IRL-1620 (TFA) 是高效，选择性的内啡肽受体 (endothelin receptor) B 型激动剂，K_i 值为 16 pM。

IRL-1620 (TFA) is a potent and selective endothelin receptor type B (ETB) agonist with a K i of 16 pM.

Solid

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

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).
has not independently confirmed the accuracy of these methods. They are for reference only.

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 Ca 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 in

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and lightPowder -80°C 2 years；-20°C 1 year

{Suc}-DEEAVYFAHLDIIW

{Suc}-Asp-Glu-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp

[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 Alzheimers disease. Neuroscience. 2015 Aug 20;301:1-11.

In Vitro: DMSO : 50 mg/mL (25.84 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (ultrasonic) (insoluble)配制储备液