2. GPCR/G Protein Neuronal Signaling
  3. mAChR Vasopressin Receptor
  4. Imidafenacin

Imidafenacin  (Synonyms: KRP-197; ONO-8025)

Cat. No.: HY-B0662 Purity: 99.26%
COA
SDS
Handling Instructions Technical Support

Imidafenacin (KRP-197; ONO-8025) is an orally active inhibitor of muscarinic (mAChR) M1 and M3 receptors. Imidafenacin potently inhibits bladder contraction in vivo and exerts an antidiuretic effect by enhancing the signaling pathway of vasopressin (antidiuretic hormone). Imidafenacin can be used in research related to overactive bladder.

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Imidafenacin

Imidafenacin Chemical Structure

CAS No. : 170105-16-5

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Based on 1 publication(s) in Google Scholar

Other Forms of Imidafenacin:

Imidafenacin Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

Imidafenacin (KRP-197; ONO-8025) is an orally active inhibitor of muscarinic (mAChR) M1 and M3 receptors. Imidafenacin potently inhibits bladder contraction in vivo and exerts an antidiuretic effect by enhancing the signaling pathway of vasopressin (antidiuretic hormone). Imidafenacin can be used in research related to overactive bladder[1][2].

IC50 & Target[1]

mAChR1

 

mAChR3

 

In Vivo

Imidafenacin (3-300 μg/kg; i.v.; single dose) dose-dependently suppresses urine production in orally water-loaded female Sprague-Dawley rats, with a maximum 50% inhibition of vehicle group urine volume at 100 μg/kg, and exerts its antidiuretic effect by enhancing components of the vasopressin signaling pathway[1].
Imidafenacin (0.05-0.2 mg/kg; p.o.; single dose) dose-dependently prevents carbamylcholine-induced reductions in bladder capacity in conscious female rats with an ID50 of 0.055 mg/kg, and significantly lowers maximum intravesical pressure at doses of 0.05, 0.1, and 0.2 mg/kg[2].
Imidafenacin (0.0625-1 mg/kg; p.o.; singe dose) dose-dependently inhibits distention-induced rhythmic bladder contractions in conscious male rats with an ID30 of 0.17 mg/kg, with effects peaking 30-50 minutes post-dosing and lasting at least 120 minutes[2].
Imidafenacin (0.3-2.4 mg/kg; p.o.; single dose) dose-dependently inhibits carbamylcholine-induced salivary secretion in conscious male rats with an ID50 of 1.5 mg/kg[2].
Imidafenacin (1-10 mg/kg; p.o.; daily; 7 days) does not impair spatial learning or memory in male rats tested in the Morris water maze task[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (female, 220-290 g, orally water-loaded)[1]
Dosage: 3-300 μg/kg
Administration: i.v.; single dose
Result: Dose-dependently suppressed urine production, with the minimum effective dose identified as 10 μg/kg.
Produced approximately 50% inhibition of urine volume relative to the vehicle group at 100 μg/kg.
Enhanced the antidiuretic effect beyond that of either agent alone when administered at 10 μg/kg in combination with desmopressin at its minimum effective dose.
Had its antidiuretic effect completely inhibited by pretreatment with 3 mg/kg mozavaptan at 10 μg/kg and 300 μg/kg.
Further suppressed urine production compared to desmopressin alone in the presence of mozavaptan when 300 μg/kg was added to a combination of 3 mg/kg mozavaptan and 0.1 μg/kg desmopressin.
Animal Model: Wistar rats (male, 190-340 g)[2]
Dosage: 1 mg/kg; 10 mg/kg
Administration: p.o.; daily; 7 days
Result: Did not alter escape latencies during the acquisition phase compared to vehicle controls at doses of 1 mg/kg and 10 mg/kg.
Showed a significant preference for the quadrant where the platform was previously placed during the spatial probe trial at doses of 1 mg/kg and 10 mg/kg, similar to vehicle controls.
Clinical Trial
Molecular Weight

319.40

Formula

C20H21N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC(C(C1=CC=CC=C1)(C2=CC=CC=C2)CCN3C(C)=NC=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 31.25 mg/mL (97.84 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1309 mL 15.6544 mL 31.3087 mL
5 mM 0.6262 mL 3.1309 mL 6.2617 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.51 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (6.51 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.26%

SDS (396 KB)

COA (261 KB) LCMS (102 KB)

Handling Instructions (2659 KB)
References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1309 mL 15.6544 mL 31.3087 mL 78.2718 mL
5 mM 0.6262 mL 3.1309 mL 6.2617 mL 15.6544 mL
10 mM 0.3131 mL 1.5654 mL 3.1309 mL 7.8272 mL
15 mM 0.2087 mL 1.0436 mL 2.0872 mL 5.2181 mL
20 mM 0.1565 mL 0.7827 mL 1.5654 mL 3.9136 mL
25 mM 0.1252 mL 0.6262 mL 1.2523 mL 3.1309 mL
30 mM 0.1044 mL 0.5218 mL 1.0436 mL 2.6091 mL
40 mM 0.0783 mL 0.3914 mL 0.7827 mL 1.9568 mL
50 mM 0.0626 mL 0.3131 mL 0.6262 mL 1.5654 mL
60 mM 0.0522 mL 0.2609 mL 0.5218 mL 1.3045 mL
80 mM 0.0391 mL 0.1957 mL 0.3914 mL 0.9784 mL
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Imidafenacin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Imidafenacin170105-16-5KRP-197 ONO-8025KRP197KRP 197ONO8025ONO 8025ONO-8025mAChRVasopressin ReceptorMuscarinic acetylcholine receptoracetylcholinevasopressin signaling pathwayoveractive bladderSprague-Dawley ratsconscious ratsmuscarinic acetylcholine M1 receptorsmuscarinic acetylcholine M3 receptorsurinary bladdercarbamylcholinesalivary secretionInhibitorinhibitorinhibit

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