MSG 606

目录号: GC50303纯度: >98%
MSG-606 对人黑皮质素 1 受体 (hMC1R) 具有强效拮抗活性和受体选择性(IC50 = 17 nM)。

MSG 606
Cas No.: 1416983-77-1
规格价格库存数量操作
1mg¥1,890.00现货
1
5mg¥4,680.00现货
1

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产品描述 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

MSG-606 对人黑皮质素 1 受体 (hMC1R) 具有强效拮抗活性和受体选择性(IC50 = 17 nM)[1]

MSG-606 是一种出色的探针,可专门针对黑色素瘤细胞进行皮肤癌诊断。 MSG-606 作为黑色素瘤细胞的拮抗剂。 MSG-606 对人黑色素瘤细胞 (A375) 的结合和 cAMP 活性,IC50 为 96 nM [1]

MSG-606(1 nmol/μl,6 μl)在蛛网膜下腔出血 (SAH) 模型中消除了 BMS-470539/MC1R 系统的神经保护作用[2]

实验参考方法 Experimental Reference Method

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

产品文档 Product Documents

化学性质Chemical Properties

CAS 号
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
分子式
C62H82N20O13S
分子量
1347.51 g/mol
溶解性
Soluble in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

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