1. GPCR/G Protein
    Neuronal Signaling
  2. Melanocortin Receptor
  3. ML-00253764 hydrochloride

ML-00253764 hydrochloride 

Cat. No.: HY-110123
Handling Instructions

ML-00253764 hydrochloride is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a Ki 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

ML-00253764 hydrochloride Chemical Structure

CAS No. : 1706524-94-8

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Description

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

IC50 & Target

Ki: 0.16 µM
IC50: 0.103 µM (melanocortin receptor 4)[1]

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].

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].

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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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ML-00253764 hydrochloride
Cat. No.:
HY-110123
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