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BIA 10-2474
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BIA 10-2474图片
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
BIA 10-2474 是一种脂肪酸酰胺水解酶 (FAAH) 抑制剂,在大鼠大脑的各个区域的 IC50 值为 50 至 70mg/kg。

Animal experiment:

Rats: Groups of rats (n=4) are pre-treated with BIA 10-2474 (2 mL/kg in 5% Tween 80 in saline i.p.) or with vehicle 40 min prior to radiotracer injection. Rats, in a restraining box, receives 3–4 MBq of high-specific activity [18F]-DOPP in 0.3mL of 10% ethanol in citrate buffer (pH 6) via the tail vein which has been vasodilated in a warm water bath. They are sacrificed by decapitation at 40 min after radiotracer administration, the brain is surgically removed from the skull and stored on ice. Brain regions are excised, blotted, and weighed while blood is collected. Radioactivity in tissues is assayed[1].

产品描述 BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 4.9 nM in HEK293T cells expressing the human recombinant enzyme). It also inhibits FAAH2, α/β-hydrolase domain-containing protein 6 (ABHD6), carboxylesterase 2 (CES2), and patatin-like phospholipase domain 6 (PNPLA6) with IC50 values of 0.4, 0.081, 2, and 11 μM, respectively. BIA 10-2474 alters expression of 161 lipid species, including FAAH substrates as well as other lipid classes, in human cortical neuron cultures indicating compound promiscuity. Formulations containing BIA 10-2474 were previously investigated clinically for the management of chronic pain but use was halted due to development of significant neurotoxicity.