メタスチン(45-54)アミド, ヒト
メタスチン(45-54)アミド, ヒト · キスペプチン-10 · キッスペプチン10 · (2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-アミノ-3-(4-ヒドロキシフェニル)プロパンアミド]-3-カルバモイルプロパンアミド]-3-(1H-インドール-3-イル)プロパンアミド]-N-[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-4-カルバムイミドアミド-1-{[(1S)-1-カルバモイル-2-フェニルエチル]カルバモイル}ブチル]カルバモイル}-3-メチルブチル]カルバモイル}メチル)カルバモイル]-2-フェニルエチル]カルバモイル}-2-ヒドロキシエチル]ブタンジアミド · KISSPEPTIN-10 · Kisspetin-10 · Kisspeptin-10 Fragment · METASTIN (45-54)
識別子と物理属性
| CAS No. | 374675-21-5 |
|---|---|
| 分子式 | C63H83N17O14 |
| 平均分子量 | 1,302.4 g/mol |
| 単同位体質量 | 1,301.63054039 g/mol |
| SMILES | CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O |
| InChIKey | RITKWYDZSSQNJI-INXYWQKQSA-N |
| PubChem CID | 25240297 |
| ChEMBL | CHEMBL376756 |
| 現地名 | メタスチン(45-54)アミド, ヒト |
化学・物理的性質
| XLogP | -1.9 |
|---|---|
| 極性表面積 | 538 |
| 水素結合供与体数 | 18 |
| 水素結合受容体数 | 16 |
| 回転可能結合数 | 38 |
| 重原子数 | 94 |
| 形式電荷 | 0 |
| 複雑度 | 2,590 |
| 密度 | 1.46±0.1 g/cm3(Predicted) |
| 貯蔵条件 | -20°C |
| 溶解度 | DMF: 15 mg/mlDMSO: 15 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.33 mg/ml1mg/mlで水に溶ける |
| 外観・状態 | A crystalline solid |
| pKa（酸解離定数） | 9.96±0.15(Predicted) |
| 色 | White to off-white |
| InChIKey | RITKWYDZSSQNJI-INXYWQKQSA-N |
安全性と法規制
| 水環境危害等級（WGK） | 3 |
|---|---|
| 貯蔵分類 | 11 - Combustible Solids |
用途
説明
Kisspeptin-10, also called Metastin (45-54), is a 10 amino acid peptide that corresponds to the bioactive C-terminal 45-54 amino acids of metastin, a metastasis suppressor gene product. It acts as a potent agonist of GPR54 (OT7T175, AXOR12), with approximately 8-fold higher binding affinity than metastin (Ki values of 0.042 and 0.34 nM, respectively, for displacement of metastin (40-54)). Metastin (45-54) induces calcium mobilization in GPR54-transfected cells (EC50 = 0.18-1.1 nM). It inhibits the migration of GPR54-transfected CHO cells at concentrations of 10-100 nM, equaling the potency of full length metastin.
使用
Kisspeptin 10 (human) is a powerful and specific activator for AXOR12 and hOT7T175 receptors. The Kisspeptin 10 (human) amide has been utilized in studies involving progesterone release from MA-10 cells and in experiments to induce gonadal differentiation in clownfish.
使用
Kisspeptin-10 (human), a member of the kisspeptin family, is a neuropeptide that regulates gonadotropin secretion. It has anti-angiogenic effects, a concentration-dependent inhibition of HUVEC proliferation and migration, and is highly expressed in the placenta, which may help to regulate angiogenesis in this tissue. Kisspeptin-10 (human) is currently undergoing clinical studies with insulin secretion in men. It is also a potential drug target for the treatment of infertility.
一般的な説明
Metastin is also known as kisspeptin 1 (KISS1). It is encoded by KISS1 gene, that is mapped to human chromosome 1q32. Metastin is a tumor suppressor protein, made up of 145 amino acids. The protein fragments contain RFamide motif at the C- terminal end. The encoded protein is expressed in the human hypothalamus, gonads, placenta, liver and pancreas. This novelpeptideis mainly isolated from the human placenta.