Description: Potent human MC1 receptor antagonist; also MC3 and MC5 partial agonist
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent human MC1 receptor antagonist (IC50 = 17 nM). Also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). Exhibits binding affinity for A375 melanoma cells in vitro. Reverses morphine-induced hyperalgesia in female mice, with no effect in male mice. γMSH analog.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solubility
Soluble to 1 mg/ml in water
Preparing Stock Solutions
The following data is based on the product molecular weight 1347.51. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
0.74 mL
3.71 mL
7.42 mL
5 mM
0.15 mL
0.74 mL
1.48 mL
10 mM
0.07 mL
0.37 mL
0.74 mL
50 mM
0.01 mL
0.07 mL
0.15 mL
Molarity Calculator
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Reconstitution Calculator
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Dilution Calculator
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Caiet al (2013) An unusual conformation of γ-melanocyte-stimulating hormone analogues leads to a selective human melanocortin 1 receptor antagonist for targeting melanoma cells. Biochemistry 52 752 PMID: 23276279
Juniet al (2010) Sex-specific mediation of opioid-induced hyperalgesia by the melanocortin-1 receptor. Anesthesiology 112 181 PMID: 19996949
Aroutet al (2015) Spinal and supraspinal N-methyl-D-aspartate and melanocortin-1 receptors contribute to a qualitative sex difference in morphine-induced hyperalgesia. Physiol.Behav. 147 364 PMID: 25982086