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RO5256390

Cat. No. M8721
RO5256390 Structure
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Biological Activity

RO5256390 is a selective agonist of trace amine-associated receptor 1 (TAAR1) and a negative modulator of dopamine transmission for studies related to schizophrenia and bulimia.

Chemical Information
Molecular Weight 218.29
Formula C13H18N2O
CAS Number 1043495-96-0
Solubility (25°C) DMSO 10 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] Morteza Zendehdel, et al. Central and peripheral methylamine-induced hypophagia is mediated via nitric oxide and TAAR 1 in neonatal layer-type chicken

[2] Catherine F Moore, et al. Trace Amine Associated Receptor 1 (TAAR1) Modulation of Food Reward

[3] Sarah W Black, et al. Trace Amine-Associated Receptor 1 Agonists as Narcolepsy Therapeutics

[4] Antonio Ferragud, et al. The Trace Amine-Associated Receptor 1 Agonist RO5256390 Blocks Compulsive, Binge-like Eating in Rats

[5] Yui Pei, et al. Activation of the trace amine-associated receptor 1 prevents relapse to cocaine seeking

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