(R)-(+)-Bay-K-8644

(R)-(+)-Bay-K-8644CAS号: 98791-67-4分子式: C16H15F3N2O4分子量: 356.3描述纯度储存/保存方法别名外观光学活性IC50PK值Ki 数据可溶性/溶解性PubChem CID靶点In vitro(体外研究)

产品描述
描述
(R)-(+)-Bay-K-8644 is a calcium channel inhibitor. (R)-(+)-Bay-K-8644 inhibits Ba2+ currents (IBa) (IC50=975 nM).
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
Bay-K-8644 ((R)-(+)-);R-4407;NI-105;(+)-BAY-K-8644
外观
yellow powder
光学活性
α20D +52.9º, c = 0.42 in 1,4-dioxane
IC50
Transient receptor potential cation channel subfamily A member 1: EC5050 = 20.8 µM (mouse)
PK值
pKa: 7.67 (Predicted), pKb: 1.5 (Predicted)
Ki 数据
Adenosine A1-R: Ki= 785 nM (mouse); Adenosine A3-R: Ki= 2.77 µM (human); Adenosine A3-R: Ki= 6.2 µM (rat); Adenosine A2A-R: Ki= 35.1 µM (rat)
可溶性/溶解性
DMSO : ≥ 300 mg/mL (841.99 mM)
PubChem CID
6604881
生物活性
靶点
IBa
In vitro(体外研究)
(±)-Bay K 8644, a conventional racemic mixture of Bay K 8644, is widely used as an L-type Ca2+ channel agonist. Each optical isomer possesses opposite effects on IBa, Bay-K-8644 (R)-(+)- as an antagonist and S(-)-Bay K 8644 as an agonist. Bay-K-8644 (R)-(+)- inhibits Ba2+ currents (IBa) (IC50=975 nM). When Bay-K-8644 (R)-(+)- (0.5 μM) is applied, IBa is suppressed to 71±10% of control. In the presence of Bay-K-8644 (R)-(+)- (0.5 μM), additional application of forskolin and sodium nitroprusside (SNP) further inhibits IBa. Bay-K-8644 (R)-(+)- is a calcium channel inhibitor.

分子结构图

(R)-(+)-Bay-K-8644