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- 详细信息
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
PF-04457845
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1020315-31-4
- 规格：
5mg/10mg/25mg/50mg/100mg
| 规格： | 5mg | 产品价格： | ￥540.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥940.0 |
| 规格： | 25mg | 产品价格： | ￥1990.0 |
| 规格： | 50mg | 产品价格： | ￥2990.0 |
| 规格： | 100mg | 产品价格： | ￥5390.0 |
| 基本信息 | |
| CAS | No.1020315-31-4 |
| 英文名称 | PF-04457845 |
| 别名 | PF04457845 |
| 分子式 | C23H20F3N5O2 |
| 分子量 | 455.43 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD18782721 |
| SMILES | C1CN(CCC1=CC2=CC(=CC=C2)OC3=NC=C(C=C3)C(F)(F)F)C(=O)NC4=NN=CC=C4 |
| InChIKey | BATCTBJIJJEPHM-UHFFFAOYSA-N |
| InChI | 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) |
| PubChem CID | 24771824 |
| 靶点 | FAAH |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | PF-04457845 是一种高效选择性的 FAAH 抑制剂，作用于 hFAAH 和 rFAAH。 |
| 生物活性 | PF-04457845 is a highly efficacious and selective FAAH inhibitor with IC50 values is 7.2±0.63 nM and 7.4±0.62 nM for hFAAH and rFAAH， respectively.[1-2] |
| IC50 | IC50: 7.2±0.63nM(hFAAH);7.4±0.62nM(rFAAH)[1] |
| In Vitro | PF-04457845 inhibits FAAH by a covalent，irreversible mechanism involving carbamylation of the active-site serine nucleophile of FAAH with high in vitro potency(kinact/Ki and IC50 values of 40300 M-1s-1 and 7.2 nM，respectively，for human FAAH). PF-04457845 has exquisite selectivity for FAAH relative to other members of the serine hydrolase superfamily as demonstrated by competitive activity-based protein profiling. PF-04457845 completely inhibits FAAH in human and mouse membrane proteomes at both 10 and 100 μM with no off targets[1]. PF-04457845 is completely selective for FAAH，and none of the other FP-reactive serine hydrolases in the tested tissues are inhibited by PF-04457845 even at 100 μM[2]. |
| 细胞实验 | Oral administration of PF-04457845 at 0.1 mg/kg results in efficacy comparable to that of naproxen at 10 mg/kg in a rat model of inflammatory pain. Oral administration of PF-04457845 causes a significant inhibition of mechanical allodynia measured after 4 h with a minimum effective dose(MED)of 0.1 mg/kg. Furthermore，at 0.1 mg/kg(p.o.)，PF-04457845 inhibits the pain response to a comparable degree as the nonsteroidal anti-inflammatory drug naproxen at 10 mg/kg[1]. FAAH is confirmed to be completely inhibited in mice treated with PF-04457845 at 1 and 10 mg/kg p.o. by competitive activity-based protein profiling(ABPP)study[2]. |
| 数据来源文献 | [1]. Johnson DS， et al. Discovery of PF-04457845: A Highly Potent， Orally Bioavailable， and Selective Urea FAAH Inhibitor. ACS Med Chem Lett. 2011 Feb 10;2(2):91-96. [Content Brief] [2]. Ahn K， et al. Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain. J Pharmacol Exp Ther. 2011 Jul;338(1):114-24. [Content Brief] |
| 单位 | 瓶 |
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IP5790 PF-04457845 代谢酶/蛋白酶 索莱宝
￥540 - 5390
