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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
16 Results for "
state-dependent
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "state-dependent" in MCE Product Catalog:
1
Research Areas:
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 .
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1 Cited Publications
Cat. No.: HY-W040555
CAS No.: 111974-74-4
Synonyms: N-Desalkylquetiapine dihydrochloride
Research Areas:
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 .
Synonyms: Vixotrigine; GSK-1014802; CNV1014802
Target:
Research Areas:
Raxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
Synonyms: Vixotrigine hydrochloride; GSK-1014802 hydrochloride; CNV1014802 hydrochloride
Target:
Research Areas:
Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
Cat. No.: HY-120751
CAS No.: 1309601-26-0
Target:
Research Areas:
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 .
Cat. No.: HY-W158030
CAS No.: 5418-95-1
Synonyms: 2GBI
Research Areas:
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 .
Synonyms: V 102862
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Co 102862 (V 102862) is a potent, broad-spectrum, state-dependent Na + channel blocker. Co 102862 is also an orally active anticonvulsant .
Cat. No.: HY-123825
CAS No.: 1432913-36-4
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GX-674 is a potent, state-dependent, isoform-selective voltage-gated sodium channel 1.7 (Nav1.7) antagonist with an IC50 of 0.1 nM at -40 mV .
Cat. No.: HY-W052508S
CAS No.: 1189866-35-0
Synonyms: N-Desalkylquetiapine-d8
Cat. No.: HY-155058
Target:
Research Areas:
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 .
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Sodium Channel inhibitor 1 is a state-dependent voltage-gated NaV1.7 inhibitor with an IC50 of 0.087 μM. Sodium Channel inhibitor 1 can be used for research of pain .
Cat. No.: HY-138816
CAS No.: 1356834-62-2
Target:
Research Areas:
Nav1.7-IN-15 (Compd 9) is a potent and state-dependent Nav1.7 antagonist, with an IC50 of 0.42 μM for hNav1.7 PX .
Cat. No.: HY-134525
CAS No.: 195988-65-9
Ro 8-4304 is a non-competitive, voltage-independent and state-dependent antagonist for NMDA receptor. Ro 8-4304 inhibits 10 μM NMDA-induced currents and 100 μM NMDA-induced currents with IC50s of 2.3 μM and 0.36 μM .
Cat. No.: HY-108504R
CAS No.: 181144-66-1
Synonyms: V 102862 (Standard)
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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 .
Cat. No.: HY-182710
CAS No.: 1081317-31-8
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Research Areas:
DA-0218 is a Nav1.7 inhibitor. DA-0218 exerts state-dependent inhibitory effects. DA-0218 alleviates formalin-induced inflammatory pain behavior and Paclitaxel-induced mechanical hyperalgesia in mice. DA-0218 inhibits Histamine-induced acute pruritus and lymphoma-induced chronic pruritus in mice. DA-0218 can be used in research related to inflammatory pain, neuropathic pain, acute pruritus and chronic pruritus .
Cat. No.: HY-120751A
CAS No.: 2751591-42-9
Target:
Research Areas:
(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 .
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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
