501684-93-1
- CAS号:501684-93-1
- 英文名:NS 1738
- 中文名:501684-93-1
- CBNumber:CB42455756
- 分子式:C14H9Cl2F3N2O2
- 分子量:365.13
- MOL File:501684-93-1.mol
- 沸点 :344.1±42.0 °C(Predicted)
- 密度 :1.617±0.06 g/cm3(Predicted)
- 储存条件 :Store at RT
- 溶解度 :DMSO (Slightly), Methanol (Slightly)
- 形态 :White crystalline solid.
- 酸度系数(pKa) :8.08±0.13(Predicted)
- 颜色 :Off-White to Light Grey
501684-93-1性质、用途与生产工艺
- 生物活性 NS 1738 (NSC 213859) 是一种新型的 α7 nAChR 正向变构调节剂。在卵母细胞实验中,正调节 α7nAChR,EC50 为 3.4 μM。
-
靶点
EC50: 3.4 μM (α7 nAChR, in oocyte experiments)
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体外研究
NS 1738 acts by increasing the peak amplitude of acetylcholine (ACh)-evoked currents at all concentrations; thus, it increased the maximal efficacy of ACh. Plotting peak current amplitude against the logarithm of the NS 1738 concentration used for preincubation reveals a sigmoidal concentration-response relationship that is well fit by the Hill equation (EC 50 =3.4 μM). Under similar experimental conditions, NS 1738 shows comparable efficacy and potency at the rat α7 nAChR (EC 50 =3.9 μM).
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体内研究
To estimate the ability of NS 1738 to permeate the blood-brain barrier, rats are administered 10 mg/kg NS 1738 intraperitoneally. Peak brain concentrations are measured approximately 30 min after injection, and they amount to ~80 ng/mL (~200 nM) at this dose. The ratio between the amount of compound entering the brain and that in plasma is AUC brain /AUC plasma =0.50. The half-life in plasma is estimated to 42 min. Incubation of NS1738 with isolated liver microsomes in vitro indicates that approximately 60 and 75% of NS 1738 is metabolized via the cytochrome P450 system in mouse and rat, respectively, within 1 h. Adult rats administered NS 1738 at 10 and 30 mg/kg i.p. immediately following the initial exposure to a juvenile rat (T1) display significant decreases in the investigative duration of a subsequent exposure to the same juvenile (T2) 2 h later (T2/T1 ratio of 0.69±0.13 and 0.61±0.07, respectively).
- 更新日期:2024/11/08
- 产品编号:HY-12151
- 产品名称:501684-93-1 NS 1738
- CAS编号:501684-93-1
- 包装:5mg
- 价格:680元
- 更新日期:2024/11/08
- 产品编号:HY-12151
- 产品名称:501684-93-1 NS 1738
- CAS编号:501684-93-1
- 包装:10mM * 1mLin DMSO
- 价格:748元
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