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Rilpivirine HCl(TMC278 DB08864)
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。
Rilpivirine HCl(TMC278 DB08864)图片
CAS NO:700361-47-3
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
Rilpivirine HCl (TMC-278; R-278474 HCl; DB-08864; Edurant; Rekambys; Cabenuva), the hydrochloride salt of Rilpivirine, is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that has been approved for the treatment of HIV-1 infections. Rilpivirine is usually used in combination with other anti-HIV drugs such as cabotegravir (trade name Cabenuva for the combination of cabotegravir+Rilpivirine, approved in 2021).
理化性质和储存条件
Molecular Weight (MW)402.88
FormulaC22H19ClN6
CAS No.700361-47-3 (HCl)
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 73 mg/mL (199.2 mM)
Water:<1 mg/mL
Ethanol: <1 mg/mL
Other infoChemical Name: (E)-4-((4-((4-(2-cyanovinyl)-2,6-dimethylphenyl)amino)pyrimidin-2-yl)amino)benzonitrile hydrochloride
InChi Key: KZVVGZKAVZUACK-BJILWQEISA-N
InChi Code: InChI=1S/C22H18N6.ClH/c1-15-12-18(4-3-10-23)13-16(2)21(15)27-20-9-11-25-22(28-20)26-19-7-5-17(14-24)6-8-19;/h3-9,11-13H,1-2H3,(H2,25,26,27,28);1H/b4-3+;
SMILES Code: N#CC1=CC=C(NC2=NC=CC(NC3=C(C)C=C(/C=C/C#N)C=C3C)=N2)C=C1.[H]Cl
SynonymsTMC-278; R-278474 HCl; DB-08864; DB08864, TMC278; D08864; TMC-278; R-278474; Edurant; Rekambys; Cabenuva; R-278474, R278474, D08864, TMC 278; Rilpivirine HCl; Edurant.
实验参考方法
In Vitro

In vitro activity: Rilpivirine shows antiviral activity with EC50 ranging from 0.1 nM to 2 nM against wild-type and selected site-directed single and double mutants of HIV-1. Rilpivirine inhibits viral replication at concentrations at which first-generation NNRTIs could not suppress replication, and produces a high genetic barrier to resistance development.

In VivoAfter iv administration of Rilpivirine, Elimination half-life ranges from 4.4 h in rat to 31 h in dog. After oral administration of Rilpivirine in PEG 400, half-life ranges between 2.8 h in rat and 39 h in dog.
Animal modelSprague–Dawley rat, beagle dog, white New Zealand rabbit, and cynomolgus monkey.
Formulation & DosageDissolved in PEG 400; 4 mg/kg ( rat); 1.25 mg/kg (other species); i.v. or p.o.
ReferencesJ Med Chem. 2005 Mar 24;48(6):1901-9; Antimicrob Agents Chemother. 2010 Feb;54(2):718-27.