Darifenacin

ChemicalBook > CAS DataBase List > Darifenacin

Product Name: Darifenacin
CAS No.: 133099-04-4
Chemical Name: Darifenacin
Synonyms: CS-773;UK88525;UK-88525;UK 88525;DARIFENACIN;Darifenacin, >=98%;Darifenacin USP/EP/BP;Tolafentrine Impurity 16;2-{(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl}-2,2-dip;2-{(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl}-2,2-diphe
CBNumber: CB1506695
Molecular Formula: C28H30N2O2
Formula Weight: 426.55
MOL File: 133099-04-4.mol

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Darifenacin Property

alpha: 25D -20.6° (c = 1.0 in methylene chloride)
Boiling point:: 614.3±55.0 °C(Predicted)
Density: 1.192±0.06 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: Soluble in DMSO
form: Powder
pka: pKa (25°): 9.2
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-1168
Product name: Darifenacin
Packaging: 5mg
Price: $80
Updated: 2021/12/16

Matrix Scientific

Product number: 093128
Product name: 2-(1-(2-(2,3-Dihydrobenzofuran-5-yl)ethyl)-pyrrolidin-3-yl)-2,2-diphenylacetamide
Purity: 95+%
Packaging: 250mg
Price: $567
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb146146
Product name: Darifenacin
Purity: >98%
Packaging: 100mg
Price: $578
Updated: 2021/12/16

Medical Isotopes, Inc.

Product number: D33903
Product name: Darifenacin-d4
Packaging: 1mg
Price: $640
Updated: 2021/12/16

AK Scientific

Product number: Q569
Product name: Darifenacin
Packaging: 250mg
Price: $815
Updated: 2021/12/16

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Darifenacin Chemical Properties,Usage,Production

Description

Darifenacin is a novel muscarinic M3 selective antagonist for the once-daily oral treatment of urinary incontinence and overactive bladder. The majority of overactive bladder symptoms are thought to result from the overactivity of the detrusor muscle, which is primarily mediated by acetylcholine-induced stimulation of muscarinic M3 receptors in the bladder. Consequently, antimuscarinic agents have become the mainstay of overactive bladder treatment. Darifenacin has a higher level of M3 selectivity than the previously marketed antimuscarinic agents. It has K_i values of 16nM for M1, 50 nM for M2, and 1.6 nM for M3 receptors. It is slightly more M3 selective than solifenacin (M1:K_i=25 nM, M2:K_i=126 nM, M3:K_i=10 nM), which was launched in 2004. Darifenacin is significantly more selective than other muscarinics such as tolterodine, oxybutynin, and trospium, which are all essentially equipotent against M1, M2, and M3 receptors. In addition,darifenacin demonstrates greater effect on tissues in which the predominant receptor type is M3 rather than M1 or M2. In vitro darifenacin inhibits carbacholinduced contractions with greater potency in isolated guinea-pig bladder (M3) than in guinea-pig atria (M2) or dog saphenous vein (M1). In animal models, it shows greater selectivity for inhibition of detrusor contraction over salivation or tachycardia.Darifenacin is supplied as a controlled release formulation, and the recommended dosage is 7.5 mg once, daily. Darifenacin is rapidly and completely absorbed from the GI tract after oral administration, with maximum plasma levels achieved after about 7 h. The elimination half-life is approximately 3 h, but because of the controlled release characteristics of the formulation, the drug is suitable for once-daily dosing. Steady-state plasma levels are achieved within 6 days of commencing treatment. Darifenacin exhibits high-protein binding (98%), a volume of distribution of 163 L, and a clearance of 40 L/h. It has low oral bioavailability (15–19%) due to extensive first-pass metabolism by CYP3A4 and CYP2D6, but this can be saturated after multiple administrations. The major circulating metabolites are produced by monohydroxylation and N-dealkylation; however, none contribute significantly to the overall clinical effect of darifenacin. Approximately 58% of the dose is excreted in urine and 44% in feces; only a small percentage (3%) of the excreted dose is unchanged darifenacin.

Originator

Pfizer (US)

Uses

Treatment for an overactive bladder.

Definition

ChEBI: 2-[(3S)-1-Ethylpyrrolidin-3-yl]-2,2-diphenylacetamide in which one of the hydrogens at the 2-position of the ethyl group is substituted by a 2,3-dihydro-1-benzofuran-5-yl group. It is a selective antagonist for the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions, and is used as the hydrobromide salt in the management of urinary incontinence.

brand name

Enablex (Novartis);Emselex.

Clinical Use

Symptomatic treatment of urinary incontinence,
frequency or urgency

Drug interactions

Potentially hazardous interactions with other drugs
Anti-arrhythmics: increased risk of antimuscarinic side effects with disopyramide
Antifungals: concentration increased by ketoconazole - avoid; avoid with itraconazole.
Antivirals: avoid with fosamprenavir, atazanavir, indinavir, lopinavir, ritonavir, saquinavir and tipranavir.
Calcium-channel blockers: avoid with verapamil
Ciclosporin: avoid concomitant use.

Metabolism

After an oral dose, darifenacin is subject to extensive first-pass metabolism and has a bioavailability of about 15-19%. Darifenacin is metabolised in the liver by the cytochrome P450 isoenzymes CYP2D6 and CYP3A4. Most of a dose is excreted as metabolites in the urine and faeces.

Darifenacin Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Darifenacin manufacturers

Hebei Mingeng Biotechnology Co., Ltd

Product: Darifenacin 133099-04-4
Price: US $200.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 1000kg/Month
Release date: 2022-11-27

Shijiazhuang Gantuo Biotechnology Co., Ltd

Product: Darifenacin 133099-04-4
Price: US $100.00/mg
Min. Order: 10mg
Purity: 99%
Supply Ability: 1000g
Release date: 2023-03-10

Hong Kong Tiansheng New Material Trading Co., Ltd

Product: Darifenacin 133099-04-4
Price: US $25.99/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 100KG
Release date: 2021-12-28

133099-04-4, DarifenacinRelated Search:

tadalafi ISOXADIFEN-ETHYL Acetaminophen PHENYL VALERATE Ethanol Piracetam Acetamide Trinexapac-ethyl Ethyl acetate Ethylparaben Thioacetamide Phenyl salicylate N,N-Dimethylacetamide 2-Cyanoacetamide Solifenacin Diphenyl ether PHENYL RESIN Phenylacetic acid

CS-773

2-(1-(2-(2,3-Dihydrobenzofuran-5-yl)ethyl)pyrrolidin-3-yl)-2,2-diphenylacetaMide

UK 88525

UK88525

UK-88525

2-{(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl}-2,2-dip

Darifenacin, >=98%

DARIFENACIN

2-[1-[2-(2,3-Dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-di(phenyl)acetamide

(3S)-1-[2-(2,3-Dihydro-5-benzofuranyl)ethyl]-α,α-diphenyl-3-pyrrolidineacetamide

2-{(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl}-2,2-dipheny

2-{(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl}-2,2-diphe

3-Pyrrolidineacetamide, 1-[2-(2,3-dihydro-5-benzofuranyl)ethyl]-α,α-diphenyl-, (3S)-

Darifenacin USP/EP/BP

(3S)-1-[2-(2,3-Dihydro-5-benzofuranyl)ethyl]-α-α-diphenyl-3-pyrrolidineacetamide Hydrobromide

Tolafentrine Impurity 16

133099-04-4

Pharmaceutical material and intermeidates

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