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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
25 Results for "
outward current
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "outward current" in MCE Product Catalog:
13
Target:
Amiodarone, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outward ionic current (IhERG) tails with an IC50 of ∼45 nM . Amiodarone induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts . Amiodarone can be used in the research of both supraventricular and ventricular arrhythmias .
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13 Publications Verification
Target:
Research Areas:
Cardiovascular Disease Infection Neurological Disease Cancer
Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outward ionic current (IhERG) tails with an IC50 of ∼45 nM . Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts . Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias .
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Research Areas:
Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC50=32 nM) . Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC50 values of 4.9 μm and 8.6 μm, respectively . Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis .
Cat. No.: HY-18740A
CAS No.: 78416-81-6
Synonyms: HL 725
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Trequinsin hydrochloride (HL 725) is a PDE inhibitor, CatSper channel activator, and sperm potassium channel modulator. Trequinsin hydrochloride targets PDE3 with an IC50 of <1 nM. Trequinsin hydrochloride enhances currents and elevates intracellular calcium and cGMP levels via direct activation of the CatSper channel, while inhibiting the outward current conductance of sperm potassium channels. Without inducing premature acrosome reaction, Trequinsin hydrochloride significantly enhances sperm hyperactivated motility, forward motility, and the ability to penetrate viscous media. Trequinsin hydrochloride exerts age-specific positive inotropic and positive lusitropic effects on rabbit ventricular papillary muscles. Trequinsin hydrochloride has been used in studies on the mechanisms underlying male infertility (e.g., asthenozoospermia) .
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o-3M3FBS is the negative control of m-3M3FBS. o-3M3FBS inhibits inward and outward currents via mechanisms independent of PLC acting in an antagonistic manner. In contrast, o-3M3FBS also causes an increase in [Ca 2+]i in an agonistic manner .
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YM-244769 is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 can also increase urine volume and urinary excretion of electrolytes in mice .
Cat. No.: HY-15691
CAS No.: 1202647-54-8
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PF-04455242 is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-04455242 blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-04455242 promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-04455242 attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-04455242 can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal .
Synonyms: 17(R),18(S)-EETeTr
Target:
Research Areas:
(17R,18S)-Epoxyeicosatetraenoic acid (17 (R),18 (S)-EETeTr) is a physiologically active fatty acid metabolite and also a vasodilator targeting BKα. (17R,18S)-Epoxyeicosatetraenoic acid activates the outward potassium current mediated by BK channels, and this effect is independent of the BKβ1 subunit, intracellular/extracellular calcium levels, and sarcoplasmic reticulum calcium release regulated by RyR3. (17R,18S)-Epoxyeicosatetraenoic acid is produced by the epoxidation of eicosapentaenoic acid mediated by CYP1A1 variants. (17R,18S)-Epoxyeicosatetraenoic acid is applicable to research related to arrhythmia .
Cat. No.: HY-111560
CAS No.: 1956337-58-8
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Research Areas:
IQM-266 is a Downstream Regulatory Element Antagonist Modulator (DREAM) ligand with a KD of 4.63 μM. IQM-266 inhibits the KV4.3/DREAM current in a concentration-, voltage-, and time-dependent-manner. IQM-266 also modulates A-type outward potassium currents (IA) from rat dorsal root ganglia (DRG) neurons. IQM-266 can be used for neurological disease research, such as Alzheimer’s disease and Huntington's disease (HD) .
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Research Areas:
YM-244769 dihydrochloride is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 dihydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 dihydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 dihydrochloride can also increase urine volume and urinary excretion of electrolytes in mice .
Target:
Research Areas:
YM-244769 hydrochloride is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 hydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 hydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 hydrochloride can also increase urine volume and urinary excretion of electrolytes in mice .
