Survodutide TFA |
Catalog No.GC72223 |
Survodutide TFA est un agoniste double sélectif puissant du récepteur du Glucagon / GLP - 1R avec des CE50 de 0,52 nm et 0,33 nm dans les cellules Cho - K1, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
The EC50 is 0.36 nM for Survodutide (BI 456906) TFA in the endogenous mouse GLP-1R in the insulinoma cell line MIN6, and the EC50 is 60 pM for GLP-1. In 0.5% human and mouse plasma, Survodutide TFA shows a similar potency to that of endogenous GLP-1. For the GCGR, in 0.5% human and mouse plasma, Survodutide TFA is 6-fold less potent (0.29 and 0.17 nM, respectively) in relation to endogenous glucagon (47 and 30 pM, respectively)[1].
Proteolytic stability of Survodutide TFA is helped by C-terminal amidation and the introduction of a non-coded amino acid 1-aminocyclobutane-1-carboxylic acid (Ac4c) in position 2, well established as the site of proteolytic activity for dipeptidyl peptidase-4. The desired extended terminal half-life of Survodutide TFA is achieved by the introduction of a glycine–serine linker in position 24, carrying a C18 di-acid[1].
Survodutide (BI 456906; 3, 10, 20, 30 nmol/kg; SC; daily; 30 days) TFA achieves a greater bodyweight-lowering efficacy in diet-induced obese mice compared with maximally effective doses of Semaglutide . Survodutide TFA dose-dependently reduces plasma glucagon[1].
Survodutide (1, 3, 10, 30, 100 nmol/kg; SC; single dose) TFA dose-dependently reducesacute food intake in WT but not in GLP-1R KO mice (Three-week-old, male, lean NMRI outbred mice)[1].
Survodutide (1, 3, 10, 30, 100 nmol/kg; SC; single dose) TFA engages the glucagon receptor in vivo upon single dosing, increases liver nicotinamide N-methyltransferase mRNA, and reduces plasma serine and glutamine[1].
Survodutide (SC injection) TFA causes mean residence times of 44 and 140 h and Tmax values of 7 and 51 h obtained in mice and dogs, respectively[1].
Pharmacokinetic Parameters of Survodutide (BI 456906) in mice and dogs[1].
Mice (20 nmol/kg; SC) | Dogs (10 nmol/kg; SC) | |
Tmax (h) | 7 | 50.7 |
Cmax (nM) | 84.9 | 62.0 |
AUC0-∞ (nM∗h) | 4640 | 9540 |
References:
[1]. Tina Zimmermann, et al. BI 456906: Discovery and preclinical pharmacology of a novel GCGR/GLP-1R dual agonist with robust anti-obesity efficacy. Mol Metab. 2022 Dec:66:101633.
Average Rating: 5
(Based on Reviews and 30 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *