IRL-1620
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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 0.70 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1820. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.55 mL | 2.75 mL | 5.49 mL |
| 5 mM | 0.11 mL | 0.55 mL | 1.1 mL |
| 10 mM | 0.05 mL | 0.27 mL | 0.55 mL |
| 50 mM | 0.01 mL | 0.05 mL | 0.11 mL |
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References
References are publications that support the products' biological activity.
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.
View Related Products by Target
Keywords: selective ETB agonists Receptors Endothelin ETB Receptor Peptide
5 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
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
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
Do you know of a great paper that uses IRL-1620 from Tocris? If so please let us know.