J 104129 fumarate

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Cat.No. 2507 - J 104129 fumarate | C24H36N2O2.C4H4O4 | CAS No. 257603-40-0
Description: Potent, selective M3 antagonist
Chemical Name: (αR)-α-Cyclopentyl-α-hydroxy-N-[1-(4-methyl-3-pentenyl)-4-piperidinyl]benzeneacetamide fumarate
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Literature

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
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 257603-40-0
PubChem ID 56972189
InChI Key HUCQUCITPHOUAC-DSSYAJFBSA-N
Smiles [H]OC(=O)\C=C\C(=O)O[H].C\C(C)=C\CCN1CCC(CC1)NC(=O)[C@@](O)(C1CCCC1)C1=CC=CC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 50.06 100
ethanol 25.03 50

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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID:


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Keywords: J 104129 fumarate, supplier, Potent, selective, M3, antagonists, Muscarinic, Receptors, Acetylcholine, ACh, J104129, fumarate, M3, Receptors, 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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