Chemical Property of Imidafenacin
Chemical Property:
- Vapor Pressure:1.96E-13mmHg at 25°C
- Refractive Index:1.602
- Boiling Point:579.709 °C at 760 mmHg
- PKA:15.72±0.50(Predicted)
- Flash Point:304.397 °C
- PSA：61.90000
- Density:1.128 g/cm3
- LogP:4.20290
- Storage Temp.:Sealed in dry,Room Temperature
- Solubility.:DMSO, Methanol
- XLogP3:2.7
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:2
- Rotatable Bond Count:6
- Exact Mass:319.168462302
- Heavy Atom Count:24
- Complexity:395
- Purity/Quality:
-
99% *data from raw suppliers
Imidafenacin *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CC1=NC=CN1CCC(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N
- Recent ClinicalTrials:A Registry Study of Patients Initiating a Course of Drug Therapy for Overactive Bladder in Taiwan, Korea and China
- Recent NIPH Clinical Trials:Combined effect of vibegron and imidafenacin
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Description
Imidafenacin, an M3/M1 muscarinic receptor antagonist, was introduced in
Japan for the oral treatment of OAB. The majority of OAB symptoms are
thought to result from overactivity of the detrusor muscle, which is primarily
mediated by acetylcholine-induced stimulation of muscarinic M3 receptors in the
bladder. Previously marketed muscarinic antagonists for OAB include propiverine,
tolterodine, oxybutynin, trospium, darifenacin, and solifenacin. In vitro,
imidafenacin is equally active against M1 and M3 receptors (Kb＝0.32 and
0.55nM, respectively), and approximately 10-fold less active against M2 receptors
(Kb＝4.13nM). Imidafenacin is chemically synthesized in three steps starting with alkylation of diphenylacetonitrile with dibromoethane, followed by condensation with 2-methylimidazole, and hydrolysis of the cyano group to a carboxamide group with 70% sulfuric acid.
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Uses
A novel therapeutic agent for overactive bladder with antimuscarinic activity, on mediator release from urothelium and detrusor overactivity induced by cerebral infarction. A muscarinic antagonist. Imidafenacin-d10 is deutirium labelled imidafenacin which is a novel therapeutic agent for overactive bladder with antimuscarinic activity, on mediator release from urothelium and detrusor overactivity induced by cerebral infarction.
