Size | Price | Stock | Qty |
---|---|---|---|
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
Other Sizes |
|
Purity: ≥98%
ln Vitro |
There is a brief rise in CREB phosphorylation caused by D159687 (1 μM, 0-24 hours), which peaks 6 hours after treatment [1]. A CREB phosphorylation of 1 μM is produced by D159687 (0.01-1 μM, 6 hours) [1].
|
---|---|
ln Vivo |
In female cynomolgus monkeys, D159687 (0.05–5 mg/kg; administered orally daily for one week) has been demonstrated to potentially recruit or enhance synapse function and raise task difficulty [2].
|
Cell Assay |
Western Blot Analysis[1]
Cell Types: HT-22 (mouse hippocampal cell line) Tested Concentrations: 1 μM Incubation Duration: 0, 1, 3, 6, 12, 24 hrs (hours) Experimental Results: Induced a transient increase in CREB phosphorylation at 6 hrs (hours) Peak treatment is achieved several hrs (hours) after treatment. Western Blot Analysis[1] Cell Types: HT-22 (mouse hippocampal cell line) Tested Concentrations: 0.01 μM, 0.1 μM, 1 μM Incubation Duration: 6 hrs (hours) Experimental Results: CREB phosphorylation is optimal at 1 μM. |
Animal Protocol |
Animal/Disease Models: Female cynomolgus monkey (4-6 years old) [2]
Doses: 0.05, 0.5, 5 mg/kg Route of Administration: Orally daily for one week Experimental Results: Synaptic function may be recruited as task difficulty increases or enhance. |
References |
[1]. Zhang C, et al. Comparison of the Pharmacological Profiles of Selective PDE4B and PDE4D Inhibitors in the Central Nervous System. Sci Rep. 2017 Jan 5;7:40115.
|
Molecular Formula |
C21H19CLN2O2
|
---|---|
Molecular Weight |
366.84
|
Exact Mass |
366.1135
|
CAS # |
1155877-97-6
|
Related CAS # |
1155877-97-6
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
O=C(N)NC1=CC=C(CC2=CC=C(OC)C(C3=CC=CC(Cl)=C3)=C2)C=C1
|
InChi Key |
RJJLUTWHJUDZFP-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C21H19ClN2O2/c1-26-20-10-7-15(12-19(20)16-3-2-4-17(22)13-16)11-14-5-8-18(9-6-14)24-21(23)25/h2-10,12-13H,11H2,1H3,(H3,23,24,25)
|
Chemical Name |
[4-[[3-(3-Chlorophenyl)-4-methoxyphenyl]methyl]phenyl]urea
|
Synonyms |
D159687 D-159687 D 159687
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : ~150 mg/mL (~408.90 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.81 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 (6.81 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 (6.81 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 | 2.7260 mL | 13.6299 mL | 27.2598 mL | |
5 mM | 0.5452 mL | 2.7260 mL | 5.4520 mL | |
10 mM | 0.2726 mL | 1.3630 mL | 2.7260 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.
Time- and concentration-dependency of A-33 and D159687 in inducing phosphorylation of CREB. (a) HT-22 cells were treated with A-33 (1 μM) for 0, 1, 3, 6, 12 and 24 hours before sample collection. (b) HT-22 cells were treated with various concentrations of A-33 and incubated for 12 hours before sample collection. (c) HT-22 cells were treated with D159687 (1 μM) for 0, 1, 3, 6, 12 and 24 hours before sample collection. (d) HT-22 cells were treated with various concentrations of D159687 for 6 hours before sample collection. Results are expressed as mean ± SEM (n = 6). *P < 0.05 and **P < 0.01 vs. vehicle treated group.[1].Sci Rep. 2017 Jan 5;7:40115. td> |
Evaluation of antidepressant-like effects of A-33 and D159687 on mice. (a) Mice were treated with vehicle, A-33, D159687, rolipram or desipramine 30 min before subjected to the FST. (b) Mice were treated with vehicle, A-33, D159687 rolipram or desipramine 30 min before subjected to the TST. (c) Mice were treated with various doses of A-33 and D159687 30 min before the locomotor activity test. (d) Mice were treated with vehicle or A-33 (0.3 mg/kg) for 7 days and subjected to the NSF 30 min after the last treatment. Results are expressed as mean ± SEM (n = 10–12). *P < 0.05 and **P < 0.01 vs. vehicle treated group.[1].Sci Rep. 2017 Jan 5;7:40115. td> |
Evaluation of anxiolytic-like effects of A-33 and D159687 on mice. (a and b) Mice were treated with vehicle, A-33, D159687 or diazepam 30 min before subjected to the EPM. (c) Mice were treated with vehicle, A-33, D159687 or diazepam 30 min before subjected to the MBT. Results are expressed as mean ± SEM (n = 10–12). *P < 0.01 vs. vehicle treated group.[1].Sci Rep. 2017 Jan 5;7:40115. td> |