产品描述: | EMPA is a high-affinity, reversible and selective orexin OX2 receptor antagonist. [3H]EMPA binds to human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively. |
靶点: |
OX2 Receptor;OXReceptor |
体内研究: |
EMPA (1-300 mg/kg; i.p.) dose-dependently reverses this [Ala11,D-Leu15]orexin-B-induced hyperlocomotion without itself significantly affecting locomotor activity (LMA) in male NMRI mice. EMPA (3-30 mg/kg; i.p.) induces a significant and dose-dependent reduction in the baseline LMA in france and male Wistar rats. EMPA (3-30 mg/kg; i.p.) demonstrates a clear dose-dependent inhibition of spontaneous activity as compared with vehicle-treated animals. |
参考文献: |
1. P Malherbe, et al. Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX2 receptor. Br J Pharmacol. 2009 Apr; 156(8): 1326-1341. |
溶解性: |
DMSO : 50 mg/mL (110.00 mM; Need ultrasonic) |
保存条件: |
2-8℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.2 ml |
11 ml |
22 ml |
5 mM |
0.44 ml |
2.2 ml |
4.4 ml |
10 mM |
0.22 ml |
1.1 ml |
2.2 ml |
50 mM |
0.044 ml |
0.22 ml |
0.44 ml |
|
注意: |
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