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Submit ReviewJ 104129 fumarate
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% (HPLC)
Biological Activity for J 104129 fumarate
J 104129 fumarate is a 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).
Compound Libraries for J 104129 fumarate
J 104129 fumarate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for J 104129 fumarate
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for J 104129 fumarate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 50.06 | 100 | |
| ethanol | 25.03 | 50 |
Preparing Stock Solutions for J 104129 fumarate
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 |
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Product Datasheets for J 104129 fumarate
References for J 104129 fumarate
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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