Nonapeptide-1 (acetate)
(Synonyms: Met-Pro-D-Phe-Arg-D-Trp-Phe-Lys-Pro-Val-NH2, MPFRWFKPV-NH2, 153N-6) 目录号 : GC45529
An MC1R antagonist
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Nonapeptide-1 is an antagonist of melanocortin receptor 1 (MC1R; Ki = 40 nM in COS-1 cells expressing human receptors).1 It is selective for MC1R over MC3R, MC4R, and MC5R (Kis = 470, 1,340, and 2,400 nM, respectively). Nonapeptide-1 inhibits cAMP accumulation and melanosome dispersion induced by α-melanocyte-stimulating hormone (α-MSH) in melanocytes with IC50 values of 2.5 and 11 nM, respectively.2
References
1. Schi•th, H.B., Muceniece, R., and Wikberg, J.E.S. Characterization of the binding of MSH-B, HB-228, GHRP-6 and 153N-6 to the human melanocortin receptor subtypes. Neuropeptides 31(6), 565-571 (1997).
2. Jayawickreme, C.K., Quillan, J.M., Graminski, G.F., et al. Discovery and structure-function analysis of α-melanocyte-stimulating hormone antagonists. J. Biol. Chem. 269(47), 29846-29854 (1994).
| Cas No. | SDF | ||
| 别名 | Met-Pro-D-Phe-Arg-D-Trp-Phe-Lys-Pro-Val-NH2, MPFRWFKPV-NH2, 153N-6 | ||
| Canonical SMILES | O=C([C@H](CCCNC(N)=N)NC([C@H](NC([C@@H]1CCCN1C([C@H](CCSC)N)=O)=O)CC2=CC=CC=C2)=O)N[C@H](CC3=CNC4=C3C=CC=C4)C(N[C@@H](CC5=CC=CC=C5)C(N[C@@H](CCCCN)C(N6CCC[C@H]6C(N[C@H](C(N)=O)C(C)C)=O)=O)=O)=O.CC(O)=O | ||
| 分子式 | C61H87N15O9S.XC2H4O2 | 分子量 | 1206.5 |
| 溶解度 | PBS (pH 7.2): 10 mg/ml | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.8288 mL | 4.1442 mL | 8.2884 mL |
| 5 mM | 0.1658 mL | 0.8288 mL | 1.6577 mL |
| 10 mM | 0.0829 mL | 0.4144 mL | 0.8288 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Effects of tea polyphenols on UVA-induced melanogenesis via inhibition of α-MSH-MC1R signalling pathway
Postepy Dermatol Alergol 2022 Apr;39(2):327-335.PMID:35645678DOI:PMC9131962
Introduction: Ultraviolet (UV) irradiation is a major environmental factor affecting photoaging, which is characterized by skin wrinkle formation and hyperpigmentation. Although many factors are involved in the melanogenesis progress, UV is thought to play a major role in tanning. The pathway of α-melanocyte-stimulating hormone (α-MSH)-melanocortin receptor 1 (MC1R) is associated with UV-induced melanogenesis. Thus, α-MSH antagonists may have applications in the prevention of melanogenesis. Aim: To investigate the effects of tea polyphenols (TPS) on pigmentation, and further explore the underlying mechanism. Material and methods: Human keratinocyte cell line (HaCaT) cells and Human epidermal melanocytes (HEM) were exposed to UVA and treated with different concentrations of TPS or Nonapeptide-1 acetate salt (N-1A). Then, cell viability, melanin content, and tyrosinase activity of both kinds of cells were detected. Quantification of α-MSH in HaCaT cells and HEM cells determined by ELISA assays. Immunohistochemistry of HEM cells was employed to further investigate the expression of melanogenesis-related proteins. Results: The different concentrations of TPS were found to decrease the melanin content, tyrosinase activity and melanogenesis-related proteins such as microphthalmia-associated transcription factor (MITF), tyrosinase-related protein (TRP)1, and TRP2. Besides, TPS inhibited α-MSH-MC1R signalling through directly suppressed α-MSH expression rather than the down-regulated expression level of MC1R. Conclusions: Our findings indicate that TPS may be a potential whitening agent for use in cosmetics and the medical treatment of hyperpigmentation disorders.