FAAH inhibitor 1是一种选择性的、可逆的脂肪酸酰胺水解酶（FAAH）抑制剂，IC50值为18±8nM。
Cas No.:326866-17-5
Sample solution is provided at 25 µL, 10mM.
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FAAH Inhibitor 1 is a selective, reversible inhibitor of fatty acid amide hydrolase (FAAH), with an IC50 value of 18±8nM[1]. FAAH Inhibitor 1 exhibits no off-target activity against other serine hydrolases and is suitable for use in research on neurological disorders[2, 3]. FAAH Inhibitor 1 acts as a dual inhibitor of both FAAH and soluble epoxide hydrolase (sEH)[4].
In vivo, FAAH Inhibitor 1 (1mg/kg), administered via intraperitoneal injection in a rat model of formalin-induced acute inflammatory pain, attenuated the licking and guarding behaviors elicited by plantar formalin injection; the resulting analgesic effect was comparable to that of ketoprofen (a conventional non-steroidal anti-inflammatory drug)[4].
References:
[1] Wang X, Sarris K, Kage K, et al. Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors[J]. Journal of medicinal chemistry, 2009, 52(1): 170-180.
[2] Dider S, Ji J, Zhao Z, et al. Molecular mechanisms involved in the side effects of fatty acid amide hydrolase inhibitors: a structural phenomics approach to proteome-wide cellular off-target deconvolution and disease association[J]. NPJ systems biology and applications, 2016, 2(1): 16023.
[3] Papa A, Pasquini S, Contri C, et al. Polypharmacological approaches for CNS diseases: focus on endocannabinoid degradation inhibition[J]. Cells, 2022, 11(3): 471.
[4] Wilt S, Kodani S, Valencia L, et al. Further exploration of the structure-activity relationship of dual soluble epoxide hydrolase/fatty acid amide hydrolase inhibitors[J]. Bioorganic & medicinal chemistry, 2021, 51: 116507.
FAAH inhibitor 1是一种选择性的、可逆的脂肪酸酰胺水解酶（FAAH）抑制剂，IC50值为18±8nM[1]。FAAH inhibitor 1对其他丝氨酸水解酶无脱靶活性，能够用于神经疾病研究[2, 3]。FAAH inhibitor 1是FAAH和可溶性环氧化物水解酶（sEH）的双重抑制剂[4]。
在体内，FAAH inhibitor 1（1mg/kg）通过腹腔注射给药治疗福尔马林诱导的急性炎症痛大鼠模型，减轻了因足底注射福尔马林引起的舔舐和守护行为，产生的镇痛效果与酮洛芬（一种传统非甾体抗炎药）相当[4]。
| Animal experiment [1]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Rats were removed from their home cages and briefly anesthetized with isoflurane. A dilute formalin solution (5%, 50µL) was then injected into the plantar surface of the right hindpaw. Rats were placed on an elevated mesh rack for observation. The amount of time spent licking or guarding the injected hindpaw was measured in seconds in 5min blocks for one hour following hindpaw injection. FAAH inhibitor 1 was dissolved in DMSO to a stock concentration of 10mM. The 10mM stock was further diluted into injectable doses (0.1 and 1.0mg/kg) using a vehicle solution comprising 10% ethanol, 10% cremophor, and 80% saline. Ketoprofen was dissolved in the same vehicle. Drugs were injected intraperitoneally in a volume of 1mL/kg. All drugs were administered 30min before hindpaw injection of formalin. |
Dosage form | 0.1, 1mg/kg; i.p. |
Applications | Intraperitoneal administration of the higher dose of FAAH inhibitor 1 attenuates licking and guarding behaviors induced by an intraplantar injection of formalin. The lower dose of FAAH inhibitor 1 was ineffective suggesting a dose-dependent relationship in antinociception. The magnitude of antinociception produced by 1mg/kg of FAAH inhibitor 1 is comparable to antinociception produced by a high dose of ketoprofen (30mg/kg). |
References: | |
| Cas No. | 326866-17-5 | SDF | |
| 别名 | Benzothiazole analog 3 | ||
| Canonical SMILES | CC1=CC=C(N=C(C2=CC=C(NC(C3CCN(S(=O)(C4=CC=CS4)=O)CC3)=O)C=C2)S5)C5=C1 | ||
| 分子式 | C24H23N3O3S3 | 分子量 | 497.65 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C,protect from light |
| 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 | 2.0094 mL | 10.0472 mL | 20.0944 mL |
| 5 mM | 401.9 μL | 2.0094 mL | 4.0189 mL |
| 10 mM | 200.9 μL | 1.0047 mL | 2.0094 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
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- Purity: >98.00% Appearance: A solid
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- SDS (Safety Data Sheet)
- Datasheet