CFMTI
目录号 : GC33146
CFMTI是一个强的，有选择性的mGluR拮抗剂，IC50是2.6nM.
Cas No.:864864-17-5
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
CFMTI is a potent and selective metabotropic glutamate receptor (mGluR) 1 allosteric antagonist with IC50 of 2.6 nM. The selectivity of CFMTI to mGluR1 over mGluR5 was >2000-fold.target : mGluRIC 50: 2.6 nMIn vitro: The IC50 values of CFMTI against human mGluR5 were 5400 ± 1200 nM, showing that the activity of CFMTI is more than 2000-fold weaker against human mGluR5 than against human mGluR1. CFMTI up to 10 μM exhibited no agonistic activity toward any group I mGluR subtypes (data not shown). The IC50 values of CFMTI were higher than 10 μM against all targets, such as NMDA receptorsIn vivo: CFMTI can dissolve in ethanol, polyethylene glycol 400, and distilled water (1:4:5, v/v/v) for intravenous administration. Oral administration of CFMTI inhibited DHPG-induced face-washing behavior in a dose-dependent manner. CFMTI produced dose-dependent inhibition of specific ex vivo binding of [3H]FTIDC to striatal and cerebellar slices in mice. CFMTI significantly inhibit hyperlocomotion induced by MAP at a dose of 2 mg/kg.
[1]. Satow A et al. Unique antipsychotic activities of the selective metabotropic glutamate receptor 1 allosteric antagonist 2-cyclopropyl-5-[1-(2-fluoro-3-pyridinyl)-5-methyl-1H-1,2,3-triazol-4-yl]-2,3-dihydro-1H-isoindol-1-one. J Pharmacol Exp Ther. 2009 Jul;330(1):179-90.
| Cas No. | 864864-17-5 | SDF | |
| Canonical SMILES | O=C1N(C2CC2)CC3=C1C=CC(C4=C(C)N(C5=CC=CN=C5F)N=N4)=C3 | ||
| 分子式 | C19H16FN5O | 分子量 | 349.36 |
| 溶解度 | DMSO : 6.2 mg/mL (17.75 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。 |
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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 | 2.8624 mL | 14.3119 mL | 28.6238 mL |
| 5 mM | 0.5725 mL | 2.8624 mL | 5.7248 mL |
| 10 mM | 0.2862 mL | 1.4312 mL | 2.8624 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。