1. GPCR/G Protein Neuronal Signaling
  2. Melanocortin Receptor
  3. Melanotan (MT)-II

Melanotan (MT)-II  (Synonyms: 美拉诺坦 (MT)-II)

目录号: HY-P0267 纯度: 99.65%
COA 产品使用指南

Melanotan (MT)-II是一种合成的黑皮质素 (melanocortin) 受体激动剂。它是可注射用的多肽荷尔蒙,可促进晒黑。

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Custom Peptide Synthesis

Melanotan (MT)-II Chemical Structure

Melanotan (MT)-II Chemical Structure

CAS No. : 121062-08-6

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MCE 顾客使用本产品发表的 1 篇科研文献

查看 Melanocortin Receptor 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Melanotan (MT)-II, a synthetic melanocortin receptor agonist, is an injectable peptide hormone used to promote tanning.

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 EC50
110 nM
Compound: MT-II
Agonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
Agonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
[PMID: 26218460]
A-375 IC50
6.7 nM
Compound: MT-II
Antagonist activity at human MC1 receptor expressed in A375 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
Antagonist activity at human MC1 receptor expressed in A375 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting
[PMID: 26218460]
HEK293 EC50
0.021 nM
Compound: MTII
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay
[PMID: 15615519]
HEK293 EC50
0.03 nM
Compound: MT-II
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
[PMID: 25347033]
HEK293 EC50
0.04 nM
Compound: MTII
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
[PMID: 15615519]
HEK293 EC50
0.05 nM
Compound: MTII
Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
[PMID: 25699138]
HEK293 EC50
0.06 nM
Compound: MT-II
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
[PMID: 25347033]
HEK293 EC50
0.17 nM
Compound: MTII
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
[PMID: 15615519]
HEK293 EC50
0.18 nM
Compound: MT-II
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
[PMID: 25347033]
HEK293 EC50
0.18 nM
Compound: MTII
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
[PMID: 15615519]
HEK293 EC50
0.19 nM
Compound: MT-II
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay
[PMID: 25347033]
HEK293 EC50
0.22 nM
Compound: MTII
Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
[PMID: 25699138]
HEK293 EC50
0.3 nM
Compound: 17
Activity against hMC1R transfected in HEK293 cells by intracellular cAMP accumulation
Activity against hMC1R transfected in HEK293 cells by intracellular cAMP accumulation
[PMID: 16539382]
HEK293 EC50
0.35 nM
Compound: MTII
Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
[PMID: 25699138]
HEK293 EC50
0.57 nM
Compound: MTII
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
[PMID: 25699138]
HEK293 IC50
1 nM
Compound: MT-II
Displacement of [125I]-NDP-alpha-MSH from human MC1 receptor expressed in HEK293 cells by gamma counting analysis
Displacement of [125I]-NDP-alpha-MSH from human MC1 receptor expressed in HEK293 cells by gamma counting analysis
[PMID: 25699148]
HEK293 EC50
1 nM
Compound: MT-II
Activity at human MC1R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
Activity at human MC1R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
[PMID: 16931008]
HEK293 EC50
1.02 nM
Compound: MT-II
Activity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
Activity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
[PMID: 25699148]
HEK293 IC50
1.1 nM
Compound: MT-II
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
[PMID: 26599352]
HEK293 IC50
1.2 nM
Compound: MT-II
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 1 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 1 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
[PMID: 26599352]
HEK293 IC50
1.2 nM
Compound: MT-II
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
[PMID: 26599352]
HEK293 EC50
1.8 nM
Compound: MT-II
Agonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
Agonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
[PMID: 26599352]
HEK293 EC50
1.8 nM
Compound: MT-II
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
[PMID: 26599352]
HEK293 EC50
1.9 nM
Compound: 17
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation
[PMID: 16539382]
HEK293 IC50
2 nM
Compound: MT-II
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis
[PMID: 25699148]
HEK293 EC50
2.1 nM
Compound: MT-II
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
[PMID: 25699148]
HEK293 IC50
2.3 nM
Compound: MT-II
Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
[PMID: 21486697]
HEK293 IC50
2.3 nM
Compound: MT-II
Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
[PMID: 21486697]
HEK293 IC50
2.3 nM
Compound: MT-II
Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis
Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis
[PMID: 25699148]
HEK293 EC50
2.3 nM
Compound: MT-II
Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
[PMID: 16931008]
HEK293 EC50
2.4 nM
Compound: MT-II
Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
[PMID: 16931008]
HEK293 EC50
2.9 nM
Compound: MT-II
Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
[PMID: 26599352]
HEK293 EC50
2.9 nM
Compound: 17
Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation
Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation
[PMID: 16539382]
HEK293 EC50
3.1 nM
Compound: MT-II
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
[PMID: 28972753]
HEK293 EC50
3.3 nM
Compound: MT-II
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX
[PMID: 26599352]
HEK293 EC50
3.3 nM
Compound: 17
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation
[PMID: 16539382]
HEK293 EC50
33.9 nM
Compound: MT-II
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
[PMID: 28972753]
HEK293 EC50
33.9 nM
Compound: MT-II
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
[PMID: 28972753]
HEK293 IC50
4.2 nM
Compound: MT-II
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
[PMID: 21486697]
HEK293 IC50
4.2 nM
Compound: MT-II
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis
[PMID: 25699148]
HEK293 EC50
5.1 nM
Compound: MT-II
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
[PMID: 25699148]
HEK293 EC50
5.7 nM
Compound: MT-II
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter
[PMID: 25699148]
HEK293 IC50
7.5 nM
Compound: MT-II
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis
[PMID: 26599352]
HEK293 IC50
8 nM
Compound: MT-II
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting
[PMID: 21486697]
HEK293 EC50
8 nM
Compound: MT-II
Activity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
Activity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation
[PMID: 16931008]
HEK293 EC50
8.6 nM
Compound: MT-II
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
[PMID: 28972753]
体外研究
(In Vitro)

