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OR-1896

Cat. No. M11045
OR-1896  Structure
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Biological Activity

Or-1896 is an active longevity metabolite of Levosimendan. Or-1896, a highly selective phosphodiesterase (PDE III) inhibitor, is a powerful vasodilator.

Chemical Information
Molecular Weight 245.28
Formula C13H15N3O2
CAS Number 220246-81-1
Solubility (25°C) DMSO ≥ 60 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] Ildik Gdny, et al. Pharmacol Rep. Levosimendan and its metabolite OR-1896 elicit KATP channel-dependent dilation in resistance arteries in vivo

[2] Marjut Louhelainen, et al. Br J Pharmacol. Effects of the calcium sensitizer OR-1896, a metabolite of levosimendan, on post-infarct heart failure and cardiac remodelling in diabetic Goto-Kakizaki rats

[3] M Koskinen, et al. Xenobiotica. Metabolism of OR-1896, a metabolite of levosimendan, in rats and humans

[4] Patricia N Banfor, et al. Am J Physiol Heart Circ Physiol. Comparative effects of levosimendan, OR-1896, OR-1855, dobutamine, and milrinone on vascular resistance, indexes of cardiac function, and O2 consumption in dogs

[5] Jaakko Puttonen, et al. Eur J Pharm Sci. Pharmacokinetics and excretion balance of OR-1896, a pharmacologically active metabolite of levosimendan, in healthy men

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