Cat. No. 1196
Biological ActivityHighly selective ETB endothelin receptor agonist (Ki values are 0.016 and 1900 nM at ETB and ETA receptors respectively). Discriminates two subpopulations of ETB receptors.
(Modifications: Asp-1 = Suc-Asp)
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
Mazzoni et al (1999) Suc-[Glu9, Ala11,15]-endothelin-1 (8-21), IRL 1620, identifies two populations of ETB receptors in guinea-pig bronchus. Br.J.Pharmacol. 127 1406. PMID: 10455290.
Haynes et al (1993) Endothelin; progress in pharmacology and physiology. TiPS 14 225. PMID: 8372400.
Sakamoto et al (1993) Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB-selective agonists. J.Biol.Chem. 268 8547. PMID: 8473300.
Takai et al (1992) A potent and specific agonist, Suc-[Glu9,Ala11,15]-endothelin-1(8-21), IRL 1620, for the ETB receptor. Biochem.Biophys.Res.Commun. 184 953. PMID: 1315540.
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Citations are publications that use Tocris products. Selected citations for IRL-1620 include:
Durgan et al (2015) Increased cerebrovascular sensitivity to endothelin-1 in a rat model of obstructive sleep apnea: a role for endothelin receptor B. J Cereb Blood Flow Metab 35 402. PMID: 25425077.
Choisy et al (2012) Modulation by endothelin-1 of spontaneous activity and membrane currents of atrioventricular node myocytes from the rabbit heart. PLoS One 7 e33448. PMID: 22479400.
Hamby et al (2012) Inflammatory mediators alter the astrocyte transcriptome and calcium signaling elicited by multiple G-protein-coupled receptors. Purinergic Signal 32 14489. PMID: 23077035.
McQueen et al (2007) Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice. Br J Pharmacol 151 278. PMID: 17351652.
Khan et al (2006) Pharmacological characterization of endothelin receptors-mediated contraction in the mouse isolated proximal and distal colon. Br J Pharmacol 147 607. PMID: 16432510.
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Keywords: IRL-1620, supplier, selective, ETB, agonists, Receptors, Endothelin, Tocris Bioscience, ETB Receptor Agonist products
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High affinity dual ETA and ETB receptor antagonist;orally bioavailable
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