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Lotrafiban hydrochloride

Cat. No. M41628
Lotrafiban hydrochloride Structure
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Biological Activity

Lotrafiban hydrochloride is an orally-active platelet GPIIb/IIIa blocker for research of coronary and cerebrovascular disease.

Chemical Information
Molecular Weight 464.99
Formula C23H33ClN4O4
CAS Number 179599-82-7
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] Eric J Topol et al. Circulation. Randomized, double-blind, placebo-controlled, international trial of the oral IIb/IIIa antagonist lotrafiban in coronary and cerebrovascular disease

[2] John R Toomey et al. Curr Drug Targets Cardiovasc Haematol Disord. The antithrombotic efficacy of lotrafiban (SB 214857) in canine models of acute coronary thrombosis

[3] D Mould et al. Clin Pharmacol Ther. A population pharmacokinetic-pharmacodynamic and logistic regression analysis of lotrafiban in patients

[4] F Liu et al. Expert Opin Investig Drugs. Lotrafiban: an oral platelet glycoprotein IIb/IIIa blocker

[5] R A Harrington et al. Circulation. Dose-finding, safety, and tolerability study of an oral platelet glycoprotein IIb/IIIa inhibitor, lotrafiban, in patients with coronary or cerebral atherosclerotic disease

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