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Temocaprilat

Cat. No. M42287
Temocaprilat Structure
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Biological Activity

Temocaprilat (Temocapril diacid) is an inhibitor of angiotensin-converting enzyme (ACE).

Chemical Information
Molecular Weight 448.56
Formula C21H24N2O5S2
CAS Number 110221-53-9
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] Hajime Takikawa et al. Hepatol Res. Biliary excretion of taurolithocholate-sulfate and temocaprilat in cholestatic rats induced by bile duct-ligation and ethinylestradiol

[2] K Püchler et al. Br J Clin Pharmacol. Single dose and steady state pharmacokinetics of temocapril and temocaprilat in young and elderly hypertensive patients

[3] H Ishizuka et al. J Pharmacol Exp Ther. Transport of temocaprilat into rat hepatocytes: role of organic anion transporting polypeptide

[4] K Püchler et al. Br J Clin Pharmacol. Pharmacokinetics of temocapril and temocaprilat after 14 once daily oral doses of temocapril in hypertensive patients with varying degrees of renal impairment

[5] H Ishizuka et al. J Pharmacol Exp Ther. Temocaprilat, a novel angiotensin-converting enzyme inhibitor, is excreted in bile via an ATP-dependent active transporter (cMOAT) that is deficient in Eisai hyperbilirubinemic mutant rats (EHBR)

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