Darifenacin

Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects[1][2][3][4][5][6].

Product Specifications

CAS Number

[133099-04-4]

Product Name Alternative

UK-88525

UNSPSC

12352005

Target

Akt; mAChR; p38 MAPK

Type

Reference compound

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway; Neuronal Signaling; PI3K/Akt/mTOR

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer; Metabolic Disease; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/darifenacin.html

Purity

99.81

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(N)C(C1=CC=CC=C1)([C@H]2CN(CCC3=CC=C(OCC4)C4=C3)CC2)C5=CC=CC=C5

Molecular Formula

C28H30N2O2

Molecular Weight

426.55

References & Citations

[1]Hegde SS, et al. Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo. Br J Pharmacol, 1997, 120 (8), 1409-1418.|[2]Iijima K, et al. Effects of the M3 receptor selective muscarinic antagonist darifenacin on bladder afferent activity of the rat pelvic nerve. Eur Urol, 2007, 52 (3), 842-847.|[3]Seo MS, et al. Suppression of voltage-gated K+ channels by darifenacin in coronary arterial smooth muscle cells. Eur J Pharmacol. 2021 Jan 15;891:173707. |[4]Hering NA, et al. Blockage of Cholinergic Signaling via Muscarinic Acetylcholine Receptor 3 Inhibits Tumor Growth in Human Colorectal Adenocarcinoma. Cancers (Basel) . 2021 Jun 28;13 (13) :3220.|[5]Khurana S, et al. Effects of modulating M3 muscarinic receptor activity on azoxymethane-induced liver injury in mice. Biochem Pharmacol. 2013 Jul 15;86 (2) :329-38.|[6]Yamada S, et al. In vivo demonstration of M3 muscarinic receptor subtype selectivity of darifenacin in mice. Life Sci. 2006 Dec 14;80 (2) :127-32.