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Results for "

inactivated state

" in MedChemExpress (MCE) Product Catalog:

15

Inhibitors & Agonists

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10015
    PAP-1
    10+ Cited Publications

    5-(4-Phenoxybutoxy)psoralen

    		 Potassium Channel Inflammation/Immunology
    PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects .
    PAP-1
  • 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 .
    TROX-1
  • HY-B0516
    Articaine hydrochloride

    Hoe-045

    		 Sodium Channel NF-κB NOD-like Receptor (NLR) Neurological Disease Inflammation/Immunology
    Articaine (Hoe-045) hydrochloride is a selective inhibitor of voltage-gated sodium channels (such as rNav1.4, hNav1.7, and rNav1.8), with an IC50 of 15.8 μM for open-state Na + channels, and IC50 of 40.6 μM and 378 μM for inactivated and resting-state Na + channels, respectively. Articaine hydrochloride exerts local anesthetic activity by inhibiting Na + influx to block nerve impulse conduction, and can also inhibit NF-κB activation and NLRP3 inflammasome pathways, exhibiting anti-inflammatory function. Articaine hydrochloride can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury) .
    Articaine hydrochloride
  • HY-157802
    LTGO-33

    		Sodium Channel Neurological Disease
    LTGO-33 is a potent and selective voltage-gated sodium channel NaV1.8 inhibitor. LTGO-33 inhibits NaV1.8 in the nM potency range and exhibits over 600-fold selectivity against human NaV1.1-NaV1.7 and NaV1.9. LTGO-33 exhibits state-independent inhibition with similar potencies on channels in the closed and inactivated conformations. LTGO-33 inhibits native TTX-R NaV1.8 currents in non-human primate and human DRG neurons, where it reduces action potential firing. LTGO-33 can be used for pain disorders research .
    LTGO-33
  • HY-136330
    Oxazosulfyl

    		Insecticide Parasite Sodium Channel Infection
    Oxazosulfyl is a sulfyl insecticide with potent and cross-spectrum insecticidal activity. Oxazosulfyl inhibits sodium currents by binding to and stabilizing the slow-inactivated state of voltage-gated sodium channels, leading to insect paralysis. Oxazosulfyl's ability to block sodium channels is correlated with its insecticidal activity .
    Oxazosulfyl
  • HY-178963
    Nav1.2-IN-2

    		Sodium Channel Calcium Channel Neurological Disease
    Nav1.2-IN-2 is a Nav1.2 inhibitor with a human IC50 of 0.18 μM. Nav1.2-IN-2 preferentially binds to the inactivated state of Nav1.2, reduces window current, suppresses neuronal depolarization and action potential generation. Nav1.2-IN-2 suppresses Veratridine (HY-N6691)-induced Ca 2+ influx. Nav1.2-IN-2 can be used for the research of epilepsy .
    Nav1.2-IN-2
  • HY-178494
    Nav1.7-IN-19

    		Sodium Channel Potassium Channel Neurological Disease
    Nav1.7-IN-19 is a potent, selective and orally active Nav1.7 inhibitor with an IC50 of 0.49 μM. Nav1.7-IN-19 shows high selectivity for Nav1.7, with selectivities of 312-fold and 662-fold against Nav1.1 and Nav1.5 in the inactivated state. Nav1.7-IN-19 exhibits weak inhibition on hERG potassium channels. Nav1.7-IN-19 exhibits analgesic effect and can be used for the research of neurological disease .
    Nav1.7-IN-19
  • HY-10015R
    PAP-1 (Standard)

    5-(4-Phenoxybutoxy)psoralen (Standard)

    		 Reference Standards Potassium Channel Inflammation/Immunology
    PAP-1 (Standard) is the analytical standard of PAP-1. This product is intended for research and analytical applications. PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects .
    PAP-1 (Standard)
  • HY-171778
    QLS-81

    		Sodium Channel Neurological Disease Inflammation/Immunology
    QLS-81 is a Nav1.7 channel inhibitor (IC50: 1.5 μM). QLS-81 has significant analgesic activity and can relieve neuropathic and inflammatory pain. QLS-81 exerts frequency-dependent inhibitory effects by inhibiting the inactivated state of Nav1.7 channels. QLS-81 can be used in the study of chronic pain .
    QLS-81
  • HY-B0516A
    Articaine

