[CAS NO. 127308-98-9] Zamifenacin fumarate

Name: Zamifenacin fumarate
Brand: Arctom Scientific
SKU: AS066927

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [127308-98-9]

Store

Catalog

AS066927

Brand

Arctom Scientific

CAS

127308-98-9

DESCRIPTION [127308-98-9]

Overview

MDL	MFCD09263617
Molecular Weight	531.60
Molecular Formula	C31H33NO7
SMILES	OC(/C=C/C(O)=O)=O.N1(C[C@@H](CCC1)OC(C2=CC=CC=C2)C3=CC=CC=C3)CCC4=CC5=C(C=C4)OCO5

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

Summary

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 C _max (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%), C _max (92 ng/mL), T _1/2 (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%), C _max (905 ng/mL), T _1/2 (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%), C _max (416 ng/mL), T _1/2 (1.1 h).

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 188.11 mM ; Need ultrasonic)

H ₂ O : 1 mg/mL ( 1.88 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8811 mL	9.4056 mL	18.8111 mL
5 mM	0.3762 mL	1.8811 mL	3.7622 mL
10 mM	0.1881 mL	0.9406 mL	1.8811 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: ≥ 2.08 mg/mL (3.91 mM); Clear solution
2.

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

Solubility: ≥ 2.08 mg/mL (3.91 mM); Clear solution
3.

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

Solubility: ≥ 2.08 mg/mL (3.91 mM); Clear solution

* All of the co-solvents are available by MCE.