Melanotan I
Based on 1 publication(s) in Google Scholar
Melanotan I (MT-I; [Nle4,D-Phe7]-α-MSH) is an α-MSH (HY-P0252) analog, synthetic melanotropic peptide, and melanocortin receptor (MCR) agonist. Melanotan I induces skin tanning by mimicking the action of α-MSH on the melanocortin 1 receptor (MC1R) in melanocytes. As an appetite suppressant, Melanotan I impairs the ability of insulin to inhibit endogenous glucose production, suppresses leptin secretion from adipose tissue, and thereby reduces voluntary feed intake in ewes. Melanotan I can be used in research related to UV-induced skin damage, polymorphic light eruption, ruminant feeding, and sexual dysfunction.
For research use only. We do not sell to patients.
- Purity: 99.04%
- CAS No.: 75921-69-6
- Formula: C78H111N21O19
- Molecular Weight:1646.85
-
Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Melanotan I
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Biological Activity
|
MC1R |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1.5 × 10-10 M
Compound: NDP-alpha-MSH
|
Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells
Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells
|
[PMID: 26988801] |
| CHO | IC50 |
1.5 x 10-10 M
Compound: NDP-alpha-MSH
|
Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
|
[PMID: 27876250] |
| HEK293 | EC50 |
0.038 nM
Compound: NDP-MSH
|
Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cells
Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cells
|
[PMID: 12477357] |
| HEK293 | EC50 |
0.071 nM
Compound: NDP-MSH
|
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cells
|
[PMID: 12477357] |
| HEK293 | EC50 |
0.098 nM
Compound: NDP-MSH
|
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells
|
[PMID: 12477357] |
| HEK293 | EC50 |
0.21 nM
Compound: NDP-MSH
|
Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cells
Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cells
|
[PMID: 12477357] |
| HEK293 | EC50 |
0.012 μM
Compound: NDP-MSH
|
Agonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cells
Agonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cells
|
[PMID: 12781199] |
| HEK293 | EC50 |
0.075 μM
Compound: NDP-MSH
|
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells
|
[PMID: 12781199] |
| HEK293 | EC50 |
0.07 nM
Compound: MT-I
|
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)
|
[PMID: 12873485] |
| HEK293 | EC50 |
0.36 nM
Compound: MT-I
|
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)
|
[PMID: 12873485] |
| HEK293 | EC50 |
0.51 nM
Compound: MT-I
|
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)
|
[PMID: 12873485] |
| HEK293 | EC50 |
0.023 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay
|
[PMID: 15615519] |
| HEK293 | EC50 |
0.062 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
|
[PMID: 15615519] |
| HEK293 | EC50 |
0.085 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
|
[PMID: 15615519] |
| HEK293 | EC50 |
0.13 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
|
[PMID: 15615519] |
| HEK293 | EC50 |
0.2 nM
Compound: 15
|
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)
|
[PMID: 15771429] |
| HEK293 | EC50 |
0.8 nM
Compound: 15
|
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)
|
[PMID: 15771429] |
| HEK293 | EC50 |
1 nM
Compound: 15
|
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)
|
[PMID: 15771429] |
| HEK293 | IC50 |
0.4 nM
Compound: 15
|
Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)
Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)
|
[PMID: 15771429] |
| HEK293 | IC50 |
2.2 nM
Compound: 15
|
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4
|
[PMID: 15771429] |
| HEK293 | IC50 |
3.3 nM
Compound: 15
|
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)
|
[PMID: 15771429] |
| HEK293 | EC50 |
0.51 nM
Compound: NDP-alpha-MSH
|
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057] |
| HEK293 | EC50 |
1 nM
Compound: NDP-alpha-MSH
|
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057] |
| HEK293 | EC50 |
1.1 nM
Compound: NDP-alpha-MSH
|
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057] |
| HEK293 | EC50 |
1.1 nM
Compound: NDP-alpha-MSH
|
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057] |
| HEK293 | EC50 |
1.2 nM
Compound: NDP-alpha-MSH
|
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057] |
| HEK293 | EC50 |
1.4 nM
Compound: NDP-alpha-MSH
|
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057] |
| HEK293 | EC50 |
1.5 nM
Compound: NDP-alpha-MSH
