| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
PQCA targets the muscarinic M1 receptor. It is a highly selective positive allosteric modulator of the M1 receptor. It binds to an allosteric site on the receptor, distinct from the orthosteric acetylcholine binding site. By binding to this site, it enhances the receptor's response to acetylcholine, potentiating M1-mediated signaling.
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| ln Vitro |
PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. It has an EC50 value of 49 nM on rhesus M1 receptors and 135 nM on human M1 receptors. It shows no activity against other muscarinic receptors. Its activity has been confirmed in various in vitro binding and functional assays.
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| ln Vivo |
PQCA (3-30 mg/kg; oral; male rhesus monkeys housed singly or in pairs) therapy decreased scopolamine deficits on PAL and CPT tests. Blockade of muscarinic signaling by scopolamine severely worsens both tasks [1].
PQCA improves cognitive measures in rat, cynomolgus macaque, and rhesus macaque. It displays robust efficacy in rodent and nonhuman primate (NHP) cognition assays. It can improve performance on translatable tests of memory and attention in rhesus monkeys. These effects are attributed to its positive allosteric modulation of M1 receptors, which are involved in cognitive function. |
| Enzyme Assay |
The primary in vitro assays for PQCA include radioligand binding assays to measure its affinity for the M1 receptor and its selectivity over other muscarinic receptors. Functional assays measure its ability to potentiate M1 receptor-mediated responses, such as calcium mobilization or inositol phosphate accumulation. Its EC50 values are determined from dose-response curves.
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| Cell Assay |
Cellular assays for PQCA involve treating cells expressing the M1 receptor with the compound and measuring its effects on receptor-mediated signaling in the presence of acetylcholine. Its ability to potentiate M1-mediated calcium mobilization or other downstream signaling events is assessed. These assays confirm its positive allosteric modulator activity.
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| Animal Protocol |
Animal/Disease Models: Ten single or paired male rhesus monkeys (6-10 years old; 5.2-10.5 kg) were administered scopolamine [1]
Doses: 3 mg/kg, 10 mg/kg or 30 mg/kg Route of Administration: Oral Experimental Results: Attenuated scopolamine deficits in paired associate learning (PAL) and continuous performance tasks (CPT). In vivo animal experiments for PQCA have been conducted in rat, cynomolgus macaque, and rhesus macaque models to assess its effects on cognitive function. The compound is administered, and its effects on memory, attention, and other cognitive parameters are evaluated using various behavioral tests. |
| ADME/Pharmacokinetics |
PQCA has a molecular weight of 388.42 g/mol. It is a small molecule that is typically used as a research reagent. Its purity is typically ≥98%. The compound is a highly selective and potent muscarinic M1 receptor positive allosteric modulator.
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| Toxicity/Toxicokinetics |
The toxicological profile of PQCA is not extensively detailed in the provided sources. As a research compound, it is not intended for human use. Standard safety precautions should be followed when handling. Its safety would need to be established through preclinical studies if it were to be developed for therapeutic applications.
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| References |
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| Additional Infomation |
PQCA is a highly selective and potent positive allosteric modulator of the muscarinic M1 receptor. It has an EC50 of 49 nM on rhesus and 135 nM on human M1 receptors. PQCA improves cognitive measures in rodent and nonhuman primate models. It is available from various chemical suppliers for research purposes.
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| Molecular Formula |
C22H20N4O3
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|---|---|
| Molecular Weight |
388.427
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| Exact Mass |
388.154
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| CAS # |
1144504-35-7
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| Related CAS # |
1401512-98-8 (sodium);1144504-35-7 (free acid);
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| PubChem CID |
25229646
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| Appearance |
White to yellow solid powder
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| LogP |
2.387
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
881
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RJTJRVASUFIDQM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H20N4O3/c23-15-22(19-6-1-3-9-24-19)7-11-25(12-8-22)14-16-13-17(21(28)29)20(27)26-10-4-2-5-18(16)26/h1-6,9-10,13H,7-8,11-12,14H2,(H,28,29)
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| Chemical Name |
1-[(4-cyano-4-pyridin-2-ylpiperidin-1-yl)methyl]-4-oxoquinolizine-3-carboxylic acid
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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 : ~10 mg/mL (~25.75 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.57 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 10.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5745 mL | 12.8723 mL | 25.7447 mL | |
| 5 mM | 0.5149 mL | 2.5745 mL | 5.1489 mL | |
| 10 mM | 0.2574 mL | 1.2872 mL | 2.5745 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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