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MK-7246 

Cat. No. M27966
MK-7246  Structure
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Biological Activity

MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5±0.5 nM.

Chemical Information
Molecular Weight 416.47
Formula C21H21FN2O4S
CAS Number 1218918-62-7
Form Solid
Solubility (25°C) DMSO 300 mg/mL (ultrasonic and warming and heat to 60°C)
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] Pierre Cheung, et al. Pharmaceutics. [18F]MK-7246 for Positron Emission Tomography Imaging of the Beta-Cell Surface Marker GPR44

[2] Pierre Cheung, et al. Biomedicines. PET Imaging of GPR44 by Antagonist [11C]MK-7246 in Pigs

[3] Jonas Eriksson, et al. Nucl Med Biol. Synthesis and preclinical evaluation of the CRTH2 antagonist [11C]MK-7246 as a novel PET tracer and potential surrogate marker for pancreatic beta-cell mass

[4] Y-H Wang, et al. Clin Pharmacol Ther. UGT2B17 genetic polymorphisms dramatically affect the pharmacokinetics of MK-7246 in healthy subjects in a first-in-human study

[5] Michel Gallant, et al. Bioorg Med Chem Lett. Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases

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