AZD1979

Names

[ Name ]:
AZD1979

[Synonym ]:
Methanone, [5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl][3-[4-(2-oxa-6-azaspiro[3.3]hept-6-ylmethyl)phenoxy]-1-azetidinyl]-
[5-(4-Methoxyphenyl)-1,3,4-oxadiazol-2-yl]{3-[4-(2-oxa-6-azaspiro[3.3]hept-6-ylmethyl)phenoxy]-1-azetidinyl}methanone
MFCD30471075
H9HGK5C4UM

Biological Activity

[Description]:

AZD1979 is a Melanin-concentrating hormone receptor 1 (MCHr1) antagonist with an IC50 of ~12 nM.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> MCHR1 (GPR24)

Research Areas >> Metabolic Disease

[Target]

IC50: ~12 nM (MCHr1)[1]

[In Vivo]

In DIO mice, initial AZD1979-mediate body weight loss is driven by decreasing food intake, but an additional component of preserving energy expenditure is apparent in pair-feeding and indirect calorimetry studies. AZD1979 also dose-dependently reduces body weight in dogs[1].

[Animal admin]

Three weeks after the light-dark cycle have been reversed, all mice are sham dosed by p.o. gavage for 6 days to habituate the animals to the procedure, randomized into experimental groups base on average body weights and dosed p.o. with AZD1979 (20, 40 or 60 μmol/kg twice daily at 8:00 h and 15:00 h) or vehicle (0.5% HPMC, 0.1% Tween twice daily) for 21 days (n=6 per group). Three mice per group are then dosed once more with the respective doses of AZD1979 (20, 40 or 60 μmol/kg p.o.) and killed after 17 h by administration of an overdose of isoflurane (anaesthesia)[1].

[References]

[1]. Ploj K, et al. Effects of a novel potent melanin-concentrating hormone receptor 1 antagonist, AZD1979, on body weight homeostasis in mice and dogs. Br J Pharmacol. 2016 Sep;173(18):2739-51.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
636.6±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₅H₂₆N₄O₅

[ Molecular Weight ]:
462.498

[ Flash Point ]:
338.8±34.3 °C

[ Exact Mass ]:
462.190308

[ LogP ]:
5.01

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.668

[ Storage condition ]:
2-8℃