431980-38-0|RN-18|RN-18|MFCD03142961-范德生物科技公司

RN-18

NMR下载 COA and HPLC MSDS下载
names：
RN-18
CAS号：
431980-38-0
MDL Number： MFCD03142961
MF(分子式)： C20H16N2O4S MW(分子量)： 380.417
EINECS:Not available Reaxys Number:Not available
Pubchem ID:1317590 Brand:BIOFOUNT

RN-18(431980-38-0)是病毒体感染因子（Vif）APOBEC相互作用和HIV-1复制的选择性抑制剂（非许可H9细胞中IC50 = 6μM），拮抗Vif功能并仅在A3G存在的情况下抑制HIV-1复制。

货品编码	规格	纯度	价格 (¥)	现价(¥)	特价(¥)	库存描述	数量	总计 (¥)

大包装询价提供各种包装，敬请垂询
收藏商品商品点评加入购物车立即购买

快速询价

收起

你想询价的产品

*产品名称：

CAS号：

产品编号：

需求描述：

请准确填写您的联系方式，以便为您提供最好的服务。

*公司名称：

*电子邮箱：

联系人：

*电话：

*验证码：

询价

中文别名	RN-18(431980-38-0);RN 18；RN18；N-（2-甲氧基苯基）-2-（4-硝基苯基）硫烷基苯甲酰胺; 2-（4-硝基苯硫基）-N-（2-甲氧基苯基）苯甲酰胺; AC1LQ42R; Ambcb6776439;
英文别名	RN-18(431980-38-0);RN-18; RN 18; RN18; N-(2-methoxyphenyl)-2-(4-nitrophenyl)sulfanylbenzamide; 2-(4-Nitrophenylthio)-N-(2-methoxyphenyl)benzamide; AC1LQ42R; Ambcb6776439;
CAS号	431980-38-0
Inchi	InChI=1S/C20H16N2O4S/c1-26-18-8-4-3-7-17(18)21-20(23)16-6-2-5-9-19(16)27-15-12-10-14(11-13-15)22(24)25/h2-13H,1H3,(H,21,23)
InchiKey	JKNUDHUHXMELIJ-UHFFFAOYSA-N
分子式 Formula	C20H16N2O4S
分子量 Molecular Weight	380.417
溶解度Solubility	生物体外In Vitro:DMSO溶解度100 mg/mL(262.87 mM;Need ultrasonic)H2O< 0.1 mg/mL(insoluble)
性状	Solid powder
储藏条件 Storage conditions	storage at -4℃ (1-2weeks), longer storage period at -20℃ (1-2years)

RN-18(431980-38-0)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tags:RN-18试剂,RN-18杂质,RN-18中间体,RN-18密度,RN-18溶解度,RN-18旋光度,RN-18闪点,RN-18结构式,RN-18合成,RN-18购买,RN-18MSDS,RN-18分子式,

产品说明	RN-18(431980-38-0)可以作为药物杂质对照品以及生物医药类试剂。
Introduction	(431980-38-0)RN-18 can be used as a reference substance for drug impurities and reagents，only for research.
Application1	RN-18是HIV-1病毒感染因子（HIV-1 Vif）的拮抗剂，在非允许细胞H9中的IC50 为6μM。
Application2
Application3

RN-18(431980-38-0)药理学：

※RN-18是病毒体感染因子（Vif）APOBEC相互作用和HIV-1复制的选择性抑制剂（非许可H9细胞中IC50 = 6μM），拮抗Vif功能并仅在A3G存在的情况下抑制HIV-1复制。

※RN-18和RN-19在非许可的H9和CEM细胞中表现出有效的抗病毒活性，但在MT4或CEM-SS细胞中则没有，证实了抗病毒活性是Vif特异的。RN-18显示出更大的效价（IC₅₀在CEM细胞中= 4.5μM）和特异性（IC₅₀两种化合物中MT4细胞中> 100μM)。在存在抑制剂RN-18的情况下，非许可H9细胞和CEM细胞中的逆转录酶活性显着降低，并呈剂量依赖性。RN-18在经修饰可稳定表达A3G的CEM-SS中也表现出抗病毒活性，但在亲本CEM-SS细胞系中却不表现出抗病毒活性。RN-18只能在A3G存在的情况下拮抗Vif功能并抑制HIV-1复制。RN-18以Vif依赖性方式增加细胞A3G水平，并增加A3G掺入病毒粒子而不会抑制一般的蛋白酶体介导的蛋白质降解。RN-18仅在存在A3G的情况下才增强Vif降解，通过增加A3G在病毒粒子中的掺入来降低病毒感染性，并增强病毒基因组的胞苷脱氨作用。

