Search Result
Results for "
Hyperpolarization
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-100945
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mAChR
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Neurological Disease
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Nitrocaramiphen hydrochloride is a selective M1 receptor antagonist (Ki: 5.5 nM). Nitrocaramiphen Hydrochloride inhibits the hyperpolarizing effect of muscarine in the muscle fibers .
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- HY-16689
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Potassium Channel
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Others
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VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca 2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission .
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- HY-124424
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Potassium Channel
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Others
Neurological Disease
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VU0071063 is a potent and specific Kir6.2/SUR1 opener (EC50=7.44 μM) and can be used for investigating Kir6.2/SUR1 expressed in the pancreas and brain. VU0071063 inhibits insulin secretion by inducing hyperpolarization of β-cell membrane potential. VU0071063 chemotype has a very steep structure-activity relationships .
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- HY-123264
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Potassium Channel
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Neurological Disease
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RL648_81 is a specific KQT-like subfamily 2/3 (KCNQ2/3) activator with an EC50 of 190 nM. RL648_81 robustly shifts the V1/2 of KCNQ2/3 channels towards hyperpolarized potentials.RL648_81 does not shift the V1/2 of either KCNQ4 or KCNQ5.RL648_81 has the potential for neurologic disorders associated with neuronal hyperexcitability research .
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- HY-101346
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- HY-N12528
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Epoxide Hydrolase
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Cardiovascular Disease
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10,11-EDT, a soluble epoxide hydrolase (sEH) substrate, is a metabolic product of adrenic acid. 10,11-EDT is an endothelium-derived hyperpolarizing factor with strong vasorelaxant effects .
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- HY-131281
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Drug Metabolite
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Others
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Ivabradine impurity 1 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker .
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- HY-131282
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Drug Metabolite
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Others
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Ivabradine impurity 2 is an Ivabradine impurity. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker .
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- HY-131283
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Drug Metabolite
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Endocrinology
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8-Demethyl Ivabradine is a metabolite of Ivabradine. Ivabradine is an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker .
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- HY-P3384
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Antibiotic
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Others
Inflammation/Immunology
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Pezadeftide is a potent antifungal peptide. Pezadeftide can enter fungal cells and cause a rapid mitochondrial response that results in hyperpolarization of the mitochondrial membrane .
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- HY-100799
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GABA Receptor
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Neurological Disease
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ZAPA sulfate is an agonist at low affinity GABAA-receptors. ZAPA sulfate induces membrane hyperpolarization of the Ascaris muscle cell with an EC50 of 10.3 μM .
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- HY-133614
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Potassium Channel
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Others
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Dihydroisopimaric acid activates large conductance Ca 2+ activated K + (BK) channels alphabeta1 in the direct measurement of BKalphabeta1 opening under whole-cell voltage clamp .
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- HY-119102
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HCN Channel
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Inflammation/Immunology
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BPU-11 is a hyperpolarization-activated cyclic nucleotide-gated (HCN) C-linker pocket (CLP) HCN4 CLP ligand. BPU-11 can be used for the research of congenital immune disease .
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- HY-161092A
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HCN Channel
Potassium Channel
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Others
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KIO-301 chloride hydrochloride is an azobenzene photoswitchable compound that blocks voltage-gated ion channels, including hyperpolarization-activated cyclic nucleotide gating (HCN, during exposure to visible light) ) and voltage-gated potassium channels (voltage-gated potassium channels) .
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- HY-122114
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Potassium Channel
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Neurological Disease
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ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC50 of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects .
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- HY-B0162A
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HCN Channel
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Cardiovascular Disease
Endocrinology
Cancer
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Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity .
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- HY-108592
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Potassium Channel
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Neurological Disease
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UCL 2077 is a selective slow-afterhyperpolarization (sAHP) channel blocker (IC50 = 500 nM in hippocampal neurons in culture), having minimal effects on Ca2+ channels, action potentials, input resistance and the medium after hyperpolarization . UCL 2077 is also a subtype-selective blocker of the epilepsy associated KCNQ channels .
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- HY-B0162
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HCN Channel
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Cardiovascular Disease
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Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity .
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- HY-N0219
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Bicuculline
Maximum Cited Publications
21 Publications Verification
(+)-Bicuculline; d-Bicuculline
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GABA Receptor
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Neurological Disease
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Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
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- HY-100418
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Potassium Channel
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Cardiovascular Disease
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SKA-111 is a selective activator of potassium phannel KCa 3.1 , evokes KCa 3.1 membrane hyperpolarization in porcine endothelial cell. SKA-111 is capable of improving Bradykinin (HY-P0206)-induced coronary dilations in the isolated rat heart and can be used for cardiovascular disease research .
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- HY-163455
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HCN Channel
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Neurological Disease
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pan-HCN-IN-1 (Compound J&J12e) is an inhibitor for hyperpolarization-activated and cyclic-nucleotide-gated 1 (HCN1) ion channel, with IC50 of 58 nM. pan-HCN-IN-1 reduces the voltage sag response and enhances EPSP summation in ex vivo rats brain slices .
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- HY-111655
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SKA-31
3 Publications Verification
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Potassium Channel
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Cardiovascular Disease
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SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure .
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- HY-B0162S
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HCN Channel
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Cardiovascular Disease
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Ivabradine-d6 is the deuterium labeled Ivabradine[1]. Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity[2][3][4][5].
