1. GPCR/G Protein Neuronal Signaling
  2. Melanocortin Receptor
  3. α-MSH

α-MSH  (Synonyms: α-Melanocyte-Stimulating Hormone)

Cat. No.: HY-P0252 Purity: 99.57%
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α-MSH (α-Melanocyte-Stimulating Hormone), an endogenous neuropeptide, is an endogenous melanocortin receptor 4 (MC4R) agonist with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC).

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Custom Peptide Synthesis

α-MSH Chemical Structure

α-MSH Chemical Structure

CAS No. : 581-05-5

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Based on 14 publication(s) in Google Scholar

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Description

α-MSH (α-Melanocyte-Stimulating Hormone), an endogenous neuropeptide, is an endogenous melanocortin receptor 4 (MC4R) agonist with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC)[1][2].

IC50 & Target

MC4R

 

Cellular Effect
Cell Line Type Value Description References
CHO EC50
0.0027 μM
Compound: alpha-MSH
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
[PMID: 20329799]
CHO EC50
1.1 nM
Compound: Alpha-MSH
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
[PMID: 15982875]
CHO EC50
1.9 nM
Compound: Alpha-MSH
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
[PMID: 15982875]
CHO IC50
118 nM
Compound: Alpha-MSH
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
[PMID: 15982875]
CHO EC50
17 nM
Compound: Alpha-MSH
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
[PMID: 15982875]
CHO IC50
19 nM
Compound: alpha-MSH
Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
[PMID: 15582434]
CHO IC50
19 nM
Compound: Alpha-MSH
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
[PMID: 15982875]
CHO IC50
19 nM
Compound: Alpha-MSH
Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
[PMID: 15982875]
CHO EC50
2.2 nM
Compound: alpha-MSH
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
[PMID: 20329799]
HEK293 EC50
0.0009 μM
Compound: alpha-MSH
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
[PMID: 20329799]
HEK293 EC50
0.04 nM
Compound: alpha-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
0.14 nM
Compound: alpha-MSH
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
[PMID: 26433448]
HEK293 EC50
0.15 nM
Compound: alpha-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
0.22 nM
Compound: alpha-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
0.22 nM
Compound: alpha-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
0.22 nM
Compound: alpha-MSH
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
[PMID: 26005535]
HEK293 EC50
0.28 nM
Compound: alpha-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
0.3 nM
Compound: alpha-MSH
Agonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
Agonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
[PMID: 26005535]
HEK293 EC50
0.36 μM
Compound: alpha-MSH
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
[PMID: 20329799]
HEK293 EC50
0.4 nM
Compound: alpha-MSH
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
[PMID: 26005535]
HEK293 EC50
0.5 nM
Compound: alpha-MSH
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
[PMID: 26433448]
HEK293 EC50
0.51 nM
Compound: alpha-MSH
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
[PMID: 26433448]
HEK293 EC50
0.52 nM
Compound: alpha-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
0.59 nM
Compound: alpha-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
0.65 nM
Compound: alpha-MSH
Agonist activity at wild type human 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 wild type human 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
0.7 nM
Compound: alpha-MSH
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
[PMID: 18271518]
HEK293 EC50
0.76 nM
Compound: alpha-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
1.12 nM
Compound: alpha-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
1.7 nM
Compound: alpha-MSH
Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
[PMID: 26005535]
HEK293 EC50
1.8 nM
Compound: 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
1.89 nM
Compound: alpha-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
156 nM
Compound: 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
16.7 nM
Compound: alpha-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
18 nM
Compound: 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
2 nM
Compound: alpha-MSH
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
[PMID: 18271518]
HEK293 EC50
2.14 nM
Compound: alpha-MSH
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
[PMID: 18271518]
HEK293 EC50
2.56 nM
Compound: alpha-MSH
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
[PMID: 18271518]
HEK293 EC50
2.6 nM
Compound: 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
2.9 nM
Compound: alpha-MSH
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
[PMID: 26433448]
HEK293 EC50
2.9 nM
Compound: 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
21 nM
Compound: 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
21 nM
Compound: 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
24.4 nM
Compound: alpha-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
27 nM
Compound: 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
3.7 nM
Compound: alpha-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]
HEK293 EC50
35.3 nM
Compound: alpha-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
4 nM
Compound: alpha-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 EC50
7.1 nM
Compound: 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
89 nM
Compound: 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
9.2 nM
Compound: alpha-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]
SAOS-2 EC50
1.8 nM
Compound: alpha-MSH
Activity at human MC1R by cAMP accumulation in SaoS2 cells
Activity at human MC1R by cAMP accumulation in SaoS2 cells
[PMID: 16678415]
SAOS-2 EC50
72.9 nM
Compound: alpha-MSH
Activity at human MC4R by cAMP accumulation in SaoS2 cells
Activity at human MC4R by cAMP accumulation in SaoS2 cells
[PMID: 16678415]
In Vitro

α-MSH modulates CNS inflammation by acting directly on melanocortin receptors in glial cells. α-MSH modulates NFκB activation. α-MSH inhibits translocation of transcription factor κB to the nucleus[3].

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

In Vivo

α-MSH (50 μg/0.2 ml saline; i.p.) given systemically effectively modulates inflammatory reactions[3].

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

Animal Model: IL-10–deficient mice[3]
Dosage: 50 µg/0.2 ml saline
Administration: I.p.
Result: Given systemically effectively modulated inflammatory reactions.
Molecular Weight

1664.88

Formula

C77H109N21O19S

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Ac-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2

Sequence Shortening

Ac-SYSMEHFRWGKPV-NH2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (60.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 12.5 mg/mL (7.51 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.6006 mL 3.0032 mL 6.0064 mL
5 mM 0.1201 mL 0.6006 mL 1.2013 mL
View the 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 and light, under nitrogen). 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.57%

References

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 and light, under nitrogen). 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 0.6006 mL 3.0032 mL 6.0064 mL 15.0161 mL
5 mM 0.1201 mL 0.6006 mL 1.2013 mL 3.0032 mL
DMSO 10 mM 0.0601 mL 0.3003 mL 0.6006 mL 1.5016 mL
15 mM 0.0400 mL 0.2002 mL 0.4004 mL 1.0011 mL
20 mM 0.0300 mL 0.1502 mL 0.3003 mL 0.7508 mL
25 mM 0.0240 mL 0.1201 mL 0.2403 mL 0.6006 mL
30 mM 0.0200 mL 0.1001 mL 0.2002 mL 0.5005 mL
40 mM 0.0150 mL 0.0751 mL 0.1502 mL 0.3754 mL
50 mM 0.0120 mL 0.0601 mL 0.1201 mL 0.3003 mL
60 mM 0.0100 mL 0.0501 mL 0.1001 mL 0.2503 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.

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Product Name:
α-MSH
Cat. No.:
HY-P0252
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