J 104129 fumarate
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).
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 500.63. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2 mL||9.99 mL||19.97 mL|
|5 mM||0.4 mL||2 mL||3.99 mL|
|10 mM||0.2 mL||1 mL||2 mL|
|50 mM||0.04 mL||0.2 mL||0.4 mL|
References are publications that support the biological activity of the product.
Mitsuya et al (1999) J-104129, a novel muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors. Bioorg.Med.Chem. 7 2555 PMID: 10632066
Mitsuya et al (2000) Discovery of a muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors among 2-[(1S,3S)-3-sulfonylaminocyclopentyl]phenylacetamide derivatives. Bioorg.Med.Chem. 8 825 PMID: 10819171
Mitsuya et al (1999) Stereoselective synthesis of a new muscarinic M3 receptor antagonist, J-104129. Bioorrg.Med.Chem.Lett. 9 2037
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Keywords: J 104129 fumarate, J 104129 fumarate supplier, Potent, selective, M3, antagonists, Muscarinic, Receptors, Acetylcholine, ACh, J104129, fumarate, 2507, Tocris Bioscience
1 Citation for J 104129 fumarate
Citations are publications that use Tocris products. Selected citations for J 104129 fumarate include:
Bader and Diener (2015) Novel aspects of cholinergic regulation of colonic ion transport. Biomed Res Int 3 e00139 PMID: 26236483
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Literature in this Area
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.