DS86760016
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.25%
- CAS No.: 1853176-89-2
- Formula: C9H11BClNO4
- Molecular Weight:243.45
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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.
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Animal Model:Immunocompetent female Swiss Webster mice (urinary tract infection, UTI model)[1]
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Dosage:7.5, 30, 220 mg/kg
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Administration:S.c.; q6h for 7 days
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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.
Chemical Information
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CAS No. 1853176-89-2
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Appearance Solid
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Molecular Weight 243.45
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Formula C9H11BClNO4
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Color Off-white to light brown
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SMILES
OB(O1)C(C(OCO2)=C2C=C3)=C3[C@H]1CN.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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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
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)
H2O : 100 mg/mL (410.76 mM; Need ultrasonic)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Purnapatre KP, et al. In Vitro and In Vivo Activities of DS86760016, a Novel Leucyl-tRNA Synthetase Inhibitor for Gram-Negative Pathogens. Antimicrob Agents Chemother. 2018;62(4):e01987-17. Published 2018 Mar 27. [Content Brief]
[2]. Kumar M, et al. DS86760016, a Leucyl-tRNA Synthetase Inhibitor with Activity against Pseudomonas aeruginosa. Antimicrob Agents Chemother. 2019;63(4):e02122-18. Published 2019 Mar 27. [Content Brief]
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 / H2O | 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 |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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