2. Search Result
Search Result
Results for "

Use-dependent block

" in MedChemExpress (MCE) Product Catalog:

27

Inhibitors & Agonists

5

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0211
    Riluzole
    Maximum Cited Publications
    14 Publications Verification

    PK 26124

    		 Sodium Channel GABA Receptor Neurological Disease Cancer
    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.
    Riluzole
  • HY-B0211A
    Riluzole hydrochloride
    Maximum Cited Publications
    14 Publications Verification

    PK 26124 hydrochloride

    		 Sodium Channel GABA Receptor Neurological Disease Cancer
    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.
    Riluzole hydrochloride
  • 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-A0093
    Mexiletine hydrochloride
    2 Publications Verification

    KOE-1173 hydrochloride

    		 Sodium Channel Cardiovascular Disease Neurological Disease
    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 .
    Mexiletine hydrochloride
  • HY-148792
    Relutrigine

    PRAX-562

    		 Sodium Channel Neurological Disease
    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 .
    Relutrigine
  • HY-B1657A
    Fosphenytoin disodium

    		Sodium Channel Neurological Disease
    Fosphenytoin sodium is a phenytoin proagent with similar anticonvulsant properties. Its main mechanism is to block frequency-dependent, use-dependent and voltage-dependent neuronal sodium channels, and therefore limit repetitive firing of action potentials.
    Fosphenytoin disodium
  • 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-12502A
    Efonidipine hydrochloride monoethanolate
    1 Publications Verification

    NZ-105 hydrochloride monoethanolate; (±)-Efonidipine hydrochloride monoethanolate

    		 Calcium Channel SARS-CoV Cardiovascular Disease Neurological Disease Cancer
    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 .
    Efonidipine hydrochloride monoethanolate
  • HY-119521
    Mexiletine
    2 Publications Verification

    KOE-1173

    		 Sodium Channel Cardiovascular Disease Neurological Disease
    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 .
    Mexiletine
  • HY-12502
    Efonidipine
    1 Publications Verification

    NZ-105; (±)-Efonidipine

    		 Calcium Channel SARS-CoV Cardiovascular Disease Neurological Disease Cancer
    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 .
    Efonidipine
  • HY-B0211R
    Riluzole (Standard)

    PK 26124 (Standard)

    		 Reference Standards Sodium Channel GABA Receptor Neurological Disease Cancer
    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.
    Riluzole (Standard)
  • 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-106718
    Barucainide

    		Sodium Channel Cardiovascular Disease
    Barucainide is an Ib-class anti-arrhythmic agent (moderately blocking sodium channel). Barucainide exhibits concentration-dependent inhibitory effects on the maximum upstroke velocity (Vmax) of Purkinje fibers and ventricular muscle in dogs. Barucainide significantly shortens the action potential duration (APD). Barucainide significantly inhibits the pacemaker activity frequency of atrial tissue in rabbits and the enhanced automaticity of Purkinje fibers under normal resting potential in response to isoproterenol. Barucainide cannot inhibit the abnormal automaticity emission frequency of canine Purkinje fibers induced by barium. Barucainide can be used for research on arrhythmias .
    Barucainide
  • HY-B0211S1
    Riluzole-13C6

    PK 26124-13C6

    		 Isotope-Labeled Compounds Sodium Channel GABA Receptor Neurological Disease Cancer
    Riluzole- 13C6 (PK 26124- 13C6) is 13C labeled Riluzole. 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.
    Riluzole-13C6
  • HY-16923
    Crobenetine

    BIII-890; BIII-890 CL free acid

    		 Sodium Channel Neurological Disease
    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 .
    Crobenetine
  • HY-12502B
    Efonidipine hydrochloride

    NZ-105 hydrochloride; (±)-Efonidipine hydrochloride

    		 Calcium Channel SARS-CoV Cardiovascular Disease Cancer
    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 .
    Efonidipine hydrochloride
  • HY-135412
    N-Methyl Duloxetine hydrochloride

    		Sodium Channel Neurological Disease
    N-Methyl Duloxetine hydrochloride is an analgesic. N-Methyl Duloxetine (hydrochloride) elicits both tonic and use-dependent block of neuronal Na + channels .
    N-Methyl Duloxetine hydrochloride
  • HY-B1657AS
    Fosphenytoin-d10 disodium