Cat. No.: HY-172140
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Research Areas:
Ebio3 is a selective potassium channel (KCNQ2) inhibitor with an IC50 of 1.2 nM. Ebio3 binds to the KCNQ2 channel through its hydrophobic tail, causing the S6 helix to move inward, which leads to the closure of the inner gate. The inhibitory effect of Ebio3 is also effective in pathogenic mutants of KCNQ2 (such as R75C and I238L), where it can inhibit outward currents by more than 80%. Ebio3 is expected to be used in the research of neurological diseases such as epilepsy .
Cat. No.: HY-119211
CAS No.: 72456-63-4
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LY 97241 accelerates the apparent rate of inactivation of transient outward K current. LY 97241 is an antiarrhythmic drug .
Cat. No.: HY-P5921
CAS No.: 152618-71-8
Synonyms: TsTx-Kα
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Cat. No.: HY-12773A
CAS No.: 86383-32-6
Synonyms: GPV-129 hydrochloride
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Research Areas:
5-Hydroxy Propafenone (hydrochloride) is an inhibitor of cardiac myocyte repolarizing currents. 5-Hydroxy Propafenone is an active metabolite of propafenone. 5-Hydroxy Propafenone (hydrochloride) inhibits transient outward potassium current (Ito) in isolated human arterial myocytes with an IC50 of 1.5 μM. 5-Hydroxy Propafenone (hydrochloride) is potent Ito inhibitor in neonatal rat ventricular myocytes .
Cat. No.: HY-126704
CAS No.: 90961-53-8
Synonyms: KC-8857
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Research Areas:
Tedisamil (KC-8857) is an antiarrhythmic compound with important biological activities. Tedisamil exhibits a significant slowing effect on heart rate, which is achieved by inhibiting the transient outward potassium current (I(to)) in the atrium. Tedisamil inhibits multiple potassium currents, including IK, K(ATP), and PKA-activated chloride channels, thereby prolonging the cardiac action potential and QT interval, and increasing cardiac reentry. Tedisamil has antiarrhythmic effects on ventricular arrhythmias and atrial flutter in animal models .
Cat. No.: HY-B0432R
CAS No.: 54063-53-5
Synonyms: SA-79 (Standard)
Research Areas:
Propafenone (Standard) is the analytical standard of Propafenone. This product is intended for research and analytical applications. Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC50=32 nM) . Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC50 values of 4.9 μm and 8.6 μm, respectively . Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis .
Cat. No.: HY-15691A
CAS No.: 1322001-35-3
Target:
Research Areas:
PF-4455242 hydrochloride is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-4455242 hydrochloride blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-4455242 hydrochloride promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-4455242 hydrochloride attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-4455242 hydrochloride can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal .
Cat. No.: HY-19397
CAS No.: 275375-69-4
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Research Areas:
BMS-223131 (Compound 1) is a potent maxi-K potassium channel opener. BMS-223131 has a strong inhibitory effect on the CYP2C9 enzyme (IC50 = 1.7 μM) and also shows varying degrees of inhibition on other common CYP enzymes such as CYP1A2, CYP2C19, CYP2D6, and CYP3A4. BMS-223131 can enhance the outward current mediated by maxi-K, by promoting K + efflux to hyperpolarize the cell membrane and reducing Ca 2+ influx. BMS-223131 can be used for the research of neurological disease, such as stroke .
Cat. No.: HY-126704A
CAS No.: 132523-84-3
Synonyms: KC-8857 dihydrochloride
Target:
Research Areas:
Tedisamil (KC-8857) dihydrochloride is an antiarrhythmic compound with important biological activities. Tedisamil dihydrochloride exhibits a significant slowing effect on heart rate, which is achieved by inhibiting the transient outward potassium current (I(to)) in the atrium. Tedisamil dihydrochloride inhibits multiple potassium currents, including IK, K(ATP), and PKA-activated chloride channels, thereby prolonging the cardiac action potential and QT interval, and increasing cardiac reentry. Tedisamil dihydrochloride has antiarrhythmic effects on ventricular arrhythmias and atrial flutter in animal models .
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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