|
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057] |
| HEK293 | EC50 |
2 nM
Compound: NDP-alpha-MSH
|
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057] |
| HEK293 | EC50 |
5.1 nM
Compound: NDP-alpha-MSH
|
Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057] |
| HEK293 | EC50 |
9 nM
Compound: NDP-alpha-MSH
|
Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
|
[PMID: 16451057] |
| HEK293 | EC50 |
0.008 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC1R expressed in HEK293 cells
Agonist activity at mouse MC1R expressed in HEK293 cells
|
[PMID: 18220330] |
| HEK293 | EC50 |
0.063 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC3R expressed in HEK293 cells
Agonist activity at mouse MC3R expressed in HEK293 cells
|
[PMID: 18220330] |
| HEK293 | EC50 |
0.078 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC5R expressed in HEK293 cells
Agonist activity at mouse MC5R expressed in HEK293 cells
|
[PMID: 18220330] |
| HEK293 | EC50 |
0.097 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC4R expressed in HEK293 cells
Agonist activity at mouse MC4R expressed in HEK293 cells
|
[PMID: 18220330] |
| HEK293 | EC50 |
0.088 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
|
[PMID: 18800761] |
| HEK293 | EC50 |
0.12 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
|
[PMID: 18800761] |
| HEK293 | EC50 |
0.26 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
|
[PMID: 18800761] |
| HEK293 | EC50 |
0.33 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay
|
[PMID: 18800761] |
| HEK293 | EC50 |
0.018 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
|
[PMID: 21306168] |
| HEK293 | EC50 |
0.03 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
|
[PMID: 21306168] |
| HEK293 | EC50 |
0.14 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
|
[PMID: 21306168] |
| HEK293 | EC50 |
0.2 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay
|
[PMID: 21306168] |
| HEK293 | EC50 |
0.05 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
|
[PMID: 23432160] |
| HEK293 | EC50 |
0.2 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
|
[PMID: 23432160] |
| HEK293 | EC50 |
0.23 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
|
[PMID: 23432160] |
| HEK293 | EC50 |
0.28 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay
|
[PMID: 23432160] |
| HEK293 | EC50 |
0.088 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
|
[PMID: 24517312] |
| HEK293 | EC50 |
0.12 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
|
[PMID: 24517312] |
| HEK293 | EC50 |
0.26 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
|
[PMID: 24517312] |
| HEK293 | EC50 |
0.33 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
|
[PMID: 24517312] |
| HEK293 | IC50 |
14 nM
Compound: NDP-MSH
|
Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells
Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells
|
[PMID: 24517312] |
| HEK293 | IC50 |
9 nM
Compound: NDP-MSH
|
Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells
Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells
|
[PMID: 24517312] |
| HEK293 | EC50 |
0.092 nM
Compound: NDP-MSH
|
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
|
[PMID: 25347033] |
| HEK293 | EC50 |
0.2 nM
Compound: NDP-MSH
|
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
|
[PMID: 25347033] |
| HEK293 | EC50 |
0.81 nM
Compound: NDP-MSH
|
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
|
[PMID: 25347033] |
| HEK293 | EC50 |
0.03 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
|
[PMID: 26959173] |
| HEK293 | EC50 |
0.24 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
|
[PMID: 26959173] |
| HEK293 | EC50 |
0.31 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
|
[PMID: 26959173] |
| HEK293 | EC50 |
0.46 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
|
[PMID: 26959173] |
| HEK293 | IC50 |
0.31 nM
Compound: NDP-MSH
|
Displacement of 125I-NDP-MSH from mouse MC1R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
Displacement of 125I-NDP-MSH from mouse MC1R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
|
[PMID: 26959173] |
| HEK293 | IC50 |
1.09 nM
Compound: NDP-MSH
|
Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
|
[PMID: 26959173] |
| HEK293 | IC50 |
4.18 nM
Compound: NDP-MSH
|
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
|
[PMID: 26959173] |
| HEK293 | EC50 |
0.4 nM
Compound: NDP-MSH
|
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
|
[PMID: 28972753] |
