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1384984-18-2
  • names:

    VXc-486

  • CAS號:

    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
SPR719(VXc-486,1384984-18-2)是一種旋轉(zhuǎn)酶B抑制劑,具有殺菌活性。VXc-486能有效抑制結(jié)核分枝桿菌的多種藥敏性和溶解性,MIC分別為0.03-0.30μg/ ml和0.08-5.48μg/ ml。
貨品編碼 規(guī)格 純度 價格 (¥) 現(xiàn)價(¥) 特價(¥) 庫存描述 數(shù)量 總計 (¥)
YZM000263-5mg 5mg >97% ¥ 5600.00 ¥ 5600.00 1-3天
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中文別名 VXc-486(1384984-18-2);SPR719;
英文別名 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號 1384984-18-2
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
溶解度Solubility
性狀 Solid
儲藏條件 Storage conditions 請根據(jù)產(chǎn)品建議的存儲條件進行存儲,Please store the product under the recommended condition sin the description.

SPR719(VXc-486,1384984-18-2)實驗注意事項:
1.實驗前需戴好防護眼鏡,穿戴防護服和口罩,佩戴手套,避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生,必要時實驗操作需要手套箱內(nèi)完成以免對實驗人員造成傷害
3.實驗后產(chǎn)生的廢棄物需分類存儲,并交于專業(yè)生物廢氣物處理公司處理,以免造成環(huán)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試劑,SPR719雜質(zhì),SPR719中間體,SPR719密度,SPR719溶解度,SPR719旋光度,SPR719閃點,SPR719熔點,SPR719購買,SPR719MSDS,

產(chǎn)品說明 SPR719(VXc-486,1384984-18-2)是一種有效的旋轉(zhuǎn)酶B的抑制劑,具有殺菌活性
IntroductionSPR719(VXc-486,1384984-18-2)is agyrase Binhibitor, with bactericidal activity. VXc86 potently inhibits multiple drugensitive isolates and drugesistant isolates of Mycobacterium tuberculosis,
Application1SPR719(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)藥理學(xué):
SPR719(VXc-486,1384984-18-2)是一種旋轉(zhuǎn)酶B抑制劑,具有殺菌活性。VXc-486能有效抑制結(jié)核分枝桿菌的多種藥敏性和溶解性,MIC分別為0.03-0.30μg/ ml和0.08-5.48μg/ ml。
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)參考文獻:
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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