CAS No.: 1235403-62-9
PF 05089771 Catalog No. CSN13891
Synonyms: Nav1.7-IN-1;F-05089771;PF-5089771
PF-05089771 is a Nav1.7 channel blocker with an IC50 of 8.6 nM.
| 规格 | 价格 | 促销价格 | 库存 | 数量 |
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纯度 & 质量文件
批次:
靶点选择性
生物活性
- 描述
- 作用机制
动物研究 剂量 给药途径 i.v., p.o.
动物药代数据 Animal Rats[4] Dogs[4] Dose 1 mg/kg (i.v.)
3 mg/kg (p.o.)0.1 mg/kg (i.v.)
3 mg/kg (p.o.)Administration i.v.
p.o.i.v.
p.o.F 27% (p.o.) 35% (p.o.) CLu 448 ml/min/kg (i.v.) 360 ml/min/kg (i.v.) T1/2 4.4 h (i.v.) 4.0 h (i.v.) Tmax 2.0 h (p.o.) 0.9 h (p.o.) CLp 6.0 ml/min/kg (i.v.) 2.7 ml/min/kg (i.v.) Cmax 541 ng/ml (p.o.) 998 ng/ml (p.o.) Vss 1.3 L/kg (i.v.) 0.2 L/kg (i.v.) - 临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点 NCT01529346 Postoperative Dental Pain Phase 2 Completed - United States, Texas ... more >> Central Texas Oral Surgery Associates Austin, Texas, United States, 78705 Premier Research Group Limited Austin, Texas, United States, 78705 PPD Development, LP Austin, Texas, United States, 78744 Collapse << NCT01772264 Healthy Phase 1 Completed - United States, Connecticut ... more >> Pfizer Investigational Site New Haven, Connecticut, United States, 06511 Collapse << NCT01165736 Healthy Phase 1 Completed - United Kingdom ... more >> Pfizer Investigational Site Edinburgh, United Kingdom, EH14 4AP Collapse << - 更多
- 参考文献
- [1] Theile JW, Fuller MD, et al. The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels. Mol Pharmacol. 2016 Nov;90(5):540-548. Epub 2016 Sep 1.
- [2] Cao L, McDonnell A, et al. Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia. Sci Transl Med. 2016 Apr 20;8(335):335ra56.
- [3] Tang Z, Chen Z, et al. Primary erythromelalgia: a review. Orphanet J Rare Dis. 2015 Sep 30;10:127.
- [4] Swain NA, Batchelor D, et al. Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7. J Med Chem. 2017 Aug 24;60(16):7029-7042.
- [5] Alexandrou AJ, Brown AR, et al. Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release. PLoS One. 2016 Apr 6;11(4):e0152405.
实验方案
- 计算器
- 储存液制备
技术信息
| CAS号 | 1235403-62-9 | 储存条件 |
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| 分子式 | C18H12Cl2FN5O3S2 | 运输 | 蓝冰 | |||
| 分子量 | 500.35 | 别名 | Nav1.7-IN-1;F-05089771;PF-5089771 | |||
| 溶解度 |
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动物实验配方 |
