Fesoterodine L-mandelate

Alias: Fesoterodine Lmandelate; Fesoterodine L mandelate
Cat No.:V39086 Purity: ≥98%
Fesoterodine L-mandelate is an orally bioactive, non-subtype-selective, competitive muscarinic receptor (mAChR) antagonist (inhibitor) with pKis of 8.0 and 7.7 for M1, M2, M3, M4, and M5 receptors, respectively.
Fesoterodine L-mandelate Chemical Structure CAS No.: 1206695-46-6
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
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Other Forms of Fesoterodine L-mandelate:

  • Fesoterodine
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Fesoterodine L-mandelate is an orally bioactive, non-subtype-selective, competitive muscarinic receptor (mAChR) antagonist (inhibitor) with pKis of 8.0 and 7.7 for M1, M2, M3, M4, and M5 receptors, respectively. ,7.4,7.3,7.5. Fesoterodine L-mandelate is used for overactive bladder (OAB).
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Fesoterodine L-mandelate increases the volume of urine produced during a voiding while decreasing the frequency, intensity, and duration of urge incontinence episodes [1]. Following oral ingestion, non-specific esterases quickly and thoroughly hydrolyze fesoterodine L-mandelate in plasma to produce desfesoterodine (5-hydroxymethyl tolterodine; SPM 7605; the active metabolite of fesoterodine).[3][4].
ln Vivo
At the lowest studied dose of 0.01 mg/kg, fesoterodine L-mandelate (0.01-1 mg/kg; IV) decreases micturition pressure and increases bladder capacity and ICI (intercontraction interval) [3].
Animal Protocol
Animal/Disease Models: Female SD (SD (Sprague-Dawley)) rat bladder (225-275 g) [3]
Doses: 0.01, 0.1 and 1 mg/kg
Route of Administration: intravenous (iv) (iv)injection
Experimental Results: At the lowest dose tested, micturition pressure diminished, bladder Capacity and ICI increased by 0.01 mg/kg.
References
[1]. Ellsworth P, et al. Fesoterodine for the treatment of urinary incontinence and overactive bladder. Ther Clin Risk Manag. 2009;5:869-76. Epub 2009 Nov 18.
[2]. Didem Yilmaz-Oral, et al. The Beneficial Effect of Fesoterodine, a Competitive Muscarinic Receptor Antagonist on Erectile Dysfunction in Streptozotocin-induced Diabetic Rats
[3]. Peter Ney, et al. Pharmacological Characterization of a Novel Investigational Antimuscarinic Drug, Fesoterodine, in Vitro and in Vivo. BJU Int. 2008 Apr;101(8):1036-42.
[4]. Martin C Michel, et al. Fesoterodine: A Novel Muscarinic Receptor Antagonist for the Treatment of Overactive Bladder Syndrome. Expert Opin Pharmacother. 2008 Jul;9(10):1787-96.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C₃₄H₄₅NO₆
Molecular Weight
563.72
CAS #
1206695-46-6
Related CAS #
Fesoterodine;286930-02-7
SMILES
O(C(C([H])(C([H])([H])[H])C([H])([H])[H])=O)C1C([H])=C([H])C(C([H])([H])O[H])=C([H])C=1[C@@]([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C([H])([H])C([H])([H])N(C([H])(C([H])([H])[H])C([H])([H])[H])C([H])(C([H])([H])[H])C([H])([H])[H].O([H])[C@]([H])(C(=O)O[H])C1C([H])=C([H])C([H])=C([H])C=1[H]
Synonyms
Fesoterodine Lmandelate; Fesoterodine L mandelate
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~177.39 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7739 mL 8.8697 mL 17.7393 mL
5 mM 0.3548 mL 1.7739 mL 3.5479 mL
10 mM 0.1774 mL 0.8870 mL 1.7739 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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