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この商品について
実験式(ヒル表記法):
C17H17N3
CAS番号:
分子量:
263.34
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
製品名
NS8593, An aminobenzimidazole derivative that selectively and reversibly blocks small conductance Ca2+-activated K+ channels in a Ca2+-dependent manner.
Quality Segment
assay
≥98% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 100 mg/mL
shipped in
wet ice
storage temp.
2-8°C
SMILES string
C1(NC(N[C@@H]2CCCC3=C2C=CC=C3)=N4)=C4C=CC=C1
InChI key
XZIZUQSOFMLIIR-CQSZACIVSA-N
General description
An aminobenzimidazole derivative that selectively and reversibly blocks small conductance Ca2+-activated K+ channels (SK1-3; Kd = 420 nM, 600 nM, and 730 nM for SK1, SK2, SK3, respectively) in a Ca2+-dependent manner. It mediates channel gating by interacting with gating structures deep within the inner pore vestibule where Ser507 and Ala532 are deemed to be important for inhibition. Interacts at a site that is distinct from the apamin binding site in SK channels. Can access high-affinity binding sites from both the inside and outside of the cell membrane. Does not affect QT intervals, but prolongs the atrial effective refractive period and prevents acetylcholine-induced atrial fibrillations in ex vivo and in vivo models. Also shown to reversibly block TRPM7 channel (IC50 = 1.6 mM) in smooth muscle cells, primary podocytes, HEK293 cells expressing TRPM7, and ventricular myocytes in a Mg2+-dependent manner and blocks the motility of cells in culture.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Chubanov, V., et al. 2012. Brit. Journ. Pharm.166, 1357.
Jenkins, D., et al. 2011. Hypertension.57, 1129.
Jenkins, D., et al. 2011. Mol. Pharm.79, 899.
Jenkins, D., et al. 2011. Mol. Pharm.79, 899.
Lasse, S., et al. 2011. J. Cardiov. Pharm.57, 672.
Diness, J., et al. 2010. Circ Arrhythm Electrophusiol.3, 380.
Ji, H., et al. 2009. Eur. J. Neurosci.9, 1883.
Strobaek, D., et al. 2006. Mol. Pharm.70, 1771.
Jenkins, D., et al. 2011. Hypertension.57, 1129.
Jenkins, D., et al. 2011. Mol. Pharm.79, 899.
Jenkins, D., et al. 2011. Mol. Pharm.79, 899.
Lasse, S., et al. 2011. J. Cardiov. Pharm.57, 672.
Diness, J., et al. 2010. Circ Arrhythm Electrophusiol.3, 380.
Ji, H., et al. 2009. Eur. J. Neurosci.9, 1883.
Strobaek, D., et al. 2006. Mol. Pharm.70, 1771.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
保管分類
11 - Combustible Solids
wgk
WGK 2
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
492031-MG: + 492031-10MG:
jan
試験成績書(COA)
製品のロット番号・バッチ番号を入力して、試験成績書(COA) を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。