GLPBio

MSG 606

Catalog No.: GC50303Purity:>98%
COASDSData Sheet
MSG-606 has potent antagonist activity and receptor selectivity for the human melanocortin 1 receptor (hMC1R) (IC50 = 17 nM) .

Products are for research use only. Not for human use. We do not sell to patients.

MSG 606
Cas No.: 1416983-77-1
1mgIn Stock
$189.00
1
5mgIn Stock
$468.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

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Description

MSG-606 has potent antagonist activity and receptor selectivity for the human melanocortin 1 receptor (hMC1R) (IC50 = 17 nM) [1].

MSG-606 is an excellent probe for targeting specifically melanoma cells for skin cancer diagnosis. MSG-606 act as antagonist toward the melanoma cells. Binding and cAMP Activities of MSG-606 against Human Melanoma Cells (A375) with IC50 of 96 nM [1].

MSG-606 (1 nmol/µl, 6 µl) abolished the neuroprotective effects of the BMS-470539/MC1R system, in a subarachnoid hemorrhage (SAH) model [2].

References:
[1]:Cai M, Stankova M, Muthu D, et al. An unusual conformation of γ-melanocyte-stimulating hormone analogues leads to a selective human melanocortin 1 receptor antagonist for targeting melanoma cells[J]. Biochemistry, 2013, 52(4): 752-764.
[2]:Xu, W., Mo, J., Ocak, U. et al. Activation of Melanocortin 1 Receptor Attenuates Early Brain Injury in a Rat Model of Subarachnoid Hemorrhage viathe Suppression of Neuroinflammation through AMPK/TBK1/NF-κB Pathway in Rats. Neurotherapeutics 17, 294-308 (2020). https://doi.org/10.1007/s13311-019-00772-x

Protocol

Animal experiment [1]:

Animal models

Male Sprague-Dawley (SD) rats

Preparation Method

Rats were randomly divided into five groups: sham, SAH + vehicle 1(10 µl sterile saline, i.n), SAH + BMS-470539 (160 µg/kg, 10 µl), SAH + BMS-470539 + vehicle 2 (6 µl sterile saline, i.c.v), and SAH + BMS-470539 + MSG-606 (1 nmol/µl, 6 µl). MSG-606 was administered 1 h before SAH via i.c.v. route. Neurological testing was performed at 24 h after SAH. Ipsilateral/left cerebral cortex was sampled for western blotting.

Dosage form

1 nmol/µl, 6 µl, i.c.v

Applications

The inhibition of MC1R with MSG-606 significantly abolished the anti-inflammatory effects of BMS-470539 when compared to SAH + BMS-470539 + vehicle 2 group

References:
[1]: Xu, W., Mo, J., Ocak, U. et al. Activation of Melanocortin 1 Receptor Attenuates Early Brain Injury in a Rat Model of Subarachnoid Hemorrhage viathe Suppression of Neuroinflammation through AMPK/TBK1/NF-κB Pathway in Rats. Neurotherapeutics 17, 294-308 (2020). https://doi.org/10.1007/s13311-019-00772-x

Chemical Properties

CAS No.
1416983-77-1
SMILES
NC(=O)CNC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H]1CSCCCC(=O)NCC(=O)N[C@@H](CC2=CNC=N2)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC2=CNC3=C2C=CC=C3)C(=O)N1
Molecular Formula
C62H82N20O13S
Molecular Weight
1347.51
Solubility
Soluble in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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