DS86760016 biochemical

DS86760016

Cat. Num. AAA227958

• Purity: 98%
• Synonyms: DS86760016; N/A; DS86760016 biochemical

• Purity/Purification: 98%

• CAS: 1853176-89-2
• Solubility: <1mg/ml refers to the product slightly soluble or insoluble
• In vitro: 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 (CL p) of 11, 29, 5.6, and 4.5 mL/min/kg in mouse, rat, monkey, and dog plasma, respectively. The plasma half-lives (t 1/2) 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 (DNAUC IV s) of 1.5, 0.6, 3.7, and 3.0 ug h kg/ml/mg in mice, rats, monkeys, and dogs, respectively[1]. 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.
• Preparation and Storage: Powder: -20 degree C for 3 years; In solvent: -80 degree C for 2 years

Structure

(DDO-2093, CAS 2250024-74-7)

Structure

(DDO-2093, CAS 2250024-74-7)

Related Product Information for DS86760016 biochemical

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 IC 50 s of 0.38, 0.62, and 0.16 uM, respectively.

References

1. Chen W, et al. Discovery of a potent MLL1 and WDR5 protein-protein interaction inhibitor with in vivo antitumor activity [published online ahead of print, 2021 Jun 28]. Eur J Med Chem. 2021;223:113677.