您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > PF-04457845
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
PF-04457845
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF-04457845图片
CAS NO:1020315-31-4
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件


Name: PF-04457845
CAS#: 1020315-31-4
Chemical Formula: C23H20F3N5O2
Exact Mass: 455.15691
Molecular Weight: 455.44121
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Technical InformationSynonym: PF-04457845; PF-4457845; PF 04457845; PF 4457845; PF04457845; PF4457845.
Chemical Name: N-pyridazin-3-yl-4-[(3-[5-(trifluoromethyl)pyridin-2-yl]oxyphenyl)methylidene]piperidine-1-carboxamide
InChi Key: BATCTBJIJJEPHM-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H20F3N5O2/c24-23(25,26)18-6-7-21(27-15-18)33-19-4-1-3-17(14-19)13-16-8-11-31(12-9-16)22(32)29-20-5-2-10-28-30-20/h1-7,10,13-15H,8-9,11-12H2,(H,29,30,32)
SMILES Code: O=C(N1CC/C(CC1)=C\C2=CC=CC(OC3=NC=C(C(F)(F)F)C=C3)=C2)NC4=NN=CC=C4
实验参考方法

PF-04457845 (PF04457845) is a novel, highly potent and selective FAAH (fatty acid amide hydrolase) inhibitor with the potential for mananing pain and other nervous system disorders. It inhibits FAAH with IC50 values of 7.2±0.63 nM and 7.4±0.62 nM for hFAAH and rFAAH, respectively. Pharmacological blockade of FAAH has emerged as a potentially attractive strategy for augmenting endocannabinoid signaling and retaining the beneficial effects of cannabinoid receptor activation, while avoiding the undesirable side effects, such as weight gain and impairments in cognition and motor control, observed with direct cannabinoid receptor 1 agonists. PF-04457845 inhibits human FAAH with high potency (k(inact)/K(i) = 40,300 M(-1)s(-1); IC(50) = 7.2 nM) and is exquisitely selective in vivo as determined by activity-based protein profiling. Oral administration of PF-04457845 produced potent antinociceptive effects in both inflammatory [complete Freund's adjuvant (CFA)] and noninflammatory (monosodium iodoacetate) pain models in rats, with a minimum effective dose of 0.1 mg/kg (CFA model). PF-04457845 displayed a long duration of action as a single oral administration at 1 mg/kg showed in vivo efficacy for 24 h with a concomitant near-complete inhibition of FAAH activity and maximal sustained elevation of anandamide in brain. Significantly, PF-04457845-treated mice at 10 mg/kg elicited no effect in motility, catalepsy, and body temperature. Based on its exceptional selectivity and in vivo efficacy, combined with long duration of action and optimal pharmacokinetic properties, PF-04457845 is a clinical candidate for the treatment of pain and other nervous system disorders.

References: J Pharmacol Exp Ther. 2011 Jul;338(1):114-24; J Med Chem. 2018 May 24;61(10):4476-4504.