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AZD1979

Katalog-Nr.GC31643

AZD1979 ist ein Antagonist des Melanin-konzentrierenden Hormonrezeptors 1 (MCHr1) mit einem IC50 von ~12 nM.

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AZD1979 Chemische Struktur

Cas No.: 1254035-84-1

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Sample solution is provided at 25 µL, 10mM.

Description of AZD1979

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

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].

[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.

Protocol of AZD1979

Animal experiment:

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.

Chemical Properties of AZD1979

Cas No. 1254035-84-1 SDF
Canonical SMILES O=C(C1=NN=C(C2=CC=C(OC)C=C2)O1)N3CC(OC4=CC=C(CN(C5)CC65COC6)C=C4)C3
Formula C25H26N4O5 M.Wt 462.5
Löslichkeit DMSO : 33.33 mg/mL (72.06 mM; ultrasonic and warming and heat to 60°C) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of AZD1979

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.1622 mL 10.8108 mL 21.6216 mL
5 mM 0.4324 mL 2.1622 mL 4.3243 mL
10 mM 0.2162 mL 1.0811 mL 2.1622 mL
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In vivo Formulation Calculator (Clear solution) of AZD1979

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Average Rating: 5 ★★★★★ (Based on Reviews and 15 reference(s) in Google Scholar.)

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