| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
GSK1292263 is a novel and potent GPR119 (G-protein-coupled receptor 119) agonist which has potential for the treatment of type 2 diabetes. It is currently undergoing phase 2 clinical trial for type 2 diabetes. GSK1292263 improves glucose regulation in animal models of diabetes, but has no effect on plasma glucose in type 2 diabetics. GSK1292263 treatment displayed little inhibition towards CYPs (CYP1A2, 2C9, 2C19, 2D6, 3A4), p-GP, OATP1B3, or OCT2. However, GSK1292263 inhibited BCRP and OATP1B1, which are transporters involved in statin disposition 1.
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| ln Vivo |
In type 2 diabetic rats, GSK1292263 increases glucose-dependent insulin production, upregulates glucagon-like peptide-1, and promotes glucose homeostasis[2].
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| Animal Protocol |
Animal/Disease Models: Male neonatal Streptozotocin (STZ)-induced SD rats (7 weeks of age)[2]
Doses: 30 mg/kg Route of Administration: Orally given; one time/day for 2 weeks Experimental Results: The AUC of plasma glucose (AUCPG) in the single treatment of the GSK1292263 group was numerically lower than that of the vehicle group, but the effect was modest . |
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| References |
[1]. X. Zhu, et al. GPR119 Agonists: A Novel Strategy for Type 2 Diabetes Treatment.
[2]. Koji Matsumoto, et al. DS-8500a, an Orally Available G Protein-Coupled Receptor 119 Agonist, Upregulates Glucagon-Like Peptide-1 and Enhances Glucose-Dependent Insulin Secretion and Improves Glucose Homeostasis in Type 2 Diabetic Rats. J Pharmacol Exp The |
| Molecular Formula |
C23H28N4O4S
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| Molecular Weight |
456.56
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| CAS # |
1032823-75-8
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| Related CAS # |
1032823-75-8;1032824-54-6 (HCl);
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| SMILES |
S(C([H])([H])[H])(C1C([H])=C([H])C(=C([H])C=1[H])C1C([H])=C([H])C(=C([H])N=1)OC([H])([H])C1([H])C([H])([H])C([H])([H])N(C2=NC(C([H])(C([H])([H])[H])C([H])([H])[H])=NO2)C([H])([H])C1([H])[H])(=O)=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (4.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 30% Propylene glycol , 5% Tween 80 , 65% D5W: 30 mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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