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ORM-3819

Cat. No. M8713
ORM-3819 Structure
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Biological Activity

Orm-3819 is a potent muscular compound that binds to cardiac troponin C (cTnC) and sensitizes the heart to Ca2+. Orm-3819 is also a selective and potent inhibitor of PDE III. Orm-3819 exhibits positive inotropic effects through Ca2+ sensitization and selective inhibition of PDE III. ORM-3819 is an effective myocardial block model in animals.

Chemical Information
Molecular Weight 397.38
Formula C19H19N5O5
CAS Number 360794-85-0
Solubility (25°C) DMSO: 30 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] No authors listed. J Cardiovasc Pharmacol. The Novel Inodilator ORM-3819 Relaxes Isolated Porcine Coronary Arteries: Role of Voltage-Gated Potassium Channel Activation: Erratum

[2] Zoltn Mrton, et al. The Novel Inodilator ORM-3819 Relaxes Isolated Porcine Coronary Arteries: Role of Voltage-Gated Potassium Channel Activation

[3] Lszl Nagy, et al. ORM-3819 promotes cardiac contractility through Ca(2+) sensitization in combination with selective PDE III inhibition, a novel approach to inotropy

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