J 104129 fumarate

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2507/10
J 104129 fumarate | CAS No. 257603-40-0 | mAChR M3 Antagonists
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Description: Potent and selective M3 antagonist

Chemical Name: (αR)-α-Cyclopentyl-α-hydroxy-N-[1-(4-methyl-3-pentenyl)-4-piperidinyl]benzeneacetamide fumarate

Purity: ≥99%

Product Details
Citations (1)
Supplemental Products
Reviews

Biological Activity

Potent M3 muscarinic receptor antagonist that displays ~ 120-fold selectivity over M2 receptors (Ki values are 4.2, 19 and 490 nM for human M3, M1 and M2 receptors respectively). Exhibits > 250-fold bronchial selectivity; inhibits ACh-induced bronchoconstriction but not ACh-induced bradycardia (KB values are 3.3 and 170 nM for rat trachea M3 and rat right atria M2 receptors respectively).

Technical Data

M.Wt:
500.63
Formula:
C24H36N2O2.C4H4O4
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol
Purity:
≥99%
Storage:
Store at +4°C
CAS No:
257603-40-0

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. J-104129, a novel muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors.
    Mitsuya et al.
    Bioorg.Med.Chem., 1999;7:2555
  2. Discovery of a muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors among 2-[(1S,3S)-3-sulfonylaminocyclopentyl]phenylacetamide derivatives.
    Mitsuya et al.
    Bioorg.Med.Chem., 2000;8:825
  3. Stereoselective synthesis of a new muscarinic M3 receptor antagonist, J-104129.
    Mitsuya et al.
    Bioorrg.Med.Chem.Lett., 1999;9:2037

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Citation for J 104129 fumarate

The citations listed below are publications that use Tocris products. Selected citations for J 104129 fumarate include:

1 Citation: Showing 1 - 1

  1. Novel aspects of cholinergic regulation of colonic ion transport.
    Authors: Bader and Diener
    Biomed Res Int  2015;3:e00139

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