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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
35 Results for "
use-dependent block
" in MedChemExpress (MCE) Product Catalog:
Products (35)
35 Results for "use-dependent block" in MCE Product Catalog:
26
16
Target:
Research Areas:
Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na + channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
16
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Riluzole hydrochloride is an anticonvulsant agent and belongs to the family of use-dependent Na + channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
14
14 Cited Publications
Synonyms: 5-(4-Phenoxybutoxy)psoralen
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Research Areas:
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 .
2
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Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research .
2
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Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research .
1
1 Cited Publications
Synonyms: NZ-105 hydrochloride monoethanolate; (±)-Efonidipine hydrochloride monoethanolate
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Efonidipine (NZ-105) hydrochloride monoethanolate is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride monoethanolate inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride monoethanolate modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride monoethanolate reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride monoethanolate improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride monoethanolate can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
1
1 Cited Publications
Synonyms: NZ-105; (±)-Efonidipine
Target:
Research Areas:
Efonidipine (NZ-105) is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine inhibits SARS-CoV-2 main protease. Efonidipine modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine reduces plasma aldosterone levels in vivo. Efonidipine improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
Synonyms: PRAX-562
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Research Areas:
Relutrigine (PRAX-562) is an orally active inhibitor of persistent sodium channel. Relutrigine potently and preferentially inhibits persistent INa induced by ATX-II (Nav 1.5 activator) or the SCN8A mutation N1768D with IC50 values of 141 nM and 75 nM, respectively. Relutrigine exhibits potent use-dependent block and reduces neuronal intrinsic excitability. Relutrigine has effective anticonvulsant activity .
Cat. No.: HY-120751
CAS No.: 1309601-26-0
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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-B1657A
CAS No.: 92134-98-0
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Fosphenytoin disodium is a prodrug of Phenytoin (HY-B0448). Fosphenytoin disodium can be converted to Phenytoin in vivo, which blocks voltage-gated sodium channels in a voltage- and use-dependent manner, prolonging inactivation and slowing recovery. Fosphenytoin disodium enhances GABA responses and, at higher concentrations, mildly modulates calcium channels and increases sodium-potassium ATPase activity. Fosphenytoin disodium raises the afterdischarge threshold, reduces the severity and duration of seizures, alleviates pain-like behavior, and protects hippocampal pyramidal neurons after ischemia without altering GFAP immunoreactivity. Fosphenytoin disodium can be used in research on acute herpes zoster pain, epilepsy, and cerebral ischemia .
Cat. No.: HY-B1751S
CAS No.: 1267657-68-0
Target:
Isotope-Labeled Compounds Sodium Channel Parasite P-glycoprotein Apoptosis Caspase Potassium Channel Cytochrome P450 PARP
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Quinidine-d3 is the deuterated-labeled Quinidine (HY-B1751H). Quinidine is an orally effective antiarrhythmic agent. Quinidine blocks the fast inward sodium current in a use-dependent manner, blocks IKr in a reverse use-dependent manner, and blocks the ultra-rapid delayed rectifier potassium current with an EC50 of 6.2 μM, while also inhibiting CYP2D6 and P-gp. Quinidine induces PARP cleavage, Caspase-3 activation, and increases the proportion of sub-G1 phase apoptotic (Apoptotic) cells . Quinidine can be used in research on ischemia/reperfusion-induced cardiac injury, drug-resistant leukemia, convulsions, and uterine sarcoma .
Research Areas:
Riluzole (Standard) is the analytical standard of Riluzole. This product is intended for research and analytical applications. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na + channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
Cat. No.: HY-10015R
CAS No.: 870653-45-5
Synonyms: 5-(4-Phenoxybutoxy)psoralen (Standard)
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Research Areas:
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 .
Target:
Sodium Channel Parasite P-glycoprotein Apoptosis Caspase Potassium Channel Cytochrome P450 PARP
Research Areas:
Quinidine sulfate is an orally effective antiarrhythmic agent. Quinidine sulfate blocks the fast inward sodium current in a use-dependent manner, blocks IKr in a reverse use-dependent manner, and blocks the ultra-rapid delayed rectifier potassium current with an EC50 of 6.2 μM, while also inhibiting CYP2D6 and P-gp. Quinidine sulfate induces PARP cleavage, Caspase-3 activation, and increases the proportion of sub-G1 phase apoptotic (Apoptotic) cells . Quinidine sulfate can be used in research on ischemia/reperfusion-induced cardiac injury, drug-resistant leukemia, convulsions, and uterine sarcoma .
Target:
Sodium Channel Parasite P-glycoprotein Apoptosis Caspase Potassium Channel Cytochrome P450 PARP
Research Areas:
Quinidine gluconic acid is an orally effective antiarrhythmic agent. Quinidine gluconic acid blocks the fast inward sodium current in a use-dependent manner, blocks IKr in a reverse use-dependent manner, and blocks the ultra-rapid delayed rectifier potassium current with an EC50 of 6.2 μM, while also inhibiting CYP2D6 and P-gp. Quinidine gluconic acid induces PARP cleavage, Caspase-3 activation, and increases the proportion of sub-G1 phase apoptotic (Apoptotic) cells . Quinidine gluconic acid can be used in research on ischemia/reperfusion-induced cardiac injury, drug-resistant leukemia, convulsions, and uterine sarcoma .
Cat. No.: HY-B0211S1
Synonyms: PK 26124-13C6
Cat. No.: HY-16923
CAS No.: 221019-25-6
Synonyms: BIII-890; BIII-890 CL free acid
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Research Areas:
Crobenetine (BIII-890), a benzomorphan derivative, is a potent, selective, and highly use-dependent Na + channel blocker. Crobenetine displaces [3H]BTX from site 2 of the Na + channel (IC50=49 nM) in rat brain synaptosomes, yet exhibits only low binding affinity for other receptors and ion channels. Crobenetine protects brain tissue from the deleterious effects of focal cerebral ischemia in rodents .
Cat. No.: HY-W013727
CAS No.: 136647-02-4
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Research Areas:
UK-78282 hydrochloride is a KV1.3 channel inhibitor with an IC50 value of 0.20 μM and a Kd of 0.39 μM. UK-78282 hydrochloride also inhibits the Kv1.4 Potassium Channel. UK-78282 hydrochloride blocks KV1.3 in a use-dependent manner and inhibits human T lymphocyte activation by regulating the cell cycle. UK-78282 hydrochloride can be used in research related to mental disorders, such as depression and schizophrenia .
Cat. No.: HY-12502B
CAS No.: 111011-53-1
Synonyms: NZ-105 hydrochloride; (±)-Efonidipine hydrochloride
Target:
Research Areas:
Efonidipine (NZ-105) hydrochloride is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
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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
