Name: Setmelanotide
Brand: TargetMol
SKU: T12882
Price: 375 CNY
Availability: InStock
Rating: 5 (10 reviews)

规格

价格

库存

数量

2 mg

¥ 375

现货

5 mg

¥ 535

现货

10 mg

¥ 803

现货

25 mg

¥ 1,714

现货

50 mg

¥ 2,571

现货

100 mg

¥ 3,857

现货

200 mg

¥ 5,785

现货

500 mg

¥ 8,677

现货

1 mL x 10 mM (in DMSO)

¥ 1,687

现货

产品介绍

生物活性

产品描述	Setmelanotide (RM-493) is a selective melanocortin-4 receptor agonist with EC50 values of 0.27 and 0.28 nM for human and rat MC4R. Setmelanotide enhances cAMP signaling, demonstrates functional selectivity, activates sympathetic preganglionic neurons to influence blood pressure, and is widely used to probe MC4R-MRAP2 interactions. Setmelanotide contributes to obesity-related research by modulating hunger and satiety circuits, reversing risperidone-induced weight gain in mice, and helping characterize MC4R variants in pediatric metabolic disorders. The anti-inflammatory actions of Setmelanotide in astrocytoma cells and the utility in combination with calorie restriction further highlight its broad value in metabolic and neuroendocrine research.
靶点活性	MC4R (rat):0.28 Nm (EC50), MC4R (human):2.1 nM (ki), MC1R (human):3.9 nM (ki), MC4R (rat):2.7 nM (ki), MC5R (human):1600 nM (EC50), MC4R (human):0.27 nM (EC50), MC3R (human):5.3nM (EC50), MC3R (human):10 nM (ki), MC1R (human):5.8 nM (EC50), MC5R (human):430 nM (ki)
体外活性	黑皮质素受体激动剂在大脑中发挥调节摄食与体重的作用，同时兼具其他独立效应。Setmelanotide 可激动人和大鼠的 MC4R，其对人 MC4R 的 Ki 值为 2.1 nM、EC50 值为 0.27 nM，对大鼠 MC4R 的 Ki 值为 2.7 nM、EC50 值为 0.28 nM [1]。
体内活性	Setmelanotide 对禁食过夜小鼠再进食行为的抑制作用具有受体特异性，该效应依赖功能性MC4R的介导，而不依赖MC3R。相较于对照组，经BIM-22493处理的Lep⁰ᵇ/Lep⁰ᵇ小鼠葡萄糖清除能力显著提升.慢性给予BIM-22493还与小鼠血糖水平及HOMA-IR的显著降低相关 [1]。在饮食诱导肥胖的非人灵长类动物模型中，经Setmelanotide处理8周（13.5%）后，动物的食物摄入量出现暂时性下降（降幅达35%），同时伴随体重的持续性降低 [2]。
别名	塞美兰肽, RM-493, RM493, IRC-022493, IRC022493, BIM-22493, BIM22493

化学信息

分子量	1117.31
分子式	C₄₉H₆₈N₁₈O₉S₂
CAS No.	920014-72-8
Smiles	C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC=CC=C4)NC(=O)[C@H](CC5=CN=CN5)NC(=O)[C@@H](C)NC(=O)[C@@H](NC([C@H](CCCNC(=N)N)NC(C)=O)=O)CSSC[C@@H](C(N)=O)NC3=O
密度	1.54 g/cm3 (Predicted)
颜色	White
物理性状	Solid
Sequence	Ac-Arg-Cys-{d-Ala}-His-Phe-Arg-Trp-Cys-NH2 (Disulfide bridge:Cys2-Cys8)
Sequence Short	Ac-RC-{d-Ala}-HFRWC-NH2 (Disulfide bridge:Cys2-Cys8)

储存&溶解度

存储

keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

H2O: 50 mg/mL (44.75 mM), Sonication is recommended.

DMSO: 100 mg/mL (89.5 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (2.95 mM), Sonication is recommeded.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	0.8950 mL	4.4750 mL	8.9501 mL	44.7503 mL
5 mM	0.1790 mL	0.8950 mL	1.7900 mL	8.9501 mL
10 mM	0.0895 mL	0.4475 mL	0.8950 mL	4.4750 mL
20 mM	0.0448 mL	0.2238 mL	0.4475 mL	2.2375 mL