EMPA

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Chemical Structure| 680590-49-2 同义名 : -
CAS号 : 680590-49-2
货号 : A1164180
分子式 : C23H26N4O4S
纯度 : 99%+
分子量 : 454.542
MDL号 : N/A
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(110 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 EMPA is a high-affinity, reversible, and selective OX2 receptor antagonist. [3H]EMPA binds to human and rat OX2-HEK293 membranes with Kd values ​​of 1.1 and 1.4 nM, respectively. EMPA competitively antagonizes orexin-A and orexin-B-induced [3H]inositol phosphate (IP) accumulation at hOX2 receptors with pA2 values ​​of 8.6 and 8.8, respectively. EMPA displaces [3H]EMPA binding on cell membranes containing human and rat OX2 receptors with Ki values ​​of 1.10±0.24 nM and 1.45±0.13 nM, respectively. In human and mouse V1a receptor binding assays, EMPA has IC50=5.75 µM, Ki=2.63 µM, IC50=12.8 µM, Ki=5.8 µM. In CHO (dHFr-) cells stably expressing hOX2 receptor, EMPA can inhibit the [Ca2+]i response induced by orexin-A or orexin-B, with IC50 values ​​of 8.8±1.7 nM and 7.9±1.7 nM, respectively[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.00mL

2.20mL

1.10mL

22.00mL

4.40mL

2.20mL
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.