J 104129 fumarate

Name: J 104129 fumarate
Brand: Tocris Bioscience
SKU: 2507

Tocris Bioscience, part of Bio-Techne | Catalog # 2507

Citations (4)

COA / SDS

Potent and selective M3 antagonist

Key Product Details

Description:	Potent and selective M₃ antagonist
Chemical Name:	(αR)-α-Cyclopentyl-α-hydroxy-N-[1-(4-methyl-3-pentenyl)-4-piperidinyl]benzeneacetamide fumarate
Purity:	≥98% (HPLC)
Molecular Weight:	500.63

View Full Technical Details for J 104129 fumarate

Technical Data
Citations

Biological Activity for J 104129 fumarate

J 104129 fumarate is a potent M₃ muscarinic receptor antagonist that displays ~ 120-fold selectivity over M₂ receptors (K_i 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 (K_B 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	≥98% (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 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	2.00 mL	9.99 mL	19.97 mL
5 mM	0.40 mL	2.00 mL	3.99 mL
10 mM	0.20 mL	1.00 mL	2.00 mL
50 mM	0.04 mL	0.20 mL	0.40 mL

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References for J 104129 fumarate

References are publications that support the biological activity of the product.

Mitsuya 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. 2000 PMID: 10819171
Mitsuya Stereoselective synthesis of a new muscarinic M₃ receptor antagonist, J-104129. Bioorrg.Med.Chem.Lett.
Mitsuya J-104129, a novel muscarinic M₃ receptor antagonist with high selectivity for M₃ over M₂ receptors. Bioorg.Med.Chem. 1999 PMID: 10632066