SN 6

生物活性靶点体外研究 SN 6 试剂级价格

SN 6

CAS号:415697-08-4
英文名:2-[[4-[(4-NITROPHENYL)METHOXY]PHENYL]METHYL]-4-THIAZOLIDINECARBOXYLIC ACID ETHYL ESTER
中文名:SN 6
CBNumber:CB4690807
分子式:C20H22N2O5S
分子量:402.46
MOL File:415697-08-4.mol

SN 6化学性质

沸点 :581.2±50.0 °C(Predicted)
密度 :1.285±0.06 g/cm3(Predicted)
储存条件 :Keep in dark place,Sealed in dry,2-8°C
溶解度 :DMSO : 62.5 mg/mL (155.29 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
形态 :Powder
酸度系数(pKa) :6.63±0.60(Predicted)
颜色 :White to light yellow

SN 6性质、用途与生产工艺

生物活性 SN-6 是一种选择性的 Na+/Ca2+ exchanger (NCX) 抑制剂。SN-6 可抑制NCX1、NCX2和NCX3，对应的IC50值分别为2.9 μM、16 μM和8.6 μM。SN-6 可消除 acetylcholine (ACh) 诱导的血管舒张。
靶点
Target Value
NCX1
(Cell-free assay) 2.9 μM
NCX3
(Cell-free assay) 8.6 μM
NCX2
(Cell-free assay) 16 μM
体外研究

SN 6 is a selective Na ⁺ /Ca ²⁺ exchanger inhibitor, which inhibits the initial rate of ⁴⁵ Ca ²⁺ uptake into NCX1, NCX2, and NCX3 transfectants with IC ₅₀ values of 2.9 ± 0.12, 16 ± 1.1, and 8.6 ± 0.27 μM. SN 6 (up to 30 μM) also less potently inhibits muscarinic acetylcholine receptor, with a higher IC ₅₀ of 18 μM. SN 6 (0.3-30 μM) completely inhibits the initial rate of Na ⁺ _i -dependent ⁴⁵ Ca ²⁺ uptake into Na ⁺ -loaded sarcolemmal vesicles in a dose dependent manner (IC ₅₀ , 5.3 ± 0.37 μM). SN 6 (0.3-10 μM) dose-dependently protects against the hypoxia/reoxygenation-induced LDH release in parental LLC-PK1 cells and NCX1 transfectants but not in K229Q transfectants. SN 6 (1-30 μM) suppresses the bidirectional outward and inward I _NCX in a concentration-dependent manner, with IC ₅₀ values of 2.3 μM and 1.9 μM, respectively. SN 6 also inhibits bidirectional current (I _NCX ) in a [Na ⁺ ]i concentration-dependent manner, with IC ₅₀ values of 3.4 μM, 2.3 μM, and 1.1 μM at 10 mM, 20 mM, and 30 mM [Na ⁺ ]i, respectively. SN 6 inhibits hypoxia/reoxygenation-induced LDH release with an IC ₅₀ value of 0.63 ± 0.15 μM in NCX1 transfectants.