MSG 606 |
カタログ番号GC50303
One-Click Copy Product Info
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MSG 606 は、ヒトメラノコルチン1受容体（hMC1R）に対して強力なアンタゴニスト活性と受容体選択性を持ち、そのIC50は17 nMである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1416983-77-1
Sample solution is provided at 25 µL, 10mM.
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MSG 606 は、ヒトメラノコルチン1受容体（hMC1R）に対して強力なアンタゴニスト活性と受容体選択性を持ち、そのIC50は17 nMである。
MSG-606は、皮膚がんの診断のために特異的にメラノーマ細胞を標的とする優れたプローブである。MSG-606はメラノーマ細胞に対してアンタゴニストとして作用する。ヒトメラノーマ細胞（A375）に対するMSG-606の結合およびcAMP活性は、IC50が96 nMである。
MSG-606（1 nmol/µl, 6 µl）は、くも膜下出血（SAH）モデルにおいて、BMS-470539/MC1Rシステムの神経保護効果を消失させた。
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
| 動物実験 [1]: | |
動物モデル | 雄性Sprague-Dawley（SD）ラット |
準備方法 | ラットを無作為に5群に分けた：偽薬、SAH＋ビークル1（10μl滅菌生理食塩水、i.n.）、SAH＋BMS-470539（160μg/kg、10μl）、SAH＋BMS-470539＋ビークル2（6μl滅菌生理食塩水、i.c.v.）、SAH＋BMS-470539＋MSG-606（1nmol/μl、6μl）。MSG-606はSAHの1時間前にi.c.v.投与した。SAH後24時間に神経学的検査を行った。同側・左大脳皮質をウェスタンブロット用に採取した。 |
投与形態 | 1nmol/μl、6μl、i.c.v. |
アプリケーション | MSG-606によるMC1R阻害は、SAH＋BMS-470539＋ビークル2群と比較して、BMS-470539の抗炎症作用を有意に消失させた |
参考文献: [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 | |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 742.1 μL | 3.7105 mL | 7.4211 mL |
| 5 mM | 148.4 μL | 742.1 μL | 1.4842 mL |
| 10 mM | 74.2 μL | 371.1 μL | 742.1 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)