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- HY-N12788
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Parasite
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Infection
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T-Cadinol is a sesquiterpene isolated from C. sylvestris that exhibits anti-Trypanosoma cruzi activity, with IC50 values of 18.2 μM and 15.8 μM against trypomastigote and amastigote forms, respectively. T-Cadinol can induce mitochondrial damage in parasites, leading to membrane hyperpolarization and decreased levels of reactive oxygen species. T-Cadinol can be used for the research of Chagas disease .
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- HY-B0162AR
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HCN Channel
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Cardiovascular Disease
Endocrinology
Cancer
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Ivabradine (hydrochloride) (Standard) is the analytical standard of Ivabradine (hydrochloride). This product is intended for research and analytical applications. Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity .
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- HY-163880
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EGFR
Ras
p38 MAPK
Reactive Oxygen Species
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Cancer
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EGFR-IN-119 (Compound 5l) is an inhibitor for EGFR with an IC50 of 84.3 nM. EGFR-IN-119 inhibits the cytotoxicity in lung cancer cell A549 with an IC50 of 1.34 μM. EGFR-IN-119 downregulates the expressions of EGFR, KRAS, and MAP2K genes, exhibits antioxidant activity through reduction of reactive oxygen species (ROS), and hyperpolarizes the mitochondrial membrane potential .
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- HY-118689
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Potassium Channel
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Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
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RA-2 is a negative-gating modulator of KCa2/3 channels with an IC50 of 17 nM. RA-2 inhibits bradykinin-induced endothelium-derived hyperpolarization (EDH)-type relaxation in U46619-precontracted rings. RA-2 can help to define the physiologic and pathomechanistic roles of KCa2/3 in the vasculature, central nervous system, and during inflammation .
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- HY-N0219R
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GABA Receptor
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Neurological Disease
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Bicuculline (Standard) is the analytical standard of Bicuculline. This product is intended for research and analytical applications. Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
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- HY-13422
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UL-FS-49; UL-FS-49CL
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HCN Channel
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Cardiovascular Disease
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Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 μM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 μM, 2.21 μM, 1.90 μM and 1.88 μM, respectively .
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- HY-118317
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Others
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Cardiovascular Disease
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Zacopride is a selective agonist with the activity of enhancing the inward rectifier potassium current (IK1) in rabbit hearts. Zacopride also exhibits significant antiarrhythmic effects, inhibiting ventricular arrhythmias by increasing IK1 without affecting atrial arrhythmias. Zacopride can hyperpolarize the resting membrane potential and shorten the action potential duration (APD) in a concentration-dependent manner. Zacopride significantly reduced the incidence of compound-induced early afterdepolarizations (EADs) at 1 μmol/L .
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- HY-108596
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Potassium Channel
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Inflammation/Immunology
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BL-1249 is a nonsteroidal anti-inflammatory agent (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM) .
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- HY-13422A
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UL-FS-49 free base; UL-FS-49CL free base
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HCN Channel
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Cardiovascular Disease
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Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively .
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- HY-D0085
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Fluorescent Dye
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Others
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DiSC3(5) is a fluorescent probe commonly used as a tracer dye to evaluate mitochondrial membrane potential. The excitation/emission wavelength of DiSC3(5) is up to 622/670 nm. DiSC3(5) can inhibit the respiratory system associated with mitochondrial NAD, and the IC50 value is 8 μM. DiSC3(5) in the presence of Na +/K +-ATPase inhibitor ouabain 2 can induce membrane hyperpolarization of Ehrlich ascites tumor cells .
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- HY-N6789
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KT5720
3 Publications Verification
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PKA
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Neurological Disease
Cancer
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KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 + concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases .
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Cat. No. |
Product Name |
Type |
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- HY-D0085
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Fluorescent Dyes/Probes
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DiSC3(5) is a fluorescent probe commonly used as a tracer dye to evaluate mitochondrial membrane potential. The excitation/emission wavelength of DiSC3(5) is up to 622/670 nm. DiSC3(5) can inhibit the respiratory system associated with mitochondrial NAD, and the IC50 value is 8 μM. DiSC3(5) in the presence of Na +/K +-ATPase inhibitor ouabain 2 can induce membrane hyperpolarization of Ehrlich ascites tumor cells .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P3384
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Antibiotic
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Others
Inflammation/Immunology
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Pezadeftide is a potent antifungal peptide. Pezadeftide can enter fungal cells and cause a rapid mitochondrial response that results in hyperpolarization of the mitochondrial membrane .
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- HY-P5387
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Peptides
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Others
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Connexin mimetic peptide 40,37GAP26 is a biological active peptide. (This peptide corresponds to the GAP26 domain of the extracellular loop of the major vascular connexins (Cx37, Cx40), designated as 37, 40Gap 26 according to Cx homology. It was used to investigate the role of gap junctions in the spread of endothelial hyperpolarizations evoked by cyclopiazonic acid (CPA) through the wall of the rodent iliac artery. The gap junction plaques constructed from Cx37 and Cx40 were abundant in the endothelium. This peptide provides inhibitory effects against subintimal hyperpolarization.)
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- HY-P5389
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Peptides
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Others
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Connexin mimetic peptide 40GAP27 is a biological active peptide. (This peptide corresponds to the GAP27 domain of the second extracellular loop of dominant vascular connexin (Cx40), designated as 40Gap 27. It was used to investigate mechanisms through which oxidant stress impairs communication via gap junctions. When administered, 40Gap27attenuates endothelium-dependent subintimal smooth muscle hyperpolarization.)
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0162S
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Ivabradine-d6 is the deuterium labeled Ivabradine[1]. Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity[2][3][4][5].
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