Cat. No.: HY-A0033

Darifenacin

(Synonyms: UK-88525)

7 Cited Publications

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Based on 7 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.

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Pureté: 99.81%
CAS No.: 133099-04-4
Formule: C₂₈H₃₀N₂O₂
Masse moléculaire:426.55

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Darifenacin Chemical Structure

CAS No.: 133099-04-4

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (7)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

IC₅₀ & Target^[3]

mAChR3

ERK1

ERK2

MMP-1

Voir tous les produits spécifiques à Isoform mAChR :

Voir tous les produits spécifiques à Isoform p38 MAPK :

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Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	>10 μM Compound: 1	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	[PMID: 22932315]
HEK293	EC₅₀	0.82 nM Compound: 4	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	[PMID: 21310610]
HEK293	EC₅₀	11 nM Compound: 2	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	[PMID: 32202101]
HEK293	EC₅₀	32 nM Compound: 2	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	[PMID: 32202101]
HEK293	EC₅₀	45 nM Compound: 2	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	[PMID: 32202101]

In Vitro

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.

Cell Viability Assay^[3]

Cell Line:

HT-29 and SW480 cells
Concentration:

0.01, 0.1, 1 and 10 μM
Incubation Time:

48 h
Result:

Reduced viability and proliferation at a concentration of 10 µM in both cell lines HT29 and SW480.

Western Blot Analysis^[3]

Cell Line:

HT-29 cells
Concentration:

0.1, 1 and 10 μM
Incubation Time:

1 h
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.

Animal Model:

HT-29 cells treated male BALB/c^nu/nu nude mice aged 6-10 weeks old (20-25 g)^[3]
Dosage:

2.5 mg/kg
Administration:

Intraperitoneal injection (i.p.); 42 days
Result:

Reduced primary tumor volume and weight, as well as liver metastases.
Had no significant effect on the weight of mice.

Animal Model:

Azoxymethane (HY-111375) treated male mice [genetic background: 129S6/SvEv X CF1 (50%:50%)]^[5]
Dosage:

3 mg/kg/day
Administration:

Subcutaneous osmotic pump; 14 weeks
Result:

Caused the mice weigh less, reduced liver-weight-to-body-weight ratios.
Increased liver nodularity and Ishak fibrosis scores.
Increased in ductular proliferation.

Chemical Information

CAS No. 133099-04-4
Appearance Solid
Masse moléculaire 426.55
Formule C₂₈H₃₀N₂O₂
Color White to off-white
SMILES

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

UK-88525
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (7)

All WB

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Journal Impact Factor

Cancer Res

Nerves Stimulates Crosstalk between Gastric Cancer and Group 3 Innate Lymphoid Cells to Enhance Immunosuppression. [Abstract]

2026 Jan 14. PMID: 41534088
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
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
Eur J Pharmacol

The effects of jatrorrhizine on contractile responses of rat ileum. [Abstract]

2011 Aug 1;663(1-3):74-9. PMID: 21596029
ACS Omega

Machine Learning for Discovery of GSK3β Inhibitors. [Abstract]

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.

Solvant et solubilité

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3444 mL

11.7220 mL

23.4439 mL

5 mM

0.4689 mL

2.3444 mL

4.6888 mL

10 mM

0.2344 mL

1.1722 mL

2.3444 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass

Concentration

Volume

Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (5.86 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
Animal Weight (Per Animal)
g
Dosing Volume (Per Animal)
μL
Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
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)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Darifenacin

7 Cited Publications

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Darifenacin

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Publications Citing Use of MedChemExpress (MCE) Darifenacin

Voir tous les produits spécifiques à Isoform mAChR

Voir tous les produits spécifiques à Isoform p38 MAPK

Voir tous les produits spécifiques à Isoform Akt

Activité biologique

Chemical Information

Publications (7)

Solvant et solubilité

Pureté et documentation