    Hoe-045 free base

    		 Sodium Channel NF-κB NOD-like Receptor (NLR) Neurological Disease Inflammation/Immunology
    Articaine (Hoe-045) is a selective inhibitor of voltage-gated sodium channels (such as rNav1.4, hNav1.7, and rNav1.8), with an IC50 of 15.8 μM for open-state Na + channels, and IC50 of 40.6 μM and 378 μM for inactivated and resting-state Na + channels, respectively. Articaine exerts local anesthetic activity by inhibiting Na + influx to block nerve impulse conduction, and can also inhibit NF-κB activation and NLRP3 inflammasome pathways, exhibiting anti-inflammatory function. Articaine can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury) .
    Articaine
  • HY-B1167A
    Ajmaline hydrochloride

    Cardiorythmine hydrochloride; (+)-Ajmaline hydrochloride

    		 Others Cardiovascular Disease
    Ajmaline hydrochloride is a Class Ia antiarrhythmic agent. It inhibits HERG potassium channels with IC50s of 1.0 μmol/l and 42.3 μmol/l in HEK cells and moth spider oocytes respectively. The inhibitory effect of Ajmaline hydrochloride is rapid, reversible, and positive frequency dependent. It acts primarily on the open state of the HERG channel and may also be combined with the inactivated state. The inhibitory effect of ajmaline hydrochloride is dependent on aromatic residues in the S6 domain, and the sensitivity is significantly reduced in the inactivation-deficient HERG S620T channel. It can also slightly affect the activation voltage of HERG channels. Ajmaline hydrochloride's inhibitory effect on HERG channels may contribute to both its potent antiarrhythmic effects and its potential proarrhythmic risk.
    Ajmaline hydrochloride
  • HY-B0516R
    Articaine hydrochloride (Standard)

    Hoe-045 (Standard)

    		 Reference Standards Sodium Channel NF-κB NOD-like Receptor (NLR) Neurological Disease
    Articaine (Hoe-045) hydrochloride (Standard) is the analytical standard of Articaine hydrochloride (HY-B0516). This product is intended for research and analytical applications. Articaine (Hoe-045) hydrochloride is a selective inhibitor of voltage-gated sodium channels (such as rNav1.4, hNav1.7, and rNav1.8), with an IC50 of 15.8 μM for open-state Na + channels, and IC50 of 40.6 μM and 378 μM for inactivated and resting-state Na + channels, respectively. Articaine hydrochloride exerts local anesthetic activity by inhibiting Na + influx to block nerve impulse conduction, and can also inhibit NF-κB activation and NLRP3 inflammasome pathways, exhibiting anti-inflammatory function. Articaine hydrochloride can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury) .
    Articaine hydrochloride (Standard)
  • HY-B0516AR
    Articaine (Standard)

    Hoe-045 free base (Standard)

    		 Reference Standards Sodium Channel NF-κB NOD-like Receptor (NLR) Inflammation/Immunology
    Articaine (Standard) is the analytical standard of Articaine (HY-B0516A). This product is intended for research and analytical applications. Articaine (Hoe-045) hydrochloride is a selective inhibitor of voltage-gated sodium channels (such as rNav1.4, hNav1.7, and rNav1.8), with an IC50 of 15.8 μM for open-state Na + channels, and IC50 of 40.6 μM and 378 μM for inactivated and resting-state Na + channels, respectively. Articaine hydrochloride exerts local anesthetic activity by inhibiting Na + influx to block nerve impulse conduction, and can also inhibit NF-κB activation and NLRP3 inflammasome pathways, exhibiting anti-inflammatory function. Articaine hydrochloride can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury) .
    Articaine (Standard)
  • HY-183709
    Nav1.8-IN-24

    		Sodium Channel Neurological Disease
    Nav1.8-IN-24 is a voltage-gated sodium channel Nav1.8 inhibitor with pIC50 values of 7.4 (resting state) and 7.5 (inactivated state), and it exhibits high selectivity for NaV1.1-1.7 subtypes. Nav1.8-IN-24 possesses in vitro safety and drug interaction profiles. Nav1.8-IN-24 can be used for the research of acute pain and chronic neuropathic pain .
    Nav1.8-IN-24
  • 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 .
    (S)-TROX-1

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