|S1658||Dofetilide||<1 mg/mL||88 mg/mL||<1 mg/mL|
|S2456||Chlorpromazine HCl||71 mg/mL||71 mg/mL||71 mg/mL|
|S1979||Amiodarone HCl||<1 mg/mL||23 mg/mL||11 mg/mL|
|S1344||Glimepiride||<1 mg/mL||11 mg/mL||<1 mg/mL|
|S1160||TRAM-34||<1 mg/mL||0.4 mg/mL||<1 mg/mL|
|S4733||Retigabine||<1 mg/mL||60 mg/mL||35 mg/mL|
|S4734||Retigabine 2HCl||75 mg/mL||75 mg/mL||25 mg/mL|
|S1426||Repaglinide||<1 mg/mL||91 mg/mL||91 mg/mL|
|S1971||Nicorandil||17 mg/mL||42 mg/mL||42 mg/mL|
|S2502||Quinine HCl Dihydrate||43 mg/mL||79 mg/mL||79 mg/mL|
|S1716||Glyburide (Glibenclamide)||<1 mg/mL||99 mg/mL||<1 mg/mL|
|S2443||Tolbutamide||<1 mg/mL||54 mg/mL||54 mg/mL|
|S3151||Gliquidone||<1 mg/mL||105 mg/mL||6 mg/mL|
|S2114||Dronedarone HCl||<1 mg/mL||80 mg/mL||40 mg/mL|
|S2489||Nateglinide||<1 mg/mL||63 mg/mL||63 mg/mL|
|S8016||Vonoprazan Fumarate (TAK-438)||<1 mg/mL||62 mg/mL||<1 mg/mL|
|S2825||ML133 HCl||<1 mg/mL||63 mg/mL||6 mg/mL|
|S2562||Hydralazine HCl||1 mg/mL||<1 mg/mL||<1 mg/mL|
|S2601||Gliclazide||<1 mg/mL||65 mg/mL||<1 mg/mL|
|S4037||Doxapram HCl||25 mg/mL||87 mg/mL||2 mg/mL|
|S4630||Diazoxide||<1 mg/mL||46 mg/mL||<1 mg/mL|
|S4632||Hexachlorophene||<1 mg/mL||81 mg/mL||81 mg/mL|
|S2073||Mitiglinide Calcium||<1 mg/mL||<1 mg/mL||2 mg/mL|
- Potassium Channel阻害剤(23)
- 新Potassium Channel製品
Dofetilide(Tikosyn) is a class III antiarrhythmic agent.
Chlorpromazine HCl is a dopamine and potassium channel inhibitor with IC50 of 6.1 and 16 μM for nward-rectifying K+ currents and time-independent outward currents
Low-micromolar amounts of chlorpromazine inhibit SARS-CoV-induced cytopathology. Vero E6 cells in 96-well plates were infected with SARS-CoV isolate Frankfurt-1 (MOI, 0.005) in the presence of 0 to 16 μM CPZ (B), given at t of +1 h p.i. Cells were incubated for 3 days, and viability was monitored using an MTS assay. In parallel, potential compound cytotoxicity was monitored in mock-infected Vero E6 cells. Graphs show the results (averages and SD) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the EC50, CC50, and SI values are given.
Drugs across therapeutic indications induce lipid formation in hiPS-CM. Lipid accumulation was detected in cardiac cells using the LipidTox plate-based fluorescent assay on the Thermo Scientific CellInsight High Content platform. A) Ten drugs increased lipid levels in hiPS-CM following 48 h treatment. The lowest drug dose that induced a N1.5-fold increase in lipid formation is shown. B) Representative images (20×) from the assay are shown to the right. All drugs had >55% cell viability at 48 h at these tested concentrations. C) Of these 10 drugs, 8 significantly increased lipid accumulation following only 24 h treatment (images not shown). All drugs had >80% cell viability at 24 h at these drug doses. The graphs represent the mean fold-change of the lowest concentration of drug that significantly induced lipid formation >1.5-fold more than vehicle control. *P<0.05, **P<0.01, and ***P<0.0001.
Glimepiride is a medium-to-long acting sulfonylurea anti-diabetic compound with an ED50 of 182 μg/kg.
(E) ELISA analysis for C-peptide levels in the presence of vehicle, diazoxide and glimepiride. (F) The fold change of C-peptide content after diazoxide and glimepiride stimulation. Diazoxide and glimepiride decreased and increased C-peptide secretion in wild-type and heterozygous mutated cells, respectively. Neither diazoxide nor glimepiride had an effect on homozygous mutated cells.
TRAM-34 is a selective and potent inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1) with Kd of 20 nM.
Repaglinide is for the treatment of type II diabetes.
Nicorandil is potassium channel activator.
(G) The fold change of C-peptide content after octreotide, nicorandil and nifedipine treatment. Octreotide, nicorandil and nifedipine decreased insulin secretion in wild-type, heterozygous mutated and homozygous mutated cells.
Quinine hydrochloride dihydrate is a natural white crystalline alkaloid having antipyretic (fever-reducing), antimalarial, analgesic (painkilling), anti-inflammatory properties and a bitter taste.
Glyburide (Glibenclamide) is an anti-diabetic compound in a class of medications known as sulfonylureas, closely related to sulfa agents.
Gliquidone is an ATP-sensitive K+ channel antagonist with IC50 of 27.2 nM.
Dronedarone HCl is a therapy for the treatment of patients with paroxysmal and persistent atrial fibrillation or atrial flutter.
Results of hit validation experiments for these four compounds for animals treated at L1 stage at four different concentrations (0.5, 5, 25, and 50 μM). The blue bars represent the values obtained from the original screen as reference points. Error bars are standard error of the mean. Statistical significance for all different doses for individual compounds was calculated with respect to the lowest concentration using two-tailed, t-test (nZ70 animals except n = 37 for Geld 25 μM). The statistical significance values are represented as P<0.05 (*) and P<0.005 (**).
Nateglinide is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.
Vonoprazan Fumarate (TAK-438)は、抗分泌性新しいカリウム競争的酸性のブロッカー（P-CAB）タイプですエージェント、可逆的に胃H+、K+-ATPaseを妨げます。IC50 が 19 nM 、 pH 6.5です。
ML133 HCl is a potent potassium channel inhibitor for Kir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5).
Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM.
Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 ¡À 30 nM
Doxapram HClはTASK-1, TASK-3, TASK-1/TASK-3 のヘテロチャネル機能を阻害、 EC50 がそれぞれ410 nM、 37 μM、 9 μMです。
Mitiglinide Calcium is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.