IRL-1620 TFA (142569-99-1 free base)

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

IRL-1620 (TFA) is a potent selective endothelin receptor B (ETB) agonist with a Ki value of 16pm.

IRL-1620 (TFA) is a potent selective endothelin receptor B (ETB) agonist with a Ki value of 16pm.(In Vitro):IRL-1620 (TFA) is the most potent 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. IRL-1620 (TFA) is 60 times more selective for the ETB receptor than ET-3 (KiETA/ KiETB=1,900).(In Vivo):IRL-1620 (TFA) (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 (TFA) (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,. IRL-1620 (TFA) 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 (TFA), 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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Others

Other Targets

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

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1934.97

C88H118F3N17O29

>98% (HPLC)

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Sequence:Suc-Asp-Glu-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp

(-20℃)

With Ice Pack

≥ 2 years