SAMT-247

[Description]:

SAMT-247 is a microbicide that selectively inactivate the viral nucleocapsid protein NCp7, causing zinc ejection and preventing RNA encapsidation. SAMT-247 shows good antiviral activity[1][2].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> HIV

Research Areas >> Infection

[Target]

HIV-1IIIB:0.6 μM (EC50)

[In Vitro]

SAMT-247 通过共价修饰 Gag 多聚蛋白[2]。 SAMT-247 在被 HIV-1IIIB 感染的 CEM-SS 细胞中显示出 EC50 为 0.6 μM 的抗病毒活性。SAMT-247 显示出较低的细胞毒性(TC50 > 100 μM)[2]。

[In Vivo]

含有 1% SAMT-247 的凝胶配方保护了六只恒河猴中的五只免受 CCR5(R5)-趋向性 SHIV 阴道感染[3]。

[References]

[1]. Helmold Hait S, et al. An SAMT-247 Microbicide Provides Potent Protection against Intravaginal Simian Immunodeficiency Virus Infection of Rhesus Macaques, whereas an Added Vaccine Component Elicits Mixed Outcomes. J Immunol. 2020 Jun 15;204(12):3315-3328.

[2]. Miller Jenkins LM, et al. Small-molecule inactivation of HIV-1 NCp7 by repetitive intracellular acyl transfer. Nat Chem Biol. 2010 Dec;6(12):887-9.

[3]. Cheng-Mayer C, et al. Delay of simian human immunodeficiency virus infection and control of viral replication in vaccinated macaques challenged in the presence of a topical microbicide. AIDS. 2011 Sep 24;25(15):1833-41.

[ Molecular Formula ]:
C₁₂H₁₄N₂O₃S

[ Molecular Weight ]:
266.32

[ Exact Mass ]:
266.07300

[ PSA ]:
114.56000

[ LogP ]:
2.02160

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ RIDADR ]:
NONH for all modes of transport

Delay of simian human immunodeficiency virus infection and control of viral replication in vaccinated macaques challenged in the presence of a topical microbicide.

AIDS 25(15) , 1833-41, (2011)

Development of an effective vaccine or topical compound to prevent HIV transmission remains a major goal for control of the AIDS pandemic. Using a nonhuman primate model of heterosexual HIV-1 transmis...

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