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Submit ReviewL-817,818
Description: Potent and selective sst5 agonist
Chemical Name: N2-[[2-(2-Naphthalenyl)-1H-benz[g]indol-3-yl]acetyl-D-lysine (2S)-2-aminopropyl ester
Purity: ≥99% (HPLC)
Biological Activity for L-817,818
L-817,818 is a potent and selective somatostatin sst5 receptor agonist. Ki values are 0.4, 3.3, 52, 64 and 82 nM for cloned human sst5, sst1, sst2, sst3 and sst4 receptors respectively. Inhibits growth hormone release from rat pituitary cells (EC50 = 3.1 nM) and insulin release from mouse pancreatic islets (EC50 = 0.3 nM) in vitro.
Compound Libraries for L-817,818
L-817,818 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for L-817,818
| M. Wt | 536.67 |
| Formula | C33H36N4O3 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 217480-27-8 |
| PubChem ID | 9937014 |
| InChI Key | NFVRGDRCCNEGBS-KCWXNJEJSA-N |
| Smiles | O=C(CC1=C(C4=CC=C(C=CC=C5)C5=C4)NC2=C1C=CC3=C2C=CC=C3)N[C@@H]([C@](OC[C@@H](N)C)=O)CCCCN |
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 for L-817,818
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 53.67 | 100 |
Preparing Stock Solutions for L-817,818
The following data is based on the product molecular weight 536.67. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 1.86 mL | 9.32 mL | 18.63 mL |
| 5 mM | 0.37 mL | 1.86 mL | 3.73 mL |
| 10 mM | 0.19 mL | 0.93 mL | 1.86 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
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Product Datasheets for L-817,818
References for L-817,818
References are publications that support the biological activity of the product.
Rohrer et al (1998) Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science 282 737 PMID: 9784130
Rohrer and Schaeffer (2000) Identification and characterization of subtype selective somatostatin receptor agonists. J.Physiol.Paris 94 211 PMID: 11087999
Strowski et al (2000) Somatostatin inhibits Ins and glucagon secretion via two receptor subtypes: An in vitro study of pancreatic islets from somatostatin receptor 2 knockout mice. Endocrinology 141 111 PMID: 10614629
If you know of a relevant reference for L-817,818, please let us know.
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Keywords: L-817,818, L-817,818 supplier, Potent, selective, sst5, agonists, Receptors, Somatostatin, L817818, 1980, Tocris Bioscience
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