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RO5203648 

Cat. No. M27700
RO5203648  Structure
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Biological Activity

RO5203648 is a potent and highly selective partial agonist of TAAR1 (Trace amine-associated receptor 1) with high affinity. RO5203648 demonstrates a novel paradigm for neuropsychiatric research.

Chemical Information
Molecular Weight 231.08
Formula C9H8Cl2N2O
CAS Number 1043491-54-8
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage 4°C, protect from light
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] Ruyan Wu, et al. CNS Drugs. Potential of Ligands for Trace Amine-Associated Receptor 1 (TAAR1) in the Management of Substance Use Disorders

[2] Guido Galley, et al. ACS Med Chem Lett. Discovery and Characterization of 2-Aminooxazolines as Highly Potent, Selective, and Orally Active TAAR1 Agonists

[3] Rachel Cotter, et al. Front Neurosci. The trace amine-associated receptor 1 modulates methamphetamine's neurochemical and behavioral effects

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

[5] Florent G Revel, et al. Biol Psychiatry. Trace amine-associated receptor 1 partial agonism reveals novel paradigm for neuropsychiatric therapeutics

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  Catalog
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Keywords: RO5203648  supplier, TAAR, inhibitors, activators


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