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AMG-076

Chemical Structure : AMG-076

CAS No.: 693823-79-9

AMG-076 (AMG076;T-71)

Catalog No.: PC-61530Not For Human Use, Lab Use Only.

AMG-076 is a potent, selective, non-peptide antagonist of MCHR1 (Melanin-concentrating hormone receptor 1) with binding IC50 of 0.6 nM, with dramatically reduced hERG liability (IC50>5 uM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

AMG-076 is a potent, selective, non-peptide antagonist of MCHR1 (Melanin-concentrating hormone receptor 1) with binding IC50 of 0.6 nM, with dramatically reduced hERG liability (IC50>5 uM); shows activity in reducing body weight in in vivo mouse models, demonstrates good selectivity for MCHR1 and possesses good pharmacokinetic properties across preclinical species.

Obesity

Phase 1 Discontinued

Physicochemical Properties

M.Wt 462.557
Formula C26H33F3N2O2
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-(2-((4aR,11R,11aS)-11-methyl-9-(trifluoromethyl)-1,3,4,4a,5,6,11,11a-octahydro-2H-pyrido[4,3-b]carbazol-2-yl)ethyl)cyclohexane-1-carboxylic acid

References

1. Mihalic JT, et al. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3781-5.

2. Motani AS, et al. Pharmacol Res Perspect. 2013 Oct;1(1):e00003.

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