Melanotan (MT)-II 是一种有效的非选择性黑皮质素受体激动剂,对 MC1、MC3、MC4 和 MC5 受体亚型具有高亲和力,这些亚型参与许多生理系统的调节,例如色素系统、能量稳态、性功能、免疫系统、炎症和心血管系统[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Melanotan (MT)-II 通过引发勃起事件和缩短第一次勃起事件发生的潜伏期,对勃起施加剂量依赖性诱导剂活性。静脉注射黑素素 (MT)-II (1 mg/kg) 后海绵体神经刺激引起的勃起反应增加,从而对勃起产生促进作用[2]
Melanotan (MT)-II 促进周围神经再生并在大鼠中具有神经保护特性。Melanotan (MT)-II 剂量为 20 μg/kg 每 48 小时,皮下注射时,显著增强大鼠坐骨神经挤压损伤后感觉功能的恢复,但剂量为 2 或 50 μg/kg 时无效果[3]
Melanotan (MT)-II 是勃起功能障碍男性阴茎勃起的有效启动剂[4]
Melanotan (MT)-II 在小鼠模型中减少食物摄入量和体重并引发产热反应[5]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

1024.18

Formula

C50H69N15O9

CAS 号
性状

固体

颜色

White to off-white

Sequence

Ac-{Nle}-Asp-His-{d-Phe}-Arg-Trp-Lys-NH2, (2→7)-lactam

Sequence Shortening

Ac-{Nle}-DH-{d-Phe}-RWK-NH2, (2→7)-lactam

中文名称

美拉诺坦 (MT)-II

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

H2O 中的溶解度 : 6.67 mg/mL (6.51 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9764 mL 4.8820 mL 9.7639 mL
5 mM 0.1953 mL 0.9764 mL 1.9528 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献
Animal Administration
[2][5]

Rats: To investigate the inducer activity on erection, melanotan (MT)-II or vehicle (saline) is acutely injected i.v., i.t. or within the PVN after a 5 min baseline recording period is obtained. ICP and MAP are then recorded for a 60 min period after saline or melanotan (MT)-II delivery. I.v. injections (three doses; 0.1, 0.3, and 1 mg/kg in saline) are performed with a catheter inserted in the jugular vein[2].

Mice: Melanotan (MT)-II (0.1 and 0.2 nM) or vehicle (artificial cerebrospinal fluid) is administered. SPA is recorded continuously every 5 min. Food intake measurements are taken 6 and 24 h postinjection. Body weight is measured every 24 h. Chow and water are available ad libitum. A 48-h interval occurrs between drug treatments[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 0.9764 mL 4.8820 mL 9.7639 mL 24.4098 mL
5 mM 0.1953 mL 0.9764 mL 1.9528 mL 4.8820 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Melanotan (MT)-II
目录号:
HY-P0267
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