الصفحة الرئيسية>>Dulaglutide (LY2189265)

Dulaglutide (LY2189265) (Synonyms: HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGG)

رقم الكتالوجGC31520

دولاغلوتايد (LY-2189265) هو مشتق جديد لهرمون الببتيد المشابه للجلوكاجون 1 (GLP-1) ذات فعالية طويلة، وذلك لعلاج مرض السكري من النمط 2.

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Dulaglutide (LY2189265) التركيب الكيميائي

Cas No.: 923950-08-7

الحجم السعر المخزون الكميّة
1mg
180٫00
متوفر
5mg
565٫00
متوفر
10mg
900٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

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:

[1]. 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.

[2]. 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.

Background

دولاغلوتايد (LY-2189265) هو مشتق جديد لهرمون الببتيد المشابه للجلوكاجون 1 (GLP-1) ذات فعالية طويلة، وذلك لعلاج مرض السكري من النمط 2.

أدى دولاغلوتيد (LY2189265) إلى تقليل تراكم الدهون في الكبد وخفض تعبير الجينات المرتبطة ببروتينات ربط قطرات الدهون، والليبوجينيس التحديثية، وتخلص TG في خلايا HepG2 المعالجة بـ PA. كما زاد دولاغلوتيد (LY2189265) من تعبير البروتينات المرتبطة بالشحمية وأكسدة حمض الدهني و FAM3A في خلايا معالجة PA[8]. أظهر استخدام دولاغلوتاز (LY2189265) زيادة كفاءة ما يسمى "microglia" لابتلاع صفائح Aβ. علاوة على ذلك، أثَّرَ استخدام دولاغلُّودِّ( LY2189265 ) على منع إِصْدارُ عُامِّلَ التهابٍ مثْل TNF-α, interleukin -1β, and IL-6، فضلاً عن زِیادَۃ نسْبَۃ جزیئات مضادَّۃ لِإِصابَۃ التهابیَّۃ مثل IL-10 المتأثرة بالتعرض لـ Aβ1-42[9].

أدت إعطاء دولاغلوتيد (LY2189265) إلى تقليل هدم العضلات واستعادة قوة العضلات عن طريق تخفيف الالتهاب من خلال مسار التوصيل بين OPA-1-TLR-9 في عضلات tibialis anterior (TA) وquadriceps (QD) لفئران المسنَّة[3]. يمكن أن يُخفِّض دولاغلوتيد (LY2189265) فرط هرمون الذكورة في فئران متلازمة تكيس المبايض PCOS من خلال ضبط محتوى SHBG في المصل وتعبير جينات 3βHSD، CYP19α1، StAR ذات الصِِّــــــغَية، وبروتينها، مثمِّلا بذلك التحكم في التطور المفرط لجُرْثُـــُ­‌‌‌‌�َى صغيرة وظهور جُرْثُ­کیستية في المبايض لديها، حاملا بذلك على تحسین حالة تكیس المبایض PCOS لديها[4]. يحسِّن دولاغلوتيد (LY2189265) القدرة على التعلم والذاكرة لفئران C57/BL6 ذات النوعية البرية من الذكور في سن 9 أسابيع (AD mice)[2].

بعد الحقن تحت الجلد، تم امتصاص Dulaglutide (LY2189265) ببطء وكان tmax في الحالة المستقرة يتراوح بين 24 إلى 72 ساعة (الوسيط = 48 ساعة). كانت نسبة الامتصاص الحيوي المطلق هي 47٪ وقُدِّر نصف العمر على أنه 4.7 يومًا. تم التوصل إلى حالة مستقرة بين 2 و4 أسابيع من جرعات التخدير ، وكان معدل التراكم حوالي 1.56.

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.

Chemical Properties

Cas No. 923950-08-7 SDF
المرادفات HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGG
Formula C149H221N37O49 M.Wt 3314.62
الذوبان > 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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