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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
23 Results for "
state-dependent
" in MedChemExpress (MCE) Product Catalog:
Products (23)
23 Results for "state-dependent" in MCE Product Catalog:
11
11 Publications Verification
Synonyms: SEP-363856 hydrochloride; SEP-856 hydrochloride
Research Areas:
Ulotaront hydrochloride (SEP-363856 hydrochloride; SEP-856 hydrochloride) is an orally active, blood-brain barrier-penetrant TAAR1 full agonist with an EC50 of 0.14 µM. Ulotaront hydrochloride is a 5-HT1A agonist and a weak agonist of 5-HT1B and 5-HT7 receptors. Ulotaront hydrochloride state-dependently modulates glutamatergic synaptic transmission in the striatum and hippocampus, reducing spontaneous glutamatergic synaptic activity and enhancing evoked synaptic responses. Ulotaront hydrochloride exhibits antipsychotic-like effects in animal models of schizophrenia and also improves glucose tolerance and reduces body weight by delaying gastric emptying and modulating central neural circuits related to energy balance. Ulotaront hydrochloride can be used in research on schizophrenia and obesity .
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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
Target:
Research Areas:
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-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 .
Cat. No.: HY-136109A
CAS No.: 1310426-33-5
Synonyms: SEP-363856; SEP-856
Research Areas:
Ulotaront (SEP-363856; SEP-856) is an orally active, blood-brain barrier-penetrant TAAR1 full agonist with an EC50 of 0.14 µM. Ulotaront is a 5-HT1A agonist and a weak agonist of 5-HT1B and 5-HT7 receptors. Ulotaront state-dependently modulates glutamatergic synaptic transmission in the striatum and hippocampus, reducing spontaneous glutamatergic synaptic activity and enhancing evoked synaptic responses. Ulotaront exhibits antipsychotic-like effects in animal models of schizophrenia and also improves glucose tolerance and reduces body weight by delaying gastric emptying and modulating central neural circuits related to energy balance. Ulotaront can be used in research on schizophrenia and obesity .
Target:
Research Areas:
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-136109E
CAS No.: 2375116-27-9
Synonyms: SEP-856 mesylate
Research Areas:
Ulotaront mesylate (SEP-363856 mesylate; SEP-856 mesylate) is an orally active, blood-brain barrier-penetrant TAAR1 full agonist with an EC50 of 0.14 µM. Ulotaront mesylate is a 5-HT1A agonist and a weak agonist of 5-HT1B and 5-HT7 receptors. Ulotaront mesylate state-dependently modulates glutamatergic synaptic transmission in the striatum and hippocampus, reducing spontaneous glutamatergic synaptic activity and enhancing evoked synaptic responses. Ulotaront mesylate exhibits antipsychotic-like effects in animal models of schizophrenia and also improves glucose tolerance and reduces body weight by delaying gastric emptying and modulating central neural circuits related to energy balance. Ulotaront mesylate can be used in research on schizophrenia and obesity .
Cat. No.: HY-W040555R
CAS No.: 111974-74-4
Synonyms: N-Desalkylquetiapine dihydrochloride (Standard)
Research Areas:
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 .
Cat. No.: HY-108504R
CAS No.: 181144-66-1
Synonyms: V 102862 (Standard)
Target:
Research Areas:
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 .
Target:
Research Areas:
Arcaine (ARC) is a competitive NMDA receptor polyamine site antagonist and Agmatinase inhibitor. Arcaine inhibits NOS. Arcaine shows anticonvulsant activity and induces state-dependent inhibitory avoidance memory impairment involving the opioid system. Arcaine can be used in research on alcohol use disorder .
Cat. No.: HY-N21743
CAS No.: 118997-92-5
Target:
Cat. No.: HY-186318
Target:
Research Areas:
ICA604025 is a state-dependent inhibitor of human Nav1.9 voltage-gated sodium channel. ICA604025 exerts stronger inhibitory effects on activated/inactivated Nav1.9 than on resting closed Nav1.9, and serves as a tool for investigating the physiological functions of Nav1.9. ICA604025 is applicable to pain-related research .
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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
