IRL-1620 TFA 

IRL-1620 (TFA) is a potent and selective endothelin receptor type B (ETB) agonist with a K_i of 16 pM^[1].

IRL-1620 (TFA) is the most potent and specific ligand for the ETB receptor (K_iETA/ K_iETB=120,000) as judged by the K_i values for ETA (19 μM) and ETB (16 PM) receptors^[1].
IRL-1620 (TFA) is 60 times more selective for the ETB receptor than ET-3 (K_iETA/ K_iETB=1,900)^[1].

MedChemExpress (MCE) 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^[1].
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,^[1].
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^[2].

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

1934.97

C₈₈H₁₁₈F₃N₁₇O₂₉

Solid

White to off-white

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

{Suc}-DEEAVYFAHLDIIW

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]

  [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.  [Content Brief]