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About This Item
經驗公式(希爾表示法):
C15H10F6N2O3
CAS號碼:
分子量::
380.24
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77
暫時無法取得訂價和供貨情況
推薦產品
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
NS1643 is ether-a-go-go (ERG) channel activator with EC50 = 10.5 μM in Xenopus oocytes and hERG channels expressed in HEK293 cells.
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
Sheeja Rajasingh et al.
Acta pharmacologica Sinica, 39(10), 1590-1603 (2018-04-06)
Induced pluripotent stem cell (iPSC)-based cardiac regenerative medicine requires the efficient generation, structural soundness and proper functioning of mature cardiomyocytes, derived from the patient's somatic cells. The most important functional property of cardiomyocytes is the ability to contract. Currently available
Serdar Durdagi et al.
Journal of molecular graphics & modelling, 74, 153-170 (2017-05-13)
The intra-cavitary drug blockade of hERG1 channel has been extensively studied, both experimentally and theoretically. Structurally diverse ligands inadvertently block the hERG1 K
K Lansu et al.
Cell death & disease, 4, e652-e652 (2013-06-08)
Traditionally the hERG1 potassium channel has been known to have a fundamental role in membrane excitability of several mammalian cells including cardiac myocytes. hERG1 has recently been found to be expressed in non-excitable cancer cells of different histogenesis, but the
Eun-Kyoung Breuer et al.
Cell death & disease, 10(3), 180-180 (2019-02-23)
Potassium ion channels are critical in the regulation of cell motility. The acquisition of cell motility is an essential parameter of cancer metastasis. However, the role of K+ channels in cancer metastasis has been poorly studied. High expression of the
Jacqueline A Treat et al.
Biochemical pharmacology, 169, 113608-113608 (2019-08-30)
Human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs) are used for many applications including safety pharmacology. However, a deficiency or complete absence of several K+ currents suggests repolarization reserve is low in hiPSC-CMs. We determined whether a dual Ito and IKr
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