| HEK293 | EC50 |
1.1 nM
Compound: NDP-MSH
|
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
|
[PMID: 28972753] |
| HEK293 | EC50 |
6.4 nM
Compound: NDP-MSH
|
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
|
[PMID: 28972753] |
| HEK293 | EC50 |
6.8 nM
Compound: NDP-MSH
|
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
|
[PMID: 28972753] |
| HEK293 | EC50 |
0.07 nM
Compound: NDP-MSH
|
Agonist activity at human MC1R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
Agonist activity at human MC1R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
|
[PMID: 29578343] |
| HEK293 | EC50 |
0.13 nM
Compound: NDP-MSH
|
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
|
[PMID: 29578343] |
| HEK293 | EC50 |
0.3 nM
Compound: NDP-MSH
|
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
|
[PMID: 29578343] |
| HEK293 | EC50 |
0.4 nM
Compound: NDP-MSH
|
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay
|
[PMID: 29578343] |
| HEK293 | EC50 |
0.051 nM
Compound: NDP-MSH
|
Full agonist activity at mouse MC1R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
Full agonist activity at mouse MC1R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
|
[PMID: 30741545] |
| HEK293 | EC50 |
0.279 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
|
[PMID: 30741545] |
| HEK293 | EC50 |
0.414 nM
Compound: NDP-MSH
|
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
|
[PMID: 30741545] |
| HEK293 | EC50 |
1.98 nM
Compound: NDP-MSH
|
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay
|
[PMID: 30741545] |
| HEK293 | EC50 |
0.01 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
|
[PMID: 31845801] |
| HEK293 | EC50 |
0.07 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
|
[PMID: 31845801] |
| HEK293 | EC50 |
0.13 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
|
[PMID: 31845801] |
| HEK293 | EC50 |
0.9 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
|
[PMID: 31845801] |
| HEK293 | IC50 |
0.29 nM
Compound: NDP-MSH
|
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 1 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 1 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
|
[PMID: 31845801] |
| HEK293 | IC50 |
1.3 nM
Compound: NDP-MSH
|
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
|
[PMID: 31845801] |
| HEK293 | IC50 |
10 nM
Compound: NDP-MSH
|
Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
|
[PMID: 31845801] |
| HEK293 | IC50 |
140 nM
Compound: NDP-MSH
|
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
|
[PMID: 31845801] |
| HEK293 | IC50 |
8.2 nM
Compound: NDP-MSH
|
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method
|
[PMID: 31845801] |
| HEK293 | EC50 |
0.012 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP AlphaScreen assay
Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP AlphaScreen assay
|
[PMID: 32184956] |
| HEK293 | EC50 |
0.19 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
|
[PMID: 32184956] |
| HEK293 | EC50 |
0.3 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
|
[PMID: 32184956] |
| HEK293 | EC50 |
1.1 nM
Compound: NDP-MSH
|
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
|
[PMID: 32184956] |
| HEL | EC50 |
0.12 μM
Compound: NDP-MSH
|
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells
|
[PMID: 12781199] |
| HEL | EC50 |
0.17 μM
Compound: NDP-MSH
|
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells
|
[PMID: 12781199] |
| MCR | EC50 |
0.000015 μM
Compound: NDP-MSH
|
Effective concentration was measured against frog skin MCR cells at 10 e-4 10 e-12 M Concentration.
Effective concentration was measured against frog skin MCR cells at 10 e-4 10 e-12 M Concentration.
|
[PMID: 9216831] |
Melanotan I (1.0 μM) does not enhance anchorage-independent clonogenic cell growth, a hallmark of malignancy, in freshly isolated human melanoma cell populations, with unaltered or slightly inhibited colony formation at 1.0 μM[2].
Melanotan I inhibits proliferation of cultured human melanoma cell lines, demonstrating differentiating (melanogenic) activity[2].
Melanotan I does not alter melanoma invasiveness in the human amniotic basement membrane model in vitro[2].
Melanotan I stimulates cAMP production and subsequent eumelanin synthesis in cultured human melanocytes with some polymorphic MC1R variants[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Melanotan I (10 μM; topical administration) does not induce skin papillomas in vjun transgenic mice, but causes local skin pigmentation[2].
