| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
Phosphodiesterase 10A (PDE10A), an enzyme that hydrolyzes both cAMP and cGMP. PQ-10 is a potent inhibitor of PDE10A with an IC50 of 4.6 nM and an ED50 of 13 mg/kg. It has a Ki of 4 nM and displays 53-fold and 68-fold selectivity over PDE3A and PDE3B, respectively. The compound shows >38-fold selectivity for PDE10 over a panel of 60 CNS-associated receptors, enzymes, and ion channels.
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| ln Vitro |
PQ-10 potently inhibits PDE10A with an IC50 of 4.6 nM and a Ki of 4 nM. The compound suppresses the growth of human non-small cell lung cancer (NSCLC) cell lines. It induces patterns of brain glucose metabolism, which can be measured using 2-deoxyglucose (2-DG) uptake. PQ-10 shows region-specific increases in 2-DG absorption in the mouse lateral habenula and globus pallidus, indicating its effects on specific brain regions.
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| ln Vivo |
PQ-10 demonstrates region-specific increases in 2-DG absorption in the mouse lateral habenula and globus pallidus, the outer portion corresponding to the globus pallidus in primates [1].
PQ-10 demonstrates region-specific increases in 2-DG absorption in the mouse lateral habenula and globus pallidus, corresponding to the globus pallidus in primates. The compound has an ED50 of 13 mg/kg for its in vivo effects. It has been shown to enhance basic auditory information processing in rats. PQ-10 induces patterns of brain glucose metabolism that may serve as a potential translational biomarker for PDE10A inhibition. |
| Enzyme Assay |
The in vitro enzyme inhibition assay for PQ-10 typically involves measuring the phosphodiesterase activity of recombinant PDE10A using a standard enzymatic assay. The enzyme is incubated with the substrate (cAMP or cGMP) and the test compound at various concentrations. The hydrolysis product is quantified using a coupled enzyme assay or HPLC, and the IC50 or Ki value is determined from the dose-response curve. Selectivity is assessed by testing the compound against other PDE isoforms.
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| Cell Assay |
The in vitro cellular assay for PQ-10 typically involves culturing cells that express PDE10A, such as neuronal cell lines or cancer cell lines. Cells are treated with varying concentrations of the compound, and the levels of cAMP or cGMP are measured using ELISA or other immunoassays. The inhibition of PDE10A activity is assessed by the increase in cyclic nucleotide levels. Cell proliferation assays can also be performed to assess the compound's antiproliferative effects.
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| Animal Protocol |
Animal/Disease Models: 24 –28 g male C57BL/6 mice, PDE10A WT and KO mice [1]
Doses: 0.16, 0.63, 2.5 and 10 mg/kg Route of Administration: subcutaneous injection Experimental Results: Area showing 2-DG uptake Specific increases in the globus pallidus (the outer segment equivalent to the globus pallidus in primates) and the lateral habenula in mice. In vivo animal studies for PQ-10 typically involve the use of rodent models to assess its effects on brain glucose metabolism and behavioral outcomes. Mice or rats are administered the compound via appropriate routes (e.g., oral or intraperitoneal) at doses such as 13 mg/kg. Brain glucose metabolism is assessed using 2-deoxyglucose (2-DG) uptake or positron emission tomography (PET) imaging. Behavioral tests are performed to evaluate the compound's effects on schizophrenia-like symptoms or other psychiatric disorders. |
| ADME/Pharmacokinetics |
PQ-10 is brain-penetrant with favorable pharmacokinetic properties. It has an ED50 of 13 mg/kg. The compound has a molecular weight of 403.43 g/mol and a molecular formula of C22H21N5O3. It shows good solubility and stability for in vivo studies. The compound induces patterns of brain glucose metabolism that can serve as a translational biomarker. Further detailed PK parameters are available from the manufacturer's data sheets.
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| Toxicity/Toxicokinetics |
Specific toxicology data for PQ-10 are not extensively reported in the public domain. The compound is intended for research use only and should be handled with appropriate laboratory safety precautions. In preclinical studies, the compound has been administered at various doses without reported severe toxicity. Comprehensive toxicity studies would be required before any clinical application.
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| References | |
| Additional Infomation |
PQ-10 is a potent and selective inhibitor of PDE10A with potential applications in psychiatric disorders such as schizophrenia. It induces patterns of brain glucose metabolism that may serve as a potential translational biomarker. The compound also suppresses the growth of human non-small cell lung cancer cell lines. It has not yet entered clinical trials and is strictly for preclinical research purposes. The molecular formula is C22H21N5O3.
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| Molecular Formula |
C22H21N5O3
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| Molecular Weight |
403.44
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| Exact Mass |
403.164
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| Elemental Analysis |
C, 65.50; H, 5.25; N, 17.36; O, 11.90
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| CAS # |
927691-21-2
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| PubChem CID |
11955614
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| Appearance |
White to off-white solid powder
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| Density |
1.333
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| LogP |
3.312
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
569
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O(C1C(OC)=CC2C(=C(N3CC[C@@H](OC4C=NC5C=CC=CC=5N=4)C3)N=CN=2)C=1)C
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| InChi Key |
UBIIFKJMNRPNMT-CQSZACIVSA-N
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| InChi Code |
InChI=1S/C22H21N5O3/c1-28-19-9-15-18(10-20(19)29-2)24-13-25-22(15)27-8-7-14(12-27)30-21-11-23-16-5-3-4-6-17(16)26-21/h3-6,9-11,13-14H,7-8,12H2,1-2H3/t14-/m1/s1
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| Chemical Name |
6,7-dimethoxy-4-[(3R)-3-quinoxalin-2-yloxypyrrolidin-1-yl]quinazoline
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| Synonyms |
PQ10; PQ 10; PQ-10
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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 : ~25 mg/mL (~61.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.20 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), 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 (6.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 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 | 2.4787 mL | 12.3934 mL | 24.7868 mL | |
| 5 mM | 0.4957 mL | 2.4787 mL | 4.9574 mL | |
| 10 mM | 0.2479 mL | 1.2393 mL | 2.4787 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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