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PF-04781340

Chemical Structure : PF-04781340

CAS No.: 1648726-56-0

PF-04781340 (PF 04781340;PF04781340)

Catalog No.: PC-61080Not For Human Use, Lab Use Only.

A potent, selective, CNS penetrant 5-HT2C receptor agonist with Ki of 3 nM and EC50 of 9 nM, without significant P-gp efflux liability.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent, selective, CNS penetrant 5-HT2C receptor agonist with Ki of 3 nM and EC50 of 9 nM, without significant P-gp efflux liability; displays >150-fold selectivity over 5-HT2B receptors agonism (EC50=1484 nM); exhibits good metabolic stability in human liver microsomes (HLM) and moderate to good passive permeability in RRCK cells.

Physicochemical Properties

M.Wt 267.376
Formula C17H21N3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-benzyl-N-methyl-6,7,8,9-tetrahydro-5H-pyrido[3,4-d]azepin-1-amine

References

1. Dvorak CA, et al. ACS Med Chem Lett. 2015 Jul 20;6(9):1015-8.

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