Darifenacin

CAT: 0804-HY-A0033-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-A0033-01Size:5 mg
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Description
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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
ERK1; ERK2; mAChR3; MMP-1
Citation 01
Br J Pharmacol. 2015 Dec;172 (23) :5619-33. |Oncotarget. 2016 Apr 5;7 (14) :18085-94. |Sci Rep. 2017 Jan 19;7:40802.|ACS Omega. 2020 Oct 12;5 (41) :26551-26561.|Eur J Pharmacol. 2011 Aug 1;663 (1-3) :74-9. |J Transl Med. 2025 Jan 23;23 (1) :112.

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