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| 5mg |
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Purity: ≥98%
WAY-262611 (WAY262611) is a novel agonist of the wingless β-Catenin pathway with the potential for the treatment of bone disorders. It increases bone formation rate with EC50 of 0.63 uM in TCF-Luciferase assay. WAY-262611 has excellent pharmacokinetic properties and showed a dose dependent increase in the trabecular bone formation rate in ovariectomized rats following oral administration. WAY-262611 acts via the Wnt β-catenin pathway and most likely through inhibition of Dkk-1. WAY-262611 has excellent pharmacokinetic properties and showed a dose dependent increase in the trabecular bone formation rate in ovariectomized rats following oral administration. WAY-262611 was discovered from a high-throughput screening (HTS) campaign to discover small molecule leads for the treatment of bone disorders concluded with the discovery of a compound with a 2-aminopyrimidine template that targeted the Wnt beta-catenin cellular messaging system. Hit-to-lead in vitro optimization for target activity and molecular properties led to the discovery of (1-(4-(naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine (5, WAY-262611).
| ln Vitro |
With its modest kinase inhibition potential, high solubility, and most powerful activity in the primary assay, WAY-262611 stands out[1].
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| ln Vivo |
After oral administration, WAY-262611 exhibits dose-dependent increase in the trabecular bone formation rate in ovariectomized rats and excellent pharmacokinetic properties. Calvariae from WAY-262611-treated wt mice exhibit statistically higher BFR, whereas similarly treated KO animals do not differ from the control group. This suggests that WAY-262611 is likely inhibiting Dkk-1 and acting through the Wnt β-catenin pathway[1].
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| Enzyme Assay |
WAY-262611 is a novel agonist of the wingless β-Catenin pathway that increases bone formation rate with EC50 of 0.63 uM in TCF-Luciferase assay. WAY-262611 has the most potent activity in the primary assay, low kinase inhibition potential, and high solubility.
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| Animal Protocol |
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| References |
[1]. Pelletier JC, et al. (1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate. J Med Chem. 2009 Nov 26;52(22):6962-5.
[2]. L Enochson, et al. GDF5 reduces MMP13 expression in human chondrocytes via DKK1 mediated canonical Wnt signaling inhibition. Osteoarthritis Cartilage. 2014 Apr;22(4):566-77 |
| Molecular Formula |
C20H22N4
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| Molecular Weight |
318.42
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| CAS # |
1123231-07-1
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| Related CAS # |
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| SMILES |
C1CN(CCC1CN)C2=NC=CC(=N2)C3=CC4=CC=CC=C4C=C3
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| InChi Key |
QHLITPHIARVDJI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H22N4/c21-14-15-8-11-24(12-9-15)20-22-10-7-19(23-20)18-6-5-16-3-1-2-4-17(16)13-18/h1-7,10,13,15H,8-9,11-12,14,21H2
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| Chemical Name |
[1-(4-naphthalen-2-ylpyrimidin-2-yl)piperidin-4-yl]methanamine
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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) |
DMSO: ~64 mg/mL ( 200.99 mM)
Water: <10 mg/mL Ethanol: <10 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (5.24 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 16.7 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: ≥ 1.67 mg/mL (5.24 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 16.7 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: ≥ 1.67 mg/mL (5.24 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 | 3.1405 mL | 15.7025 mL | 31.4051 mL | |
| 5 mM | 0.6281 mL | 3.1405 mL | 6.2810 mL | |
| 10 mM | 0.3141 mL | 1.5703 mL | 3.1405 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.
J Med Chem.2009 Nov 26;52(22):6962-5. |
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