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WAY 207024 dihydrochloride

Cat. No. M7484
WAY 207024 dihydrochloride Structure
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Biological Activity

WAY 207024 dihydrochloride is a gonadotropin releasing hormone receptor (GnRH-R) antagonist. Exhibits potent affinity (IC50 values are 12 and 71 nM for human and rat GnRH receptors respectively). Lowers plasma leuteinizing hormone levels in the rat. Orally active.

Chemical Information
Molecular Weight 549.54
Formula C30H32N6.2HCl
CAS Number 872002-73-8
Solubility (25°C) DMSO 46.71 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] Takei, et al. Antimicrob Agents Chemother. Inhibitory activities of gatifloxacin (AM-1155), a newly developed fluoroquinolone, against bacterial and mammalian type II topoisomerases.

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