Survodutide TFA 产品活性：Survodutide (BI 456906) TFA 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 TFA 是一种 29 个氨基酸的肽，是含有 C18 脂肪酸的有效酰化肽。Survodutide TFA 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-tfa.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) 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). 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. In Vivo: 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 (HY-114118; 20, 100 nmol/kg). Survodutide TFA dose-dependently reduces plasma glucagon. 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). 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. 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. 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 | Survodutide | NNC-0640 | Mazdutide 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。