Darifenacin HBr

Catalog No.S3144 Synonyms: UK-88525

Darifenacin HBr Chemical Structure

Molecular Weight(MW): 507.46

Darifenacin is a selective M3 muscarinic receptor antagonist with pKi of 8.9.

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In DMSO USD 140 In stock
USD 110 In stock
USD 770 In stock
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Biological Activity

Description Darifenacin 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 NH71O3dHfW6ldHnvckBie3OjeR?= NF;RVWFC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJIJmfGF{LXHkdoVvd2OncITvdkBmgHC{ZYPz[YQhcW5iSFXLJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJI9nKGODTWCgcIV3\WxiYX\0[ZIhOTBibXnud{BjgSC{YXTpc4ludXWwb3Hzd4F6NCCHQ{WwQVAvODByOEKg{txO Mn\1NlE{OTB4MUC=
H292 cells MnvzSpVv[3Srb36gZZN{[Xl? MXTB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIHHkdoVv\XKpaXOgZoV1[TJicnXj[ZB1d3JiZYjwdoV{e2WmIHnuJGgzQTJiY3XscJMh[XO|ZYPz[YQh[XNic4TpcZVt[XSrb36gc4Yh[0GPUDDhZ4N2dXWuYYTpc44h[W[2ZYKgOlAhdWmwczygSWM2OD1yLkCxOVg2KM7:TR?= MnP4NlE4OjN5MkS=
HEK293 cells NETwd4JHfW6ldHnvckBie3OjeR?= MULB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIHLleIEzKGGmcnXu[ZJocWNicnXj[ZB1d3JiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjc4Pld5Nm\CCjczDjRW1RKGGlY4XteYxifGmxbjD1d4lv\yCdMUK1TX1kSU2SIHL5JJNkcW62aXzsZZRqd25iY3;1cpRqdmduIFXDOVA:OC5yMEC3PVQ{KM7:TR?= M1f1RlI2PjJ7M{m0
CHO-K1 cells MlHVSpVv[3Srb36gZZN{[Xl? M1rGN2lvcGmkaYTpc44hd2ZiZnHzeEB{d2SrdX2gZ5VzemWwdDCoTW5iMSCrbjDDbIlv\XOnIFjhcZN1\XJiT4\hdpkhMEOKTzmgT|Eh[2WubIOgeJJidnOoZXP0[YQhf2m2aDDoeY1idiCQYY[xMlUhdWWjc4Xy[YQhfXOrbnegTY9vX2:{a4OgVZVifHS{bzDheZRwdWG2ZXSgdIF1[2hiY3zhcZAheGyjdH\vdo0tKEmFNUC9NU42QDR6OTFOwG0> M3yyOlI2ODh5N{Wz
PC3 M3fvUnBzd2yrZnXyZZRqd25iYYPzZZk> NW\LXohiOTBizszNJIFv\CB{MDFOwG0> NHfwTHZjdG:la3Hk[UBw\iCFSGLNN{BjgSCmYYLp[oVv[WOrbjDjc5Vt\CCnZn\lZ5RqfmWueTDy[YR2[2ViY3XscEBxem:uaX\ldoF1cW:w MUGyOlA4OTR6Nh?=
22Rv1 MlT4VJJwdGmoZYLheIlwdiCjc4PhfS=> NF3t[YIyOCEQvF2gZY5lKDJyIN88US=> NWT0OGdT[myxY3vh[IUhd2ZiQ1jSUVMh[nliZHHybYZmdmGlaX6gZ492dGRiZX\m[YN1cX[nbImgdoVlfWOnIHPlcIwheHKxbHnm[ZJifGmxbh?= MmTLNlYxPzF2OE[=
H1299 M1\SVnBzd2yrZnXyZZRqd25iYYPzZZk> MYOwMlPjiJNzMECgxtVO NWPkRnU2PzJiaB?= M3GybJNq\26rZnnjZY51dHliaX7obYJqfGWmIFixNlk6KGOnbHygdJJwdGmoZYLheIlwdiCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? MXqyN|I5PTJ4Mx?=

... Click to View More Cell Line Experimental Data

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

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 powder
in solvent
Synonyms UK-88525

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03602508 Active not recruiting Overactive Bladder (OAB) Astellas Pharma Singapore Pte. Ltd.|Astellas Pharma Inc July 20 2018 --
NCT03572231 Recruiting Overactive Bladder (OAB) Astellas Pharma Singapore Pte. Ltd.|Astellas Pharma Inc July 19 2018 --
NCT03602508 Active not recruiting Overactive Bladder (OAB) Astellas Pharma Singapore Pte. Ltd.|Astellas Pharma Inc July 20 2018 --
NCT03572231 Recruiting Overactive Bladder (OAB) Astellas Pharma Singapore Pte. Ltd.|Astellas Pharma Inc July 19 2018 --
NCT02143570 Completed Overactive Bladder Universidad de Valparaiso|Recalcine (GynoPharm) May 2014 Phase 3
NCT02143570 Completed Overactive Bladder Universidad de Valparaiso|Recalcine (GynoPharm) May 2014 Phase 3

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AChR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID