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Art. -Nr.: HY-124740

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ML00253764

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

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Reinheit: 99.71%
CAS. Nr.: 681847-92-7
Formel: C₁₈H₁₈BrFN₂O
Molecular Weight:377.25

Speicherung:

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

ML00253764 Chemical Structure

CAS. Nr.: 681847-92-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Alle Melanocortin Receptor Isoform-spezifische Produkte anzeigen :

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.

Chemical Information

CAS. Nr. 681847-92-7
Appearance Solid
Molecular Weight 377.25
Formel C₁₈H₁₈BrFN₂O
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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ML00253764

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

Alle Melanocortin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ML00253764

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

Alle Melanocortin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ML00253764 Related Classifications

HY-124740 Related Classifications