| CAS NO: | 898235-65-9 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 346.4 |
| Cas No. | 898235-65-9 |
| Formula | C21H22N4O |
| Solubility | ≤0.3mg/ml in ethanol;2mg/ml in DMSO;3mg/ml in dimethyl formamide |
| Chemical Name | N-phenyl-4-(2-quinolinylmethyl)-1-piperazinecarboxamide |
| Canonical SMILES | O=C(Nc1ccccc1)N1CCN(CC1)Cc1ccc2ccccc2n1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
PF-622 is a potent, time-dependent, irreversible FAAH inhibitor [1].
Fatty acid amide hydrolase (FAAH), belongs to a member of an unusual class of serine hydrolases, is an integral membrane enzyme involved in regulating the fatty acid amide family of lipid transmitters. Genetic or pharmacological inactivation of FAAH leads to elevated endogenous levels of fatty acid amides with analgesic, anti-inflammatory, anxiolytic, and antidepressant phenotypes. The FAAH is an attractive drug target for the treatment of pain [1].
In vitro: PF-622 inhibited the activity of FAAH in a time-dependent manner with the IC50 values of 0.99 and 0.033 μM in human recombinant FAAH for 5 and 60 minutes, respectively [1]. In various human and murine tissue proteome samples, PF-622 showed highly selectivity for FAAH in relative to other serine hydrolases, showing no discernable off-site activity up to 500 μM [1]. PF-622 at 1 μM decreased IL-2 production in both healthy subjects and in HCV patients [2].
References:
[1] Ahn K, Johnson D S, Fitzgerald L R, et al. Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity[J]. Biochemistry, 2007, 46(45): 13019-13030.
[2] Patsenker E, Sachse P, Chicca A, et al. Elevated levels of endocannabinoids in chronic hepatitis C may modulate cellular immune response and hepatic stellate cell activation[J]. International journal of molecular sciences, 2015, 16(4): 7057-7076.
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