501684-93-1
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- CAS号:
- 501684-93-1
- 英文名:
- NS 1738
- 英文别名:
- NS 1738;NSC 213859;NS 1738 (NSC 213859);1-(5-Chloro-2-hydroxy-phenyl)-3-(2-chloro-5-trifluoromethyl-phenyl)-urea;N-(5-Chloro-2-hydroxyphenyl)-N'-[2-chloro-5-(trifluoromethyl)phenyl]urea;Urea, N-(5-chloro-2-hydroxyphenyl)-N'-[2-chloro-5-(trifluoromethyl)phenyl]-;NS 1738,Nicotinic acetylcholine receptors,NSC213859,inhibit,Inhibitor,nAChR,NS-1738,NSC-213859,NS1738
- 中文名:
- 501684-93-1
- 中文别名:
- 化合物NS 1738;1-(5-氯-2-羟基苯基)-3-(2-氯-5-(三氟甲基)苯基)脲
- CBNumber:
- CB42455756
- 分子式:
- C14H9Cl2F3N2O2
- 分子量:
- 365.13
- MOL File:
- 501684-93-1.mol
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501684-93-1化学性质
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沸点:
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344.1±42.0 °C(Predicted)
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密度:
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1.617±0.06 g/cm3(Predicted)
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储存条件:
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Store at RT
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溶解度:
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DMSO (Slightly), Methanol (Slightly)
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形态:
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White crystalline solid.
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酸度系数(pKa):
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8.08±0.13(Predicted)
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颜色:
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Off-White to Light Grey
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501684-93-1性质、用途与生产工艺
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。
EC50: 3.4 μM (α7 nAChR, in oocyte experiments)
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).
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).
501684-93-1
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更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/01/25 | HY-12151 | 501684-93-1 NS 1738 | 501684-93-1 | 5mg | 680元 |
2024/01/25 | HY-12151 | 501684-93-1 NS 1738 | 501684-93-1 | 10mM * 1mLin DMSO | 748元 |
501684-93-1, 501684-93-1 相关搜索:
- 合成有机化合物配体
- 1-(5-氯-2-羟基苯基)-3-(2-氯-5-(三氟甲基)苯基)脲
- 化合物NS 1738
- 501684-93-1
- NS 1738,Nicotinic acetylcholine receptors,NSC213859,inhibit,Inhibitor,nAChR,NS-1738,NSC-213859,NS1738
- NS 1738 (NSC 213859)
- Urea, N-(5-chloro-2-hydroxyphenyl)-N'-[2-chloro-5-(trifluoromethyl)phenyl]-
- 1-(5-Chloro-2-hydroxy-phenyl)-3-(2-chloro-5-trifluoromethyl-phenyl)-urea
- NSC 213859
- N-(5-Chloro-2-hydroxyphenyl)-N'-[2-chloro-5-(trifluoromethyl)phenyl]urea
- NS 1738