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Dulaglutide

Names

[ CAS No. ]:
923950-08-7

[ Name ]:
Dulaglutide

[Synonym ]:
Imidazo[1,2-a]pyridin-3-amine, N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-(2-furanyl)-
N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-2-(2-furyl)imidazo[1,2-a]pyridin-3-amine

Biological Activity

[Description]:

Dulaglutide (LY2189265) is a glucagon-like peptide-1 (GLP-1) receptor agonist. Sequence: His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Glu-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Gly-Gly;HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGG.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Glucagon Receptor
Research Areas >> Metabolic Disease
Peptides

[Target]

GLP-1 receptor[1]


[In Vivo]

Dulaglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist. No specific Dulaglutide-related cause of death is identified. Survival is numerically increased for both genders of animals in all Dulaglutide treatment groups and reaches statistical significance (P≤0.05) in the 0.5- and 5-mg/kg males and in the 0.05-, 0.5-, and 1.5-mg/kg females. Mean times to peak plasma concentration values of Dulaglutide are observed at 12 hours after dosing on day 1 and rang between 12 and 48 hours at week 52. The incidence of thyroid C-cell adenoma is significantly (P≤0.05) increased compare with controls in males and females at the Dulaglutide 0.5-, 1.5-, and 5-mg/kg doses[1].

[Animal admin]

The tumorigenic potential of Dulaglutide is evaluated in rats and transgenic mice. Rats are injected sc twice weekly for 93 weeks with Dulaglutide 0, 0.05, 0.5, 1.5, or 5 mg/kg corresponding to 0, 0.5, 7, 20, and 58 times, respectively. Transgenic mice are dosed sc twice weekly with Dulaglutide 0, 0.3, 1, or 3 mg/kg for 26 weeks[1].

[References]

[1]. Byrd RA, et al. Chronic Toxicity and Carcinogenicity Studies of the Long-Acting GLP-1 Receptor AgonistDulaglutide in Rodents. Endocrinology. 2015 Jul;156(7):2417-28.


[Related Small Molecules]

Exenatide acetate salt | Adomeglivant | Exendin Fragment 9-39 | MK 0893 | GLP-1(7-36) Acetate | GLP-1 (7-37) | Lixisenatide | LGD-6972 | Taspoglutide | GRA Ex-25 | GLP-1 receptor agonist 1 | GLP-1 receptor agonist-1

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C149H221N37O49

[ Molecular Weight ]:
3314.62

[ LogP ]:
3.81

[ Index of Refraction ]:
1.706

[ Storage condition ]:
-20°C


Related Compounds