| Bioactivity | 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]. | ||||||
| Invitro | 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]。 0 --> NN1177 TFA 相关抗体: | ||||||
| In Vivo | 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]. | ||||||
| Name | NN1177 TFA | ||||||
| Sequence | H-Aib-QGT FTSDL SKYLE SKRAR EFVQW LL-K(-γGlu-γGlu-Ser-Glu-Ser-γGlu-γGlu-C18 diacid)-T-NH2 | ||||||
| Formula | C206H323N51O66.xC2HF3O2 | ||||||
| Molar Mass | 4570.07 (free base) | ||||||
| Appearance | 固体 | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage | Sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
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| Reference | [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. [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. [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. |
NN1177 TFA
CAS: F: C206H323N51O66.xC2HF3O2 W: 4570.07 (free base)
NN1177 (NNC9204-1177) TFA is a long-acting GLP-1/glucagon receptor co-agonist. NN1177 TFA can induce a dose-dependent bo
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