GlpBio

BIA 10-2474

目录号: GC18174纯度: >98.00%同义词: 3-(1-(环己基(甲基氨基甲酰基)-1H-咪唑-4-基)吡啶1-氧化物
An inhibitor of FAAH
BIA 10-2474
Cas No.: 1233855-46-3
规格价格库存数量操作
5mg¥1,509.00现货
1
10mg¥2,726.00现货
1
50mg¥3,119.00现货
1
100mg¥4,950.00现货
1
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产品描述 Description

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.

实验参考方法 Experimental Reference Method

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].

References:

[1]. Tong J, et al. Inhibition of fatty acid amide hydrolase by BIA 10-2474 in rat brain. J Cereb Blood Flow Metab. 2016 Sep 20.
[2]. Kaur R, et al. What failed BIA 10-2474 Phase I clinical trial Global speculations and recommendations for future Phase I trials. J Pharmacol Pharmacother. 2016 Jul-Sep;7(3):120-6

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
1233855-46-3
同义词
3-(1-(环己基(甲基氨基甲酰基)-1H-咪唑-4-基)吡啶1-氧化物
化学名
N-cyclohexyl-N-methyl-4-(1-oxido-3-pyridinyl)-1H-imidazole-1-carboxamide
SMILES
CN(C(N1C=NC(C2=C[N+]([O-])=CC=C2)=C1)=O)C3CCCCC3
分子式
C16H20N4O2
分子量
300.4 g/mol
溶解性
DMSO : 2.2 mg/mL (7.32 mM; Need ultrasonic)
保存条件
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°C，然后在超声波浴中震荡一段时间。
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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol