PNU-120596
(Synonyms: NSC 216666) 目录号 : GC11643
An α7 neuronal nAChR modulator
Cas No.:501925-31-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
PNU-120596 is a positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptor (nAChR) [1].
PNU-120596 is a type 2 PAM. In cell-based assay, PNU-120596 significantly increases the Ca2+-mediated signal at the concentration of 3μM. It enhances the ACh-evoked Ca22+ flux with EC50 value of 216nM in SH-EP1 cells. PNU-120596 also markedly increases the agonist-evoked currents as well as the current duration in Xenopus oocytes. PNU-120596 is specific to α7nAChR over other neuronal nicotinic acetylcholine receptors. PNU-120596 also potentiates the ACh responses mediated byα7nAChRs in rat hippocampal interneurons. It is considered that PNU-120596 modulates the ACh-dependent increase via enhancing the excitatory effect of ACh on GABAergic interneurons. Furthermore, PNU-120596 is found to improve performance in rodent recognition memory model with increasing the phosphorylation of CREB [1, 2].
References:
[1] Hurst R S, Hajós M, Raggenbass M, et al. A novel positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. The Journal of neuroscience, 2005, 25(17): 4396-4405.
[2] Bertrand D, Gopalakrishnan M. Allosteric modulation of nicotinic acetylcholine receptors. Biochemical pharmacology, 2007, 74(8): 1155-1163.
| Cas No. | 501925-31-1 | SDF | |
| 别名 | NSC 216666 | ||
| 化学名 | 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methyl-1,2-oxazol-3-yl)urea | ||
| Canonical SMILES | CC1=CC(=NO1)NC(=O)NC2=CC(=C(C=C2OC)OC)Cl | ||
| 分子式 | C13H14ClN3O4 | 分子量 | 311.73 |
| 溶解度 | ≥ 31.2mg/mL in DMSO | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2079 mL | 16.0395 mL | 32.079 mL |
| 5 mM | 0.6416 mL | 3.2079 mL | 6.4158 mL |
| 10 mM | 0.3208 mL | 1.604 mL | 3.2079 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。