NS 1738
(Synonyms: NSC 213859) 目录号 : GC13064
A positive allosteric modulator of α7-containing nAChRs
Cas No.:501684-93-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Animal experiment: |
Rats[1]Sprague-Dawley rats are used. Adult (2-4 months; 400-450 g) and juvenile (50-60 g) animals are allowed to acclimate to the test room for 90 to 120 min before starting. After acclimation, adult rats are placed alone in their respective test cages. After a brief habituation period (30 min), they are allowed to interact for 5 min with a juvenile rat (trial; T1). During the interactive trial, the adult exhibits investigative behaviors that include close following, grooming, and/or sniffing of the juvenile for as much as 40 to 50% of the trial duration. The time of the investigative interaction is recorded in seconds. The juvenile rat is then removed, and the adult rats are immediately administered varying doses of NS 1738 (10 and 30 mg/kg NS-1738 i.p.) [prepared in 5% ethanol/95% hydroxypropyl-B-cyclodextrin (34% solution); 2.0 mL/kg i.p. ] or Nicotine (0.1 mg/kg i.p.), and then they are returned to their home cage. A second 5-min interactive trial (T2) is conducted 120 min later in the same test cage, and investigative behavior of the adult rat is again monitored and the time is recorded. Recognition ratios of time spent investing the familiar juvenile in T2 divided by time spent investigating the juvenile in T1 are calculated. |
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References: [1]. Timmermann DB, et al. An allosteric modulator of the alpha7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo. J Pharmacol Exp Ther. 2007 Oct;323(1):294-307. |
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NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nAChR, with respect to positive modulation of α7 nAChR (EC50=3.4 μM 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 (EC50=3.4 μM). Under similar experimental conditions, NS 1738 shows comparable efficacy and potency at the rat α7 nAChR (EC50=3.9 μM)[1].
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 AUCbrain /AUCplasma=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)[1].
Reference:
[1]. Timmermann DB, et al. An allosteric modulator of the alpha7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo. J Pharmacol Exp Ther. 2007 Oct;323(1):294-307.
| Cas No. | 501684-93-1 | SDF | |
| 别名 | NSC 213859 | ||
| 化学名 | 1-(5-chloro-2-hydroxyphenyl)-3-(2-chloro-5-(trifluoromethyl)phenyl)urea | ||
| Canonical SMILES | ClC1=C(C=C(C(F)(F)F)C=C1)NC(NC2=CC(Cl)=CC=C2O)=O | ||
| 分子式 | C14H9Cl2F3N2O2 | 分子量 | 365.13 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 25 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml,Ethanol: 10 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7388 mL | 13.6938 mL | 27.3875 mL |
| 5 mM | 0.5478 mL | 2.7388 mL | 5.4775 mL |
| 10 mM | 0.2739 mL | 1.3694 mL | 2.7388 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。