CAY10435
目录号 : GC40821
A potent, selective FAAH inhibitor
Cas No.:288862-73-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. CAY10435 is a selective, potent inhibitor of rat FAAH exhibiting a Ki value of 0.57 nM. Using a proteonomics approach, CAY10435 was screened against the serine hydrolase family of enzymes, of which FAAH is a member. In this assay, CAY10435 exhibited IC50 values of 0.81 nM, 83 nM, and 50 µM for FAAH, triacylglycerol hydrolase (TGH), and an uncharacterized hydrolase (KIAA1363), respectively. Knowledge of the specificity of CAY10435 obtained from this experiment should allow for more accurate interpretation of results using the inhibitor in complex environments such as whole cells or animals.
| Cas No. | 288862-73-7 | SDF | |
| Canonical SMILES | CCCCCCCCCCCC(=O)c1oc2cccnc2n1 | ||
| 分子式 | C18H26N2O2 | 分子量 | 302.4 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:2): .05mg/ml,Ethanol: 10 mg/ml | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3069 mL | 16.5344 mL | 33.0688 mL |
| 5 mM | 0.6614 mL | 3.3069 mL | 6.6138 mL |
| 10 mM | 0.3307 mL | 1.6534 mL | 3.3069 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Tentative Identification of Phytochemicals from Smilax glabra and Smilax corbularia Extracts by LC-QTOF/MS and Their Bioactive Potential
Plants (Basel) 2022 Aug 11;11(16):2089.PMID:36015393DOI:10.3390/plants11162089.
The Smilacaceae family has been used as a food source and herbal medicine for a long time. This study aims to identify the phytochemicals extracted from Smilax glabra and Smilax corbularia by using LC-QTOF/MS analysis and determine their bioactive potential. Compounds were identified from S. glabra and S. corbularia extracts by LC-QTOF-MS and it was found that longistylin A and CAY10435 have higher degrees of matching compounds (99.66% and 99.87%). Smilax glabra showed antioxidant capacity, i.e., DPPH and ABTS at percentage inhibitions of 71.94 ± 1.46% and 59.84 ± 4.80%, respectively, and FRAP at 730.69 ± 33.62 mg AAE/100 g sample. The total phenolic compound contents of the ethanol, methanol, and water extracts were 0.017 ± 0.001, 0.015 ± 0.001, and 0.016 ± 0.001 mg GAE/g, respectively, while the total flavonoid contents were 0.043 ± 0.002, 0.033 ± 0.002, and 0.006 ± 0.003 mg QE/g, respectively. The anti-inflammatory capacity showed 97.26% protection and 2.74% hemolysis. The antimicrobial activity can inhibit Gram-positive bacteria with a minimum inhibitory concentration (MIC) of 62.5 mg/mL and a minimum bactericidal concentration (MBC) of 500 mg/mL. Smilax corbularia showed antioxidant capacity, i.e., DPPH and ABTS at percentage inhibitions of 72.24 ± 0.64% and 39.87 ± 2.37%, respectively, and FRAP at 208.33 ± 50.80 mg AAE/100 g sample. The total phenolic compound contents of the ethanol, methanol, and water extracts were 0.006 ± 0.000, 0.007 ± 0.002, and 0.002 ± 0.001 mg GAE/g, respectively, while the total flavonoid contents of the ethanol and methanol extracts were 0.012 ± 0.001 and 0.008 ± 0.000 mg QE/g, respectively. The anti-inflammatory capacity showed 96.64% protection and 3.36% hemolysis. The antimicrobial activity of the extracts can inhibit Gram-positive bacteria with a MIC of 31.25 mg/mL and MBC of 125 mg/mL for the ethanol extract and a MIC of 125 mg/mL and MBC of 62.5 mg/mL for the methanol extract. In conclusion, Smilax glabra and Smilax corbularia were found to contain several phytochemicals that can be used for further study. Both Smilax species can also be used as sources of antioxidants and herbal medicines for killing Gram-positive bacteria.
Ex vivo imaging of fatty acid amide hydrolase activity and its inhibition in the mouse brain
J Pharmacol Exp Ther 2006 Mar;316(3):1088-97.PMID:16278311DOI:10.1124/jpet.105.094748.
There is recent behavioral evidence that fatty acid amide hydrolase (FAAH) inhibitors produce a subset of cannabinoid receptor agonist effects, suggesting both anandamide-specific behavioral functions and possible regional differences in FAAH inhibitory effects. Here, we introduce a novel imaging method to quantify regional differences in brain FAAH activity. Upon intravenous [3H]anandamide administration, brain FAAH activity generates [3H]arachidonic acid, which is promptly trapped in membrane phospholipids. As a result, wild-type (WT) brains accumulate tritium in a regionally specific manner that is dependent upon regional FAAH activity, whereas brains from FAAH knockout (KO) mice show a uniform [3H]anandamide distribution. Increasing doses of anandamide + [3H]anandamide fail to alter regional tritium accumulation, suggesting insensitivity toward this process by anandamide-induced changes in regional cerebral blood flow. Regional tritiated metabolite levels in WT brains were highest in the somatosensory and visual cortices and the thalamus. Treatment with methylarachidonyl fluorophosphonate (MAFP) (1 mg/kg i.p.) reduced regional tritium accumulation in the somatosensory and visual cortices (p < 0.01), and at higher doses, the thalamus (p < 0.05). The selective FAAH inhibitor 1-oxazolo[4,5-b]pyridin-2-yl-1-dodecanone (CAY10435), although having similar efficacy as MAFP in reducing tritium in the thalamus and somatosensory and visual cortices, also reduces caudate putamen and cerebellum (p < 0.01) activity. These data indicate FAAH activity generates heterogeneous regional accumulation of [3H]anandamide and metabolites, and they suggest the modulation of endocannabinoid tone by FAAH inhibitors depends upon not only the dose and compound used but also on the degree of FAAH expression in the brain regions examined. This imaging method determines regionally specific FAAH inhibition and can elucidate the in vivo effects of pharmacological agents targeting anandamide inactivation.