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346007

Glucagon-Like Peptide 1 Receptor Agonist II

Name: Glucagon-Like Peptide 1 Receptor Agonist II
Brand: MM

Sinónimos:

Glucagon-Like Peptide 1 Receptor Agonist II, 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine, Glucagon-Like Peptide 1 Receptor Agonist II, Compound B

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Fórmula empírica (notación de Hill):

C₂₀H₁₇F₃N₂O₂S

Número CAS:

1371569-69-5

Peso molecular:

406.42

MDL number:

MFCD23143626

UNSPSC Code:

51111800

NACRES:

NA.77

Assay:

>95% (HPLC)

Form:

solid

Storage condition:

OK to freeze, protect from light

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Propiedades

assay

>95% (HPLC)

Quality Segment

100

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

off-white

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

−20°C

SMILES string

FC(F)(F)c1nc(nc(c1)c2cc(ccc2)OCc3ccccc3)[S](=O)CC

InChI

1S/C20H17F3N2O2S/c1-2-28(26)19-24-17(12-18(25-19)20(21,22)23)15-9-6-10-16(11-15)27-13-14-7-4-3-5-8-14/h3-12H,2,13H2,1H3

InChI key

NTDFYGSSDDMNHI-UHFFFAOYSA-N

Descripción

General description

A pyrimidine small molecule that acts as a GLP-1 allosteric agonist that induces cAMP signaling in HEK293 cells expressing the GLP-1 receptor with EC₅₀ = 0.66 µM and 99% efficacy (similar data with rat GLP-1 receptor), does not compete with radiolabelled GLP-1 in receptor binding assays, and is not active in cells expressing the GLP-2, GIP, PTH, or glucagon receptors. In rodent islets, insulin secretion increases in a dose-dependent and glucose-dependent manner, either alone or in an additive fashion when combined with the endogenous GLP-1 peptide. In vivo, this molecule exhibits insulinotropic effects when dosed at 10mg/kg in SD rats undergoing an IVGTT and a hyperglycemic clamp. It is also shown to increase insulin secretion in perifusion assays involving normal and diabetic human islets ex vivo, at concentrations between 1 and 10 µM.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Sloop, KW., et al. 2010. Diabetes.59, 3099.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

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Este artículo	346003	371706	119135
Sigma-Aldrich 346007 Glucagon-Like Peptide 1 Receptor Agonist II	Sigma-Aldrich 346003 Glucagon Receptor Antagonist II	Sigma-Aldrich 371706 GPR40 Agonist	Sigma-Aldrich 119135 Adenosine A1 Receptor Agonist I, CPA
description -	description The Glucagon Receptor Antagonist II, also referenced under CAS 191034-25-0, controls the biological activity of Glucagon Receptor.	description The GPR40 Agonist, also referenced under CAS 885101-89-3, controls the biological activity of GPR40. This small molecule/inhibitor is primarily used for Cell Signaling applications.	description -
form solid	form solid	form solid	form solid
assay >95% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥99% (HPLC)
Quality Level 100	Quality Level 100	Quality Level 100	Quality Level 100
manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®
storage temp. −20°C	storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C
solubility DMSO: 100 mg/mL	solubility DMSO: 45 mg/mL, ethanol: 45 mg/mL	solubility DMSO: 40 mg/mL	solubility 1 M HCl: 100 mM, DMSO: 100 mM, ethanol: 25 mM

Clase de almacenamiento

11 - Combustible Solids

¿Qué está pasando?

WGK 3

Punto de inflamación (°F)

Not applicable

Punto de inflamación (°C)

Not applicable

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