loading...
Cat. No.: HY-W052508S
CAS No.: 1189866-35-0
Synonyms: N-Desalkylquetiapine-d8
Norquetiapine-d8 (N-Desalkylquetiapine-d8) is the deuterium labeled Norquetiapine.Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation .
loading...
    loading...
Cat. No.: HY-W040555R
CAS No.: 111974-74-4
Synonyms: N-Desalkylquetiapine dihydrochloride (Standard)
Norquetiapine dihydrochloride (Standard) (N-Desalkylquetiapine dihydrochloride (Standard)) is the analytical standard of Norquetiapine dihydrochloride (HY-W040555). This product is intended for research and analytical applications. Norquetiapine ( N-Desalkylauetiapine) dihydrochloride, a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine dihydrochloride selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine dihydrochloride blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine dihydrochloride shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine dihydrochloride can be used for the study of depression and inflammation .
loading...
    loading...
Cat. No.: HY-108504R
CAS No.: 181144-66-1
Synonyms: V 102862 (Standard)
Research Areas:  

Neurological Disease

Co 102862 (Standard) is the analytical standard of Co 102862 (HY-108504). This product is intended for research and analytical applications. Co 102862 (V 102862) is a potent, broad-spectrum, state-dependent Na+ channel blocker. Co 102862 is also an orally active anticonvulsant .
loading...
    loading...
Cat. No.: HY-120751A
CAS No.: 2751591-42-9
Research Areas:  

Neurological Disease

(S)-TROX-1 is the S-enantiomer of TROX-1 (HY-120751). TROX-1 is a selective, orally active and brain-penetrant N-type calcium channel (Cav2.2) inhibitor with an IC50 value of 0.11 μM. TROX-1 exerts state-dependent and use-dependent inhibition, preferentially targets open/inactivated channels, blocks depolarization-associated calcium influx, and fully blocks calcium influx in rat dorsal root ganglion neurons. TROX-1 reverses inflammatory-induced hyperalgesia, nerve injury-induced allodynia. TROX-1 can be used for the research of pain .
loading...
    loading...
  • 1