Zamifenacinfumarate
- Product Name
- Zamifenacinfumarate
- CAS No.
- 127308-98-9
- Chemical Name
- Zamifenacinfumarate
- Synonyms
- UK-76654 fumarate;Zamifenacinfumarate;Zamifenacin fumarate, 10 mM in DMSO;Zamifenacin fumarate, M3 receptor antagonist;(3R)-1-[2-(1-,3-Benzodioxol-5-yl)ethyl]-3-(diphenylmethoxy)piperidinefumarate;(R)-3-(Benzhydryloxy)-1-(2-(benzo[d][1,3]dioxol-5-yl)ethyl)piperidine fumarate;gut,UK 76654,bowel,inhibit,Inhibitor,Muscarinic acetylcholine receptor,UK-76654,muscarinic,mAChR,motility,syndrome,irritable,Zamifenacin fumarate,Zamifenacin,UK76654,colonic
- CBNumber
- CB81075168
- Molecular Formula
- C31H33NO7
- Formula Weight
- 531.61
- MOL File
- 127308-98-9.mol
Zamifenacinfumarate Property
- storage temp.
- Inert atmosphere,2-8°C
- solubility
- Soluble to 100 mM in DMSO and to 25 mM in ethanol
- form
- Powder
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- Z150705
- Product name
- ZamifenacinFumarate
- Packaging
- 25mg
- Price
- $295
- Updated
- 2021/12/16
- Product number
- B7114
- Product name
- Zamifenacinfumarate
- Packaging
- 10mg
- Price
- $315
- Updated
- 2021/12/16
- Product number
- CS-0029052
- Product name
- Zamifenacin(fumarate)
- Purity
- 99.77%
- Packaging
- 10mg
- Price
- $400
- Updated
- 2021/12/16
- Product number
- CS-0029052
- Product name
- Zamifenacin(fumarate)
- Purity
- 99.77%
- Packaging
- 5mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- CS-0029052
- Product name
- Zamifenacin(fumarate)
- Purity
- 99.77%
- Packaging
- 25mg
- Price
- $780
- Updated
- 2021/12/16
Zamifenacinfumarate Chemical Properties,Usage,Production
Uses
Zamifenacin Fumarate is a selective antagonist of mAChR M3 (M3 muscarinic receptor).
Biological Activity
Selective M 3 muscarinic receptor antagonist (pK i values are 8.52, 7.93, 7.90 and 7.78 for M 3 , M 2 , M 1 and M 4 receptors respectively). Displays higher affinity at ileal M 3 receptors (pK i = 9.3) compared to oesophageal and tracheal M 3 receptors (pK i values are 8.8 and 8.2 respectively). In vivo, inhibits gastrointestinal motility in the absence of cardiovascular effects.
in vivo
Zamifenacin exhibits moderate oral bioavailability (mouse 26%, rat 64%, dog 100%) and Cmax (mouse 92, rat 905, dog 416 ng/mL) following oral administration (mouse 13.2, rat 20 and, dog 5 mg/kg)[2].
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].
| Animal Model: | Male CDl mice (mean weight 23 g)[2] |
| Dosage: | 5.3 mg/kg for i.v.; 13.2 mg/kg for oral (Pharmacokinetic Analysis) |
| Administration: | Intravenous administration and oral administration |
| Result: | Oral bioavailability (26%), Cmax (92 ng/mL), T1/2 (1.1 h). |
| Animal Model: | Male and female CD rats (mean weight 210 g)[2] |
| Dosage: | 5.0 mg/kg for i.v.; 20 mg/kg for oral (Pharmacokinetic Analysis) |
| Administration: | Intravenous administration and oral administration |
| Result: | Oral bioavailability (64%), Cmax (905 ng/mL), T1/2 (6.0 h). |
| Animal Model: | Male and two female beagle dogs (13-16 kg)[2] |
| Dosage: | 1.0 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis) |
| Administration: | Intravenous administration and oral administration |
| Result: | Oral bioavailability (100%), Cmax (416 ng/mL), T1/2 (1.1 h). |
Zamifenacinfumarate Preparation Products And Raw materials
Raw materials
Preparation Products
Zamifenacinfumarate Suppliers
- Tel
- --
- Fax
- --
- customerservice@tocris.co.uk
- Country
- United Kingdom
- ProdList
- 5726
- Advantage
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