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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
18 Results for "
inactivated state
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "inactivated state" in MCE Product Catalog:
13
13 Publications Verification
Synonyms: 5-(4-Phenoxybutoxy)psoralen
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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 .
Cat. No.: HY-120751
CAS No.: 1309601-26-0
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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-B0516
CAS No.: 23964-57-0
Synonyms: Hoe-045
Research Areas:
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) .
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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 .
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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 .
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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 .
Cat. No.: HY-178494
CAS No.: 3097995-73-5
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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 .
Cat. No.: HY-10015R
CAS No.: 870653-45-5
Synonyms: 5-(4-Phenoxybutoxy)psoralen (Standard)
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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 .
Cat. No.: HY-171778
CAS No.: 2835455-57-5
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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 .
Cat. No.: HY-B0516A
CAS No.: 23964-58-1
Synonyms: Hoe-045 free base
Research Areas:
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) .
Synonyms: Cardiorythmine hydrochloride; (+)-Ajmaline hydrochloride
Target:
Cat. No.: HY-B0516AR
CAS No.: 23964-58-1
Synonyms: Hoe-045 free base (Standard)
Research Areas:
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) .
Cat. No.: HY-B0516R
CAS No.: 23964-57-0
Synonyms: Hoe-045 (Standard)
Research Areas:
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) .
Cat. No.: HY-183709
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Research Areas:
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 .
Cat. No.: HY-W699451
Cat. No.: HY-120751A
CAS No.: 2751591-42-9
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(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.: HY-13551C
CAS No.: 80277-14-1
Synonyms: m-AMSA isethionate; Acridinyl anisidide isethionate
Target:
Topoisomerase DNA/RNA Synthesis DNA Alkylator/Crosslinker ERK Akt GSK-3 Bcl-2 Family Caspase Apoptosis Potassium Channel
Research Areas:
Amsacrine isethionate (m-AMSA isethionate) is a Topoisomerase II inhibitor. Amsacrine isethionate intercalates into DNA. Amsacrine isethionate induces Ca 2+-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine isethionate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine isethionate blocks HERG potassium channels in the open/inactivated state. Amsacrine isethionate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine isethionate exhibits anti-leukemic activity. Amsacrine isethionate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine isethionate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies .
Cat. No.: HY-13551D
CAS No.: 80277-11-8
Synonyms: m-AMSA lactate; Acridinyl anisidide lactate
Target:
Topoisomerase DNA/RNA Synthesis DNA Alkylator/Crosslinker ERK Akt GSK-3 Bcl-2 Family Caspase Apoptosis Potassium Channel
Research Areas:
Amsacrine lactate (m-AMSA lactate) is a Topoisomerase II inhibitor. Amsacrine lactate intercalates into DNA. Amsacrine lactate induces Ca 2+-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine lactate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine lactate blocks HERG potassium channels in the open/inactivated state. Amsacrine lactate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine lactate exhibits anti-leukemic activity. Amsacrine lactate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine lactate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies .
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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
