1384984-18-2|SPR719|VXc-486|-范德生物科技公司

SPR719

NMR下载 COA and HPLC MSDS下载
names：
VXc-486
CAS号：
1384984-18-2
MDL Number：
MF(分子式)： C21H25FN6O3 MW(分子量)： 428.46
EINECS: Reaxys Number:
Pubchem ID:57524959 Brand:BIOFOUNT

SPR719(VXc-486,1384984-18-2)是一种旋转酶B抑制剂，具有杀菌活性。VXc-486能有效抑制结核分枝杆菌的多种药敏性和溶解性，MIC分别为0.03-0.30μg/ ml和0.08-5.48μg/ ml。

货品编码	规格	纯度	价格 (¥)	现价(¥)	特价(¥)	库存描述	数量	总计 (¥)
YZM000263-5mg	5mg	>97%	¥ 5600.00	¥ 5600.00		1-3天	- +	¥ 0.00

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中文别名	VXc-486(1384984-18-2);SPR719;
英文别名	VXc-486(1384984-18-2);(R)-1-ethyl-3-(6-fluoro-5-(2-(2-hydroxypropan-2-yl)pyrimidin-5-yl)-7-(tetrahydrofuran-2-yl)-1H-benzo[d]imidazol-2-yl)urea;:VXC-486;EOS-60709;1-ethyl-3-[5-fluoro-6-[2-(2-hydroxypropan-2-yl)pyrimidin-5-yl]-4-[(2R)-oxolan-2-yl]-1H-benzimidazol-2-yl]ureaChemicalbook;(R)-1-ethyl-3-(6-fluoro-5-(2-(2-hydroxypropan-2-yl)pyrimidin-5-yl)-7-(tetrahydrofuran-2-yl)-1H-benzo[d]imidazol-2-yl)urea;SPR719;
CAS号	1384984-18-2
SMILES	O=C(NC1=NC2=CC(C3=CN=C(C(C)(O)C)N=C3)=C(F)C([C@@H]4OCCC4)=C2N1)NCC
Inchi	InChI=1S/C21H25FN6O3/c1-4-23-20(29)28-19-26-13-8-12(11-9-24-18(25-10-11)21(2,3)30)16(22)15(17(13)27-19)14-6-5-7-31-14/h8-10,14,30H,4-7H2,1-3H3,(H3,23,26,27,28,29)/t14-/m1/s1
InchiKey	BKUISYCLLXCBJV-CQSZACIVSA-N
分子式 Formula	C21H25FN6O3
分子量 Molecular Weight	428.46
闪点 FP
熔点 Melting point	No data available
沸点 Boiling point
Polarizability极化度	45.0±0.5 10-24cm3
密度 Density	1.4±0.1 g/cm3
蒸汽压 Vapor Pressure
溶解度Solubility
性状	Solid
储藏条件 Storage conditions	请根据产品建议的存储条件进行存储,Please store the product under the recommended condition sin the description.

SPR719(VXc-486,1384984-18-2)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：SPR719试剂,SPR719杂质,SPR719中间体,SPR719密度,SPR719溶解度,SPR719旋光度,SPR719闪点,SPR719熔点,SPR719购买,SPR719MSDS,

产品说明	SPR719(VXc-486,1384984-18-2)是一种有效的旋转酶B的抑制剂，具有杀菌活性
Introduction	SPR719(VXc-486,1384984-18-2)is agyrase Binhibitor, with bactericidal activity. VXc86 potently inhibits multiple drugensitive isolates and drugesistant isolates of Mycobacterium tuberculosis,
Application1	SPR719(VXc-486,1384984-18-2)with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively.
Application2
Application3

SPR719(VXc-486,1384984-18-2)药理学：

警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理
备注	实验过程中防止吸入、食入，做好安全防护

Locher CP, et al. A novel inhibitor of gyrase B is a potent drug candidate for treatment of tuberculosis and nontuberculosis mycobacterial infections. Antimicrob Agents Chemother. 2015 Mar;59(3):1455-

SPR719(VXc-486,1384984-18-2)参考文献：

1、A novel inhibitor of gyrase B is a potent drug candidate for treatment of tuberculosis and nontuberculosis mycobacterial infections
Christopher P Locher 1, Steven M Jones 2, Brian L Hanzelka 2, Emanuele Perola 2, Carolyn M Shoen 3, Michael H Cynamon 3, Andile H Ngwane 4, Ian J Wiid 4, Paul D van Helden 4, Fabrice Betoudji 5, Eric L Nuermberger 5, John A Thomson

Abstract New drugs to treat drug-resistant tuberculosis are urgently needed. Extensively drug-resistant and probably the totally drug-resistant tuberculosis strains are resistant to fluoroquinolones like moxifloxacin, which target gyrase A, and most people infected with these strains die within a year. In this study, we found that a novel aminobenzimidazole, VXc-486, which targets gyrase B, potently inhibits multiple drug-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis in vitro (MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively) and reduces mycobacterial burdens in lungs of infected mice in vivo. VXc-486 is active against drug-resistant isolates, has bactericidal activity, and kills intracellular and dormant M. tuberculosis bacteria in a low-oxygen environment. Furthermore, we found that VXc-486 inhibits the growth of multiple strains of Mycobacterium abscessus, Mycobacterium avium complex, and Mycobacterium kansasii (MICs of 0.1 to 2.0 μg/ml), as well as that of several strains of Nocardia spp. (MICs of 0.1 to 1.0 μg/ml). We made a direct comparison of the parent compound VXc-486 and a phosphate prodrug of VXc-486 and showed that the prodrug of VXc-486 had more potent killing of M. tuberculosis than did VXc-486 in vivo. In combination with other antimycobacterial drugs, the prodrug of VXc-486 sterilized M. tuberculosis infection when combined with rifapentine-pyrazinamide and bedaquiline-pyrazinamide in a relapse infection study in mice. Furthermore, the prodrug of VXc-486 appeared to perform at least as well as the gyrase A inhibitor moxifloxacin. These findings warrant further development of the prodrug of VXc-486 for the treatment of tuberculosis and nontuberculosis mycobacterial infections.

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