索伐肽
中文名称 | 索伐肽 |
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中文同义词 | 索伐肽;化合物 T15595;索伐肽 SOVATELTIDE 142569-99-1;IRL-1620 TFA盐 |
英文名称 | IRL-1620 |
英文同义词 | IRL-1620, HUMAN;IRL-1620;ENDOTHELIN-1(8-21), N-SUC-[GLU9, ALA11,15];N-SUC-[GLU9, ALA11,15]ENDOTHELIN-I (8-21);N-SUCCINYL-[GLU9, ALA11,15]-ENDOTHELIN, 8-21;SUC-ASP-GLU-GLU-ALA-VAL-TYR-PHE-ALA-HIS-LEU-ASP-ILE-ILE-TRP;SUC-ASP-GLU-GLU-ALA-VAL-TYR-PHE-ALA-HIS-LEU-ASP-ILE-ILE-TRP-OH;SUCCINYL-(GLU9,ALA11,15)-ENDOTHELIN-1 (8-21) |
CAS号 | 142569-99-1 |
分子式 | C86H117N17O27 |
分子量 | 1820.95 |
EINECS号 | |
相关类别 | 药物多肽;医药原料;Endothelin receptor |
Mol文件 | 142569-99-1.mol |
结构式 |
索伐肽 性质
沸点 | 2096.6±65.0 °C(Predicted) |
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密度 | 1.347±0.06 g/cm3(Predicted) |
储存条件 | −20°C |
溶解度 | 溶于二甲基亚砜 |
形态 | 粉末 |
酸度系数(pKa) | 3.39±0.10(Predicted) |
颜色 | 白色 |
水溶解性 | Soluble in water (0.5 mg/ml) |
序列 | Suc-Asp-Glu-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp-OH |
IC50: 16 pM (Endothelin receptor B), 19 μM (Endothelin receptor A)
IRL-1620 is the most potent and specific ligand for the ETB receptor (K i ETA/ K i ETB=120,000) as judged by the K i values for ETA (19 μM) and ETB (16 PM) receptors. IRL-1620 is 60 times more selective for the ETB receptor than ET-3 (K i ETA/ K i ETB=1,900).
IRL-1620 (1-100 nM) induces contractions of the guinea pig trachea. The effective concentration that produces 30 % of 60 mM KCI-induced contraction is estimated to be 28 nM for IRL 1620. IRL-1620 (1-100 nM) increases cytosolic Ca 2+ in the vascular endothelium ([Ca]E) with little effect on resting muscle tone, and relaxes the norepinephrine-stimulated tone with an increase in [Ca]E, in rat aorta,. IRL-1620 improves both acquisition (learning) and retention (memory) on the water maze task and enhances angiogenic and neurogenic remodeling. Rats treated with IRL-1620 significantly reduces the cognitive impairment induced by Aβ. IRL-1620 treatment enhances the number of blood vessels labeled with VEGF compared to vehicle treatment. IRL-1620, restores analgesic tolerance to morphine and oxycodone, but it does not affect morphine and oxycodone induced decrease in NGF/PI3K expression. IRL-1620 attenuates opioid tolerance without the involvement of NGF/PI3K pathway.
纯度(HPLC) ≥98.0%
醋酸根含量5.0%~12.0%
水分含量≤8.0%
肽含量≥80.0%
安全信息
WGK Germany | 3 |
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提供商 | 语言 |
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英文
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