| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Muscarinic M₃ receptor. It displays selectivity for M₃ receptors (pKi = 8.52) over M₂ (7.93), M₁ (7.90), and M₄ (7.78).
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|---|---|
| ln Vitro |
Zamifenacin is a selective M₃ receptor antagonist. It displays higher affinity at ileal M₃ receptors (pKi = 9.3) compared to oesophageal and tracheal M₃ receptors (pKi = 8.8 and 8.2, respectively). This tissue selectivity contributes to its gut-specific effects.
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| ln Vivo |
After oral dosing (13.2 for mice, 20 for rats, and 5 mg/kg for dogs), zamifenacin has moderate oral bioavailability (26% in mice, 64% in rats, and 100% in dogs) and Cmax (92 in mice, 905 in rats, and 416 ng/mL in dogs) [2]. Following intravenous treatment, zamifenacin has a terminal elimination half-life (mouse 2.1, rat 6.0, and dogs 1.1 h) L/kg; rats 5.0, and dogs 1.0 mg/kg) [2].
Zamifenacin inhibits gastrointestinal motility in vivo in the absence of cardiovascular effects. In animal models, it has been shown to significantly reduce colonic motility. |
| Enzyme Assay |
In vitro receptor binding and functional assays are used to characterize zamifenacin. Radioligand binding assays determine its affinity (pKi) for various muscarinic receptor subtypes. Functional assays, such as measuring the inhibition of smooth muscle contraction in isolated tissue preparations (e.g., ileum, trachea), assess its antagonist potency and tissue selectivity.
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| Cell Assay |
In vitro cellular assays typically involve cells expressing recombinant muscarinic receptors. The compound's ability to block receptor-mediated signaling, such as calcium mobilization or IP3 accumulation, is measured. These assays help confirm its potency and selectivity profile.
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| Animal Protocol |
Animal/Disease Models: Male CD1 mice (average weight 23g) [2]
Doses: intravenous (iv) (iv)injection 5.3mg/kg; intravenous (iv) (iv)injection 5.3mg/kg. Oral administration 13.2 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: intravenous (iv) (iv)and oral Experimental Results: Oral bioavailability (26%), Cmax (92 ng/mL), T1/2 (1.1 h) Animal/Disease Models: Male and female CD rats (mean body weight 210 g) [2] Doses: 5.0 mg/kg intravenously (iv) (iv)(iv); 20 mg/kg orally (pharmacokinetic/PK/PK analysis) Route of Administration: intravenous (iv) (iv)and oral Experimental Results: Oral Bioavailability (64%), Cmax (905 ng/mL) ), T1/2 (6.0 h). Animal/Disease Models: Male and two female beagle dogs (13-16 kg) [2] Doses: intravenous (iv) (iv)injection 1.0 mg/kg; oral 5 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: intravenous (iv) (iv)administration and oral administration Experimental Results: Oral bioavailability (100%), Cmax (416 ng/mL), T1/2 (1.1 h). In vivo efficacy studies are conducted in animal models of gastrointestinal motility, such as the mouse or rat. Zamifenacin is administered, and its effect on colonic motility is measured. These studies have shown that it significantly reduces motility. |
| ADME/Pharmacokinetics |
Zamifenacin exhibits moderate oral bioavailability, with values of 26% in mouse, 64% in rat, and 100% in dog. Its Cmax values are 92 ng/mL in mouse, 905 ng/mL in rat, and 416 ng/mL in dog. The terminal elimination half-life in mice is 2.1 hours.
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| Toxicity/Toxicokinetics |
Specific toxicological data is not provided in the references. As a research compound, it is for laboratory use only and not for human therapeutic applications.
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| References |
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| Additional Infomation |
Zamifenacin fumarate is a research tool for studying the role of muscarinic M₃ receptors in gastrointestinal motility. It was under investigation for the treatment of IBS. It is not approved for clinical use.
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| Molecular Formula |
C27H29NO3.C4H4O4
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|---|---|
| Molecular Weight |
531.59622
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| Exact Mass |
531.226
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| CAS # |
127308-98-9
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| Related CAS # |
Zamifenacin;127308-82-1
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| PubChem CID |
60196362
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| Appearance |
White to off-white solid powder
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| Boiling Point |
700.2ºC at 760mmHg
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| Flash Point |
377.3ºC
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| LogP |
4.878
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
39
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| Complexity |
632
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1C[C@@H](CN(C1)CCC2=CC3=C(C=C2)OCO3)OC(C4=CC=CC=C4)C5=CC=CC=C5.C(=C/C(=O)O)\C(=O)O
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| InChi Key |
PMHKTAIGYOVZEZ-DSSYAJFBSA-N
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| InChi Code |
InChI=1S/C27H29NO3.C4H4O4/c1-3-8-22(9-4-1)27(23-10-5-2-6-11-23)31-24-12-7-16-28(19-24)17-15-21-13-14-25-26(18-21)30-20-29-25;5-3(6)1-2-4(7)8/h1-6,8-11,13-14,18,24,27H,7,12,15-17,19-20H2;1-2H,(H,5,6)(H,7,8)/b;2-1+/t24-;/m0./s1
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| Chemical Name |
(3S)-3-benzhydryloxy-1-[2-(1,3-benzodioxol-5-yl)ethyl]piperidine;(E)-but-2-enedioic acid
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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, 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) |
DMSO : ~100 mg/mL (~188.11 mM)
H2O : ~1 mg/mL (~1.88 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8811 mL | 9.4056 mL | 18.8111 mL | |
| 5 mM | 0.3762 mL | 1.8811 mL | 3.7622 mL | |
| 10 mM | 0.1881 mL | 0.9406 mL | 1.8811 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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