IC87201
目录号 : GC30847
An inhibitor of the nNOS-PSD-95 protein-protein interaction
Cas No.:866927-10-8
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');)
;)
IC87201 is an inhibitor of the protein-protein interaction between neuronal nitric oxide synthase (nNOS) and post-synaptic density protein 95 (PSD-95).1 It inhibits the binding of PSD-95 to nNOS (IC50 = 31 ?M). IC87201 inhibits NMDA-induced cGMP production, a marker of PSD-95-dependent NOS activation, in primary rat hippocampal neurons (IC50 = 2.7 ?M). IC87201 (10 ?M) reduces MPP+-induced production of reactive oxygen species (ROS), cytochrome c release, and apoptosis in primary rat cortical neurons.2 In vivo, IC87201 decreases thermal hyperalgesia in mice (ED50 = 0.1 mg/kg), as well as mechanical allodynia in a rat model of neuropathic pain induced by chronic constriction injury (CCI). It also reduces immobility time in the forced swim and tail suspension tests in mice when administered at a dose of 1 mg/kg.3
1.Florio, S.K., Loh, C., Huang, S.M., et al.Disruption of nNOS-PSD95 protein-protein interaction inhibits acute thermal hyperalgesia and chronic mechanical allodynia in rodentsBr. J. Pharmacol.158(2)494-506(2009) 2.Hu, W., Guan, L.-S., Dang, X.-B., et al.Small-molecule inhibitors at the PSD-95/nNOS interface attenuate MPP+-induced neuronal injury through Sirt3 mediated inhibition of mitochondrial dysfunctionNeurochem. Int.7957-64(2014) 3.Doucet, M.V., Levine, H., Dev, K.K., et al.Small-molecule inhibitors at the PSD-95/nNOS interface have antidepressant-like properties in miceNeuropsychopharmacology38(8)1575-1584(2013)
Animal experiment: | MK-801 is dissolved in saline and administered intraperitoneally (i.p.) in a within subjects dosing paradigm in order of increasing dose (0.1, 0.2, and 0.3 mg/kg). IC87201 (1, 4 and 10 mg/kg) and ZL006 (10 mg/kg) are dissolved in a vehicle containing 3% DMSO with the remaining 97% comprised of 1:1:18 of emulphor:ethanol:0.9% NaCl. Active compounds are compared with equivalent volumes of the appropriate vehicle in each case. MK-801, IC87201, and ZL006 are administered 30 min prior to behavioral testing. All drugs are administered intraperitoneally (i.p.) in a volume of 1 mL/kg[2]. |
References: [1]. Bach A, et al. Biochemical investigations of the mechanism of action of small molecules ZL006 and IC87201 as potential inhibitors of the nNOS-PDZ/PSD-95-PDZ interactions. Sci Rep. 2015 Jul 16;5:12157. | |
| Cas No. | 866927-10-8 | SDF | |
| Canonical SMILES | OC1=C(Cl)C=C(Cl)C=C1CNC2=CC=C3N=NNC3=C2 | ||
| 分子式 | C13H10Cl2N4O | 分子量 | 309.15 |
| 溶解度 | DMSO : ≥ 28 mg/mL (90.57 mM) | 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 | 3.2347 mL | 16.1734 mL | 32.3468 mL |
| 5 mM | 0.6469 mL | 3.2347 mL | 6.4694 mL |
| 10 mM | 0.3235 mL | 1.6173 mL | 3.2347 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet