Insulin efsitora alfa (Synonyms: LY-3209590) |
Catalog No.GC74561
One-Click Copy Product Info
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Insulin efsitora alfa (LY-3209590) is a selective agonist of insulin receptor (IR).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2131038-11-2
Sample solution is provided at 25 µL, 10mM.
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Insulin efsitora alfa (LY-3209590) is a selective agonist of insulin receptor (IR). Insulin efsitora alfa is a fusion protein composed of human IR agonists fused with the crystallizable (Fc) domain of human immunoglobulin G2 (IgG2) fragment, with a molecular weight of 64.1 kDa. Insulin efsitora alfa is well tolerated and has potential applications in diabetes.
Insulin efsitora alfa (0.01-100 nM) stimulates human insulin receptor isoform A (hIR-A) and human insulin receptor isoform B (hIR-B) phosphorylation in HEK293 cells with EC50 values of 4241 nM and 391 nM, respectively[2].Insulin efsitora alfa (20 µM; 30 min) significantly promotes the dephosphorylation of hIR-A and hIR-B[2].Insulin efsitora alfa stimulates the lipogenesis of 3T3-L1 adipocytes and the proliferation of SAOS-2 and H4IIE cells with EC50 values of 19 nM, 134 nM and 20 nM, respectively[2].
Insulin efsitora alfa (3, 10 and 30 nmol/kg; s.c.; single dose) significantly reduces blood glucose in diabetes rats treated with Streptozotocin [2].
References:
[1]. Heise T, et al. Pharmacokinetic and pharmacodynamic properties of the novel basal insulin Fc (insulin efsitora alfa), an insulin fusion protein in development for once-weekly dosing for the treatment of patients with diabetes. Diabetes Obes Metab. 2023 Apr;25(4):1080-1090.
[2]. Moyers JS, et al. Preclinical Characterization of LY3209590, a Novel Weekly Basal Insulin Fc-Fusion Protein. J Pharmacol Exp Ther. 2022 Sep;382(3):346-355.
| Cas No. | 2131038-11-2 | SDF | |
| Synonyms | LY-3209590 | ||
| Formula | M.Wt | ||
| Solubility | Storage | ||
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A liquid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)