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A55453

Cat. No. M25419
A55453 Structure
Synonym:

A-55453

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Biological Activity

A55453 is a prazosin analogue and a potent α1-adrenergic antagonist.

Chemical Information
Molecular Weight 464.56
Formula C25H32N6O3
CAS Number 89687-06-9
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] Xing-Chen Guo, et al. Mar Drugs. Absolute Configurations and Chitinase Inhibitions of Quinazoline-Containing Diketopiperazines from the Marine-Derived Fungus Penicillium polonicum

[2] Z Ke, et al. Neoplasma. Expression of DPC4/Smad4 in non-small-cell lung carcinoma and its relationship with angiogenesis

[3] K E Dickinson, et al. Mol Pharmacol. Photoaffinity cross-linking of a radioiodinated probe, 125I-A55453, into alpha 1-adrenergic receptors

[4] J W Lomasney, et al. J Biol Chem. Mammalian alpha 1-adrenergic receptor. Purification and characterization of the native receptor ligand binding subunit

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