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Etravirine(R165335 TMC125)
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。
Etravirine(R165335 TMC125)图片
CAS NO:269055-15-4
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
Molecular Weight (MW)435.28
FormulaC20H15BrN6O
CAS No.269055-15-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 42 mg/mL (96.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info

Chemical Name: 4-(6-Amino-5-bromo-2-(4-cyanoanilino)pyrimidin-4-yloxy)-3,5-dimethylbenzonitrile

InChi Key: PYGWGZALEOIKDF-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H15BrN6O/c1-11-7-14(10-23)8-12(2)17(11)28-19-16(21)18(24)26-20(27-19)25-15-5-3-13(9-22)4-6-15/h3-8H,1-2H3,(H3,24,25,26,27)

SMILES Code: N#CC1=CC(C)=C(OC2=NC(NC3=CC=C(C#N)C=C3)=NC(N)=C2Br)C(C)=C1

SynonymsR-165335; TMC-125; R165335; TMC125; R 165335; TMC 125; R165335; Etravirine. Intelence.
实验参考方法
In Vitro

In vitro activity: Etravirine (TMC125), is highly active against wild-type HIV-1 with EC50 of 1.4 nM to 4.8 nM and shows some activity against HIV-2 with EC50 of 3.5 μM. TMC125 also inhibits a series of HIV-1 group M subtypes and circulating recombinant forms and a group O virus.

In VivoEtravirine has a high genetic barrier to the development of resistance. In phase IIb trials in treatment-experienced patients, including those infected with virus resistant to NNRTIs and protease inhibitors (PIs), TMC125 is active against HIV resistant to currently available NNRTIs, with a similar tolerability profile to that of the control group.
Animal modelNA
Formulation & DosageNA
References

J Med Chem. 2004 May 6;47(10):2550-60; Antimicrob Agents Chemother. 2004 Dec;48(12):4680-6; Lancet. 2007 Jul 7;370(9581):39-48.