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Imidafenacin AChR inhibitor

Cat.No.S5385

Imidafenacin (KRP-197, ONO-8025) is a urinary antispasmodic of the anticholinergic class. It is a novel antimuscarinic agent with safety and efficacy, has been clinically used for the treatment of overactive bladder. This compound is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM). IC50 value: 0.3 nM(M3).
Imidafenacin AChR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 319.40

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S538501 DMSO]63 mg/mL]false]]]false]]]false Purity: 99.6%
99.6

Chemical Information, Storage & Stability

Molecular Weight 319.40 Formula

C20H21N3O

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 170105-16-5 -- Storage of Stock Solutions

Synonyms KRP-197, ONO-8025 Smiles CC1=NC=CN1CCC(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N

Solubility

In vitro
Batch:

DMSO : 63 mg/mL ( (197.24 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
M3 receptor [1]
(Cell-free assay)
0.3 nM
M3 receptor [1]
(Cell-free assay)
0.317 nM(Kd)
M2 receptor [1]
(Cell-free assay)
4.13 nM
References

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