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142569-99-1

中文名稱 索伐肽
英文名稱 IRL-1620
CAS 142569-99-1
分子式 C86H117N17O27
分子量 1820.95
MOL 文件 142569-99-1.mol
更新日期 2024/12/23 10:30:23
142569-99-1 結(jié)構(gòu)式 142569-99-1 結(jié)構(gòu)式

基本信息

中文別名
索伐肽
英文別名
IRL-1620
SPI-1620
Sovateltide
IRL-1620, HUMAN
28: PN: WO2007112069 SEQID
M.W. 1820.97 C86H117N17O27
SUC-[GLU9, ALA11,15]-ENDOTHELIN-1 (8-21)
N-SUC-[GLU9, ALA11,15]ENDOTHELIN-I (8-21)
ENDOTHELIN-1(8-21), N-SUC-[GLU9, ALA11,15]
SUCCINYL-(GLU9,ALA11,15)-ENDOTHELIN-1 (8-21)
所屬類別
生物化工:多肽

物理化學(xué)性質(zhì)

沸點(diǎn)2096.6±65.0 °C(Predicted)
密度1.347±0.06 g/cm3(Predicted)
儲存條件−20°C
儲存條件−20°C
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)3.39±0.10(Predicted)
形態(tài)powder
顏色white
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

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H332-H302-H312
WGK Germany3
WGK Germany3

常見問題列表

生物活性
IRL-1620 是高效,選擇性的內(nèi)啡肽受體 (endothelin receptor) B 型激動劑,Ki 值為 16 pM。
靶點(diǎn)

IC50: 16 pM (Endothelin receptor B), 19 μM (Endothelin receptor A)

體外研究

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).

體內(nèi)研究

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.

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