Fig. 1 · Structure

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Melanotan II

Cat. No. A12646 CAS 121062-08-6
Melanotan II is a high affinity melanocortin receptor agonist (Ki values are 0.67, 6.6, 34 and 46 nM for MC1, MC4, MC3 and MC5 receptors respectively).

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
A-375 EC50 110 nM Agonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting [PMID: 26218460]
A-375 IC50 6.7 nM Antagonist activity at human MC1 receptor expressed in A375 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting [PMID: 26218460]
HEK293 EC50 0.021 nM Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay [PMID: 15615519]
HEK293 EC50 0.03 nM Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay [PMID: 25347033]
HEK293 EC50 0.04 nM Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay [PMID: 15615519]
HEK293 EC50 0.05 nM Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay [PMID: 25699138]
HEK293 EC50 0.06 nM Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay [PMID: 25347033]
HEK293 EC50 0.17 nM Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay [PMID: 15615519]
HEK293 EC50 0.18 nM Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay [PMID: 25347033]
HEK293 EC50 0.18 nM Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay [PMID: 15615519]
HEK293 EC50 0.19 nM Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay [PMID: 25347033]
HEK293 EC50 0.22 nM Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay [PMID: 25699138]
HEK293 EC50 0.3 nM Activity against hMC1R transfected in HEK293 cells by intracellular cAMP accumulation [PMID: 16539382]
HEK293 EC50 0.35 nM Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay [PMID: 25699138]
HEK293 EC50 0.57 nM Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay [PMID: 25699138]
HEK293 IC50 1 nM Displacement of [125I]-NDP-alpha-MSH from human MC1 receptor expressed in HEK293 cells by gamma counting analysis [PMID: 25699148]
HEK293 EC50 1 nM Activity at human MC1R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation [PMID: 16931008]
HEK293 EC50 1.02 nM Activity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter [PMID: 25699148]
HEK293 IC50 1.1 nM Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis [PMID: 26599352]

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Specifications

Manufacturer Adooq Bioscience
Actions Agonist
CAS Number 121062-08-6
Formula C50H69N15O9
Molecular Weight 1024.18
SMILES
CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)CC2=CN=CN2)CC3=CC=CC=C3)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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