ML-00253764 hydrochloride

Name: ML-00253764 hydrochloride
Brand: MedChemExpress
SKU: HY-110123
Rating: 4.5 (1 reviews)

Cat. No.: HY-110123 Purity: 99.47%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

ML-00253764 hydrochloride is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a K_i and IC₅₀ of 0.16 µM and 0.103 µM, respectively.

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

ML-00253764 hydrochloride Chemical Structure

CAS No. : 1706524-94-8

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 135	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 230	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 500	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1450	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of ML-00253764 hydrochloride:

ML00253764 Get quote

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•Related Screening Libraries:

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View All Melanocortin Receptor Isoform Specific Products:

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MC1R MC3R MC2R MC4R MC5R

Biological Activity
Purity & Documentation
References
Customer Review

Description

ML-00253764 hydrochloride is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a K_i and IC₅₀ of 0.16 µM and 0.103 µM, respectively^[1].

IC₅₀ & Target

MC4R

In Vitro

ML-00253764 displaces NDP-α-MSH binding with a mean IC₅₀ of 0.32 μM, 0.81 μM and 2.12 μM for hMC4-R, hMC3-R and hMC5-R, respectively^[1].
ML-00253764 (100 µM) decreases cAMP production induced by [NLE4,D-Phe7]-α-melanocyte stimulating hormone ([NDP]-α-MSH) by 20% in MC4R-expressing HEK293 cell membranes, but has no effect on cAMP levels in MC3R- or MC5R-expressing membranes^[1].

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

In Vivo

ML-00253764 (subcutaneous injection; 3, 10, or 30 mg/kg; once daily) shows protection against tumor-induced body weight loss upon chronic, peripheral dosing in CT-26 tumor bearing BALB/c mice^[1].
ML-00253764 dissolves in polyethylene glycol 200/saline (1:10) in a volume of 10 mL/kg (For reference only)^[1].

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

Animal Model:	CT-26 tumor bearing BALB/c mice^[1]
Dosage:	3, 10, or 30 mg/kg
Administration:	Subcutaneous injection; 3, 10, or 30 mg/kg; once daily
Result:	Reduced tumor-induced weight loss in a mouse model.

Molecular Weight

413.71

Formula

C₁₈H₁₉BrClFN₂O

CAS No.

1706524-94-8

Appearance

Solid

Color

Off-white to light yellow

SMILES

FC1=C(CCC2=CC(Br)=CC=C2OC)C(C3=NCCN3)=CC=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL (30.21 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	2.4172 mL	12.0858 mL	24.1715 mL
5 mM	0.4834 mL	2.4172 mL	4.8343 mL
10 mM	0.2417 mL	1.2086 mL	2.4172 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 (sealed storage, away from moisture). 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: ≥ 1.25 mg/mL (3.02 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (3.02 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (3.02 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.47%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (254 KB) HNMR (258 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Vos TJ, et al. Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model. J Med Chem. 2004 Mar 25;47(7):1602-4. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.4172 mL	12.0858 mL	24.1715 mL	60.4288 mL
	5 mM	0.4834 mL	2.4172 mL	4.8343 mL	12.0858 mL
	10 mM	0.2417 mL	1.2086 mL	2.4172 mL	6.0429 mL
	15 mM	0.1611 mL	0.8057 mL	1.6114 mL	4.0286 mL
	20 mM	0.1209 mL	0.6043 mL	1.2086 mL	3.0214 mL
	25 mM	0.0967 mL	0.4834 mL	0.9669 mL	2.4172 mL
	30 mM	0.0806 mL	0.4029 mL	0.8057 mL	2.0143 mL