| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg | |||
| Other Sizes |
| Targets |
PDE9[1]
|
|---|---|
| ln Vitro |
An oral, specific, and potent inhibitor of phosphodiesterase 9 (PDE 9) is irsenontrine (E2027)[3].
|
| ln Vivo |
In rats given Scopolamine, irsenontrine (0.3, 3.3 mg/kg; po) significantly reduces the proportion of the rats' investigation of the new object[1]. The combined treatment group of memantine hydrochloride (1 mg/kg; po) and irsenontrine (1 mg/kg; po) shows a considerably higher percentage of novel object exploration than memantine hydrochloride (1 mg/kg) alone[1].
|
| References | |
| Additional Infomation |
Irsenontrine is being studied in the clinical trial NCT03467152 (a study evaluating the efficacy, safety and tolerability of E2027 (hereinafter referred to as Irsenontrine) in patients with Lewy body dementia).
|
| Molecular Formula |
C22H22N4O3
|
|---|---|
| Molecular Weight |
390.435084819794
|
| Exact Mass |
390.169
|
| CAS # |
1429509-82-9
|
| Related CAS # |
(R)-Irsenontrine;1429509-81-8;Irsenontrine maleate;1630083-70-3
|
| PubChem CID |
136253996
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.4
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
29
|
| Complexity |
619
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
O1CC[C@@H](C1)N1C2=C(C(NC3C=C(C4C(C)=CN=C(C=4C)OC)C=CC2=3)=O)C=N1
|
| InChi Key |
CKJDCNZBABIEBZ-HNNXBMFYSA-N
|
| InChi Code |
InChI=1S/C22H22N4O3/c1-12-9-23-22(28-3)13(2)19(12)14-4-5-16-18(8-14)25-21(27)17-10-24-26(20(16)17)15-6-7-29-11-15/h4-5,8-10,15H,6-7,11H2,1-3H3,(H,25,27)/t15-/m0/s1
|
| Chemical Name |
7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-[(3S)-oxolan-3-yl]-5H-pyrazolo[4,3-c]quinolin-4-one
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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: 12.5 mg/mL (32.02 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.20 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), suspension solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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: ≥ 1.25 mg/mL (3.20 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 12.5 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: ≥ 1.25 mg/mL (3.20 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 | 2.5612 mL | 12.8061 mL | 25.6121 mL | |
| 5 mM | 0.5122 mL | 2.5612 mL | 5.1224 mL | |
| 10 mM | 0.2561 mL | 1.2806 mL | 2.5612 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.
Link: https://clinicaltrials.gov/ct2/show/NCT04764669
Conditions:Lewy Body Disease|Parkinson DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT03467152
Conditions:Dementia With Lewy BodiesLink: https://clinicaltrials.gov/ct2/show/NCT04023877
Conditions:Dementias With Lewy Bodies
Title:A Study to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of E2027 in Healthy Subjects
Status:Completed
updateDate:2018-09-07
Ctid:NCT02873156
Link: https://clinicaltrials.gov/ct2/show/NCT02873156
Conditions:Healthy SubjectsLink: https://clinicaltrials.gov/ct2/show/NCT02415790
Conditions:Healthy ParticipantsLink: https://clinicaltrials.gov/ct2/show/NCT02947711
Conditions:Healthy SubjectsProducts are for research use only; We do not sell to patients
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