1. Anti-infection
  2. Bacterial
  3. MAC-545496

MAC-545496 是糖肽抗性相关蛋白 R (GraR) 的纳摩尔抑制剂。MAC-545496 对全长 GraR 蛋白具有很强的结合亲和力 (Kd ≤ 0.1 nM)。 MAC-545496 是一种抗毒剂,可逆转耐甲氧西林的菌株 (MRSA) 中的 β-内酰胺耐药性。

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MAC-545496 Chemical Structure

MAC-545496 Chemical Structure

CAS No. : 838810-96-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥830
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1 mg ¥380
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5 mg ¥750
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10 mg ¥1200
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25 mg ¥2200
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50 mg ¥3500
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200 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA)[1].

IC50 & Target

Glycopeptide-resistance-associated protein R (GraR)[1]

体外研究
(In Vitro)

MAC-545496 potently synergizes with Cefuroxime; concentrations as low as 0.03 µg/mL (~75 nM) lowers the β-lactam MIC from 512 to 8 µg/mL against S. aureus USA300. MAC545496 also synergizes with Cefuroxime and Oxacillin against a collection of ten S. aureus clinical isolates. In addition, MAC-545496 potentiates the effect of Cefuroxime against representatives of other circulating MRSA strains such as USA100, USA400 and USA500 to different extents, with the exception of CMRSA4, a USA200/EMRSA16 isolate. MAC-545496 also synergizes with the antimicrobial peptides colistin and polymyxin B[1].
MAC-545496 shows inhibition of mprF expression in a concentration-dependent manner; the IC50 value is 0.0376 µg/mL[1].
MAC-545496 also inhibits the citrateinduced biofilm formation in the wild type in a concentration dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

In vivo, MAC-545496 is effective as a monotherapy for MRSA infected Galleria mellonella larvae. MAC-545496 activity is evidenced by increased survival of the drug-treated larvae as compared to infected untreated ones. This corresponded to concentration-dependent killing of S. aureus in the hemolymph of the larvae observed from the CFUs recovered from the hemolymph 200 min after infection. Treatment of S. aureus-infected larvae with MAC-545496 occurred 30min after infection that mimics acquiring bacterial infection before initiating antimicrobial therapy [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

419.89

Formula

C18H18ClN5O3S

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 250 mg/mL (595.39 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3816 mL 11.9079 mL 23.8158 mL
5 mM 0.4763 mL 2.3816 mL 4.7632 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

MAC-545496 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3816 mL 11.9079 mL 23.8158 mL 59.5394 mL
5 mM 0.4763 mL 2.3816 mL 4.7632 mL 11.9079 mL
10 mM 0.2382 mL 1.1908 mL 2.3816 mL 5.9539 mL
15 mM 0.1588 mL 0.7939 mL 1.5877 mL 3.9693 mL
20 mM 0.1191 mL 0.5954 mL 1.1908 mL 2.9770 mL
25 mM 0.0953 mL 0.4763 mL 0.9526 mL 2.3816 mL
30 mM 0.0794 mL 0.3969 mL 0.7939 mL 1.9846 mL
40 mM 0.0595 mL 0.2977 mL 0.5954 mL 1.4885 mL
50 mM 0.0476 mL 0.2382 mL 0.4763 mL 1.1908 mL
60 mM 0.0397 mL 0.1985 mL 0.3969 mL 0.9923 mL
80 mM 0.0298 mL 0.1488 mL 0.2977 mL 0.7442 mL
100 mM 0.0238 mL 0.1191 mL 0.2382 mL 0.5954 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
MAC-545496
目录号:
HY-130613
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