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TAK 21d

Cat. No. M7349
TAK 21d Structure
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Biological Activity

TAK 21d is a potent FAAH inhibitor; (IC50 values are 0.28 and 0.72 nM, at rat and human FAAH respectively). Displays analgesic effects in vivo models of neuropathic and inflammatory pain. Brain penetrant.

Chemical Information
Molecular Weight 397.38
Formula C19H17F2N7O
CAS Number 1143578-94-2
Solubility (25°C) 1eq. HCl 7.95 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] Hyafil, et al. Cancer Res. In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative.

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