Darifenacin HBr

Catalog No.S3144 Synonyms: UK-88525

For research use only.

Darifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.

Darifenacin HBr Chemical Structure

CAS No. 133099-07-7

Selleck's Darifenacin HBr has been cited by 1 Publication

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Biological Activity

Description Darifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.
Targets
M3 mAChR [1]
8.9(pKi)
In vitro

Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced concentration-dependent contraction of the isolated bladder of rat. [1] Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6 µM. Darifenacin (100 nM) shows a significantly greater permeability for darifenacin in the basolateral to apical direction resulting in an efflux ratio in BBMEC monolayers of approximately 2.6. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK cells NVfESHRxTnWwY4Tpc44h[XO|YYm= MlPSRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDi[ZRiOi2jZILlco9k\XC2b4Kg[ZhxemW|c3XkJIlvKEiHSzDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDv[kBkSU2SIHzleoVtKGGodHXyJFExKG2rboOgZpkhemGmaX;pcY12dm:jc4PhfUwhTUN3ME2wMlAxODh{IN88US=> NXvDRldrOjF|MUC2NVA>
H292 cells MUPGeY5kfGmxbjDhd5NigQ>? NX7rTlF7SWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBi\HKnbnXy[4lkKGKndHGyJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCKMkmyJINmdGy|IHHzd4V{e2WmIHHzJJN1cW23bHH0bY9vKG:oIHPBUXAh[WOldX31cIF1cW:wIHHmeIVzKDZyIH3pcpMtKEWFNUC9NE4xOTV6NTFOwG0> MoO3NlE4OjN5MkS=
HEK293 cells MmeySpVv[3Srb36gZZN{[Xl? MkLhRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDi[ZRiOiCjZILlcoVz\2mlIILlZ4VxfG:{IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ2FOWCCjY3P1cZVt[XSrb36geZNqdmdiW{GyOWle[0GPUDDifUB{[2mwdHnscIF1cW:wIHPveY51cW6pLDDFR|UxRTBwMECwO|k1OyEQvF2= MXOyOVYzQTN7NB?=
CHO-K1 cells M13RXGZ2dmO2aX;uJIF{e2G7 MnTvTY5pcWKrdHnvckBw\iCoYYP0JJNw\Gm3bTDjeZJz\W62IDjJUoEqKGmwIFPobY5me2ViSHHtd5RmeiCRdnHyfUApS0iRKTDLNUBk\WyuczD0doFve2[nY4Tl[EB4cXSqIHj1cYFvKE6jdkGuOUBu\WG|dYLl[EB2e2mwZzDJc45Yd3KtczDReYF1fHKxIHH1eI9u[XSnZDDwZZRkcCClbHHtdEBxdGG2Zn;ycUwhUUN3ME2xMlU5PDh7IN88US=> M4nVfVI2ODh5N{Wz
PC3 Mlz1VJJwdGmoZYLheIlwdiCjc4PhfS=> NILPSZEyOCEQvF2gZY5lKDJyIN88US=> MlHKZoxw[2ujZHWgc4YhS0iUTUOgZpkh\GG{aX\lcoFkcW5iY3;1cIQh\W[oZXP0bZZmdHlicnXkeYNmKGOnbHygdJJwdGmoZYLheIlwdg>? M{LjUFI3ODdzNEi2
22Rv1 NXTBNndRWHKxbHnm[ZJifGmxbjDhd5NigQ>? MmfjNVAh|ryPIHHu[EAzOCEQvF2= NUL0ZY5q[myxY3vh[IUhd2ZiQ1jSUVMh[nliZHHybYZmdmGlaX6gZ492dGRiZX\m[YN1cX[nbImgdoVlfWOnIHPlcIwheHKxbHnm[ZJifGmxbh?= MYqyOlA4OTR6Nh?=
H1299 NWXCeYZ[WHKxbHnm[ZJifGmxbjDhd5NigQ>? MYewMlPjiJNzMECgxtVO M1m2ZVczKGh? NHfiW|l{cWewaX\pZ4FvfGy7IHnubIljcXSnZDDINVI6QSClZXzsJJBzd2yrZnXyZZRqd25iaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? NF;idIwzOzJ6NUK2Ny=>
In vivo Darifenacin produces dose-dependent inhibition of amplitude of volume-induced bladder contractions(VIBCAMP), producing 35% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50–55%. [1] Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers. [3] Darifenacin (7.5 mg and 15 mg, daily) reduces the number of incontinence episodes per week from baseline by 67.7% and 72.8% respectively compared with 55.9% with placebo in patients with overactive bladder (OAB). Darifenacin (7.5 mg and 15 mg, daily) also shows significantly superior to placebo for improvements in micturition frequency, bladder capacity, frequency of urgency, severity of urgency and number of incontinence episodes leading to a change in clothing or pads in patients with overactive bladder (OAB). [4]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(197.05 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 507.46
Formula

C28H30N2O2.HBr

CAS No. 133099-07-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5.Br

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00712322 Terminated Drug: Darifenacin Neurogenic Detrusor Overactivity Warner Chilcott October 31 2008 Phase 2
NCT00703703 Completed Drug: Darifenacin|Drug: Tolterodine|Drug: Placebo Healthy Novartis|Procter and Gamble May 2008 Phase 1
NCT00921245 Completed Drug: Darifenacin (Emselex BAY79-4998) Overactive Bladder Bayer June 2007 --
NCT00413790 Completed Drug: Darifenacin|Drug: Tolterodine|Drug: Placebo Healthy Novartis|Procter and Gamble November 2006 Phase 4
NCT00413426 Completed Drug: Darifenacin (DAR328) Healthy Novartis|Procter and Gamble June 2006 Phase 1
NCT00366002 Completed Drug: Darifenacin Overactive Bladder (OAB) Novartis|Procter and Gamble June 2006 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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