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Dapivirine

Dapivirine用途

Dapivirine(TMC 120, TMC 120 R147681)是HIV非核苷逆转录酶抑制剂(NNRTI),IC50为24 nM,能抑制包括NNRTI抗性的各种HIV-1毒株。

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Dapivirine名称

[ CAS 号 ]:
244767-67-7

[ 中文名 ]:
Dapivirine

[ 英文名 ]:
Dapivirine (TMC120)

[英文别名 ]:

Dapivirine (TMC120)
TMC120
R-147681
UNII: TCN4MG2VXS
Dapivirine
UNII-TCN4MG2VXS
dapivirinum

Dapivirine生物活性

[ 描述 ]:

Dapivirine(TMC 120, TMC 120 R147681)是HIV非核苷逆转录酶抑制剂(NNRTI),IC50为24 nM,能抑制包括NNRTI抗性的各种HIV-1毒株。

[ 相关类别 ]:

信号通路 >> 抗感染 >> HIV

信号通路 >> 抗感染 >> 逆转录酶

研究领域 >> 感染

[参考文献]

[1]. Van Herrewege Y, et al. In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides. Antimicrob Agents Chemother. 2004 Jan;48(1):337-9.

[2]. Fletcher P, et al. Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor. Antimicrob Agents Chemother. 2009 Feb;53(2):487-95.

[3]. Di Fabio S, et al. Inhibition of vaginal transmission of HIV-1 in hu-SCID mice by the non-nucleoside reverse transcriptase inhibitor TMC120 in a gel formulation. AIDS. 2003 Jul 25;17(11):1597-604.

[4]. Nel AM, et al. Pharmacokinetics of 2 dapivirine vaginal microbicide gels and their safety vs. Hydroxyethyl cellulose-based universal placebo gel. J Acquir Immune Defic Syndr. 2010 Oct;55(2):161-9.

[相关活性小分子]

Dapivirine物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
557.9±60.0 °C at 760 mmHg

[ 分子式 ]:
C₂₀H₁₉N₅

[ 分子量 ]:
329.398

[ 闪点 ]:
291.2±32.9 °C

[ 精确质量 ]:
329.164032

[ PSA ]:
73.63000

[ LogP ]:
3.98

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.649

[ 储存条件 ]:
-20°C

Dapivirine安全信息

[ 危害码 (欧洲) ]:
Xi

Dapivirine

Dapivirine用途

Dapivirine名称

Dapivirine生物活性

Dapivirine物理化学性质

Dapivirine安全信息

Dapivirine合成路线

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