[CAS NO. 1032823-75-8]  GSK1292263

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PRODUCTS SPECIFICATIONS [1032823-75-8]

Catalog
HY-12066
Brand
MCE
CAS
1032823-75-8

DESCRIPTION [1032823-75-8]

Overview

MDLMFCD18385004
Molecular Weight456.56
Molecular FormulaC23H28N4O4S
SMILESCC(C1=NOC(N2CCC(CC2)COC3=CN=C(C=C3)C4=CC=C(C=C4)S(C)(=O)=O)=N1)C

For research use only. We do not sell to patients.


Summary

GSK-1292263 is an orally available GPR119 agonist with pEC 50 s of 6.9 and 6.7 for human and rat GPR119 , respectively. GSK-1292263 can be used for the research of type 2 diabetes mellitus (T2DM) [1] .


In Vivo

GSK1292263 upregulates glucagon-like peptide-1 and enhances glucose-dependent insulin secretion and improves glucose homeostasis in type 2 diabetic rats [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male neonatal Streptozotocin (STZ)-induced SD rats (7 weeks of age) [2]
Dosage: 30 mg/kg
Administration: Orally given; once a day for 2 weeks
Result: The AUC of plasma glucose (AUC PG ) in the single treatment of the GSK1292263 group was numerically lower than that of the vehicle group, but the effect was modest.

Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT01128621 GlaxoSmithKline
Diabetes Mellitus, Type 2
November 23, 2009 Phase 2
NCT01218204 GlaxoSmithKline
Dyslipidaemias|Dyslipidemias
September 14, 2010 Phase 2
NCT01119846 GlaxoSmithKline
Diabetes Mellitus, Type 2
June 5, 2009 Phase 2

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 20 mg/mL ( 43.81 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1903 mL 10.9515 mL 21.9029 mL
5 mM 0.4381 mL 2.1903 mL 4.3806 mL
10 mM 0.2190 mL 1.0951 mL 2.1903 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2 mg/mL (4.38 mM); Clear solution

* All of the co-solvents are available by MCE.