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MIV-150 (PC 815) Sale

(Synonyms: PC 815) 目录号 : GC32390

A non-nucleoside reverse transcriptase inhibitor

MIV-150 (PC 815) Chemical Structure

Cas No.:231957-54-3

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产品描述

MIV-150 is a tight-binding, allosteric inhibitor of reverse transcriptase that is active against HIV-1 and HIV-2 (both EC50s = 1 nM in vitro).1 It has been shown to inactivate viruses that are resistant to other antiviral drugs, including non-nucleoside reverse transcriptase inhibitors, nucleoside reverse transcriptase inhibitors, and protease inhibitors.1 Although MIV-150 possesses poor oral bioavailability, it demonstrates efficacy when formulated as a topical microbicide.2,3

1.Fernández-Romero, J.A., Thorn, M., Turville, S.G., et al.Carrageenan/MIV-150 (PC-815), a combination microbicideSex. Transm. Dis.34(1)9-14(2007) 2.Turville, S.G., Aravantinou, M., Miller, T., et al.Efficacy of Carraguardr-based microbicides in vivo despite variable in vitro activityPLoS One3(9)e3162(2008) 3.Singer, R., Derby, N., Rodriguez, A., et al.The nonnucleoside reverse transcriptase inhibitor MIV-150 in carrageenan gel prevents rectal transmission of simian/human immunodeficiency virus infection in macaquesJ. Virol.85(11)5504-5512(2011)

Chemical Properties

Cas No. 231957-54-3 SDF
别名 PC 815
Canonical SMILES O=C(N[C@@H]1[C@H](C2=C(F)C=CC(C(CC)=O)=C2O)C1)NC3=NC=C(C#N)C=C3
分子式 C19H17FN4O3 分子量 368.36
溶解度 DMF: 30 mg/mL,DMSO: 30 mg/mL,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/mL,Ethanol: 0.25 mg/mL 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.7147 mL 13.5737 mL 27.1474 mL
5 mM 0.5429 mL 2.7147 mL 5.4295 mL
10 mM 0.2715 mL 1.3574 mL 2.7147 mL
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Research Update

Carrageenan/MIV-150 (PC-815), a combination microbicide

Sex Transm Dis 2007 Jan;34(1):9-14.PMID:16924181DOI:10.1097/01.olq.0000223287.46097.4b

Objective: The objective of this article is to study the effect of PC-815, a novel combination microbicide containing carrageenan and the nonnucleoside reverse transcriptase inhibitor (NNRTI) MIV-150, in blocking HIV-1 and HIV-2 infections in vitro as compared with Carraguard alone. Goal: The goal of this study was to develop a combination microbicide that is more efficacious than Carraguard against HIV-1 and HIV-2. Study design: The microtiter syncytial assay was used to evaluate: 1) the antiviral and virucidal activity of MIV-150 against HIV-1MN; 2) the additive effect of MIV-150 when combined with carrageenan; and 3) a possible interference of seminal fluid in the antiviral activity of these compounds. Results: MIV-150 effectively inactivated free virus. Combination of MIV-150 and Carraguard demonstrated an additive antiviral effect. Seminal fluid had no effect on the antiviral activity of MIV-150 or Carraguard. The average concentration that blocks 50% of infection (EC50) for PC-815 was approximately 10 times stronger than Carraguard for the different clinical isolates used in the study. Conclusion: Theoretically, PC-815 is likely to be a more efficacious microbicide than Carraguard.