Zamifenacin
Based on 1 Customer Validation
Zamifenacin (UK-76654) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome.
For research use only. We do not sell to patients.
- Purity: 99.24%
- CAS No.: 127308-82-1
- Formula: C27H29NO3
- Molecular Weight:415.52
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Muscarinic M3 receptor[1]
Zamifenacin exhibits terminal elimination half-lives (mouse 2.1, rat 6.0 and, dog 1.1 h) due to high plasma clearance (68, 35, and 39 mL/min/kg respectively) combined with large volumes of distribution (12.5, 19.0, and 3.5 L/kg respectively) following intravenous administration (mouse 5.3, rat 5.0 and, dog 1.0 mg/kg)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CDl mice (mean weight 23 g)[2]
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Dosage:5.3 mg/kg for i.v.; 13.2 mg/kg for oral (Pharmacokinetic Analysis)
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Administration:Intravenous administration and oral administration
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Result:Oral bioavailability (26%), Cmax (92 ng/mL), T1/2 (2.1 h).
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Animal Model:Male and female CD rats (mean weight 210 g)[2]
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Dosage:5.0 mg/kg for i.v.; 20 mg/kg for oral (Pharmacokinetic Analysis)
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Administration:Intravenous administration and oral administration
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Result:Oral bioavailability (64%), Cmax (905 ng/mL), T1/2 (6.0 h).
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Animal Model:Male and two female beagle dogs (13-16 kg)[2]
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Dosage:1.0 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
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Administration:Intravenous administration and oral administration
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Result:Oral bioavailability (100%), Cmax (416 ng/mL), T1/2 (1.1 h).
Chemical Information
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CAS No. 127308-82-1
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Appearance Solid
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Molecular Weight 415.52
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Formula C27H29NO3
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Color Off-white to light yellow
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SMILES
N1(C[C@@H](CCC1)OC(C2=CC=CC=C2)C3=CC=CC=C3)CCC4=CC5=C(C=C4)OCO5
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Synonyms
UK-76654
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 100 mg/mL (240.66 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (6.02 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 (6.02 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
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.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Houghton LA, et al. Zamifenacin (UK-76, 654) a potent gut M3 selective muscarinic antagonist, reduces colonic motor activity in patients with irritable bowel syndrome. Aliment Pharmacol Ther. 1997 Jun;11(3):561-8. [Content Brief]
[2]. Beaumont KC, et al. Pharmacokinetics and metabolism of Zamifenacin in mouse, rat, dog and man. Xenobiotica. 1996 Apr;26(4):459-71. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4066 mL | 12.0331 mL | 24.0662 mL | 60.1656 mL |
| 5 mM | 0.4813 mL | 2.4066 mL | 4.8132 mL | 12.0331 mL | |
| 10 mM | 0.2407 mL | 1.2033 mL | 2.4066 mL | 6.0166 mL | |
| 15 mM | 0.1604 mL | 0.8022 mL | 1.6044 mL | 4.0110 mL | |
| 20 mM | 0.1203 mL | 0.6017 mL | 1.2033 mL | 3.0083 mL | |
| 25 mM | 0.0963 mL | 0.4813 mL | 0.9626 mL | 2.4066 mL | |
| 30 mM | 0.0802 mL | 0.4011 mL | 0.8022 mL | 2.0055 mL | |
| 40 mM | 0.0602 mL | 0.3008 mL | 0.6017 mL | 1.5041 mL | |
| 50 mM | 0.0481 mL | 0.2407 mL | 0.4813 mL | 1.2033 mL | |
| 60 mM | 0.0401 mL | 0.2006 mL | 0.4011 mL | 1.0028 mL | |
| 80 mM | 0.0301 mL | 0.1504 mL | 0.3008 mL | 0.7521 mL | |
| 100 mM | 0.0241 mL | 0.1203 mL | 0.2407 mL | 0.6017 mL |
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