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

Zamifenacin (Synonyms: UK-76654)

Cat. No.: HY-123337 Purity: 99.74%
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

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 275 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 400 In-stock
Estimated Time of Arrival: December 31
25 mg USD 780 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1150 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1600 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (240.66 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4066 mL 12.0331 mL 24.0662 mL
5 mM 0.4813 mL 2.4066 mL 4.8132 mL
10 mM 0.2407 mL 1.2033 mL 2.4066 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.02 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ZamifenacinUK-76654UK76654UK 76654mAChRMuscarinic acetylcholine receptorgutmuscarinicM3colonicmotilityirritablebowelsyndromeInhibitorinhibitorinhibit

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Zamifenacin
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