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ER 50891 quarterhydrate

Cat. No. M42600
ER 50891 quarterhydrate Structure
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Biological Activity

ER 50891 quarterhydrate is a potent antagonist of retinoic acid receptor α(RARα).

Chemical Information
Molecular Weight 437.02
Formula C29H24N2O2.1/4H2O
Form Solid
Storage -20°C, dry, sealed
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] Jillian L Kyzer et al. Arch Pharm (Weinheim). Investigation of selective retinoic acid receptor alpha antagonist ER-50891 and related analogs for male contraception

[2] Siqian Wang et al. Drug Des Devel Ther. The Antagonist of Retinoic Acid Receptor α, ER-50891 Antagonizes the Inhibitive Effect of All-Trans Retinoic Acid and Rescues Bone Morphogenetic Protein 2-Induced Osteoblastogenic Differentiation

[3] Wei Sun et al. FEBS Open Bio. All-trans retinoic acid and human salivary histatin-1 promote the spreading and osteogenic activities of pre-osteoblasts in vitro

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