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state-dependent

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Calcium Channel (2) Drug Isomer (1) Drug Metabolite (2) HCN Channel (2) iGluR (1) Isotope-Labeled Compounds (1) NOD-like Receptor (NLR) (1) Reference Standards (1) Serotonin Transporter (2) Sodium Channel (8) Vasopressin Receptor (1)
By Research Areas:	Cancer (1) Cardiovascular Disease (2) Inflammation/Immunology (1) Neurological Disease (14)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W052508

Norquetiapine 1 Publications Verification N-Desalkylquetiapine	Drug Metabolite 5-HT Receptor HCN Channel Serotonin Transporter	Neurological Disease
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-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 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 .

HY-12796A

Raxatrigine hydrochloride Vixotrigine hydrochloride; GSK-1014802 hydrochloride; CNV1014802 hydrochloride	Sodium Channel	Neurological Disease
Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.

HY-12796

Raxatrigine Vixotrigine; GSK-1014802; CNV1014802	Sodium Channel	Neurological Disease
Raxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.

HY-120751

TROX-1	Calcium Channel	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 .

HY-W158030

2-Guanidinobezimidazole 2GBI	NOD-like Receptor (NLR) Vasopressin Receptor	Cardiovascular Disease Neurological Disease Cancer
2-Guanidinobezimidazole (2GBI) is a NLRP3 agonist with a K_D 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 .

HY-108504

Co 102862 V 102862	Sodium Channel	Neurological Disease
Co 102862 (V 102862) is a potent, broad-spectrum, state-dependent Na ⁺ channel blocker. Co 102862 is also an orally active anticonvulsant .

HY-123825

GX-674	Sodium Channel	Cardiovascular Disease Neurological Disease
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 .

HY-W052508S

Norquetiapine-d8 N-Desalkylquetiapine-d₈	Isotope-Labeled Compounds	Others Neurological Disease Inflammation/Immunology
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-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 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 .

HY-155058

Nav1.3 channel inhibitor 1	Sodium Channel	Neurological Disease
Nav1.3 channel inhibitor 1 (compound 15b) is a state-dependent voltage-gated sodium channel Na_v1.3 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 .

HY-W040555

Norquetiapine dihydrochloride 1 Publications Verification N-Desalkylquetiapine dihydrochloride	Drug Metabolite 5-HT Receptor HCN Channel Serotonin Transporter	Neurological Disease
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-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 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 .

HY-138816

Nav1.7-IN-15	Sodium Channel	Neurological Disease
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 .

HY-134525

Ro 8-4304	iGluR	Others
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 .

HY-108504R

Co 102862 (Standard) V 102862 (Standard)	Reference Standards Sodium Channel	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 .

HY-182710

DA-0218	Sodium Channel	Neurological Disease
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 .

HY-120751A

(S)-TROX-1	Drug Isomer Calcium Channel	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 .

Cat. No.	Product Name	Chemical Structure

HY-W052508S

Norquetiapine-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-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 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 .

Norquetiapine-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-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 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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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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