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MSG 606

カタログ番号GC50303

MSG 606 は、選択的 MC1R (メラノコルチン 1 受容体) 拮抗薬であり、神経保護効果の研究に使用できます。

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

MSG 606 化学構造

Cas No.: 1416983-77-1

サイズ 価格 在庫数 個数
1 mg
$215.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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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

Background

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

Chemical Properties

Cas No. 1416983-77-1 SDF
Canonical 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
Formula C62H82N20O13S M.Wt 1347.51
溶解度 Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 0.7421 mL 3.7105 mL 7.4211 mL
5 mM 0.1484 mL 0.7421 mL 1.4842 mL
10 mM 0.0742 mL 0.3711 mL 0.7421 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 4 reference(s) in Google Scholar.)

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