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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
APD597 (formerly known as JNJ-38431055) is a novel potent and selective GPR119 agonist/modulator, which has the potential for the treatment of type 2 diabetes. Glucagon like peptide-1 (GLP-1) is essential for maintaining β-cell function and maintaining glucose homeostasis. Nowadays, dipeptidyl peptidase-4 (DPP4) inhibition and G protein-coupled receptor 119 (GPR119) activation are the two main strategies for increasing endogenous GLP-1 activity. The EC50 for hGPR119 in APD597 is 46 nM. A unique nutrient-dependent dual elevation of insulin and glucagon like peptide 1/glucose-dependent insulinotropic peptide levels is mediated in vivo by GPR119 agonists. For preclinical development, PD597 was chosen due to its good solubility, lower potential for drug-drug interactions, and agonist potency that was well-balanced with intrinsic activity.
| Targets |
hGPR119 ( EC50 = 46 nM ); CYP2C9 ( IC50 = 5.8 μM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
APD597 is a GPR119 agonist with an EC50 of 46 nM for hGPR119 that is used to treat type 2 diabetes.
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| Cell Assay |
The GPR119 modulators 5-fluoro-4,6-dialkoxypyrimidine were identified and refined for in vitro agonist activity. A novel lead compound with lower CYP2C9 inhibitory potential and better agonist efficacy than our clinical compound (APD597) has been found. It was discovered that this improved lead worked well both by itself and in conjunction with a Dipeptidyl peptidase-4 (DPP-4) inhibitor in rodent models of glucose regulation.
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| Animal Protocol |
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| References |
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| Molecular Formula |
C₂₁H₂₉N₅O₆S
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| Molecular Weight |
479.55
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| Exact Mass |
479.18
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| Elemental Analysis |
C, 52.60; H, 6.10; N, 14.60; O, 20.02; S, 6.69
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| CAS # |
897732-93-3
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CC1=C(C=CC(=N1)S(=O)(=O)C)NC2=C(C(=NC=N2)OC3CCN(CC3)C(=O)OC(C)C)OC
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| InChi Key |
WPDCHTSXOPUOII-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H29N5O6S/c1-13(2)31-21(27)26-10-8-15(9-11-26)32-20-18(30-4)19(22-12-23-20)25-16-6-7-17(24-14(16)3)33(5,28)29/h6-7,12-13,15H,8-11H2,1-5H3,(H,22,23,25)
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| Chemical Name |
propan-2-yl 4-[5-methoxy-6-[(2-methyl-6-methylsulfonylpyridin-3-yl)amino]pyrimidin-4-yl]oxypiperidine-1-carboxylate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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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: ≥ 2.5 mg/mL (5.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0853 mL | 10.4264 mL | 20.8529 mL | |
| 5 mM | 0.4171 mL | 2.0853 mL | 4.1706 mL | |
| 10 mM | 0.2085 mL | 1.0426 mL | 2.0853 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.
 HBK001 activates GPR119 and induces insulin secretionex vivoand incretins releasein vivo.Sci Rep. 2017; 7: 4351. |
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