Darifenacin hydrobromide
Darifenacin hydrobromide
CAS: 133099-07-7
Molecular Formula: C28H29BrN2O2
Darifenacin hydrobromide - Names and Identifiers
| Name | Darifenacin hydrobromide |
| Synonyms | Darifenacin HBr Darifenacin hydrobro DARFENACIN HYDROBROMIDE Darifenacin hydrobromide Darifenacine Hydrobromide Darifenacin hydrobroMide R {1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]-3-pyrrolidnyl}-2,2-diphenylacetamide hydrobromide (3S)-1-[2-(2,3-Dihydro-5-benzofuranyl)ethyl]-α-α-diphenyl-3-pyrrolidineacetaMide HydrobroMide 2-[(3S)-1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenyl-acetamide hydrobromide 2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenyl-ethanamide hydrobromide Darifenacin Hydrobromide ((3S)-1-[2-(2,3-Dihydro-5-benzofuranyl)ethyl]-a-a-diphenyl-3-pyrrolidineacetamide Hydrobromide |
| CAS | 133099-07-7 |
| EINECS | 603-705-7 |
| InChI | InChI=1/C28H30N2O2.BrH/c29-27(31)28(23-7-3-1-4-8-23,24-9-5-2-6-10-24)25-14-17-30(20-25)16-13-21-11-12-26-22(19-21)15-18-32-26;/h1-12,19,25H,13-18,20H2,(H2,29,31);1H |
Darifenacin hydrobromide - Physico-chemical Properties
| Molecular Formula | C28H29BrN2O2 |
| Molar Mass | 505.44606 |
| Melting Point | 228-2300C |
| Boling Point | 637°C at 760 mmHg |
| Specific Rotation(α) | 25D -30.3° (c = 1.0 in methylene chloride) |
| Flash Point | 339°C |
| Solubility | DMSO: soluble20mg/mL, clear |
| Vapor Presure | 1.11E-16mmHg at 25°C |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | -20°C |
| Use | Darifenacin HBr is a selective M3 muscarinic(M3 muscarinic) receptor antagonist with pKi of 8.9. |
| In vitro study | Darifenacin shifted the agonist curve non-parallel to the right and significantly inhibited the maximal response of (+)-cis-dioxolane to produce concentration-dependent contractions in the isolated rat bladder. Darifenacin produced a concentration-dependent increase in R123 (P-glycoprotein probe) accumulation in MDCK Cells. Darifenacin stimulated ATPase activity in P-gp cell membranes in a concentration-dependent response manner, with an ED50 value of 1.6 µm apparently estimated. Darifenacin (100 nM) exhibited significantly greater permeability in the basal-to-apical direction, resulting in an efflux rate of approximately 2.6 for the BBMEC monolayer. |
| In vivo study | Darifenacin dose-dependently inhibited the amplitude of volume-induced bladder contraction (VIBC AMP), producing a 35% inhibition at a dose of 283.3 nmol/kg, with a maximum inhibition of about 50-55%. In female Sprague-Dawley rats, Darifenacin (0.1 mg/kg I. v.) decreased bladder afferent A δ and C fiber activity, and the reduction of the peak on the C fiber may be more significant than the reduction on the δ fiber. In patients with overactive bladder (OAB), Darifenacin (7.5 mg and 15 mg daily) reduced the number of weekly incontinence episodes to 67.7 and 72.8 percent of baseline, respectively, the placebo was only reduced to 55.9 percent. In patients with overactive bladder (OAB), Darifenacin (7.5 mg and 15 mg, daily) improves voiding frequency, bladder capacity, frequency and severity of urinary urgency, and the number of occurrences of urinary incontinence, the effect was significantly better than placebo. |
Darifenacin hydrobromide - Risk and Safety
| WGK Germany | 3 |
| HS Code | 2934990002 |
Darifenacin hydrobromide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.971 ml | 9.853 ml | 19.706 ml |
| 5 mM | 0.394 ml | 1.971 ml | 3.941 ml |
| 10 mM | 0.197 ml | 0.985 ml | 1.971 ml |
| 5 mM | 0.039 ml | 0.197 ml | 0.394 ml |
Last Update：2024-01-02 23:10:35
Darifenacin hydrobromide - Reference Information
| biological activity | Darifenacin HBr (UK-88525) is a selective M3 muscarinic(M3 muscarinic) receptor antagonist, pKi is 8.9. |
| Target | Value |
| M3 mAChR | 8.9(pKi) |
| use | treat patients with overactive bladder (OAB) accompanied by urge urinary incontinence, urgency and frequent urination. |
Last Update：2024-04-09 15:16:47
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Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
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Product Name: Darifenacin HBr Visit Supplier Webpage Request for quotationCAS: 133099-07-7
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Mobile: 18021002903
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