警示图
危险性	warning
危险性警示	Not available
安全声明	H303+H313+H333
安全防护	P264+P280+P305+P351+P338+P337+P313
备注	实验过程中防止吸入、食入，做好安全防护

Mohammed I, et al. SAR and Lead Optimization of an HIV-1 Vif-APOBEC3G Axis Inhibitor. ACS Med Chem Lett. 2012 Jun 14;3(6):465-469.

Nathans R, et al. Small-molecule inhibition of HIV-1 Vif. Nat Biotechnol. 2008 Oct;26(10):1187-92.

Synthesis, biological evaluation and molecular docking study of N-(2-methoxyphenyl)-6-((4-nitrophenyl)sulfonyl)benzamide derivatives as potent HIV-1 Vif antagonists European journal of medicinal chemi

Synthesis and structure-activity relationship studies of HIV-1 virion infectivity factor (Vif) inhibitors that block viral replication ChemMedChem

Small-molecule inhibition of HIV-1 Vif Nature biotechnology 18806783 2008-10-01

RN-18(431980-38-0)参考文献：

1.Small-molecule inhibition of HIV-1 Vif.
Nathans R;Cao H;Sharova N;Ali A;Sharkey M;Stranska R;Stevenson M;Rana TM Nat Biotechnol. 2008 Oct;26(10):1187-92. doi: 10.1038/nbt.1496. Epub 2008 Sep 21.

The HIV-1 protein Vif, essential for in vivo viral replication, targets the human DNA-editing enzyme, APOBEC3G (A3G), which inhibits replication of retroviruses and hepatitis B virus. As Vif has no known cellular homologs, it is an attractive, yet unrealized, target for antiviral intervention. Although zinc chelation inhibits Vif and enhances viral sensitivity to A3G, this effect is unrelated to the interaction of Vif with A3G. We identify a small molecule, RN-18, that antagonizes Vif function and inhibits HIV-1 replication only in the presence of A3G. RN-18 increases cellular A3G levels in a Vif-dependent manner and increases A3G incorporation into virions without inhibiting general proteasome-mediated protein degradation. RN-18 enhances Vif degradation only in the presence of A3G, reduces viral infectivity by increasing A3G incorporation into virions and enhances cytidine deamination of the viral genome. These results demonstrate that the HIV-1 Vif-A3G axis is a valid target for developing small molecule-based new therapies for HIV infection or for enhancing innate immunity against viruses.

2.Synthesis, biological evaluation and molecular docking study of N-(2-methoxyphenyl)-6-((4-nitrophenyl)sulfonyl)benzamide derivatives as potent HIV-1 Vif antagonists.
Zhou M;Luo RH;Hou XY;Wang RR;Yan GY;Chen H;Zhang RH;Shi JY;Zheng YT;Li R;Wei YQ Eur J Med Chem. 2017 Mar 31;129:310-324. doi: 10.1016/j.ejmech.2017.01.010. Epub 2017 Jan 12.

Viral infectivity factor (Vif) is protective against APOBEC3G (A3G)-mediated viral cDNA hypermutations, and development of molecules that inhibit Vif mediated A3G degradation is a novel strategy for blocking HIV-1 replication. Through optimizations of the central ring of N-(2-methoxyphenyl)-2-((4-nitrophenyl)thio)benzamide (RN-18), we found a potent compound 12c with EC;50; value of 1.54 μM, enhancing the antiviral activity more than 150-fold compared with RN-18 in nonpermissive H9 cells. 12c protected A3G from degradation by inhibiting Vif function. Besides, 12c suppressed different HIV-1 clinical strains (HIV-1;KM018;, HIV-1;TC-1; and HIV-1;WAN;) and drug-resistant strains (NRTI, NNRTI, PI, and FI) with relatively high activities. Amidation of 12c with glycine gave a prodrug 13a, improving the water solubility about 2600-fold compared with 12c. Moreover, 13a inhibited the virus replication efficiently with an EC;50; value of 0.228 μM. These results suggested that the prodrug 13a is a promising candidate agent for the treatment of AIDS.

对不起，暂无产品评价！

MSDS

SDS 1.0 中文

展开

SDS 1.0 英文

展开