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IRL-1620

Catalog No. T15595 CAS 142569-99-1

IRL-1620 is an effective and selective agonist of endothelin receptor type B (ETB) (Ki: 16 pM).

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IRL-1620, CAS 142569-99-1

Pack Size	Availability	Price/USD	Quantity
500 μg	35 days	$ 660.00

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Biological Description

Chemical Properties

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Description	IRL-1620 is an effective and selective agonist of endothelin receptor type B (ETB) (Ki: 16 pM).
Targets&IC50	ETA receptor:19 μM, ETB receptor:16 pM
In vitro	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].
In vivo	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].

Molecular Weight	1820.974
Formula	C86H117N17O27
CAS No.	142569-99-1

Storage

keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Takai M, et al. A potent and specific agonist, Suc-[Glu9,Ala11,15]-endothelin-1(8-21), IRL 1620, for the ETB receptor. Biochem Biophys Res Commun. 1992 Apr 30;184(2):953-9. 2. Briyal S, et al. Stimulation of endothelin B receptors by IRL-1620 decreases the progression of Alzheimer's disease. Neuroscience. 2015 Aug 20;301:1-11. 3. Gulati S, et al. Attenuation of opioid tolerance by ETB receptor agonist, IRL-1620, is independent of an accompanied decrease in nerve growth factor in mice. Heliyon. 2017 Jun 7;3(6):e00317.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

IRL-1620 142569-99-1 Others IRL1620 IRL 1620 inhibitor inhibit

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