| Size | Price | Stock | Qty |
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| 500μg |
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| 1mg |
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| Other Sizes |
| Targets |
Insulin efsitora alfa targets the insulin receptor (IR), a receptor tyrosine kinase. As a selective IR agonist, it binds to the receptor and activates its intrinsic tyrosine kinase activity, initiating downstream signaling cascades such as the PI3K-Akt and MAPK pathways. This activation promotes glucose uptake, glycogen synthesis, and lipogenesis, thereby regulating glucose homeostasis. Its selectivity for IR over other receptors is a key feature of its mechanism.
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| ln Vitro |
With EC50 values of 4241 nM and 4241 nM, respectively, insulin efsitora alfa (0.01-100 nM) stimulates the phosphorylation of human insulin receptor isotype A (hIR-A) and human insulin receptor subtype B (hIR-B) in HEK293 cells. 391 nanometers [2]. Significantly, insulin efsitora alfa (20 µM; 30 min) increases hIR-A and hIR-B dephosphorylation [2]. With EC50 values of 19 nM, 134 nM, and 20 nM, respectively, insulin efsitora alfa stimulates lipogenesis in 3T3-L1 adipocytes and proliferation of SAOS-2 and H4IIE cells [2].
In vitro, Insulin efsitora alfa exhibits potent agonistic activity at the insulin receptor, with EC50 values of 19 nM, 134 nM, and 20 nM respectively. Its activity is typically assessed using cell-based assays that measure receptor phosphorylation, glucose uptake, and downstream signaling in IR-expressing cell lines. These studies confirm its efficacy in activating insulin signaling pathways. |
| ln Vivo |
In diabetic rats treated with streptozotocin (HY-13753), insulin efsitora alfa (3, 10 and 30 nmol/kg; subcutaneous injection; single dose) dramatically lowered blood glucose levels [2].
In vivo, Insulin efsitora alfa is being developed as a once-weekly treatment for diabetes. Its long-acting profile is attributed to its fusion to the IgG2 Fc domain, which extends its half-life. Studies in animal models of diabetes have demonstrated its efficacy in lowering blood glucose levels and improving glycemic control. Its favorable pharmacokinetic and pharmacodynamic properties support its clinical development. |
| Enzyme Assay |
Cell-free assays for Insulin efsitora alfa typically involve measuring its binding affinity to the insulin receptor using surface plasmon resonance (SPR) or enzyme-linked immunosorbent assay (ELISA). These assays are used to characterize the potency and specificity of the fusion protein. Additionally, the compound's purity and integrity are assessed using SDS-PAGE and size-exclusion chromatography.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of Insulin efsitora alfa. Cells expressing the insulin receptor are treated with the fusion protein, and receptor phosphorylation is measured to assess its agonistic activity. Downstream signaling events, such as Akt phosphorylation, are also assessed. Glucose uptake assays are used to measure the compound's metabolic effects. These assays confirm that Insulin efsitora alfa effectively activates insulin signaling.
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| Animal Protocol |
In vivo animal experiments typically involve administering Insulin efsitora alfa to rodent models of diabetes, such as diet-induced obese mice or streptozotocin-induced diabetic mice. The compound is usually administered via subcutaneous injection. Blood glucose levels are monitored over time to assess its glucose-lowering efficacy and duration of action. Pharmacokinetic studies are conducted to measure plasma concentrations of the fusion protein.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Insulin efsitora alfa are characterized by its long half-life, which supports once-weekly dosing. The fusion to the IgG2 Fc domain extends its circulation time by facilitating neonatal Fc receptor (FcRn)-mediated recycling. Its molecular weight of 64.1 kDa and its design as a fusion protein contribute to its favorable pharmacokinetic profile, including good bioavailability and sustained exposure.
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| Toxicity/Toxicokinetics |
The toxicity profile of Insulin efsitora alfa is generally favorable, with adverse events typically related to its mechanism of action as an insulin receptor agonist. Common side effects may include hypoglycemia, injection site reactions, and weight gain. In preclinical studies, the compound has been shown to be well-tolerated, with a safety profile that supports its clinical development.
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| References |
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| Additional Infomation |
Insulin efsitora alfa (LY-3209590) is a novel insulin analog in clinical development for the treatment of type 2 diabetes. It is a selective insulin receptor agonist and a fusion protein. Its once-weekly dosing regimen offers a potential advantage over conventional daily insulin therapies, improving patient convenience and adherence. It is currently being investigated in clinical trials.
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| CAS # |
2131038-11-2
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| Appearance |
Colorless to light yellow liquid
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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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