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化驗
≥98% (HPLC)
形狀
solid
顏色
white to off-white
溶解度
DMSO: ≥20 mg/mL
儲存溫度
2-8°C
SMILES 字串
Oc1ccc(cc1NC(=O)Nc2cc(ccc2O)C(F)(F)F)C(F)(F)F
InChI
1S/C15H10F6N2O3/c16-14(17,18)7-1-3-11(24)9(5-7)22-13(26)23-10-6-8(15(19,20)21)2-4-12(10)25/h1-6,24-25H,(H2,22,23,26)
InChI 密鑰
NJFVQMRYJZHGME-UHFFFAOYSA-N
生化/生理作用
The new diphenylurea compound 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643) was tested in hERG channel. In Xenopus laevis oocytes, NS1643 increased both steady-state and tail current at all voltages tested. The EC50 value for hERG channel activation was 10.5 μM. The effect could be reverted by application of the specific hERG channel inhibitor 4′-[[1-[2-(6-methyl-2-pyridyl)ethyl]-4-piperidinyl]carbonyl]-methanesulfonanilide (E-4031) at 100 nM. Application of NS1643 also resulted in a prolonged postrepolarization refractory time. hERG channel activation by small molecules such as NS1643 increases the repolarization reserve and presents a new antiarrhythmic approach.
特點和優勢
This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
訊號詞
Danger
危險聲明
危險分類
Acute Tox. 3 Oral - Eye Irrit. 2
儲存類別代碼
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
個人防護裝備
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
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Acta pharmacologica Sinica, 39(10), 1590-1603 (2018-04-06)
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The intra-cavitary drug blockade of hERG1 channel has been extensively studied, both experimentally and theoretically. Structurally diverse ligands inadvertently block the hERG1 K
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Human induced pluripotent stem cell-derived cardiomyocytes (hiPS-CMs) are emerging as new and human-relevant source in vitro model for cardiac safety assessment that allow us to investigate a set of 20 reference drugs for predicting cardiac arrhythmogenic liability using optical action
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