Nonapeptide-1 acetate salt
(Synonyms: Melanostatine-5 acetate salt) 目录号 : GC36756
An MC1R antagonist
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- 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
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 subtypesNeuropeptides31(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 antagonistsJ. Biol. Chem.269(47)29846-29854(1994)
| Cas No. | SDF | ||
| 别名 | Melanostatine-5 acetate salt | ||
| 分子式 | C63H91N15O11S | 分子量 | 1266.56 |
| 溶解度 | Water: 50 mg/mL (39.48 mM) | 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 | 0.7895 mL | 3.9477 mL | 7.8954 mL |
| 5 mM | 0.1579 mL | 0.7895 mL | 1.5791 mL |
| 10 mM | 0.079 mL | 0.3948 mL | 0.7895 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.