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| 25mg |
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Purity: ≥98%
Fesoterodine Fumarate (SPM907; Toviaz, SPM-907), the fumarate salt of Fesoterodine which is a prodrug of 5-hydroxymethyl tolterodine, is a muscarinic AChR receptor antagonist that has been approved for treating overactive bladder syndrome.
| ln Vitro |
Fesoterodine fumarate raises the volume expelled with each micturition while reducing the frequency, intensity, and urgency of incontinence episodes[1]. Following oral administration, nonspecific esterases quickly and completely hydrolyze fesoterodine fumarate in plasma to produce desfesoterodine, an active metabolite of fesoterodine (5-hydroxymethyl tolterodine; SPM 7605 ; HY-76569)[3][4].
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| ln Vivo |
At the lowest studied dose of 0.01 mg/kg, fesoterodine fumarate (0.01-1 mg/kg; IV) decreases micturition pressure, increases bladder capacity, and increases ICIs (intercontraction intervas)[3].
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| Animal Protocol |
Animal/Disease Models: Bladders from female SD (Sprague-Dawley) rats (225-275 g)[3]
Doses: 0.01, 0.1 and 1 mg/kg Route of Administration: IV Experimental Results: decreased the micturition pressure and increased bladder capacity and ICIs at the lowest dose tested of 0.01 mg/kg. |
| References |
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| Additional Infomation |
Fesoterodine Fumarate is the fumarate salt form of fesoterodine, a competitive muscarinic receptor antagonist with muscle relaxant and urinary antispasmodic properties. Fesoterodine is rapidly hydrolyzed in vivo into its active metabolite 5-hydroxy methyl tolterodine, which binds and inhibits muscarinic receptors on the bladder detrusor muscle, thereby preventing bladder contractions or spasms caused by acetylcholine. This results in the relaxation of bladder smooth muscle and greater bladder capacity, in addition to a reduction in involuntary muscle contractions and involuntary loss of urine. The active metabolite does not interact with alpha-adrenergic, serotonergic, histaminergic and excitatory amino acid receptors and is eliminated via renal excretion.
See also: Fesoterodine (has active moiety). Drug Indication Treatment of the symptoms (increased urinary frequency and / or urgency and / or urgency incontinence) that may occur in patients with overactive-bladder syndrome. |
| Molecular Formula |
C26H37NO3.C4H4O4
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| Molecular Weight |
527.65
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| Exact Mass |
527.288
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| CAS # |
286930-03-8
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| Related CAS # |
Fesoterodine;286930-02-7;Fesoterodine-d7 fumarate;2747918-94-9
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| PubChem CID |
9849808
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| Appearance |
White to off-white solid powder
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| Boiling Point |
518.9ºC at 760 mmHg
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| Melting Point |
72-78ºC
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| Flash Point |
267.6ºC
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| LogP |
5.092
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
38
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| Complexity |
610
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)C(=O)OC1=C(C=C(C=C1)CO)[C@H](CCN(C(C)C)C(C)C)C2=CC=CC=C2.C(=C/C(=O)O)\C(=O)O
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| InChi Key |
MWHXMIASLKXGBU-RNCYCKTQSA-N
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| InChi Code |
InChI=1S/C26H37NO3.C4H4O4/c1-18(2)26(29)30-25-13-12-21(17-28)16-24(25)23(22-10-8-7-9-11-22)14-15-27(19(3)4)20(5)6;5-3(6)1-2-4(7)8/h7-13,16,18-20,23,28H,14-15,17H2,1-6H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t23-;/m1./s1
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| Chemical Name |
(E)-but-2-enedioic acid;[2-[(1R)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl] 2-methylpropanoate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| 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 (e.g. under nitrogen), avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.74 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 (4.74 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (189.52 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8952 mL | 9.4760 mL | 18.9520 mL | |
| 5 mM | 0.3790 mL | 1.8952 mL | 3.7904 mL | |
| 10 mM | 0.1895 mL | 0.9476 mL | 1.8952 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.
Calculation results
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.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01605617 | Terminated Has Results | Drug: Fesoterodine fumarate Drug: Placebo Procedure: Percu taneous Tibial Nerve Stimulation (PTNS) |
Overactive Bladder | Mayo Clinic | June 2012 | Phase 4 |
| NCT02614482 | Completed | Drug: Fesoterodine | Overactive Bladder | Stéphane Bolduc | October 2015 | Phase 3 |
| NCT01260311 | Completed Has Results | Drug: Fesoterodine | Over Active Bladder | Pfizer | February 2011 | |
| NCT02327936 | Completed | Drug: Fesoterodine Drug: Oxybutynin XL |
Overactive Bladder | Stéphane Bolduc | December 2014 | Phase 3 |
| NCT01054222 | Completed Has Results | Drug: Fesoterodine | Urinary Bladder, Overactive | Pfizer | May 2010 | Phase 4 |
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