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Abediterol

Cat. No. M41764
Abediterol Structure
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Biological Activity

Abediterol (LAS100977) is an inhaled long-acting β2-adrenoceptor agonist (LABA) and can be used for the research of asthma and chronic obstructive pulmonary disease (COPD).

Chemical Information
Molecular Weight 460.51
Formula C25H30F2N2O4
CAS Number 915133-65-2
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] Mario Cazzola et al. Respir Med. Ultra-LABAs for the treatment of asthma

[2] Israel Ramos et al. Eur J Pharmacol. Abediterol (LAS100977), an inhaled long-acting β2-adrenoceptor agonist, has a fast association rate and long residence time at receptor

[3] Jutta Beier et al. Pharmacol Res Perspect. Efficacy, safety, and tolerability of once-daily abediterol in patients with stable, persistent asthma: a Phase II, randomized, 7-day, crossover study

[4] Jutta Beier et al. BMC Pulm Med. Abediterol, a novel long-acting β2-agonist: bronchodilation, safety, tolerability and pharmacokinetic results from a single-dose, dose-ranging, active-comparator study in patients with COPD

[5] J Beier et al. Respir Med. Abediterol (LAS100977), a novel long-acting β2-agonist: efficacy, safety and tolerability in persistent asthma

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