Name: IRL-1620
Brand: TargetMol
SKU: T15595
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

500 μg

¥ 6,690

35日内发货

生物活性

产品描述	IRL-1620 is an effective and selective agonist of endothelin receptor type B (ETB) (Ki: 16 pM).
靶点活性	ETB receptor:16 pM, ETA receptor:19 μM
体外活性	IRL-1620 is 60 times more selective for the ETB receptor than ET-3 (KiETA/ KiETB=1,900). IRL-1620 is the most effective and specific ligand for the ETB receptor (KiETA/ KiETB=120,000) as judged by the Ki values for ETA (19 μM) and ETB (16 PM) receptors[1].
体内活性	IRL-1620 improves both acquisition (learning) and retention (memory) on the water maze task and enhances angiogenic and neurogenic remodeling. In rat aorta, IRL-1620 (1-100 nM) enhances 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. IRL-1620 (1-100 nM) causes contractions of the guinea pig trachea. For IRL 1620, the effective concentration that produces 30 % of 60 mM KCI-induced contraction is estimated to be 28 nM [1]. Rats treated with IRL-1620 obviously decreases 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].

化学信息

分子量	1820.974
分子式	C₈₆H₁₁₇N₁₇O₂₇
CAS No.	142569-99-1
Smiles	CC[C@H](C)[C@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)CCC(O)=O)C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(O)=O \|@:102\|
密度	1.31g/cm3
Sequence	{Suc}-Asp-Glu-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp
Sequence Short	{Suc}-DEEAVYFAHLDIIW