Bioactivity | LSN3160440 is an allosteric modulator of GLP-1R, which acts as a protein–protein interaction (PPI) stabilizer or molecular glue to assist in the adhesion of inactive GLP-1 (9-36) NH2 on GLP-1R[1][2]. |
Invitro | LSN3160440 binds between the TM1 and TM2 interfaces of GLP-1R, and the benzimidazole group of LSN3160440 interacts with GLP-1R in a variety of ways, such as van der Waals contacts with Leu142, π‒π stacking with Tyr145, and frequent water bridging with Lys202[1]. |
Name | LSN3160440 |
CAS | 2765539-59-9 |
Formula | C27H27Cl2N3O |
Molar Mass | 480.43 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Hui-Jun Liao, et al. Investigating Potential GLP-1 Receptor Agonists in Cyclopeptides from Pseudostellaria heterophylla, Linum usitatissimum, and Drymaria diandra, and Peptides Derived from Heterophyllin B for the Treatment of Type 2 Diabetes: An In Silico Study. Metabolites. 2022 Jun 15;12(6):549. [2]. Hongyu Wu, et al. Molecular glues modulate protein functions by inducing protein aggregation: A promising therapeutic strategy of small molecules for disease treatment. Acta Pharm Sin B. 2022 Sep;12(9):3548-3566. |