2. Anti-infection
  3. Bacterial
  4. DS86760016

DS86760016 是一种亮氨酸-tRNA 合成酶 (LeuRS) 抑制剂，对多药耐药 (MDR) 革兰氏阴性菌, 如大肠杆菌、肺炎克雷伯菌和铜绿假单胞菌，具有抗菌活性。DS86760016 对大肠杆菌、铜绿假单胞菌和鲍曼不动杆菌的 LeuRS 酶有抑制作用，IC50 分别为 0.38、0.62 和 0.16 μM。

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DS86760016 Chemical Structure

DS86760016 Chemical Structure

CAS No. : 1853176-89-2

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规格 价格 是否有货 数量
1 mg ￥1495
In-stock
5 mg ￥3740
In-stock
10 mg ￥5950
In-stock
25 mg 现货 询价
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100 mg   询价  

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Customer Review

Other Forms of DS86760016:

DS86760016 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DS86760016 is a potent leucyl-tRNA synthetase (LeuRS) inhibitor with activity against multidrug-resistant (MDR) Gram-negative bacteria, such as Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. DS86760016 inhibits LeuRS enzymes from Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii, with IC50s of 0.38, 0.62, and 0.16 μM, respectively[1][2].

体外研究
(In Vitro)

DS86760016 inhibits some Gram-negative bacteria with an MICs ranging from 0.25 to 2 μg/ml. The MIC of DS86760016 against Gram-positive bacteria is >32 μg/ml. DS86760016 is active against both susceptible and these MDR P. aeruginosa, E. coli, and K. pneumoniae strains, with an MIC90 of 2 μg/ml[1].

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

DS86760016 相关抗体:
体内研究
(In Vivo)

DS86760016 (7.5-220 mg/kg; s.c.; q6h for 7 days) shows moderate spontaneous resistance (FSR)[1].
The pharmacokinetic (PK) parameters of DS86760016 in mouse, rat, monkey, and dog plasma by the intravenous (i.v.) route are test. DS86760016 shows lower intravenous plasma clearances (CLp) of 11, 29, 5.6, and 4.5 ml/min/kg in mouse, rat, monkey, and dog plasma, respectively. The plasma half-lives (t1/2) for DS86760016 are 1.9, 1.5, 8.6, and 8.3 h in mice, rats, monkeys, and dogs, respectively. The lower plasma clearance resulted in higher plasma exposures for DS86760016, with dose-normalized areas under the curve after i.v. administration (DNAUCIVs) of 1.5, 0.6, 3.7, and 3.0 μg h kg/ml/mg in mice, rats, monkeys, and dogs, respectively[1].

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

Animal Model: Immunocompetent female Swiss Webster mice (urinary tract infection, UTI model)[1]
Dosage: 7.5, 30, 220 mg/kg
Administration: S.c.; q6h for 7 days
Result: Bacteria resistant to DS86760016 were detected in a few animals after 1 day of treatment at doses of 7.5 and 30 mg/kg q6h; however, no resistant bacteria were detected at these doses after 7 days of treatment. No resistance was observed in any of the mice treated at a dose of 220 mg/kg q6h.
分子量

243.45

Formula

C9H11BClNO4
CAS 号
性状

固体

颜色

Off-white to light brown

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (410.76 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 4.1076 mL 20.5381 mL 41.0762 mL
5 mM 0.8215 mL 4.1076 mL 8.2152 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 (sealed storage, away from moisture)。-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

只
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

DS86760016 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 (sealed storage, away from moisture)。-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 4.1076 mL 20.5381 mL 41.0762 mL 102.6905 mL
5 mM 0.8215 mL 4.1076 mL 8.2152 mL 20.5381 mL
10 mM 0.4108 mL 2.0538 mL 4.1076 mL 10.2690 mL
15 mM 0.2738 mL 1.3692 mL 2.7384 mL 6.8460 mL
20 mM 0.2054 mL 1.0269 mL 2.0538 mL 5.1345 mL
25 mM 0.1643 mL 0.8215 mL 1.6430 mL 4.1076 mL
30 mM 0.1369 mL 0.6846 mL 1.3692 mL 3.4230 mL
40 mM 0.1027 mL 0.5135 mL 1.0269 mL 2.5673 mL
50 mM 0.0822 mL 0.4108 mL 0.8215 mL 2.0538 mL
60 mM 0.0685 mL 0.3423 mL 0.6846 mL 1.7115 mL
80 mM 0.0513 mL 0.2567 mL 0.5135 mL 1.2836 mL
100 mM 0.0411 mL 0.2054 mL 0.4108 mL 1.0269 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.

Keywords:

DS867600161853176-89-2DS 86760016DS-86760016Bacterialmultidrug-resistantLeuRSbacteriaGram-negativeInhibitorinhibitorinhibit

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目录号：
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