JP83
目录号 : GC12546
A potent, irreversible FAAH inhibitor
Cas No.:887264-44-0
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
IC50: 14 nM for the human recombinant enzyme
JP83 is an irreversible fatty acyl amide hydrolase (FAAH) inhibitor.
The enzyme fatty acyl amide hydrolase (FAAH) is capable of hydrolyzing anandamide and other esters and amides with long unsaturated acyl chains, which is widely expressed in brain and other tissues.
In vitro: JP83 was identified as an irreversible FAAH inhibitor of the carbamate class when it was tested using radiolabeled oleamide as the substrate. MS results indicated that it inhibited FAAH by carbamylation of the enzyme’s serine nucleophile. In addition, JP83 was found to be able to inhibit FAAH with equal or greater potency than URB597 [1].
In vivo: Mice were treated with JP104, a close analog of JP83, after which they were sacrificed and their tissues removed for click chemistry analysis. It was found that at 1 mg/kg of JP104, FAAH labeling was ~80% of maximum in the brain, while none of the liver and kidney targets were modified to greater than 20%. Furthermore, the nearly complete inactivation of brain FAAH by JP104 at 1 mg/kg was confirmed by competitive ABPP studies with FP-Rh. In contrast, JP104 couldnot reduce the intensity of FP-Rh signals in liver and kidney proteomes significantly [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Alexander, J. P., and Cravatt, B.F. Mechanism of carbmate inactivation of FAAH: Implications for the design of covalent inhibitors and in vivo functional probes for enzymes. Chemistry & Biology 12, 1179-1187 (2005).
| Cas No. | 887264-44-0 | SDF | |
| 化学名 | 3'-carbamoyl-biphenyl-3-yl-hexylphenylcarbamate | ||
| Canonical SMILES | O=C(NCCCCCCc1ccccc1)Oc1cccc(c1)c1cccc(c1)C(=O)N | ||
| 分子式 | C26H28N2O3 | 分子量 | 416.5 |
| 溶解度 | ≤1mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 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 | 2.401 mL | 12.0048 mL | 24.0096 mL |
| 5 mM | 0.4802 mL | 2.401 mL | 4.8019 mL |
| 10 mM | 0.2401 mL | 1.2005 mL | 2.401 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。