Melanotan I (4 mg; subcutaneous injection; single sustained-release injection) increases the eumelanin content in guinea pig skin by 2.5-fold, induces persistent pigmentation lasting up to 10 months, and shows no toxicity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Suffolk ewes (3.5 yr old, body weight 84-96 kg, body condition score 3.3-4.0)[1]
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Dosage:0.0003 nmol/h; 0.003 nmol/h; 0.03 nmol/h
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Administration:i.c.v.; continuous; 24-82 h
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Result:Reduced voluntary dry matter intake by 50% (from 2,108 g DM/d to ~1,054 g DM/d) and energy intake from 1.8-fold maintenance to 1.1-fold maintenance; the appetite-suppressant effect was first detected 6-24 h after infusion initiation and sustained for 72 h.
Reduced dry matter intake by ~40% (from 2,170 g to 1,293 g) and energy intake from 1.8-fold maintenance to 1.01-fold maintenance; increased plasma triiodothyronine (T3) from 1.27 ng/mL to 1.60 ng/mL and plasma thyroxine (T4) from 5.50 ng/mL to 8.31 ng/mL in an intake-independent manner, with no effect on plasma glucose, insulin, cortisol, or free fatty acids.
Increased plasma T3, tended to reduce plasma leptin, had no effect on basal plasma glucose, fatty acids, insulin, or glucose entry rate, but blunted insulin-dependent suppression of endogenous glucose production during hyperinsulinemic-euglycemic clamps at both low and high insulin infusion rates.
Reduced plasma leptin with no effect on plasma adiponectin.
Chemical Information
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CAS No. 75921-69-6
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Appearance Solid
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Molecular Weight 1646.85
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Formula C78H111N21O19
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Color White to off-white
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Synonyms
MT-I; [Nle4,D-Phe7]-α-MSH
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Sequence
Ac-Ser-Tyr-Ser-{Nle}-Glu-His-{d-Phe}-Arg-Trp-Gly-Lys-Pro-Val-NH2
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Sequence Shortening
Ac-SYS-{Nle}-EH-{d-Phe}-RWGKPV-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Theranostics
2020 Aug 13;10(24):11110-11126. PMID: 33042273
Solvent & Solubility
DMSO : 100 mg/mL (60.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL (30.36 mM)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (1.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (1.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (60.72 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Ehrhardt RA, et al. Effects of the central melanocortin system on feed intake, metabolic hormones and insulin action in the sheep. Journal of animal science. 2023 Jan 03;101:skad398. [Content Brief]
[2]. Hadley ME, et al. Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization. Peptides. 2006 Apr;27(4):921-30. [Content Brief]
[3]. Ückert S, et al. Melanocortin receptor agonists in the treatment of male and female sexual dysfunctions: results from basic research and clinical studies. Expert opinion on investigational drugs. 2014 Nov;23(11):1477-83. [Content Brief]
Complete Stock Solution Preparation Table
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 0.6072 mL | 3.0361 mL | 6.0722 mL | 15.1805 mL |
| 5 mM | 0.1214 mL | 0.6072 mL | 1.2144 mL | 3.0361 mL | |
| 10 mM | 0.0607 mL | 0.3036 mL | 0.6072 mL | 1.5180 mL | |
| 15 mM | 0.0405 mL | 0.2024 mL | 0.4048 mL | 1.0120 mL | |
| 20 mM | 0.0304 mL | 0.1518 mL | 0.3036 mL | 0.7590 mL | |
| 25 mM | 0.0243 mL | 0.1214 mL | 0.2429 mL | 0.6072 mL | |
| 30 mM | 0.0202 mL | 0.1012 mL | 0.2024 mL | 0.5060 mL | |
| DMSO | 40 mM | 0.0152 mL | 0.0759 mL | 0.1518 mL | 0.3795 mL |
| 50 mM | 0.0121 mL | 0.0607 mL | 0.1214 mL | 0.3036 mL | |
| 60 mM | 0.0101 mL | 0.0506 mL | 0.1012 mL | 0.2530 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.