A muscarinic M3 receptor antagonist
Related Products
Active Metabolite(s)
278523-hydroxy Darifenacin
Labeled Version(s)
33701Darifenacin-d4
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Darifenacin (hydrobromide)

Item No. 14424

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[2-(2,3-dihydro-5-benzofuranyl)ethyl]-α,α-diphenyl-3-pyrrolidineacetamide, monohydrobromide
CAS Number
133099-07-7
Synonyms
  • UK 88525-04
Molecular Formula
C28H30N2O2 • HBr
Formula Weight
507.5
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 2 mg/mlEthanol: 0.3 mg/ml
λmax
205, 287 nm
SMILES
NC(C(C1=CC=CC=C1)(C2=CC=CC=C2)[C@H]3CN(CCC4=CC=C(OCC5)C5=C4)CC3)=O.Br
InChi Code
InChI=1S/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/t25-;/m1./s1
InChi Key
UQAVIASOPREUIT-VQIWEWKSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $75

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    25 mg

    $178

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    50 mg

    $333

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    100 mg

    $553

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    Product Description

    Darifenacin is an antagonist of M3 muscarinic acetylcholine receptors (mAChRs; Ki = 0.76 nM).1 It is selective for M3 over M1, M2, M4, and M5 mAChRs (Kis = 7.08, 44.67, 45.71, and 9.33 nM, respectively). Darifenacin selectively inhibits contractions in isolated guinea pig ileum, bladder, and trachea (pA2s = 9.44, 8.66, and 8.7, respectively), tissues that endogenously express high levels of M3 mAChRs, over isolated rabbit vas deferens and isolated guinea pig atria (pA2s = 7.9 and 7.48, respectively), which endogenously express M1 and M2 mAChRs, respectively. It inhibits micturition pressure (ED50 = 0.089 mg/kg, i.v.), as well as micturition interval and volume in rats. Formulations containing darifenacin have been used in the treatment of overactive bladder.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wallis, R.M., and Napier, C.M. Muscarinic antagonists in development for disorders of smooth muscle function. Life Sci. 64(6-7), 395-401 (1999).