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AZD8154

Cat. No. M21171
AZD8154  Structure
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Biological Activity

AZD8154 is a novel inhaled selective PI3Kγδ dual inhibitor targeting airway inflammatory diseases.

Chemical Information
Molecular Weight 551.68
Formula C27H29N5O4S2
CAS Number 2215022-45-8
Solubility (25°C) DMSO : 25 mg/mL
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] Gail M Gauvreau, et al. Eur Respir J. Allergen provocation tests in respiratory research: building on 50 years of experience

[2] Krishna Tulasi Kirla, et al. Respir Med. Diurnal variation in DLCO and non-standardized study procedures may cause a false positive safety signal in clinical trials

[3] Muhammad Waqas Sadiq, et al. Br J Clin Pharmacol. Characterisation of pharmacokinetics, safety and tolerability in a first-in-human study for AZD8154, a novel inhaled selective PI3Kγδ dual inhibitor targeting airway inflammatory disease

[4] Matthew W D Perry, et al. J Med Chem. Discovery of AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma

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  Catalog
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