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PF-05089771
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-05089771图片
CAS NO:1235403-62-9
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

产品介绍
理化性质和储存条件
Molecular Weight (MW) 500.34
Formula C18H12Cl2FN5O3S2
CAS No.1235403-62-9 (free base);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:>35 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES O=S(C1=CC(Cl)=C(OC2=CC=C(Cl)C=C2C3=C(N)NN=C3)C=C1F)(NC4=CSC=N4)=O
Synonyms PF05089771; PF 05089771; PF-05089771
实验参考方法
In Vitro

In vitro activity: PF-05089771 is a potent and subtype selective NaV1.7 inhibitor with IC50 of 11 nM. It binds to a site in the voltage sensing domain and interacts with the voltage-sensor domain (VSD) of domain IV. PF-05089771 exhibits a slow onset of block that is depolarization and concentration dependent, with a similarly slow recovery from block. Furthermore, the onset of block by PF-05089771 develops with similar rates using protocols that bias channels into predominantly fast- or slow-inactivated states, suggesting that channel inhibition is less dependent on the availability of a particular inactivated state than the relative time that the channel is depolarized.


Kinase Assay: PF-05089771 is a potent and subtype selective NaV1.7 inhibitor with IC50 of 11 nM. It binds to a site in the voltage sensing domain and interacts with the voltage-sensor domain (VSD) of domain IV.

In Vivo
Animal model
Formulation & Dosage
References J Med Chem. 2017 Aug 24;60(16):7029-7042.