耗材描述
Survodutide
产品活性:Survodutide (BI 456906) 是一种有效的、选择性的胰高血糖素受体/GLP-1 受体 (GCGR/GLP-1R) 双重激动剂,在 CHO-K1 细胞中的 EC50 值分别为 0.52 nM 和 0.33 nM。Survodutide 是一种 29 个氨基酸的肽,是含有 C18 脂肪酸的有效酰化肽。Survodutide 通过增加能量消耗和减少食物摄入来实现强大的抗肥胖功效。
产品来源: https://www.medchemexpress.cn/survodutide.html
研究领域:GPCR/G Protein
作用靶点:GLP Receptor | GCGR
In Vitro: The EC50 is 0.36 nM for Survodutide (BI 456906) 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 shows a similar potency to that of endogenous GLP-1. For the GCGR, in 0.5% human and mouse plasma, Survodutide is 6-fold less potent (0.29 and 0.17 nM, respectively) in relation to endogenous glucagon (47 and 30 pM, respectively).
Proteolytic stability of Survodutide 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 is achieved by the introduction of a glycine–serine linker in position 24, carrying a C18 di-acid.
In Vivo: Survodutide (BI 456906; 3, 10, 20, 30 nmol/kg; SC; daily; 30 days) achieves a greater bodyweight-lowering efficacy in diet-induced obese mice compared with maximally effective doses of Semaglutide (HY-114118; 20, 100 nmol/kg). Survodutide dose-dependently reduces plasma glucagon.
Survodutide (1, 3, 10, 30, 100 nmol/kg; SC; single dose) dose-dependently reducesacute food intake in WT but not in GLP-1R KO mice (Three-week-old, male, lean NMRI outbred mice).
Survodutide (1, 3, 10, 30, 100 nmol/kg; SC; single dose) engages the glucagon receptor in vivo upon single dosing, increases liver nicotinamide N-methyltransferase mRNA, and reduces plasma serine and glutamine.
Survodutide (SC injection) causes mean residence times of 44 and 140 h and Tmax values of 7 and 51 h obtained in mice and dogs, respectively.
Pharmacokinetic Parameters of Survodutide (BI 456906) in mice and dogs.
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
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Peptide Library | Semaglutide | Exendin-4 | Liraglutide | Tirzepatide hydrochloride | Glucagon (1-29), bovine, human | Exendin(9-39) amide | Retatrutide | Orforglipron | GLP-1(7-37) | GLP-1(7-36), amide acetate | MK 0893 | Adomeglivant | BETP | Cotadutide acetate | GLP-1R Antagonist 1 | Danuglipron | GLP-1(9-36)amide | GLP-2(1-33)(human) | Oxyntomodulin (bovine, porcine) | Lixisenatide | Beinaglutide | Lotiglipron | NNC-0640 | Mazdutide | GLP-1R agonist 2
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