    		Isotope-Labeled Compounds Sodium Channel Neurological Disease
    Fosphenytoin-d10 (disodium) is deuterium labeled Fosphenytoin (disodium). Fosphenytoin sodium is a phenytoin proagent with similar anticonvulsant properties. Its main mechanism is to block frequency-dependent, use-dependent and voltage-dependent neuronal sodium channels, and therefore limit repetitive firing of action potentials.
    Fosphenytoin-d10 disodium
  • HY-B0211S
    Riluzole-13C,15N2

    PK 26124-13C,15N2

    		 GABA Receptor Sodium Channel Neurological Disease
    Riluzole- 13C, 15N2 is the 13C and 15N labeled Riluzole . 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 .
    Riluzole-13C,15N2
  • HY-B1657AR
    Fosphenytoin disodium (Standard)

    		Reference Standards Sodium Channel Neurological Disease
    Fosphenytoin (disodium) (Standard) is the analytical standard of Fosphenytoin (disodium). This product is intended for research and analytical applications. Fosphenytoin sodium is a phenytoin proagent with similar anticonvulsant properties. Its main mechanism is to block frequency-dependent, use-dependent and voltage-dependent neuronal sodium channels, and therefore limit repetitive firing of action potentials.
    Fosphenytoin disodium (Standard)
  • HY-A0093R
    Mexiletine hydrochloride (Standard)

    KOE-1173 hydrochloride (Standard)

    		 Sodium Channel Reference Standards Cardiovascular Disease Neurological Disease
    Mexiletine (hydrochloride) (Standard) is the analytical standard of Mexiletine (hydrochloride). This product is intended for research and analytical applications. 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 .
    Mexiletine hydrochloride (Standard)
  • HY-119521S
    Mexiletine-d3

    KOE-1173-d3

    		 Isotope-Labeled Compounds Cardiovascular Disease Neurological Disease
    Mexiletine-d3 (KOE-1173-d3) is deuterium labeled Mexiletine. 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 .
    Mexiletine-d3
  • HY-119521S1
    Mexiletine-d6

    KOE-1173-d6

    		 Isotope-Labeled Compounds Sodium Channel Cardiovascular Disease Neurological Disease
    Mexiletine-d6 (KOE-1173-d6) is deuterium labeled Mexiletine. 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 .
    Mexiletine-d6
  • HY-12502AR
    Efonidipine hydrochloride monoethanolate (Standard)

    NZ-105 hydrochloride monoethanolate (Standard); (±)-Efonidipine hydrochloride monoethanolate (Standard)

    		 Reference Standards Calcium Channel SARS-CoV Cardiovascular Disease
    Efonidipine (NZ-105) hydrochloride monoethanolate (Standard) is the analytical standard of Efonidipine hydrochloride monoethanolate (HY-12502AR). This product is intended for research and analytical applications. 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 .
    Efonidipine hydrochloride monoethanolate (Standard)
  • HY-B0211AR
    Riluzole hydrochloride (Standard)

    PK 26124 hydrochloride (Standard)

    		 Sodium Channel GABA Receptor Reference Standards Neurological Disease Cancer
    Riluzole hydrochloride (Standard) is the analytical standard of Riluzole hydrochloride. This product is intended for research and analytical applications. 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.
    Riluzole hydrochloride (Standard)
  • HY-136995
    AFD-21 maleate

    		Sodium Channel Cardiovascular Disease
    AFD-21 maleate is a drug with antiarrhythmic activity. AFD-21 maleate inhibits sodium channels by binding to sodium channels in an inactive state, with both use-dependent and voltage-dependent effects. The unbinding rate of AFD-21 maleate is similar to that of Class I antiarrhythmic drugs with moderate kinetics. AFD-21 maleate can cause a slight prolongation of the action potential duration and significantly reduce the maximum rise rate of the action potential at certain concentrations. AFD-21 maleate also showed use-dependent blocking effects as stimulation frequency increased .
    AFD-21 maleate
  • 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

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

  

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

  

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: