| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Talsaclidine targets muscarinic acetylcholine receptors (mAChRs), specifically the M1, M2, and M3 subtypes. It acts as a full agonist at the M1 subtype and as a partial agonist at the M2 and M3 subtypes. The compound selectively targets the M1 subtype of mAChRs, which are critical for cognitive processes such as learning and memory.
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| ln Vitro |
In vitro, Talsaclidine demonstrates full agonism at the M1 muscarinic receptor subtype and partial agonism at M2 and M3 subtypes. It has preferential neuron-stimulating properties. The compound enhances cholinergic neurotransmission. Detailed IC₅0 or EC₅0 values are not extensively documented in the available literature.
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| ln Vivo |
In vivo, Talsaclidine is used for cholinergic substitution therapy of Alzheimer's disease. It promotes cognitive function and neuronal communication. The compound's unique profile of action is due to partial agonism at M2 and M3 receptors combined with full agonism at M1 receptors. Further clinical data are available in the published literature.
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| Enzyme Assay |
The in vitro receptor binding assay for muscarinic receptors uses membrane preparations from cells expressing M1, M2, or M3 receptors. Competitive binding is performed using radiolabeled muscarinic antagonists (such as [3H]-NMS or [3H]-QNB) in the presence of varying concentrations of Talsaclidine. Functional assays measure receptor-mediated intracellular calcium mobilization or GTPgammaS binding to assess agonism. EC₅0 values are calculated from dose-response curves.
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| Cell Assay |
For in vitro cell-based assays, cells expressing muscarinic receptor subtypes (M1, M2, or M3) are cultured and treated with Talsaclidine at various concentrations. Receptor activation is measured by calcium mobilization using fluorescent indicators (such as Fura-2 or Fluo-4) or by measuring cAMP accumulation. Cells are maintained under standard culture conditions and experiments are typically performed in triplicate.
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| Animal Protocol |
In vivo animal studies for Talsaclidine typically involve rodent models of cognitive impairment (such as aged rats or pharmacologically induced models). The compound is administered orally or intraperitoneally at various doses. Cognitive function is assessed using behavioral tests such as the Morris water maze, radial arm maze, or novel object recognition. Cholinergic markers may be measured in brain tissue to confirm target engagement.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Talsaclidine are not extensively documented. The compound has molecular weight 165.23. It is a small molecule muscarinic agonist with expected oral bioavailability. The compound is soluble in DMSO and typically formulated for in vitro and in vivo studies. Further detailed PK parameters (half-life, Cmax, AUC, bioavailability) would require dedicated studies.
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| Toxicity/Toxicokinetics |
Toxicological data for Talsaclidine are not well characterized in the public domain. As a research compound, standard safety precautions should be observed. Muscarinic agonists as a class may have potential side effects including cholinergic effects (bradycardia, salivation, gastrointestinal disturbances). Comprehensive toxicity profiling would be required for therapeutic development.
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| References |
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| Additional Infomation |
Tasacrifice has been used in trials investigating the treatment of Alzheimer's disease.
Talsaclidine (CAS# 147025-53-4) is a novel M1-receptor selective muscarinic agonist for Alzheimer's disease research. It is a full agonist at M1 and a partial agonist at M2 and M3 subtypes. The compound enhances cholinergic neurotransmission and promotes cognitive function. It is also known as WAL-2014 and is not approved for clinical use. |
| Molecular Formula |
C10H15NO
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|---|---|
| Molecular Weight |
165.2322
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| Exact Mass |
165.115
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| CAS # |
147025-53-4
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| PubChem CID |
71792
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| Appearance |
Light yellow to yellow liquid
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| Density |
1.06g/cm3
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| Boiling Point |
251.1ºC at 760mmHg
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| Flash Point |
73.3ºC
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| Vapour Pressure |
0.0208mmHg at 25°C
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| Index of Refraction |
1.525
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| LogP |
0.668
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
12
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| Complexity |
197
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C#CCO[C@H]1CN2CCC1CC2
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| InChi Key |
XVFJONKUSLSKSW-JTQLQIEISA-N
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| InChi Code |
InChI=1S/C10H15NO/c1-2-7-12-10-8-11-5-3-9(10)4-6-11/h1,9-10H,3-8H2/t10-/m0/s1
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| Chemical Name |
(3R)-3-prop-2-ynoxy-1-azabicyclo[2.2.2]octane
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.0522 mL | 30.2608 mL | 60.5217 mL | |
| 5 mM | 1.2104 mL | 6.0522 mL | 12.1043 mL | |
| 10 mM | 0.6052 mL | 3.0261 mL | 6.0522 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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