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WIN 64338 hydrochloride

Cat. No. M7488
WIN 64338 hydrochloride Structure
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Biological Activity

WIN 64338 hydrochloride is a the first potent, non-peptide, competitive bradykinin B2 receptor antagonist. In organ bath studies, WIN 64338 inhibits [3H]-bradykinin binding on guinea pig trachea with nanomolar affinity but is not active in the rabbit aorta (the classical bradykinin B1 preparation).

Chemical Information
Molecular Weight 783.95
Formula C45H68ClN4OP.HCl
CAS Number 163727-74-0
Solubility (25°C) DMSO 58.8 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] Borsch-Haubold, et al. J Biol Chem. Direct inhibition of cyclooxygenase-1 and -2 by the kinase inhibitors SB 203580 and PD 98059.

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