ML00253764

Name: ML00253764
Brand: MedChemExpress
SKU: HY-124740
Rating: 4.5 (1 reviews)

Cat. No.: HY-124740 Purity: 99.70%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity.

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

ML00253764 Chemical Structure

CAS No. : 681847-92-7

Size	Stock	Quantity

Free Sample (0.1 - 0.5 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of ML00253764:

ML-00253764 hydrochloride Get quote

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Melanocortin Receptor Isoform Specific Products:

View All Isoforms

MC1R MC3R MC2R MC4R MC5R

Biological Activity
Purity & Documentation
References
Customer Review

Description

ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	1030 nM Compound: 5	Antagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation Antagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	IC₅₀	160 nM Compound: 5	Antagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation Antagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	IC₅₀	2708 nM Compound: 5	Antagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation Antagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	IC₅₀	2860 nM Compound: 5	Antagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation Antagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	IC₅₀	2900 nM Compound: 5	Antagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation Antagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	IC₅₀	355 nM Compound: 5	Antagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation Antagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	IC₅₀	3770 nM Compound: 5	Antagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation Antagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	IC₅₀	560 nM Compound: 5	Antagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation Antagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	IC₅₀	6190 nM Compound: 5	Antagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulation Antagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]
HEK293	IC₅₀	708 nM Compound: 5	Antagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation Antagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	[PMID: 16451057]

In Vitro

ML00253764 (0.001-50 μM, 24 h or 72 h) has significant time- and concentration-dependent inhibitory activity on the proliferation of human glioblastoma cells, and the IC₅₀ value for U-118 cells is 6.56 μM, which can induce U -87 cells apoptosis and show significant inhibition of ERK1/2 phosphorylation in both cell lines^[1].

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

In Vivo

ML00253764(30 mg/kg, s.c., daily, 34 days) can inhibit inhibit tumor growth in CD nu/nu male mice infected with U-87 cells^[1].

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

Molecular Weight

377.25

Formula

C₁₈H₁₈BrFN₂O

CAS No.

681847-92-7

Appearance

Solid

Color

White to off-white

SMILES

FC1=C(CCC2=CC(Br)=CC=C2OC)C(C3=NCCN3)=CC=C1

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 : 66.67 mg/mL (176.73 mM; Need ultrasonic; 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	2.6508 mL	13.2538 mL	26.5076 mL
5 mM	0.5302 mL	2.6508 mL	5.3015 mL
10 mM	0.2651 mL	1.3254 mL	2.6508 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 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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.70%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (252 KB) HNMR (266 KB) LCMS (269 KB)

Handling Instructions (2659 KB)

References

[1]. Francesca Vaglini, et al. Melanocortin Receptor-4 and Glioblastoma Cells: Effects of the Selective Antagonist ML00253764 Alone and in Combination with Temozolomide In Vitro and In Vivo. Mol Neurobiol. 2018 Jun;55(6):4984-4997. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.6508 mL	13.2538 mL	26.5076 mL	66.2691 mL
	5 mM	0.5302 mL	2.6508 mL	5.3015 mL	13.2538 mL
	10 mM	0.2651 mL	1.3254 mL	2.6508 mL	6.6269 mL
	15 mM	0.1767 mL	0.8836 mL	1.7672 mL	4.4179 mL
	20 mM	0.1325 mL	0.6627 mL	1.3254 mL	3.3135 mL
	25 mM	0.1060 mL	0.5302 mL	1.0603 mL	2.6508 mL
	30 mM	0.0884 mL	0.4418 mL	0.8836 mL	2.2090 mL
	40 mM	0.0663 mL	0.3313 mL	0.6627 mL	1.6567 mL
	50 mM	0.0530 mL	0.2651 mL	0.5302 mL	1.3254 mL
	60 mM	0.0442 mL	0.2209 mL	0.4418 mL	1.1045 mL
	80 mM	0.0331 mL	0.1657 mL	0.3313 mL	0.8284 mL
	100 mM	0.0265 mL	0.1325 mL	0.2651 mL	0.6627 mL

ML00253764 Related Classifications

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:

ML00253764681847-92-7ML 00253764ML-00253764Melanocortin ReceptorMC ReceptorMC4RERK1/2AktapoptosisanticancerInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

ML00253764

Customer Review

Other Forms of ML00253764:

ML00253764 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Melanocortin Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

ML00253764 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

ML00253764 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report