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Imidafenacin

CAS No.
170105-16-5
Chemical Name:
Imidafenacin
Synonyms
Uritos;Staybla;ONO 8025;Midanacin;Midanasine;4-(2-methyL;Imidafenacin;Midana new API;)-2,2-diphenyL;Imidafenacin-d10
CBNumber:
CB11485032
Molecular Formula:
C20H21N3O
Molecular Weight:
319.4
MDL Number:
MFCD09833703
MOL File:
170105-16-5.mol
Last updated:2024-12-12 15:32:36

Imidafenacin Properties

Melting point 184-187°C
Boiling point 579.7±50.0 °C(Predicted)
Density 1.12±0.1 g/cm3(Predicted)
storage temp. Sealed in dry,Room Temperature
solubility DMSO, Methanol
pka 15.72±0.50(Predicted)
form Solid
color White
InChI InChI=1S/C20H21N3O/c1-16-22-13-15-23(16)14-12-20(19(21)24,17-8-4-2-5-9-17)18-10-6-3-7-11-18/h2-11,13,15H,12,14H2,1H3,(H2,21,24)
InChIKey SQKXYSGRELMAAU-UHFFFAOYSA-N
SMILES N1(CCC(C2=CC=CC=C2)(C2C=CC=CC=2)C(N)=O)C=CN=C1C
FDA UNII XJR8Y07LJO

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H335-H302-H319-H315
Precautionary statements  P264-P270-P301+P312-P330-P501-P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P

Imidafenacin price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
TRC I275013 Imidafenacin-d10 170105-16-5 2.5mg $250 2021-12-16 Buy
Usbiological 280397 Imidafenacin 170105-16-5 250mg $333 2021-12-16 Buy
American Custom Chemicals Corporation API0019335 IMIDAFENACIN 95.00% 170105-16-5 25MG $225.75 2021-12-16 Buy
Biosynth Carbosynth FI24546 Imidafenacin 170105-16-5 50mg $263 2021-12-16 Buy
AK Scientific X5003 Imidafenacin 170105-16-5 100mg $36 2021-12-16 Buy
Product number Packaging Price Buy
I275013 2.5mg $250 Buy
280397 250mg $333 Buy
API0019335 25MG $225.75 Buy
FI24546 50mg $263 Buy
X5003 100mg $36 Buy

Imidafenacin Chemical Properties,Uses,Production

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.

Chemical Properties

White Solid

Originator

Kyorin (Japan)

Uses

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.

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.

Definition

ChEBI: Imidafenacin is a diarylmethane.

brand name

Staybla

Mechanism of action

Imidafenacin binds to and antagonizes muscarinic M1 and M3 receptors with high affinity. It also antagonizes muscarinic M2 receptors but with lower affinity. M3 receptors stimulate the contraction of the detrusor muscle in the bladder via the release of calcium from the sarcoplasmic reticulum. M2 receptors are also present in the detrusor muscle but inhibit adenylate cyclase, which reduces the relaxation mediated by β adrenergic receptors. Finally, M1 receptors are present in the parasympathetic neurons, which release acetylcholine in the bladder. They act as an autocrine positive feedback loop and further increase the release of acetylcholine. Antagonism of these receptors by imidafenacin prevents contraction of the bladder's detrusor muscle, prevents inhibition of the relation produced by sympathetic tone, and reduces acetylcholine release. Together, these reduce the frequency of urination.

Side effects

Like all medicines, imidafenacin can cause side effects, but not everybody will experience them. This drug can cause sleepiness, blurred vision, stomach upset, constipation, and increased triglyceride levels.

Synthesis

Diphenylacetonitrile (53) was alkylated with dibromoethane in the presence of NaNH2 in toluene to give bromide compound 54. The bromide 54 was condensed with 2-methylimidazole in the presence of Et3N in hot DMF to afford 2-methylimidazole derivative 55. Hydrolysis of the cyano group of 55 with 70% sulfuric acid provided imidafenacin (VII).

Synthesis_170105-16-5

Imidafenacin Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 185)Suppliers
Supplier Tel Email Country ProdList Advantage
Beijing Hope Pharmaceutical Co., Ltd.
+86-010-67886402 +8613611125266 market@hopelife.cn China 72 58
Hebei Weibang Biotechnology Co., Ltd
+8615531157085 abby@weibangbio.com China 8807 58
Hebei Mojin Biotechnology Co., Ltd
+86 13288715578 +8613288715578 sales@hbmojin.com China 12834 58
Henan Bao Enluo International TradeCo.,LTD
+86-17331933971 +86-17331933971 deasea125996@gmail.com China 2472 58
Zibo Hangyu Biotechnology Development Co., Ltd
+86-0533-2185556 +8617865335152 Mandy@hangyubiotech.com China 10986 58
hebei hongtan Biotechnology Co., Ltd
+86-86-1913198-3935 +8617331935328 sales03@chemcn.cn China 970 58
Hebei Zhuanglai Chemical Trading Co.,Ltd
+8613343047651 admin@zlchemi.com China 3002 58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
+86-18600796368 +86-18600796368 sales@sjar-tech.com China 462 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512 info@tianfuchem.com China 21634 55
career henan chemical co
+86-0371-86658258 +8613203830695 sales@coreychem.com China 29880 58

View Lastest Price from Imidafenacin manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Imidafenacin pictures 2024-12-25 Imidafenacin
170105-16-5
US $10.00 / kg 1kg 99% 20ton Hebei Zhuanglai Chemical Trading Co.,Ltd
Imidafenacin pictures 2024-12-24 Imidafenacin
170105-16-5
US $20.00 / kg 1kg 98% 2000kg hebei hongtan Biotechnology Co., Ltd
Imidafenacin pictures 2024-12-23 Imidafenacin
170105-16-5
US $0.00 / g 1g More Than 99% 100kg/Month BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
  • Imidafenacin pictures
  • Imidafenacin
    170105-16-5
  • US $10.00 / kg
  • 99%
  • Hebei Zhuanglai Chemical Trading Co.,Ltd
  • Imidafenacin pictures
  • Imidafenacin
    170105-16-5
  • US $20.00 / kg
  • 98%
  • hebei hongtan Biotechnology Co., Ltd
  • Imidafenacin pictures
  • Imidafenacin
    170105-16-5
  • US $0.00 / g
  • More Than 99%
  • BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
ONO 8025 Staybla Uritos 1H-IMidazole-1-butanaMide,2-Methyl-a,a-diphenyl- IMidafenacin DISCONTINUED-PATENTED PRODUCT 4-(2-METHYL-1H-IMIDAZOL-1-YL)-2,2-DIPHENYLBUTANAMIDE 2-Methyl-α,α-diphenyl-1H-iMidazole-1-butanaMide 4-(2-Methyl-1-iMidazolyl)-2,2- diphenylbutanaMide Imidafenacin KRP-197; ONO-8025 Imidafenacin-d10 Midana new API 4-(2-methyL 1H-Imidazole-1-butanamide, 2-methyl-α,α-diphenyl- )-2,2-diphenyL 4-(2-methylimidazol-1-yl)-2,2-diphenylbutanamide Midanacin C20H21N3O Imidafenacin 170105-16-5 Midanasine 170105-16-5 Imidazoles, Pyrroles, Pyrazoles, Pyrrolidines Amines Heterocycles Intermediates & Fine Chemicals Pharmaceuticals