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Arylomycin A2

Cat. No. M45087
Arylomycin A2 Structure
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Biological Activity

Arylomycin A2 is an antibiotic and lipopeptide type I signal peptidase (SPase I) inhibitor with antibacterial activity.

Chemical Information
Molecular Weight 824.96
Formula C42H60N6O11
CAS Number 459844-20-3
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] Hülya Aldemir, et al. Chemistry. Carrier Protein-Free Enzymatic Biaryl Coupling in Arylomycin A2 Assembly and Structure of the Cytochrome P450 AryC

[2] Hülya Aldemir, et al. Chemistry. Carrier Protein-Free Enzymatic Biaryl Coupling in Arylomycin A2 Assembly and Structure of the Cytochrome P450 AryC

[3] Ngiap-Kie Lim, et al. Org Lett. Macrolactamization Approaches to Arylomycin Antibiotics Core

[4] Tucker C Roberts, et al. J Nat Prod. Synthesis and biological characterization of arylomycin B antibiotics

[5] Chuanyun Luo, et al. Biochemistry. Crystallographic analysis of bacterial signal peptidase in ternary complex with arylomycin A2 and a beta-sultam inhibitor

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