SA72

目录号: GC31239纯度: >98%
SA72是高度选择性的脂肪酸酰胺水解酶(FAAH)抑制剂。

SA72
Cas No.: 934809-60-6
规格价格库存数量操作
1mg¥11,424.00现货
1
5mg¥22,848.00现货
1
10mg¥38,824.00现货
1
20mg¥68,544.00现货
1

文献被引

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    183(7):1867-1883 (2020)
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产品描述 Description

SA72 is a highly selective fatty acid amide hydrolase (FAAH) inhibitor.

Fatty acid amide hydrolase (FAAH) is the primary regulator of several bioactive lipid amides including anandamide. Inhibitors of FAAH are potentially useful for the treatment of pain, anxiety, depression, and other nervous system disorders. However, FAAH inhibitors must display selectivity for this enzyme relative to the numerous other serine hydrolases present in the human proteome in order to be therapeutically acceptable. SA-72 is also a carbamate inhibitor. However, SA-72 shows exceptional selectivity for FAAH. Tested carboxylesterases are not off-targets for SA-72. SA-72 does not have major effects on the level of carboxylesterase activities in liver microsomes[1].

[1]. Zhang D, et al. Fatty acid amide hydrolase inhibitors display broad selectivity and inhibit multiple carboxylesterases as off-targets. Neuropharmacology. 2007 Mar;52(4):1095-105.

实验参考方法 Experimental Reference Method

Kinase experiment:

Rat liver microsomes and cytosol are as sources of carboxylesterase to screen activity. Assays are conducted in 96-well microtiter plates at room temperature. Briefly, 0.5 mg liver microsomes or 2 mg cytosol are incubated with 10 mM SA72 for 30 min and then substrate p-nitrophenyl acetate is added to a final concentration of 1 mM. The plate is read 10 min after substrate addition at 405 nm for the appearance of the p-nitrophenol. The carboxylesterase activities in liver extracts without inhibitor added are set at 100% and the remaining carboxylesterase activities after incubation with inhibitors are calculated relative to the control[1].

References:

[1]. Zhang D, et al. Fatty acid amide hydrolase inhibitors display broad selectivity and inhibit multiple carboxylesterases as off-targets. Neuropharmacology. 2007 Mar;52(4):1095-105.

产品文档 Product Documents

化学性质Chemical Properties

CAS 号
934809-60-6
SMILES
O=C(OCC(N)=O)NCCCC1OCC(C2=C3C=CC(OC)=CC3=CC=C2)CO1
分子式
C21H26N2O6
分子量
402.44 g/mol
溶解性
Soluble in DMSO
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