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SPR719

Cat. No. M28299
SPR719 Structure
Synonym:

VXc-486

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Biological Activity

SPR719 (VXc-486) is a gyrase B inhibitor, with bactericidal activity. SPR719 potently inhibits multiple agent-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively.

Chemical Information
Molecular Weight 428.46
Formula C21H25FN6O3
CAS Number 1384984-18-2
Form Solid
Solubility (25°C) DMSO 20 mg/mL (ultrasonic and adjust pH to 2 with HCl)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Wassihun Wedajo Aragaw, et al. Microbiol Spectr. In Vitro Resistance against DNA Gyrase Inhibitor SPR719 in Mycobacterium avium and Mycobacterium abscessus

[2] Sacha J Pidot, et al. PLoS Negl Trop Dis. In vitro activity of SPR719 against Mycobacterium ulcerans, Mycobacterium marinum and Mycobacterium chimaera

[3] Dereje Abate Negatu, et al. Antimicrob Agents Chemother. Piperidine-4-Carboxamides Target DNA Gyrase in Mycobacterium abscessus

[4] Lian J Pennings, et al. Antimicrob Agents Chemother. The Benzimidazole SPR719 Shows Promising Concentration-Dependent Activity and Synergy against Nontuberculous Mycobacteria

[5] Barbara A Brown-Elliott, et al. Antimicrob Agents Chemother. In Vitro Susceptibility Testing of a Novel Benzimidazole, SPR719, against Nontuberculous Mycobacteria

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