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Principaux documents

G8048

Sigma-Aldrich

GLP-1R agonist

≥98% (HPLC), powder, glucose homeostasis regulator

Synonyme(s) :

2-Quinoxalinamine, 6,7-dichloro-N-(1,1-dimethylethyl)-3-(methylsulfonyl)-, 6,7-dichloro-2-methylsulfonyl-3-N-tert-butylaminoquinoxaline (DMB), Compound 2

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5 MG
282,00 $
25 MG
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About This Item

Formule empirique (notation de Hill) :
C13H15Cl2N3O2S
Numéro CAS:
281209-71-0
Poids moléculaire :
348.25
Numéro MDL:
MFCD11521508
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

282,00 $

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Nom du produit

GLP-1R agonist, ≥98% (HPLC)

Essai

≥98% (HPLC)

Forme

powder

Conditions de stockage

desiccated

Couleur

light brown-yellow

Solubilité

DMSO: ≥10 mg/mL

Température de stockage

2-8°C

Chaîne SMILES 

[S](=O)(=O)(C)c1nc2c(nc1NC(C)(C)C)cc(c(c2)Cl)Cl

InChI

1S/C13H15Cl2N3O2S/c1-13(2,3)18-11-12(21(4,19)20)17-10-6-8(15)7(14)5-9(10)16-11/h5-6H,1-4H3,(H,16,18)

Clé InChI

GNZCSGYHILBXLL-UHFFFAOYSA-N

Description générale

Glucagon-like peptide-1 receptor (GLP-1R) agonist is a potential oral drug for modulating glucagon-like peptide (GLP)-1 in diabetic patients.[1] GLP-1R agonists play a key role in lowering glycated hemoglobin levels.[2] It improves glycemic control and maintenance of body weight.[3]

Actions biochimiques/physiologiques

GLP-1R is a small molecule GLP-1 receptor agonist.
GLP-1R is a small molecule GLP-1 receptor agonist. GLP-1 receptor signaling is a predominant mechanism for regulating glucose homeostasis. This compound represents a unique non-peptide tool for studying the role of GLP-1 in both in vivo and in vitro diabetes and obesity models.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Certificats d'analyse (COA)

Lot/Batch Number
0000419815
0000419815
0000385216
0000385184
0000329364

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Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

Juliana de F Germano et al.
Scientific reports, 10(1), 8284-8284 (2020-05-20)
Given that adverse remodeling is the leading cause of heart failure and death in the USA, there is an urgent unmet need to develop new methods in dealing with this devastating disease. Here we evaluated the efficacy of a short-course
GLP-1 receptor agonists: a review of head-to-head clinical studies.
Trujillo JM, et al.
Therapeutic advances in endocrinology and metabolism, 6(1), 19-28 (2015)
Juliana de Freitas Germano et al.
International journal of molecular sciences, 22(16) (2021-08-28)
Cardiovascular disease is the main cause of death worldwide, making it crucial to search for new therapies to mitigate major adverse cardiac events (MACEs) after a cardiac ischemic episode. Drugs in the class of the glucagon-like peptide-1 receptor agonists (GLP1Ra)
Small-molecule agonists for the glucagon-like peptide 1 receptor.
Knudsen LB, et al.
Proceedings of the National Academy of Sciences of the USA, 104(3), 937-942 (2007)
Long-acting glucagon-like peptide 1 receptor agonists: a review of their efficacy and tolerability.
Garber AJ.
Diabetes Care, 34(Supplement 2), S279-S284 (2011)

Questions

1–3 of 3 Questions  

  1. Is it possible to resuspend the aginist in DMSO and then dilute it in PBS without causing precipitation or affecting its solubility, with the goal of injecting it into a murine ?model

    1 answer

    1. This product has not been studied in-house for in vivo applications. Please refer to published literature for relevant citations regarding its use in murine models.

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  2. What is the mechanism of action for this compound? Additionally, is the structural information available for this compound?

    What is the mechanism of action for this compound? Additionally, is the structural information available for this compound?

    1 answer

    1. The compound known as compound 2 was discovered through functional screening, demonstrating that it enhances the binding of GLP-1 to the receptor rather than competing with it. It functions as an ago-allosteric modulator, acting as both an agonist and an allosteric modulator. This compound is specific to the GLP-1 receptor and induces insulin release from wild-type mouse islets, as detailed in a specific article. For information on the structure of compound 2, please refer to Figure 2 in the publication "Proc Natl Acad Sci U S A. 2007 Jan 16; 104(3): 937–942." The PMID for the article is 17213325, and it can be accessed at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1783418/.

      Helpful?

  3. What is the molecular weight of GLP1 agonist 8048 in grams ?

    1 answer

    1. The molecular weight of this product is 348.25. This value can be interpreted in units of daltons or grams per mole.

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