生物活性
CFM-2 is a potent and selective non-competitive AMPAR antagonist[1]. CFM-2 possesses anticonvulsant activity in various models of seizures[2].
体外研究(In Vitro)
CFM-2 inhibits the extracellular signal regulated kinase (ERK1/2) pathway, CFM-2 reduced phosphorylation of cAMP-responsive element binding protein (CREB), suppressed expression of cyclin D1, upregulated the cell cycle regulators and tumor suppressor proteins p21 and p53 and decreased number of lung adenocarcinoma cells in G2 and S phases of the cell cycle.
体内研究(In Vivo)
Pretreatment with CFM-2 delays the progression of seizure rank during repeated administration of pentylentetrazole. At the end of the period of repeated pentylentetrazole treatment (6 weeks) the mean seizure score was 0 in vehicle treated controls, 4.3 in animals treated with vehicle + pentylentetrazole, 2.2 in rats treated chronically with CFM-2 (20 μmol/kg; i.p.) + pentylentetrazole and 1.0 in rats treated repeatedly with CFM-2 (50 μmol/kg; i.p.) + pentylenetetrazole. CFM-2 is also able to antagonize the long-term increase in sensitivity of the convulsant effects of GABA function inhibitors in pentylentetrazole-kindled animals[1].
Intrathecal application of two selective non-competitive AMPAR antagonists, CFM-2 (25 and 50 μg) and GYKI 52466 (50μg), significantly attenuated mechanical and thermal hypersensitivities on the ipsilateral hind paw at 2 and 24 h post-CFA injection. Neither CFM-2 nor GYKI 52466 affects the contralateral basal responses to thermal and mechanical stimuli[4].
分子量
311.34
性状
Solid
Formula
C17H17N3O3
CAS 号
178616-26-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro:
DMSO : ≥ 50 mg/mL (160.60 mM)
* "≥" means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 3.2119 mL 16.0596 mL 32.1192 mL
5 mM 0.6424 mL 3.2119 mL 6.4238 mL
10 mM 0.3212 mL 1.6060 mL 3.2119 mL
*
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, 6 months; -20°C, 1 month。-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。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: