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

Zamifenacin (Synonyms: UK-76654)

Cat. No.: HY-123337
Handling Instructions

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

For research use only. We do not sell to patients.

Zamifenacin Chemical Structure

Zamifenacin Chemical Structure

CAS No. : 127308-82-1

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10 mM * 1  mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 400 In-stock
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25 mg USD 780 In-stock
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50 mg USD 1150 In-stock
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100 mg USD 1600 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Zamifenacin (UK-76654) 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 (2.1 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

415.52

Formula

C₂₇H₂₉NO₃

CAS No.

127308-82-1

SMILES

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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

ZamifenacinUK-76654UK76654UK 76654mAChRMuscarinic acetylcholine receptorgutmuscarinicM3colonicmotilityirritablebowelsyndromeInhibitorinhibitorinhibit

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