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LSN 3318839

Cat. No. 7959 Submit a Review Datasheet / COA / SDS
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Description: Glucagon-like peptide-1 receptor (GLP1-R) positive allosteric modulator
Chemical Name: (R)-2-(2-(1-((R)-1-(2,6-Dichloro-3-cyclopropylphenyl)ethyl)-1H-imidazo[4,5-c]pyridin-6-yl)phenyl)propanoic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for LSN 3318839

LSN 3318839 is a potent glucagon-like peptide-1 receptor (GLP1-R) positive allosteric modulator (EC50 = 14 nM). Acts as a molecular glue to stabilize peptide ligand and GLP1 receptor interaction. Potentiates activity of GLP-1 (7-36) (Cat. No. 2082) and the low-affinity metabolite GLP-1 (9-36) (Cat. No. 3266). LSN 3318839 alone or in combination with Sitagliptin (Cat. No. 6816) lowers glucose levels in animal models of diabetes. LSN 3318839 is orally bioavailable.

Technical Data for LSN 3318839

M. Wt 480.39
Formula C26H23Cl2N3O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2764704-18-7
PubChem ID 162641136
InChI Key JPJWHCNGSBCZMI-HUUCEWRRSA-N
Smiles C[C@H](C1=C(C(C2CC2)=CC=C1Cl)Cl)N3C4=CC(C5=C(C=CC=C5)[C@@H](C)C(O)=O)=NC=C4N=C3

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 LSN 3318839

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 48.04 100

Preparing Stock Solutions for LSN 3318839

The following data is based on the product molecular weight 480.39. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.08 mL 10.41 mL 20.82 mL
5 mM 0.42 mL 2.08 mL 4.16 mL
10 mM 0.21 mL 1.04 mL 2.08 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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References for LSN 3318839

References are publications that support the biological activity of the product.

Willard et al (2021) Discovery of an orally efficacious positive allosteric modulator of the glucagon-like peptide-1 receptor. J.Med.Chem. 64 3439 PMID: 33721487

If you know of a relevant reference for LSN 3318839, please let us know.

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Citations for LSN 3318839

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Peptides Involved in Appetite Modulation Scientific Review

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.