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VA-012

Chemical Structure : VA-012

CAS No.: 885898-58-8

VA-012 (VA012)

Catalog No.: PC-62010Not For Human Use, Lab Use Only.

VA-012 is a potent, selective 5-HT2C receptor positive allosteric modulator (PAM) that exhibits dose-dependent potentiation of 5-HT efficacy with EC50 of 16 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

VA-012 is a potent, selective 5-HT2C receptor positive allosteric modulator (PAM) that exhibits dose-dependent potentiation of 5-HT efficacy with EC50 of 16 nM; shows no significant off-target activities, and low binding competition with serotonin or other orthosteric ligands; increases the anorectic effect combined with the SSRI sertraline; reduces food intake and body weight gain without causing CNS-related malaise.

Physicochemical Properties

M.Wt 313.4
Formula C21H19N3
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

1-(Phenylmethyl)-N-3-pyridinyl-1H-indole-3-methanamine

References

1. García Cárceles J, et al. J Med Chem. 2017 Nov 8. doi: 10.1021/acs.jmedchem.7b00994.

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