A muscarinic acetylcholine receptor antagonist
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Imidafenacin

Item No. 37420

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-methyl-α,α-diphenyl-1H-imidazole-1-butanamide
CAS Number
170105-16-5
Synonyms
  • KRP 197
  • ONO-8025
Molecular Formula
C20H21N3O
Formula Weight
319.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: Slightly solubleDMSO: Slightly soluble
SMILES
O=C(C(C1=CC=CC=C1)(CCN2C(C)=NC=C2)C3=CC=CC=C3)N
InChi Code
InChI=1S/C20H21N3O/c1-16-22-13-15-23(16)14-12-20(19(21)24,17-8-4-2-5-9-17)18-10-6-3-7-11-18/h2-11,13,15H,12,14H2,1H3,(H2,21,24)
InChi Key
SQKXYSGRELMAAU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    25 mg

    $51

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    100 mg

    $162

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    250 mg

    $279

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    500 mg

    $456

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    Product Description

    Imidafenacin is an antagonist of muscarinic acetylcholine receptors (mAChRs; Kis = 7.55, 22.6, 1.42, 8.86, and 2.63 nM, respectively, for recombinant human M1-M5 receptors).1 It binds to isolated guinea pig bladders (Kb = 0.813 nM) and inhibits ACh release from isolated rat bladders (IC50 = 0.747 nM). Imidafenacin (10-300 µg/kg) reduces urine volume in orally water-loaded rats.2 Formulations containing imidafenacin have been used in the treatment of overactive bladder.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kobayashi, F., Yageta, Y., Segawa, M., et al. Effects of imidafenacin (KRP-197/ONO-8025), a new anti-cholinergic agent, on muscarinic acetylcholine receptors. High affinities for M3 and M1 receptor subtypes and selectivity for urinary bladder over salivary gland. Arzneimittelforschung 57(2), 92-100 (2007).

    2. Yamazaki, T., Fukata, A., and Muraki, Y. Imidafenacin exerts the antidiuretic effect by enhancing vasopressin-related responses in orally water-loaded rats. Eur. J. Pharmacol. 791, 72-77 (2016).