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| Targets |
Sabcomeline targets the muscarinic M1 receptor. It is a selective M1 receptor partial agonist. By preferentially stimulating M1 receptors, it enhances cholinergic neurotransmission in the central nervous system while limiting peripheral side effects linked to non-selective muscarinic agonists.
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| ln Vitro |
In vitro, sabcomeline is a potent and selective M1 receptor partial agonist. It activates M1 receptors, enhancing cholinergic signaling. Its selectivity for M1 over other muscarinic receptor subtypes reduces peripheral side effects. It has been used to study cholinergic pathways involved in learning and memory.
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| ln Vivo |
In vivo, sabcomeline was under development for the treatment of Alzheimer's disease. By enhancing cholinergic neurotransmission, it was expected to improve cognitive function in Alzheimer's patients. It has been studied in preclinical and clinical settings. Further development was discontinued for reasons not detailed in the search results.
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| Enzyme Assay |
In vitro receptor binding assays for sabcomeline typically involve competitive radioligand binding using membrane preparations expressing human muscarinic receptor subtypes (M1, M2, M3, M4, M5). Membranes are incubated with radiolabeled ligands (e.g., [³H]-NMS) and varying concentrations of the compound. Ki values are calculated from displacement curves. Functional activity is assessed by measuring calcium mobilization or cAMP accumulation.
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| Cell Assay |
Cell-based assays for sabcomeline involve culturing cells expressing recombinant muscarinic M1 receptors (e.g., CHO or HEK-293 cells). Cells are treated with sabcomeline at concentrations ranging from 0.1 nM to 10 µM. Receptor activation is measured by calcium mobilization using fluorescent indicators. Functional selectivity is assessed by comparing responses at different muscarinic receptor subtypes.
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| Animal Protocol |
In vivo animal experiments for sabcomeline typically involve administration to rodent models via oral gavage or intraperitoneal injection. Cognitive function is assessed by Morris water maze, novel object recognition, or other behavioral tests. Cholinergic neurotransmission is evaluated by measuring acetylcholine levels. Pharmacokinetic parameters are evaluated by measuring compound levels in blood and brain.
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| ADME/Pharmacokinetics |
Sabcomeline HCl (molecular weight ~380-400) is orally active. It penetrates the blood-brain barrier to reach its central nervous system targets. It is metabolized in the liver and excreted via bile and urine. Detailed pharmacokinetic parameters are available in preclinical literature. Its development was discontinued for Alzheimer's disease.
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| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for sabcomeline HCl from the search results. As a muscarinic M1 receptor agonist, potential side effects may include cholinergic effects such as nausea, vomiting, and diarrhea. Comprehensive toxicological evaluation has likely been conducted in preclinical development. The compound is for research use only.
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| References |
McArthur RA, Gray J, Schreiber R. Cognitive effects of muscarinic M1 functional agonists in non-human primates and clinical trials. Curr Opin Investig Drugs. 2010 Jul;11(7):740-60. Review. PubMed PMID: 20571970.
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| Additional Infomation |
See also: Sabcomeline (has active moiety).
Sabcomeline HCl (CAS#: 159912-58-0) is a selective muscarinic M1 receptor partial agonist. It was developed for Alzheimer's disease treatment. It enhances cholinergic neurotransmission in the CNS. It limits peripheral side effects by M1 selectivity. It is a research tool for studying cholinergic pathways. |
| Molecular Formula |
C10H16CLN3O
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|---|---|
| Molecular Weight |
193.2456
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| Exact Mass |
229.098
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| CAS # |
159912-58-0
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| Related CAS # |
Sabcomeline;159912-53-5
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| PubChem CID |
9577994
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| Appearance |
White to off-white solid powder
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| Boiling Point |
278.1ºC at 760 mmHg
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| Flash Point |
122ºC
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| Vapour Pressure |
0.00436mmHg at 25°C
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| LogP |
1.594
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
283
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CO/N=C(\C#N)/[C@H]1CN2CCC1CC2.Cl
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| InChi Key |
INJWRVWKJFJRFO-SCRZZQONSA-N
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| InChi Code |
InChI=1S/C10H15N3O.ClH/c1-14-12-10(6-11)9-7-13-4-2-8(9)3-5-13/h8-9H,2-5,7H2,1H31H/b12-10+/t9-/m0./s1
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| Chemical Name |
(R)-3-Quinuclidineglyoxylonitrile (Z)-O-methyloxime, monohydrochloride
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| Synonyms |
BCI-224 BRL-55473 CEB-2424 SB-202026A BCI224 BRL55473 CEB2424 SB202026A. Memric.
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
H2O : ~125 mg/mL (~544.16 mM)
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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 | 5.1746 mL | 25.8732 mL | 51.7464 mL | |
| 5 mM | 1.0349 mL | 5.1746 mL | 10.3493 mL | |
| 10 mM | 0.5175 mL | 2.5873 mL | 5.1746 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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