AZD1979

Cat. No.: HY-U00257 Purity: 98.09%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

AZD1979 Chemical Structure

CAS No. : 1254035-84-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 187	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 187	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 170	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 530	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1350	In-stock	Estimated Time of Arrival: December 31
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Protocol
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Description

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

IC₅₀ & Target

IC50: ~12 nM (MCHr1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	> 40 μM Compound: 103; AZD1979	Antagonist activity at human MCHR2 expressed in CHO cells after 60 to 75 mins by FLIPR assay Antagonist activity at human MCHR2 expressed in CHO cells after 60 to 75 mins by FLIPR assay	[PMID: 26741166]
CHO	IC₅₀	27 nM Compound: 103; AZD1979	Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay Antagonist activity at human MCHR1 expressed in CHO cell membranes preincubated for 5 mins followed by addition of MCH peptide measured after 45 mins by [35S]GTPgammaS binding assay	[PMID: 26741166]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

462.50

Formula

C₂₅H₂₆N₄O₅

CAS No.

1254035-84-1

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=NN=C(C2=CC=C(OC)C=C2)O1)N3CC(OC4=CC=C(CN(C5)CC65COC6)C=C4)C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (72.06 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.09%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (248 KB) HNMR (264 KB) LCMS (259 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

Animal Administration
^[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1622 mL	10.8108 mL	21.6216 mL	54.0541 mL
	5 mM	0.4324 mL	2.1622 mL	4.3243 mL	10.8108 mL
	10 mM	0.2162 mL	1.0811 mL	2.1622 mL	5.4054 mL
	15 mM	0.1441 mL	0.7207 mL	1.4414 mL	3.6036 mL
	20 mM	0.1081 mL	0.5405 mL	1.0811 mL	2.7027 mL
	25 mM	0.0865 mL	0.4324 mL	0.8649 mL	2.1622 mL
	30 mM	0.0721 mL	0.3604 mL	0.7207 mL	1.8018 mL
	40 mM	0.0541 mL	0.2703 mL	0.5405 mL	1.3514 mL
	50 mM	0.0432 mL	0.2162 mL	0.4324 mL	1.0811 mL
	60 mM	0.0360 mL	0.1802 mL	0.3604 mL	0.9009 mL

AZD1979 Related Classifications

Metabolic Disease Endocrinology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZD19791254035-84-1AZD 1979AZD-1979MCHR1 (GPR24)Melanin concentrating hormone receptor 1Inhibitorinhibitorinhibit

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AZD1979

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