| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Otenzepad targets the muscarinic acetylcholine receptor M2 subtype (mAChR M2), which is predominantly located in the heart and brain. As a selective M2 antagonist, it blocks the inhibitory effects of acetylcholine at M2 receptors, leading to increased acetylcholine release and enhanced cholinergic transmission. This mechanism may have therapeutic applications in cognitive disorders and cardiac arrhythmias.
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| ln Vitro |
In vitro, otenzepad acts as a selective antagonist at the muscarinic M2 receptor. Its binding affinity (Ki) for M2 receptors has been confirmed in radioligand binding assays. It shows selectivity over other muscarinic receptor subtypes. Its functional antagonism is confirmed in assays measuring M2 receptor-mediated signaling, such as inhibition of cAMP accumulation.
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| ln Vivo |
In comparison to vehicle-injected controls, otenzepad (0.5, 1 mg/kg, subcutaneous injection, rats) greatly enhanced victory retention acquisition [2]. When compared to vehicle control, otenzepad (2 mg/kg, SC, rat) greatly increased retention [2]. Otenzepad increases the effects of glucose and counteracts the effects of insulin on memory when given intraperitoneally to mice at doses of 0.3, 1.0, or 3.0 mg/kg [3].
In vivo, otenzepad has been studied for its effects on cognitive function and cardiac function. By blocking M2 autoreceptors, it increases acetylcholine release, which may improve cognitive performance. Its effects on heart rate and cardiac conduction have also been investigated. However, specific in vivo efficacy data are limited. |
| Enzyme Assay |
Cell-free assays for otenzepad are radioligand binding assays using membrane preparations from cells expressing muscarinic M2 receptors. The compound's binding affinity (Ki) is determined by its ability to displace a labeled muscarinic receptor ligand such as [3H]N-methylscopolamine. Its selectivity over other muscarinic subtypes is confirmed.
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| Cell Assay |
Cellular assays for otenzepad are performed using cell lines expressing muscarinic M2 receptors. Cells are treated with varying concentrations of otenzepad, and M2 receptor-mediated signaling is assessed by measuring the inhibition of forskolin-stimulated cAMP accumulation. Its antagonist activity is confirmed.
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| Animal Protocol |
Animal/Disease Models: 48 male Long-Evans rats (325-350 g) [2].
Doses: 0.25, 0.5, 1.0 and 2.0 mg/kg. Route of Administration: SC once on the nape of the neck. Experimental Results: Doses of 0.5 and 1.0 mg/kg Dramatically improved acquisition relative to vehicle control, whereas doses of 0.25 and 2.0 mg/kg had no effect. Animal/Disease Models: Adult male Swiss mice (age 60-70 days; weight 25-30 grams) [3]. Doses: 0.3, 1.0 or 3.0 mg/kg. Management: IP once. Experimental Results: Retention was enhanced in an inverted U dose-response manner, with significant enhancement observed at 1.0 mg/kg (U15,15 = 49, p < 0.02 compared to saline-injected controls). In vivo animal experiments for otenzepad are conducted in rodent models of cognitive impairment and cardiac arrhythmias. Animals are administered otenzepad orally or intraperitoneally, and cognitive performance is assessed using behavioral tests. Heart rate and cardiac function are measured. |
| ADME/Pharmacokinetics |
Otenzepad has a molecular weight of 391.47 g/mol and a molecular formula of C22H29N5O2. It is a solid powder. It is soluble in DMSO and should be stored under recommended conditions. Its pharmacokinetic properties are not well characterized.
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| Toxicity/Toxicokinetics |
The toxicological profile of otenzepad has not been extensively characterized. As a muscarinic M2 antagonist, it may have effects on heart rate and cognitive function. No significant toxicity has been reported. Comprehensive toxicology studies are lacking. It is a research compound and is not approved for clinical use.
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| References |
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| Additional Infomation |
11-[2-[2-(diethylaminomethyl)-1-piperidinyl]-1-oxoethyl]-5H-pyrido[2,3-b][1,4]benzodiazepine-6-one is a benzodiazepine drug.
Otenzepad is a selective muscarinic M2 receptor antagonist used as a research compound to study cholinergic signaling. It has been studied for its potential in treating cognitive disorders and cardiac arrhythmias. It is not approved for clinical use. |
| Molecular Formula |
C24H31N5O2
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| Molecular Weight |
421.55
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| Exact Mass |
421.248
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| CAS # |
102394-31-0
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| PubChem CID |
107867
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| Appearance |
White to off-white solid powder
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| Density |
1.171 g/cm3
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| Boiling Point |
573.2ºC at 760 mmHg
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| Flash Point |
300.5ºC
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| LogP |
3.214
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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 |
6
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| Heavy Atom Count |
31
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| Complexity |
625
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(CC)CC1CCCCN1CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4
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| InChi Key |
UBRKDAVQCKZSPO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H31N5O2/c1-3-27(4-2)16-18-10-7-8-15-28(18)17-22(30)29-21-13-6-5-11-19(21)24(31)26-20-12-9-14-25-23(20)29/h5-6,9,11-14,18H,3-4,7-8,10,15-17H2,1-2H3,(H,26,31)
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| Chemical Name |
11-[2-[2-(diethylaminomethyl)piperidin-1-yl]acetyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one
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| Synonyms |
AF-DX-116 AF-DX 116 Otenzepad
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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 (~59.31 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 | 2.3722 mL | 11.8610 mL | 23.7220 mL | |
| 5 mM | 0.4744 mL | 2.3722 mL | 4.7444 mL | |
| 10 mM | 0.2372 mL | 1.1861 mL | 2.3722 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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