2. GPCR/G Protein Neuronal Signaling
  3. Melanocortin Receptor
  4. MC4R Antagonist-1

MC4R Antagonist-1 (compound 1) is an MC4R-selective antagonist (IC50<10 nM). MC4R Antagonist-1 can be used for the research of cachexia, anorexia, anorexia nervosa, involuntary weight loss, failure to thrive, sarcopenia, muscle wasting, muscle weakness, frailty, osteoporosis.

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

MC4R Antagonist-1

MC4R Antagonist-1 Chemical Structure

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MC4R Antagonist-1 Related Antibodies

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Description

MC4R Antagonist-1 (compound 1) is an MC4R-selective antagonist (IC50<10 nM). MC4R Antagonist-1 can be used for the research of cachexia, anorexia, anorexia nervosa, involuntary weight loss, failure to thrive, sarcopenia, muscle wasting, muscle weakness, frailty, osteoporosis[1].

IC50 & Target

MC4R

<10 nM (IC50)

In Vitro

MC4R Antagonist-1 (compound 1) (0.1-1000 nM; 8-16 h) restores α-MSH-induced cAMP signaling in HEK293 cells overexpressing T162I-MC4R, with an EC50 < 50 nM and an Emax > 150%[1].
MC4R Antagonist-1 (10 μM; 10-16 h) significantly increases plasma membrane MC4R levels and elevates the plasma membrane/total MC4R ratio in HEK293 cells transfected with 24 MC4R loss-of-function mutants[1].
MC4R Antagonist-1 forms only 4 GSH adducts with a total relative abundance of 3.6% in an in vitro human liver microsome system, and no GSH adducts are produced in the absence of liver microsomes[1].

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

MC4R Antagonist-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: HEK293 cells transiently transfected with 24 loss-of-function MC4R variants
Concentration: 0.75 μM, 10 μM
Incubation Time: 10-16 h
Result: Significantly increased plasma membrane MC4R levels and the ratio of plasma membrane to total cellular MC4R for all tested MC4R loss-of-function variants.
In Vivo

MC4R Antagonist-1 (compound 1) (30-60 mpk; subcutaneous injection; twice daily; 19 days) significantly reduces body weight and cumulative food intake in homozygous MC4RR165Q/R165Q MC4R-deficient obese mouse models[1].

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

Animal Model: Homozygous MC4RR165Q/R165Q MC4R-deficient (MC4R-D) mice (8 weeks old, single-housed, preconditioned with 45% high-fat diet)[1]
Dosage: 10 mpk, 30 mpk, 60 mpk
Administration: subcutaneous injection, twice daily (BID) for 19 days
Result: At 30 mpk and 60 mpk BID, significantly decreased body weight and cumulative food intake compared with the vehicle-treated group, whereas 10 mpk BID did not produce significant effects on body weight or cumulative food intake.
Molecular Weight

477.53

Formula

C25H28FN7O2
SMILES

C[C@H](C1=CC(OC)=NC=C1F)C(N2C[C@@]3(CC2)CN(C)C4=CC(C5=NC=CC=N5)=C(C)N=C4N3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MC4R Antagonist-1 Related Classifications

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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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:

MC4R Antagonist-1Melanocortin ReceptorMC ReceptorMC4Rcachexiasarcopeniaanorexia nervosafrailtymuscle weaknessfailure to thriveanorexiamuscle wastinginvoluntary weight lossInhibitorinhibitorinhibit

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