Dulaglutide (LY2189265) (Synonyms: HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGG) |
| Katalog-Nr.GC31520 |
Dulaglutide (LY2189265) ist ein neuartiges, langwirkendes Glucagon-ähnliches Peptid 1 (GLP-1) Analogon zur Behandlung von Typ-2-Diabetes mellitus (T2DM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 923950-08-7
Sample solution is provided at 25 µL, 10mM.
Dulaglutide (LY2189265) ist ein neuartiges, langwirkendes Glucagon-ähnliches Peptid 1 (GLP-1) Analogon zur Behandlung von Typ-2-Diabetes mellitus (T2DM) [1].
Dulaglutide (LY2189265) reduzierte signifikant die hepatische Lipidakkumulation und verringerte die Expression von Genen, die mit Lipidtröpfchen-bindenden Proteinen, de novo Lipogenese und TG-Synthese in PA-behandelten HepG2-Zellen assoziiert sind. Dulaglutide (LY2189265) erhöhte auch die Expression von Proteinen, die mit Lipolyse und Fettsäureoxidation sowie FAM3A in PA-behandelten Zellen assoziiert sind[8]. Dulaglutide (LY2189265) förderte signifikant die Phagozytose von Mikroglia und die Beseitigung der Aβ-Plaques. Darüber hinaus hemmte die Dulaglutide (LY2189265)-Behandlung die Produktion von proinflammatorischen Faktoren, einschließlich Tumornekrosefaktor (TNF)-α, Interleukin-1β und IL-6, während die Menge an antiinflammatorischen Molekülen wie IL-10, die durch Aβ1-42-Exposition beeinflusst wurden, erhöht wurde[9].
Die Verabreichung von Dulaglutide (LY2189265) verringerte den Muskelschwund und stellte die Muskelkraft wieder her, indem sie die Entzündung durch den OPA-1-TLR-9-Signalweg in den Tibialis-anterior- (TA) und Quadrizepsmuskeln (QD) alter Mäuse reduzierte[3]. Dulaglutide (LY2189265) kann die Hyperandrogenämie bei PCOS-Ratten durch Regulierung des Serum-SHBG-Gehalts und der Expression von 3βHSD-, CYP19α1- und StAR-verwandten Genen und Proteinen reduzieren, wodurch die übermäßige Entwicklung kleiner Follikel und die Bildung von Zystenfollikeln in den Ovarien von PCOS-Ratten gehemmt und das polyzystische Ovar bei PCOS-Ratten verbessert wird[4]. Dulaglutide (LY2189265) verbessert die Lern- und Gedächtnisfähigkeit bei 9 Wochen alten männlichen Wildtyp-C57/BL6-Mäusen (AD-Mäusen)[2].
Nach subkutaner Injektion wurde Dulaglutide (LY2189265) langsam resorbiert und das tmax im Steady-State-Bereich lag zwischen 24 und 72 Stunden (Median = 48 Stunden) [5，6]. Die absolute Bioverfügbarkeit betrug 47 % und die Halbwertszeit wurde auf 4,7 Tage geschätzt. Der Steady-State wurde zwischen 2 und 4 Wochen der Dosierung erreicht und das Akkumulationsverhältnis betrug etwa 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.
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells were pretreated with 400 μM PA for 24 hours, followed by treatment with or without 100 nM Dulaglutide (LY2189265) for 24 hours. |
Reaction Conditions | 100 nM Dulaglutide (LY2189265) for 24 hours. |
Applications | 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. |
| Animal experiment [2]: | |
Animal models | Young (4 months) and old (24 months) C57BL/6J male mice |
Preparation Method | The mice were subcutaneously administered 600 μg/kg/week Dulaglutide (LY2189265) for 4 weeks. Body weight and food intake were assessed daily. The mice were weighed and humanely sacrificed after 4 weeks of treatment. |
Dosage form | 600 μg/kg/week Dulaglutide (LY2189265) for 4 weeks |
Applications | 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. |
References: | |
| Cas No. | 923950-08-7 | SDF | |
| Überlieferungen | HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGG | ||
| Formula | C149H221N37O49 | M.Wt | 3314.62 |
| Löslichkeit | > 40mg/mL in water | Storage | Store at -20°C |
| 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. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.3017 mL | 1.5085 mL | 3.0169 mL |
| 5 mM | 0.0603 mL | 0.3017 mL | 0.6034 mL |
| 10 mM | 0.0302 mL | 0.1508 mL | 0.3017 mL |
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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