Dulaglutide (LY2189265) (Synonyms: HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGG) |
| Catalog No.GC31520 |
Dulaglutide (LY-2189265) is a novel, long-acting glucagon-like peptide 1 (GLP-1) analog for the treatment of type 2 diabetes mellitus (T2DM).
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Cas No.: 923950-08-7
Sample solution is provided at 25 µL, 10mM.
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Dulaglutide (LY-2189265) is a novel, long-acting glucagon-like peptide 1 (GLP-1) analog for the treatment of type 2 diabetes mellitus (T2DM) [1].
Dulaglutide (LY2189265) significantly decreased hepatic lipid accumulation and reduced the expression of genes associated with lipid droplet binding proteins, de novo lipogenesis, and TG synthesis in PA-treated HepG2 cells. Dulaglutide (LY2189265) also increased the expression of proteins associated with lipolysis and fatty acid oxidation and FAM3A in PA-treated cells[8].Dulaglutide (LY2189265) significantly promoted microglia to phagocytose and get rid of the Aβ plague. Additionally, Dulaglutide (LY2189265) treatment inhibited the production of pro-inflammatory factors, including tumor necrosis factor (TNF)-α, interleukin -1β, and IL-6, whereas increased the load of anti-inflammatory molecules such as IL-10 affected by Aβ1-42 exposure[9].
Dulaglutide (LY2189265) administration attenuated muscle wasting and restored muscle strength by reducing inflammation through the OPA-1-TLR-9 signaling pathway in the tibialis anterior (TA) and quadriceps (QD) muscles of aged mice[3]. Dulaglutide (LY2189265) may reduce the hyperandrogenemia of PCOS rats by regulating the content of serum SHBG and the expression of 3βHSD, CYP19α1, and StAR related genes and proteins, thereby inhibiting the excessive development of small follicles and the formation of cystic follicles in the ovaries of PCOS rats, thereby improving polycystic ovary in PCOS rats[4]. Dulaglutide (LY2189265) improves learning and memory ability in 9-week-old male wild-type C57/BL6 mice (AD mice)[2].
After subcutaneous injection, Dulaglutide (LY2189265) was slowly absorbed and tmax at steady state ranged from 24 to 72 h (median = 48 h) [5，6]. The absolute bioavailability was 47% and the half-life was estimated at 4.7 days. Steady state was achieved between 2 and 4 weeks of dosing and the accumulation ratio was approximately 1.56[7].
References:
[1]:Jimenez-Solem E, Rasmussen MH, et,al. Dulaglutide, a long-acting GLP-1 analog fused with an Fc antibody fragment for the potential treatment of type 2 diabetes. Curr Opin Mol Ther. 2010 Dec;12(6):790-7. PMID: 21154170.
[2]: Jiang Guo-Jing, ZHOU Mei, et,al. Protective effects of dura glycopeptide on learning and memory loss and synaptic degeneration in AD mice [J]. Medical theory & practice,2021,34(14):2365-2368.
[3]: Khin PP, Hong Y, et,al. Dulaglutide improves muscle function by attenuating inflammation through OPA-1-TLR-9 signaling in aged mice. Aging (Albany NY). 2021 Sep 19;13(18):21962-21974. doi: 10.18632/aging.203546. Epub 2021 Sep 19. PMID: 34537761; PMCID: PMC8507261.
[4]: Wu LM, Wang YX, et,al. Dulaglutide, a long-acting GLP-1 receptor agonist, can improve hyperandrogenemia and ovarian function in DHEA-induced PCOS rats. Peptides. 2021 Nov;145:170624. doi: 10.1016/j.peptides.2021.170624. Epub 2021 Aug 8. PMID: 34375684.
[5]: Barrington P, Chien JY, et,al. A 5-week study of the pharmacokinetics and pharmacodynamics of LY2189265, a novel, long-acting glucagon-like peptide-1 analogue, in patients with type 2 diabetes. Diabetes Obes Metab. 2011 May;13(5):426-33. doi: 10.1111/j.1463-1326.2011.01364.x. Epub 2011 Jan 19. PMID: 21251178.
[6]: Barrington P, Chien JY, et,al. LY2189265, a long-acting glucagon-like peptide-1 analogue, showed a dose-dependent effect on insulin secretion in healthy subjects. Diabetes Obes Metab. 2011 May;13(5):434-8. doi: 10.1111/j.1463-1326.2011.01365.x. Epub 2011 Jan 19. PMID: 21251179.
[7]: Scheen AJ. Dulaglutide (LY-2189265) for the treatment of type 2 diabetes. Expert Rev Clin Pharmacol. 2016;9(3):385-99. doi: 10.1586/17512433.2016.1141046. Epub 2016 Feb 6. PMID: 26761217.
[8]: Lee J, Hong SW, et,al. Dulaglutide Ameliorates Palmitic Acid-Induced Hepatic Steatosis by Activating FAM3A Signaling Pathway. Endocrinol Metab (Seoul). 2022 Feb;37(1):74-83. doi: 10.3803/EnM.2021.1293. Epub 2022 Feb 9. PMID: 35144334; PMCID: PMC8901965.
[9]: Wang Y, Han B. Dulaglutide Alleviates Alzheimer's Disease by Regulating Microglial Polarization and Neurogenic Activity. Comb Chem High Throughput Screen. 2022 Jul 26. doi: 10.2174/1386207325666220726163514. Epub ahead of print. PMID: 35894460.
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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