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Description: Highly selective ETB agonist
Biological Activity
Highly 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.
Technical Data
| M. Wt | 1820 |
| Formula | C86H117N17O27 |
| Sequence |
DEEAVYFAHLDIIW (Modifications: Asp-1 = Suc-Asp) |
| Storage | Desiccate at -20°C |
| CAS Number | 142569-99-1 |
| PubChem ID | 16130933 |
| InChI Key | DXPHNGAMYPPTBJ-TZMIJSMNSA-N |
| Smiles | CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1=CNC=N1)NC(=O)[C@H](C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)CCC(O)=O)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solubility | Soluble to 0.70 mg/ml in water |
Product Datasheets
References
References are publications that support the biological activity of the product.
Haynes et al (1993) Endothelin; progress in pharmacology and physiology. TiPS 14 225 PMID: 8372400
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
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
If you know of a relevant reference for IRL-1620, please let us know.
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Keywords: IRL-1620, IRL-1620 supplier, selective, ETB, agonists, Receptors, Endothelin, 1196, Tocris Bioscience
8 Citations for IRL-1620
Citations are publications that use Tocris products. Selected citations for IRL-1620 include:
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
Ou et al (2014) Adaptive regulation of endothelin receptor type-A and type-B in vascular smooth muscle cells during pregnancy in rats. J Cell Physiol 229 489 PMID: 24105843
Mazzuca et al (2013) Enhanced endothelin receptor type B-mediated vasodilation and underlying [Ca2+]i in mesenteric microvessels of pregnant rats. Br J Pharmacol 169 1335 PMID: 23646960
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
Giachini et al (2009) Interleukin-10 attenuates vascular responses to endothelin-1 via effects on ERK1/2-dependent pathway. Am J Physiol Heart Circ Physiol 296 H489 PMID: 19074677
McQueen et al (2007) Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice. Br J Pharmacol 151 278 PMID: 17351652
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
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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