| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
PDE-9 inhibitor targets phosphodiesterase 9 (PDE9), an enzyme that specifically hydrolyzes cGMP. Inhibition of PDE9 leads to elevated cGMP levels, causing enhanced NMDA signaling and contributing to an increase in synaptic plasticity and stabilization. This makes PDE9 a promising target for neurodegenerative diseases.
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| ln Vitro |
In vitro, PDE-9 inhibitor promotes neurotransmitter release and neuronal plasticity by increasing cGMP levels. The compound is evaluated in cell-based assays measuring cGMP accumulation and downstream signaling markers. Inhibition of PDE9 activity leads to enhanced synaptic function and neuroprotection in neuronal cell cultures.
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| ln Vivo |
In vivo, PDE-9 inhibitors have been shown to improve symptoms of erectile dysfunction in wild-type animal models and increase dopamine levels. They also activate neutrophils and platelets, which may be due to their ability to inhibit TNF-alpha production. These compounds show potential for treating neurodegenerative diseases such as Alzheimer's disease by improving cognitive function and synaptic plasticity.
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| Enzyme Assay |
In vitro enzyme assays for PDE-9 inhibitor are performed using purified recombinant PDE9 enzyme. The compound is incubated with the enzyme and a cGMP substrate in a reaction buffer. PDE9 activity is measured by detecting the hydrolysis product GMP using a phosphatase-coupled luminescence assay (e.g., IMAP or Transcreener). IC₅0 values are determined from dose-response curves generated with serial dilutions of the compound.
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| Cell Assay |
Cellular assays for PDE-9 inhibitor are conducted using neuronal cell lines or primary neurons. Cells are treated with the compound at concentrations ranging from 0.1 nM to 10 uM for 1-24 hours. Intracellular cGMP levels are measured by ELISA or immunoassay. Phosphorylation of downstream targets (e.g., VASP or CREB) is assessed by Western blot. Neurite outgrowth and synaptic protein expression are evaluated by immunocytochemistry.
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| Animal Protocol |
In vivo studies for PDE-9 inhibitor are conducted in rodent models of neurodegenerative diseases (e.g., Alzheimer's transgenic mice) or cognitive function models. The compound is administered via oral gavage at doses of 1-30 mg/kg once or twice daily. Cognitive performance is assessed using Morris water maze, novel object recognition, or fear conditioning tests. Brain cGMP levels and synaptic markers are measured post-mortem.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of PDE-9 inhibitor include good oral bioavailability and brain penetration, which are essential for CNS drug development. The compound is designed to achieve sufficient brain exposure to inhibit PDE9 activity. Metabolic stability and half-life are optimized for once- or twice-daily dosing. The compound is typically formulated for oral administration in preclinical studies.
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| Toxicity/Toxicokinetics |
Toxicological data for PDE-9 inhibitor are not extensively characterized in the literature. As a research compound, standard safety assessments include evaluation of cytotoxicity in cell-based assays and acute toxicity in animal models. No significant adverse effects have been reported at pharmacologically active doses.
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| Additional Infomation |
PDE-9 inhibitor is a research-use compound not approved for clinical therapeutic applications. It represents a promising therapeutic strategy for neurodegenerative diseases by enhancing cGMP signaling and synaptic plasticity. The compound is used in neuroscience research to study the role of PDE9 in cognition, memory, and neuroprotection.
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| Molecular Formula |
C22H27N5O2
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|---|---|
| Molecular Weight |
393.48208
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| Exact Mass |
393.216
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| CAS # |
1082743-70-1
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| PubChem CID |
135886459
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| Appearance |
White to off-white solid powder
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| Density |
1.39
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| LogP |
3.056
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
629
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@@H]1CN(C[C@H]1C2=NC3=C(C=NN3C4CCOCC4)C(=O)N2)CC5=CC=CC=C5
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| InChi Key |
RVEJWGYZBXCGGM-DNVCBOLYSA-N
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| InChi Code |
InChI=1S/C22H27N5O2/c1-15-12-26(13-16-5-3-2-4-6-16)14-19(15)20-24-21-18(22(28)25-20)11-23-27(21)17-7-9-29-10-8-17/h2-6,11,15,17,19H,7-10,12-14H2,1H3,(H,24,25,28)/t15-,19-/m1/s1
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| Chemical Name |
6-[(3S,4S)-1-benzyl-4-methylpyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one
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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 |
| 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 : ≥ 100 mg/mL (~254.14 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.25 mg/mL (8.26 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 32.5 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. Solubility in Formulation 2: ≥ 3.25 mg/mL (8.26 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 32.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5414 mL | 12.7071 mL | 25.4143 mL | |
| 5 mM | 0.5083 mL | 2.5414 mL | 5.0829 mL | |
| 10 mM | 0.2541 mL | 1.2707 mL | 2.5414 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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