Darifenacin hydrobromide
Based on 9 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.78%
- CAS. Nr.: 133099-07-7
- Formel: C28H31BrN2O2
- Molecular Weight:507.46
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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- Reinheit & Dokumentation
- Verweise
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Publications Citing Use of MedChemExpress (MCE) Darifenacin hydrobromide
More- Cancer Cell. 2026 Jul 24:S1535-6108(26)00305-3.
- Cancer Res. 2026 Jan 14. [Abstract]
- J Neuroinflammation. 2026 May 25. [Abstract]
- J Transl Med. 2025 Jan 23;23(1):112. [Abstract]
- Br J Pharmacol. 2015 Dec;172(23):5619-33. [Abstract]
- Eur J Pharmacol. 2011 Aug 1;663(1-3):74-9. [Abstract]
- ACS Omega. 2020 Oct 12;5(41):26551-26561. [Abstract]
- Sci Rep. 2017 Jan 19:7:40802. [Abstract]
- Oncotarget. 2016 Apr 5;7(14):18085-94. [Abstract]
Customer Validation & Images
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WB
Biologische Aktivität
Beschreibung
IC50 & Target
[3]|
mAChR3 |
MMP-1 |
ERK1 |
ERK2 |
In Vitro
Non-salt dose:
Darifenacin (0.01-100 μM; 5 min) inhibits the Kv currents in concentration-dependent manners with an IC50 value of 0.34 μM and a Hill coefficient of 0.84 in coronary arterial smooth muscle cells[2].
Darifenacin (0.01-10 μM; 1-48 h) inhibits cell viability, invasion and MMP-1 expression in colorectal cancer cells, and inhibits the phosphorylation of p38, ERK1/2 and Akt induced by muscarinic acetylcholine [3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HT-29 and SW480 cells
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Concentration:0.01, 0.1, 1 and 10 μM
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Incubation Time:48 h
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Result:Reduced viability and proliferation at a concentration of 10 µM in both cell lines HT29 and SW480.
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Cell Line:HT-29 cells
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Concentration:0.1, 1 and 10 μM
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Incubation Time:1 h
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Result:Inhibited the phosphorylation levels of p38, ERK1/2 and Akt.
In Vivo
Darifenacin (2.5 mg/kg; intraperitoneal injection; 42 days) has an antitumor effect in a xenograft mouse model of colorectal cancer[3].
Darifenacin (0.1 mg/kg; intravenous injection; Single dose) decreases the afferent activity of bladder Aδ and C fibers in female rats[4].
Darifenacin (3 mg/kg/day; subcutaneous osmotic pump; 14 weeks) increases the severity of liver damage caused by Azoxymethane (HY-111375)[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HT-29 cells treated male BALB/cnu/nu nude mice aged 6-10 weeks old (20-25 g)[3]
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Dosage:2.5 mg/kg
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Administration:Intraperitoneal injection (i.p.); 42 days
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Result:Reduced primary tumor volume and weight, as well as liver metastases.
Had no significant effect on the weight of mice.
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Animal Model:Azoxymethane (HY-111375) treated male mice [genetic background: 129S6/SvEv X CF1 (50%:50%)][5]
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Dosage:3 mg/kg/day
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Administration:Subcutaneous osmotic pump; 14 weeks
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Result:Caused the mice weigh less, reduced liver-weight-to-body-weight ratios.
Increased liver nodularity and Ishak fibrosis scores.
Increased in ductular proliferation.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 133099-07-7
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Appearance Solid
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Molecular Weight 507.46
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Formel C28H31BrN2O2
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Color White to off-white
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SMILES
O=C(C(C1=CC=CC=C1)([C@@H]2CCN(CCC3=CC4=C(OCC4)C=C3)C2)C5=CC=CC=C5)N.Br
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Synonyms
UK-88525 hydrobromide
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (9)
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Journal Impact Factor
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Most Recent
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Cancer Res
Nerves Stimulates Crosstalk between Gastric Cancer and Group 3 Innate Lymphoid Cells to Enhance Immunosuppression. [Abstract]2026 Jan 14. PMID: 41534088 -
J Neuroinflammation
PVNOXT regulates acinar cell-mediated inflammatory response via DMVACh projections to the acinar cell. [Abstract]2026 May 25. PMID: 42186091 -
J Transl Med
Increased nerve density adversely affects outcome in colorectal cancer and denervation suppresses tumor growth. [Abstract]2025 Jan 23;23(1):112. PMID: 39849539 -
Br J Pharmacol
Activation of M3 cholinoceptors attenuates vascular injury after ischaemia/reperfusion by inhibiting the Ca2+/calmodulin-dependent protein kinase II pathway. [Abstract]2015 Dec;172(23):5619-33. PMID: 25953628 -
Eur J Pharmacol
2011 Aug 1;663(1-3):74-9. PMID: 21596029 -
ACS Omega
2020 Oct 12;5(41):26551-26561. PMID: 33110983 -
Sci Rep
Acetylcholine acts through M3 muscarinic receptor to activate the EGFR signaling and promotes gastric cancer cell proliferation. [Abstract]2017 Jan 19:7:40802. PMID: 28102288 -
Oncotarget
MACC1 mediates acetylcholine-induced invasion and migration by human gastric cancer cells. [Abstract]2016 Apr 5;7(14):18085-94. PMID: 26919111
Darifenacin hydrobromide purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Apr 5;7(14):18085-94. [Abstract]
MACC1 is up-regulated by ACh through p-AMPK. A. ACh stimulates AMPK phosphorylation via M3R. B. Inhibition of AMPK activity by Dorsomorphin (8 μM) suppresses the induction of MACC1 expression by ACh. p-AMPK levels increase after ACh stimulation, and pretreatment of Darifenacin attenuates the ACh-induced increase of p-AMPK.
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 33.33 mg/mL (65.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
Reinheit & Dokumentation
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Data Sheet (283 KB)
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SDS (393 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[2]. 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. [Content Brief]
[3]. 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. [Content Brief]
[4]. 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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9706 mL | 9.8530 mL | 19.7060 mL | 49.2650 mL |
| 5 mM | 0.3941 mL | 1.9706 mL | 3.9412 mL | 9.8530 mL | |
| 10 mM | 0.1971 mL | 0.9853 mL | 1.9706 mL | 4.9265 mL | |
| 15 mM | 0.1314 mL | 0.6569 mL | 1.3137 mL | 3.2843 mL | |
| 20 mM | 0.0985 mL | 0.4926 mL | 0.9853 mL | 2.4632 mL | |
| 25 mM | 0.0788 mL | 0.3941 mL | 0.7882 mL | 1.9706 mL | |
| 30 mM | 0.0657 mL | 0.3284 mL | 0.6569 mL | 1.6422 mL | |
| 40 mM | 0.0493 mL | 0.2463 mL | 0.4926 mL | 1.2316 mL | |
| 50 mM | 0.0394 mL | 0.1971 mL | 0.3941 mL | 0.9853 mL | |
| 60 mM | 0.0328 mL | 0.1642 mL | 0.3284 mL | 0.8211 mL |
Darifenacin hydrobromide Related Classifications
HY-A0012 Related Classifications
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