NN1177 TFA  (Synonyms: NNC9204-1177 TFA)

NN1177 (NNC9204-1177) TFA is a long-acting GLP-1/glucagon receptor co-agonist. NN1177 TFA can induce a dose-dependent body weight loss in diet-induced obese (DIO) mice^[1][2].

NN1177 (100 nM，3 天) TFA 可降低新鲜分离的人肝细胞中 CYP3A4 mRNA 的表达 (57.2-71.7%) 和活性 (18.5-51.5%)^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

NN1177 (3 或 5 nmol/kg，皮下注射) 可诱导饮食诱导肥胖 (DIO) 小鼠体重减轻、脂肪量减少以及糖耐量改善^[1]。
NN1177 (0.75-4 nmol/kg，皮下注射，每日一次，持续 8 周) 可降低喂食富含果糖和高脂肪饮食的 C57Bl/6 小鼠 (NASH 模型) 的肝脏脂肪以及炎症和纤维化相关生物标志物 (NASH 模型)^{[2]< /sup>.}

4570.07 (free base)

C₂₀₆H₃₂₃N₅₁O₆₆.xC₂HF₃O₂

固体

White to off-white

His-{Aib}-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Tyr-Leu-Glu-Ser-Lys-Arg-Ala-Arg-Glu-Phe-Val-Gln-Trp-Leu-Leu-{Lys(gGlu-gGlu-Ser-Glu-Ser-gGlu-gGlu-C18 diacid)}-Thr-NH2

H-{Aib}-QGTFTSDLSKYLESKRAREFVQWLL-{Lys(γGlu-γGlu-Ser-Glu-Ser-γGlu-γGlu-C18 diacid)}-T-NH2

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [1]. Simonsen L, et al. Preclinical evaluation of a protracted GLP-1/glucagon receptor co-agonist: Translational difficulties and pitfalls. PLoS One. 2022 Mar 4;17(3):e0264974.  [Content Brief]

  [2]. Monfeuga T, et al. Evaluation of long acting GLP1R/GCGR agonist in a DIO and biopsy-confirmed mouse model of NASH suggest a beneficial role of GLP-1/glucagon agonism in NASH patients. Mol Metab. 2023 Dec 7;79:101850.  [Content Brief]

  [3]. Säll C, et al. In vitro CYP450 enzyme down-regulation by GLP-1/glucagon co-agonist does not translate to observed drug-drug interactions in the clinic. Drug Metab Dispos. 2022 Jun 9:DMD-AR-2022-000865.  [Content Brief]