2. Anti-infection
  3. Bacterial
  4. DS86760016

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.

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DS86760016 Chemical Structure

DS86760016 Chemical Structure

CAS No. : 1853176-89-2

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Description

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].

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].

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

DS86760016 Related Antibodies
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].

MedChemExpress (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.
Molecular Weight

243.45

Formula

C9H11BClNO4
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

OB(O1)C(C(OCO2)=C2C=C3)=C3[C@H]1CN.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (410.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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DS86760016 Related Classifications

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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