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JNJ 303

Cat. No. M14256
JNJ 303 Structure
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Biological Activity

JNJ 303 is a potent IKs blocker with an IC50 value of 64 nM. JNJ 303 does not have any effects on other cardiac channels at concentrations of 3.3 μM for INa, Ica, Ito, and IKr. JNJ 303 induces QT-prolongations and causes unprovoked torsades de pointes (TdP).

Chemical Information
Molecular Weight 440.98
CAS Number 878489-28-2
Solubility (25°C) DMSO 62.5 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] Rachael L DiSantostefano, et al. Using Societal Values to Inform Public Health Policy During the COVID-19 Pandemic: The Role of Health Preference Research

[2] Dejan Milentijevic, et al. Risk of Stroke Outcomes in Atrial Fibrillation Patients Treated with Rivaroxaban and Warfarin

[3] Edward Phillips, et al. Safety and effectiveness of REALIZE adjustable gastric band: 5-year prospective study

[4] Susann Bjrk, et al. Evaluation of Optogenetic Electrophysiology Tools in Human Stem Cell-Derived Cardiomyocytes

[5] C Kang, et al. β-adrenergic stimulation augments transmural dispersion of repolarization via modulation of delayed rectifier currents I Ks and I Kr in the human ventricle

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