Insulin efsitora alfa
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 98.70%
- CAS No.: 2131038-11-2
- Molecular Weight:64.1 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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INS (insulin, IDDM1, IDDM2, "insulin-dependent diabetes mellitus 2")-IGHG2 Fc (Fragment constant)
ELISA, FACS, Functional assay
Chemical Information
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CAS No. 2131038-11-2
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Appearance Liquid
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Molecular Weight 64.1 kDa
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Color Colorless to light yellow
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SMILES
[Insulin efsitora alfa]
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Synonyms
LY-3209590
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Shipping
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (257 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)