Tocris/Zamifenacin fumarate/2579/10/10 mg-蚂蚁淘生物

Description: Selective M₃ antagonist Alternative Names: UK 76654 Chemical Name: (3R)-1-[2-(1-,3-Benzodioxol-5-yl)ethyl]-3-(diphenylmethoxy)piperidine fumarate Purity: ≥99% (HPLC) Biological Activity Technical Data Solubility Calculators DatasheetsReferences

Biological Activity

Selective M₃ muscarinic receptor antagonist (pK_i values are 8.52, 7.93, 7.90 and 7.78 for M₃, M₂, M₁ and M₄ receptors respectively). Displays higher affinity at ileal M₃ receptors (pK_i = 9.3) compared to oesophageal and tracheal M₃ receptors (pK_i values are 8.8 and 8.2 respectively). Inhibits gastrointestinal motility in vivo in the absence of cardiovascular effects.

Compound Libraries

Zamifenacin fumarate is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	531.6
Formula	C₂₇H₂₉NO₃.C₄H₄O₄
Storage	Desiccate at +4°C
Purity	≥99% (HPLC)
CAS Number	127308-98-9
PubChem ID	20056967
InChI Key	PMHKTAIGYOVZEZ-ZHWJIHCSSA-N
Smiles	C1(CCN3C[C@H](OC(C5=CC=CC=C5)C4=CC=CC=C4)CCC3)=CC=C(OCO2)C2=C1.C(C=CC(O[H])=O)(O[H])=O

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	53.16	100
ethanol	13.29	25

Preparing Stock Solutions

The following data is based on the product molecular weight 531.6. 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.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg

1 mM	1.88 mL	9.41 mL	18.81 mL
5 mM	0.38 mL	1.88 mL	3.76 mL
10 mM	0.19 mL	0.94 mL	1.88 mL
50 mM	0.04 mL	0.19 mL	0.38 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet Safety Datasheet Select another language: English German French Spanish View SDS

References

References are publications that support the products\' biological activity.

Wallis (1995) Pre-clinical and clinical pharmacology of selective muscarinic M₃ receptor antagonists. Life Sci. 56 861 PMID: 10188786

Watson et al (1995) Characterization of the interaction of zamifenacin at muscarinic receptors in vitro. Eur.J.Pharmacol. 285 135 PMID: 8566131

Choppin (2002) Muscarinic receptors in isolated urinary bladder smooth muscle from different mouse strains. Br.J.Pharmacol. 137 522 PMID: 12359634

Keywords: Zamifenacin fumarate, supplier, Selective, M3, antagonists, Muscarinic, Receptors, Acetylcholine, ACh, UK76654, UK, 76654, M3, Receptors, M3, Receptors, Tocris Bioscience