Darifenacin
Based on 10 publication(s) in Google Scholar
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.81%
- CAS 番号: 133099-04-4
- 分子式: C28H30N2O2
- 分子量:426.55
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Darifenacin
More- Cancer Cell. 2026 Jul 24:S1535-6108(26)00305-3.
- Cancer Res. 2026 Jan 14. [Abstract]
- Cell Rep Med. 2026 Sep 15;7(9):102994.
- 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
生物活性
製品説明
IC50 & Target
[3]|
mAChR3 |
ERK1 |
ERK2 |
MMP-1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
>10 μM
Compound: 1
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Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase in GTPgamma35S binding by scintillation proximity assay
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase in GTPgamma35S binding by scintillation proximity assay
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[PMID: 22932315] |
| HEK293 | EC50 |
0.82 nM
Compound: 4
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Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
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[PMID: 21310610] |
| HEK293 | EC50 |
11 nM
Compound: 2
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Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition a
Antagonist activity at muscarinic M3 receptor (unknown origin) expressed in HEK293 cells coexpressing EA tagged beta-arrestin2 assessed as inhibition of carbachol-induced beta-arrestin2 recruitment preincubated for 30 mins followed by carbachol addition a
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[PMID: 32202101] |
| HEK293 | EC50 |
32 nM
Compound: 2
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Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
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[PMID: 32202101] |
| HEK293 | EC50 |
45 nM
Compound: 2
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Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
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[PMID: 32202101] |
体外実験
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.
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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.
体内実験
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.
化学情報
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CAS 番号 133099-04-4
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性状 Solid
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分子量 426.55
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分子式 C28H30N2O2
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Color White to off-white
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SMILES
O=C(N)C(C1=CC=CC=C1)([C@H]2CN(CCC3=CC=C(OCC4)C4=C3)CC2)C5=CC=CC=C5
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別名
UK-88525
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (10)
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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 -
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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 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.
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (234.44 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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 (5.86 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (5.86 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
純度とドキュメンテーション
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データシート (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[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. 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 | 2.3444 mL | 11.7220 mL | 23.4439 mL | 58.6098 mL |
| 5 mM | 0.4689 mL | 2.3444 mL | 4.6888 mL | 11.7220 mL | |
| 10 mM | 0.2344 mL | 1.1722 mL | 2.3444 mL | 5.8610 mL | |
| 15 mM | 0.1563 mL | 0.7815 mL | 1.5629 mL | 3.9073 mL | |
| 20 mM | 0.1172 mL | 0.5861 mL | 1.1722 mL | 2.9305 mL | |
| 25 mM | 0.0938 mL | 0.4689 mL | 0.9378 mL | 2.3444 mL | |
| 30 mM | 0.0781 mL | 0.3907 mL | 0.7815 mL | 1.9537 mL | |
| 40 mM | 0.0586 mL | 0.2930 mL | 0.5861 mL | 1.4652 mL | |
| 50 mM | 0.0469 mL | 0.2344 mL | 0.4689 mL | 1.1722 mL | |
| 60 mM | 0.0391 mL | 0.1954 mL | 0.3907 mL | 0.9768 mL | |
| 80 mM | 0.0293 mL | 0.1465 mL | 0.2930 mL | 0.7326 mL | |
| 100 mM | 0.0234 mL | 0.1172 mL | 0.2344 mL | 0.5861 mL |
Darifenacin 関連分類
HY-A0033 関連分類
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