CAS NO: | 142569-99-1 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | IRL-1620 is a potent and selectiveendothelin receptortype B (ETB)agonist with aKiof 16 pM. | |
IC50& Target |
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体外研究 (In Vitro) | IRL-1620 is the most potent and specific ligand for the ETB receptor (KiETA/ KiETB=120,000) as judged by the Kivalues for ETA (19 μM) and ETB (16 PM) receptors[1].IRL-1620 is 60 times more selective for the ETB receptor than ET-3 (KiETA/ KiETB=1,900)[1]. | |
体内研究 (In Vivo) | 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[1].IRL-1620 (1-100 nM) increases cytosolic Ca2+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,[1].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[2].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[3]. | |
分子量 | 1820.95 | |
Formula | C86H117N17O27 | |
CAS 号 | 142569-99-1 | |
Sequence | {Suc}-Asp-Glu-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp | |
Sequence Shortening | {Suc}-DEEAVYFAHLDIIW | |
运输条件 | Room temperature in continental US; may vary elsewhere. | |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |