Otenzepad
Based on 3 publication(s) in Google Scholar
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.93%
- CAS 番号: 102394-31-0
- 分子式: C24H31N5O2
- 分子量:421.54
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Otenzepad
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生物活性
製品説明
IC50 & Target
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mAChR2 |
体内実験
Otenzepad (2 mg/kg, s.c., in rats) significantly improved retention relative to vehicle controls[2].
Otenzepad (0.3, 1.0, or 3.0 mg/kg, ip, in mice) potentiates the effects of glucose and reverses the effects of insulin on memory[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Forty-eight male Long-Evans rats (325-350 g)[2].
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Dosage:0.25, 0.5, 1.0 and 2.0 mg/kg.
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Administration:S.C. on the dorsum of the neck once.
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Result:Doses of 0.5 and 1.0 mg/kg significantly improved acquisition relative to vehicle controls, while doses of 0.25 and 2.0 mg/kg had no effect.
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Animal Model:Adult male Swiss mice (age 60–70 days; weight 25-30 g)[3].
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Dosage:0.3, 1.0, or 3.0 mg/kg.
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Administration:IP once.
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Result:Enhanced retention in an inverted-U dose–response manner, with significant enhancement seen at 1.0 mg/kg (U15,15 = 49, p < 0.02, compared with saline-saline-injected control group).
化学情報
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CAS 番号 102394-31-0
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性状 Solid
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分子量 421.54
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分子式 C24H31N5O2
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Color White to off-white
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SMILES
O=C1NC2=CC=CN=C2N(C(CN3C(CN(CC)CC)CCCC3)=O)C4=CC=CC=C14
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別名
AF-DX 116
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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J Nanobiotechnology
Magnetic vagus nerve stimulation alleviates myocardial ischemia-reperfusion injury by the inhibition of pyroptosis through the M2AChR/OGDHL/ROS axis in rats. [Abstract]2023 Nov 14;21(1):421. PMID: 37957640
Otenzepad purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2023 Nov 14;21(1):421. [Abstract]
Western blot analysis of protein level of OGDHL (GAPDH as an internal control) and quantification of OGDHL activity in NRCMs incubated with or without Otenzepad (an M2 receptor antagonist) under H/R or ACh treatment.
Otenzepad purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2023 Nov 14;21(1):421. [Abstract]
Immunofluorescence staining of NRCMs for GSDMD-N (green) and DAPI (blue) in NRCMs incubated with or without Otenzepad (an M2 receptor antagonist) under H/R or ACh treatment.
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Mol Cell Endocrinol
Vagotomy suppresses food intake by increasing GLP-1 secretion via the M3 AChR-AMPKα pathway in mice. [Abstract]2025 Apr 1:599:112464. PMID: 39848433
Otenzepad purchased from MedChemExpress. Usage Cited in: Mol Cell Endocrinol. 2025 Apr 1:599:112464. [Abstract]
The secretion of GLP-1 in STC-1 supernatant was tested by ELISA kits treated with Otenzepad (AF-DX 116).
溶剤 & 溶解度
体外:
DMSO : 25 mg/mL (59.31 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (282 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Bloom JW, et al. Heterogeneity of the M1 muscarinic receptor subtype between peripheral lung and cerebral cortex demonstrated by the selective antagonist AF-DX 116. Life Sci. 1987 Jul 27;41(4):491-6. [Content Brief]
[2]. Packard MG, et al. Post-training injection of the acetylcholine M2 receptor antagonist AF-DX 116 improves memory. Brain Res. 1990 Jul 30;524(1):72-6. [Content Brief]
[3]. Kopf SR, et al. AF-DX 116, a presynaptic muscarinic receptor antagonist, potentiates the effects of glucose and reverses the effects of insulin on memory. Neurobiol Learn Mem. 1998 Nov;70(3):305-13. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3723 mL | 11.8613 mL | 23.7225 mL | 59.3064 mL |
| 5 mM | 0.4745 mL | 2.3723 mL | 4.7445 mL | 11.8613 mL | |
| 10 mM | 0.2372 mL | 1.1861 mL | 2.3723 mL | 5.9306 mL | |
| 15 mM | 0.1582 mL | 0.7908 mL | 1.5815 mL | 3.9538 mL | |
| 20 mM | 0.1186 mL | 0.5931 mL | 1.1861 mL | 2.9653 mL | |
| 25 mM | 0.0949 mL | 0.4745 mL | 0.9489 mL | 2.3723 mL | |
| 30 mM | 0.0791 mL | 0.3954 mL | 0.7908 mL | 1.9769 mL | |
| 40 mM | 0.0593 mL | 0.2965 mL | 0.5931 mL | 1.4827 mL | |
| 50 mM | 0.0474 mL | 0.2372 mL | 0.4745 mL | 1.1861 mL |
Otenzepad 関連分類
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