1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. Zamifenacin fumarate

Zamifenacin fumarate (Synonyms: UK-76654 fumarate)

Cat. No.: HY-107649 Purity: >99.0%
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Zamifenacin fumarate (UK-76654 fumarate) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome.

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Zamifenacin fumarate Chemical Structure

Zamifenacin fumarate Chemical Structure

CAS No. : 127308-98-9

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Description

Zamifenacin fumarate (UK-76654 fumarate) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome[1].

IC50 & Target

Muscarinic M3 receptor[1]

In Vivo

Zamifenacin exhibits moderate oral bioavailability (mouse 26%, rat 64%, dog 100%) and Cmax (mouse 92, rat 905, dog 416 ng/mL) following oral administration (mouse 13.2, rat 20 and, dog 5 mg/kg)[2].
Zamifenacin exhibits terminal elimination half-lives (mouse 2.1, rat 6.0 and, dog 1.1 h) due to high plasma clearance (68, 35, and 39 mL/min/kg respectively combined with large volumes of distribution (12.5, 19.0, and 3.5 L/kg respectively) following intravenous administration (mouse 5.3, rat 5.0 and, dog 1.0 mg/kg)[2].

Animal Model: Male CDl mice (mean weight 23 g)[2]
Dosage: 5.3 mg/kg for i.v.; 13.2 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (26%), Cmax (92 ng/mL), T1/2 (1.1 h).
Animal Model: Male and female CD rats (mean weight 210 g)[2]
Dosage: 5.0 mg/kg for i.v.; 20 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (64%), Cmax (905 ng/mL), T1/2 (6.0 h).
Animal Model: Male and two female beagle dogs (13-16 kg)[2]
Dosage: 1.0 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (100%), Cmax (416 ng/mL), T1/2 (1.1 h).
Molecular Weight

531.60

Formula

C₃₁H₃₃NO₇

CAS No.

127308-98-9

SMILES

OC(/C=C/C(O)=O)=O.N1(C[[email protected]@H](CCC1)OC(C2=CC=CC=C2)C3=CC=CC=C3)CCC4=CC5=C(C=C4)OCO5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >99.0%

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Keywords:

ZamifenacinUK-76654UK76654UK 76654mAChRMuscarinic acetylcholine receptorgutmuscarinicM3colonicmotilityirritablebowelsyndromeInhibitorinhibitorinhibit

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Zamifenacin fumarate
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