| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
M4 mAChR agonist-1 selectively targets the M4 subtype of muscarinic acetylcholine receptors (mAChRs), which are G protein-coupled receptors expressed in the central nervous system. M4 receptors are involved in regulating dopamine release, cognition, and movement, making them a therapeutic target for schizophrenia and other CNS disorders.
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| ln Vitro |
M4 mAChR agonist-1 demonstrates agonist activity against human M4 with an EC50 >10 microM. In calcium mobilization assays using CHO cells co-expressing the human M4 receptor and Gqi5, it exhibits a maximum effect of 25.0% relative to acetylcholine. It is a potent M4 agonist within its class.
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| ln Vivo |
Dedicated in vivo efficacy studies for M4 mAChR agonist-1 are not extensively documented. As a research tool for CNS disorders, it is hypothesized to modulate cholinergic signaling and dopamine release in the brain. It may serve as a lead compound for developing M4 positive allosteric modulators (PAMs).
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| Enzyme Assay |
The agonist activity is measured using a cell-based functional assay rather than a cell-free enzyme assay. CHO cells stably expressing the human M4 receptor and a chimeric G-protein (Gqi5) are treated with varying concentrations of M4 mAChR agonist-1. Receptor activation is measured by calcium mobilization using a fluorescent calcium indicator.
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| Cell Assay |
CHO cells expressing M4 mAChR are cultured and treated with M4 mAChR agonist-1 across a concentration range (e.g., 1 nM to 100 microM). Intracellular calcium flux is measured. The EC50 (>10 microM) and maximum effect (25.0% relative to acetylcholine) are calculated. The effect on downstream signaling can also be assessed.
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| Animal Protocol |
Dedicated in vivo protocols for M4 mAChR agonist-1 are not well-documented. A standard protocol would involve systemic administration to rodents, followed by measurement of dopamine release in the striatum or assessment of cognitive function in behavioral assays (e.g., prepulse inhibition or novel object recognition).
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| ADME/Pharmacokinetics |
Detailed PK parameters for M4 mAChR agonist-1 are not extensively documented. It has a molecular weight of 290.38 g/mol and is soluble in DMSO (1.45 mg/mL). Its physicochemical properties may support CNS penetration, but comprehensive PK data are not publicly available.
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| Toxicity/Toxicokinetics |
Toxicological data for M4 mAChR agonist-1 are not available in standard profiles. As a research chemical, comprehensive toxicology studies have not been performed. Standard laboratory safety precautions apply.
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| References | |
| Additional Infomation |
M4 mAChR agonist-1 is a potent agonist identified as compound 10a in a series of thieno[2,3-d]pyrimidine-based M4 PAMs. It is a research tool for studying muscarinic receptor pharmacology and CNS disorders. The compound is not an approved drug.
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| Molecular Formula |
C14H18N4OS
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|---|---|
| Molecular Weight |
290.38
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| Exact Mass |
290.12
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| CAS # |
785705-53-5
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| PubChem CID |
2091326
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| Appearance |
Light yellow to brown solid powder
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| LogP |
2.1
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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 |
2
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| Heavy Atom Count |
20
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| Complexity |
372
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1(C2N=CN=C3SC(C)=C(C)C3=2)CCC(C(N)=O)CC1
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| InChi Key |
KOMCJGHOPXNACW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H18N4OS/c1-8-9(2)20-14-11(8)13(16-7-17-14)18-5-3-10(4-6-18)12(15)19/h7,10H,3-6H2,1-2H3,(H2,15,19)
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| Chemical Name |
1-(5,6-dimethylthieno[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~20 mg/mL (~68.88 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (7.16 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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 | 3.4438 mL | 17.2188 mL | 34.4376 mL | |
| 5 mM | 0.6888 mL | 3.4438 mL | 6.8875 mL | |
| 10 mM | 0.3444 mL | 1.7219 mL | 3.4438 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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