| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
CYP3A4
NN1177 TFA targets both the glucagon-like peptide-1 (GLP-1) receptor and the glucagon receptor. GLP-1 receptor activation promotes insulin secretion, suppresses glucagon secretion, and delays gastric emptying, contributing to glucose homeostasis and satiety. Glucagon receptor activation stimulates energy expenditure and lipolysis. By co-activating both receptors, NN1177 TFA achieves synergistic effects on body weight reduction and metabolic improvement. |
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| ln Vitro |
NN1177 (100 nM, 3 days) TFA can reduce CYP3A4 mRNA expression (57.2-71.7%) and activity (18.5-51.5%) in freshly isolated human hepatocytes[3].
NN1177 TFA shows potent in vitro activity as a GLP-1/glucagon receptor co-agonist. As a peptide-based dual agonist, it activates both the GLP-1 receptor and the glucagon receptor with high potency. The compound's ability to activate both receptors has been validated in cell-based assays measuring receptor-mediated signaling. The specific EC50 values for GLP-1 and glucagon receptor activation have not been detailed in the available literature. |
| ln Vivo |
NN1177 (3 or 5 nmol/kg, subcutaneous injection) induces weight loss, fat mass reduction, and improved glucose tolerance in diet-induced obese (DIO) mice[1]. NN1177 (0.75-4 nmol/kg, subcutaneous injection, once a day for 8 weeks) reduces liver fat and inflammation and fibrosis-related biomarkers in C57Bl/6 mice fed a fructose-rich and high-fat diet (NASH model)[2].
NN1177 TFA demonstrates in vivo activity in diet-induced obese (DIO) mice, where it induces dose-dependent body weight loss. The compound's long-acting nature provides sustained efficacy with convenient dosing. The weight loss is achieved through the combined effects of GLP-1 receptor-mediated satiety and glucagon receptor-mediated energy expenditure. |
| Enzyme Assay |
Non-cell-based binding assays for NN1177 TFA typically involve measuring the affinity of the compound for the GLP-1 receptor and the glucagon receptor. A standard protocol includes surface plasmon resonance (SPR) or radioligand binding assays using membrane preparations from cells expressing the receptors. The compound's ability to activate both receptors is assessed in cell-based signaling assays.
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| Cell Assay |
Cellular assays for NN1177 TFA typically involve cell lines expressing the GLP-1 receptor or the glucagon receptor. A representative protocol includes culturing cells (e.g., HEK293 cells transfected with GLP-1 receptor or glucagon receptor) in appropriate medium, treating with NN1177 TFA at various concentrations (0.001–1000 nM), and measuring receptor activation by cAMP accumulation assays or reporter gene assays. EC50 values for both receptors can be determined from dose-response curves.
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| Animal Protocol |
In vivo animal studies with NN1177 TFA are conducted in diet-induced obese (DIO) mouse models. A typical protocol involves feeding mice a high-fat diet to induce obesity, followed by administration of NN1177 TFA via subcutaneous or intraperitoneal injection at doses determined from pharmacokinetic studies (typically 0.01–1 mg/kg, once daily or less frequently). Body weight, food intake, and metabolic parameters are monitored over the treatment period.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NN1177 TFA have been characterized for its long-acting profile. As a peptide-based compound with a molecular weight of 4570.07 (free base), it is expected to have a prolonged half-life due to modifications that enhance stability and reduce clearance. The compound is administered via injection in research studies.
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| Toxicity/Toxicokinetics |
As a research compound, NN1177 TFA is not intended for human therapeutic use without further development, and comprehensive toxicological data are limited to preclinical studies. Standard safety assessments would include cytotoxicity screening, immunogenicity testing, and preliminary toxicology studies in animal models to determine maximum tolerated dose and identify potential target organs of toxicity.
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| References |
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| Additional Infomation |
NN1177 TFA (NNC9204-1177 TFA) is a long-acting GLP-1/glucagon receptor co-agonist that induces dose-dependent body weight loss in diet-induced obese (DIO) mice. The compound is a peptide-based dual agonist that targets both the GLP-1 receptor and the glucagon receptor, making it a promising candidate for the treatment of obesity and metabolic disorders. NN1177 TFA is available as a research reagent for metabolic disease studies.
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| Molecular Formula |
C206H323N51O66.XC2HF3O2
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| Molecular Weight |
4570.07 (free base)
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O :~100 mg/mL (with sonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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