URB597
(Synonyms: FAAH Inhibitor II, URB-597, URB 597, KDS-4103) 目录号 : GC15951
An inhibitor of FAAH
Cas No.:546141-08-6
Sample solution is provided at 25 µL, 10mM.
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URB597, also known as KDS-4103, is a potent and selective inhibitor of fatty-acid amide hydrolase (FAAH), an enzyme catalyzing the intracellular hydrolysis of the endocannabinoid anandamide, with values of 50% inhibition concentration IC50 of 5 nM and 3 nM in rat brain membranes and human liver microsomes respectively. Study results have shown that, through intraperitoneal (i.p.) administration, URB597 potently inhibits FAAH in rat brain with a median inhibitory dose ID50 of 0.15 mh/kg. However, URB597 fails to show significant inhibition against a few other cannabinoid-related targets (such as cannabinoid receptors and anandamide transport) as well as a broad range of receptors, ion channels, transporters and enymes.
Reference
[1].Daniele Piomelli, Giorgio Tarzia, Andrea Duranti, Andrea Tontini, Marco Mor, Timothy R. Compton, Oliver Dasse, Edward P. Monaghan, Jeff A. Parrot and David Putman. Pharmacological profile of the selective FAAH inhibitor KDS-4103 (URB597). CNS Drug Review 2006; 12(1): 21-38
| Cell experiment [1]: | |
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Cell lines |
Rat brain cortical neurons |
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Preparation method |
The solubility of this compound in DMSO is > 16.9 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
10 nM |
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Applications |
URB597 selectively inhibited the breakdown of [3H]anandamide without reducing its carrier-mediated uptake, which caused non-metabolized [3H]anandamide to accumulate in, and finally exit from the cortical neurons. The accumulated [3H]anandamide was released from the neurons back into the media via passive diffusion rather than reverse transport. |
| Animal experiment [1]: | |
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Animal models |
Rats |
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Dosage form |
0.3 mg/kg; i.p. |
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Applications |
In rats, URB597 rapidly inhibited FAAH (< 15 mins) and its inhibitory effect could last for over 12 hrs. Meanwhile, the contents of anandamide and other fatty-acid ethanolamides were significantly elevated in brain. In addition, URB597 markedly enhanced the hypothermic response caused by a sub-threshold dose of anandamide (5 mg/kg; i.p.). However, when injected alone, URB597 showed no effect on body temperature. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Daniele Piomelli, Giorgio Tarzia, Andrea Duranti, Andrea Tontini, Marco Mor, Timothy R. Compton, Oliver Dasse, Edward P. Monaghan, Jeff A. Parrot and David Putman. Pharmacological profile of the selective FAAH inhibitor KDS-4103 (URB597). CNS Drug Review 2006; 12(1): 21-38. | |
| Cas No. | 546141-08-6 | SDF | |
| 别名 | FAAH Inhibitor II, URB-597, URB 597, KDS-4103 | ||
| 化学名 | [3-(3-carbamoylphenyl)phenyl] N-cyclohexylcarbamate | ||
| Canonical SMILES | C1CCC(CC1)NC(=O)OC2=CC=CC(=C2)C3=CC(=CC=C3)C(=O)N | ||
| 分子式 | C20H22N2O3 | 分子量 | 338.4 |
| 溶解度 | ≥ 16.9 mg/mL in DMSO, ≥ 4.55 mg/mL in EtOH with ultrasonic and warming | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9551 mL | 14.7754 mL | 29.5508 mL |
| 5 mM | 0.591 mL | 2.9551 mL | 5.9102 mL |
| 10 mM | 0.2955 mL | 1.4775 mL | 2.9551 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet