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G8048

Sigma-Aldrich

GLP-1R agonist

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

Synonym(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
2 150,00 kr
25 MG
6 940,00 kr

2 150,00 kr

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5 MG
2 150,00 kr
25 MG
6 940,00 kr

About This Item

Empirical Formula (Hill Notation):
C13H15Cl2N3O2S
CAS Number:
281209-71-0
Molecular Weight:
348.25
MDL number:
MFCD11521508
UNSPSC Code:
12352200
NACRES:
NA.77

2 150,00 kr

Please contact Customer Service for Availability
Request a Bulk Order

Product Name

GLP-1R agonist, ≥98% (HPLC)

Quality Level

100

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

light brown-yellow

solubility

DMSO: ≥10 mg/mL

storage temp.

2-8°C

SMILES string

[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)

InChI key

GNZCSGYHILBXLL-UHFFFAOYSA-N

General description

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]

Biochem/physiol Actions

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000419815
0000419815
0000385216
0000385184
0000329364

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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)
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
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)
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)

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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