Cat. No.: HY-A0012

Darifenacin hydrobromide

(Synonyms: UK-88525 hydrobromide)

8 Cited Publications

Customer Review

Based on 8 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.

For research use only. We do not sell to patients.

Purity: 99.78%
CAS No.: 133099-07-7
Formula: C₂₈H₃₁BrN₂O₂
Molecular Weight:507.46

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Darifenacin hydrobromide Chemical Structure

CAS No.: 133099-07-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[3]

mAChR3

MMP-1

ERK1

ERK2

All mAChR Isoforms :

All p38 MAPK Isoforms :

All Akt Isoforms :

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.

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

Non-salt dose:
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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 133099-07-7
Appearance Solid
Molecular Weight 507.46
Formula C₂₈H₃₁BrN₂O₂
Color White to off-white
SMILES

O=C(C(C1=CC=CC=C1)([C@@H]2CCN(CCC3=CC4=C(OCC4)C=C3)C2)C5=CC=CC=C5)N.Br
Synonyms

UK-88525 hydrobromide
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (8)

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
J Neuroinflammation

PVNOXT regulates acinar cell-mediated inflammatory response via DMVACh projections to the acinar cell. [Abstract]

2026 May 25. PMID: 42186091
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 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.

Solvent & Solubility

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)

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

1.9706 mL

9.8530 mL

19.7060 mL

5 mM

0.3941 mL

1.9706 mL

3.9412 mL

10 mM

0.1971 mL

0.9853 mL

1.9706 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 (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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

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Molecular Weight Molecular Weight

Dilution Calculator

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

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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 (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.

Protocol 2

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Handling Instructions (2659 KB)

References

[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

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

Keywords

Darifenacin hydrobromide

8 Cited Publications

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Darifenacin hydrobromide

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Publications Citing Use of MedChemExpress (MCE) Darifenacin hydrobromide

All mAChR Isoforms

All p38 MAPK Isoforms

All Akt Isoforms

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Purity & Documentation

References