Darifenacin (hydrobromide)

Darifenacin (hydrobromide)

• CAS Number: 133099-07-7
• UNSPSC Description: Darifenacin (UK-88525) hydrobromide is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin hydrobromide binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin hydrobromide can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin hydrobromide inhibits tumor growth in colorectal cancer cells and has anti-tumor effects[1][2][3][4][5][6].
• Target Antigen: Akt; mAChR; p38 MAPK
• Type: Reference compound
• Related Pathways: GPCR/G Protein;MAPK/ERK Pathway;Neuronal Signaling;PI3K/Akt/mTOR
• Applications: Cancer-programmed cell death
• Field of Research: Cancer; Metabolic Disease; Neurological Disease
• Assay Protocol: https://www.medchemexpress.com/Darifenacin-hydrobromide.html
• Purity: 99.97
• Solubility: DMSO : 33.33 mg/mL (ultrasonic)
• Smiles: O=C(C(C1=CC=CC=C1)([C@@H]2CCN(CCC3=CC4=C(OCC4)C=C3)C2)C5=CC=CC=C5)N.Br
• Molecular Weight: 507.46
• 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.ACS Omega. 2020 Oct 12;5(41):26551-26561.|Eur J Pharmacol. 2011 Aug 1;663(1-3):74-9. |Br J Pharmacol. 2015 Dec;172(23):5619-33. |Oncotarget. 2016 Apr 5;7(14):18085-94. |Sci Rep. 2017 Jan 19;7:40802.
• Shipping Conditions: Room Temperature
• Storage Conditions: 4°C (Powder, sealed storage, away from moisture)
• Clinical Information: Launched