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Iclaprim

Cat. No. M29023
Iclaprim Structure
Synonym:

AR-100

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Quality Control & Documentation
Biological Activity

Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.

Chemical Information
Molecular Weight 354.4
Formula C19H22N4O3
CAS Number 192314-93-5
Form Solid
Solubility (25°C) DMSO 30 mg/mL (Need ultrasonic and warming)
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] Stephanie Noviello, et al. Expert Rev Anti Infect Ther. Iclaprim: a differentiated option for the treatment of skin and skin structure infections

[2] David B Huang, et al. Future Microbiol. Iclaprim, a dihydrofolate reductase inhibitor antibiotic in Phase III of clinical development: a review of its pharmacology, microbiology and clinical efficacy and safety

[3] Carrie A Sincak, et al. Ann Pharmacother. Iclaprim, a novel diaminopyrimidine for the treatment of resistant gram-positive infections

[4] Andrew Morgan, et al. Future Microbiol. Iclaprim: a novel dihydrofolate reductase inhibitor for skin and soft tissue infections

[5] Stephan A Kohlhoff, et al. Expert Opin Investig Drugs. Iclaprim

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Keywords: Iclaprim, AR-100 supplier, Antibiotic, inhibitors, activators


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