| Size | Price | Stock | Qty |
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| 2mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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Purity: ≥98%
5-hydroxymethyl tolterodine (Desfesoterodine, PNU 200577, PNU-200577, 5HMT, 5HM; 5-HMT, 5-HM), the active metabolite of tolterodine which is a medication used treat overactive bladder, is a novel and potent muscarinic receptor antagonist with a Kb of 0.84 nM. It is a major and pharmacologically active metabolite of tolterodine which used to treat frequent urination, urinary incontinence, or urinary urgency. . 5-hydroxymethyl tolterodine produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips. 5-hydroxymethyl tolterodine antagotizes muscarinic receptors with a pA2 of 9.1.
| ln Vitro |
Desfesoterodine inhibits the contraction of isolated urinary bladder strips in guinea pigs in vitro in a competitive and concentration-dependent manner[1]. Desfesoterodine is not selective for any muscarinic receptor subtype, according to radioligand binding studies conducted in homogenates of guinea-pig tissues and Chinese hamster ovary cell lines expressing human muscarinic m1-m5 receptors[1].
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| ln Vivo |
After moderate and high dosages, desfesoterodine (PNU-200577; 5-Hydroxymethyl Tolterodine; 0.1 and 1 mg/kg; IV) dramatically enhances bladder compliance[4]. When used in anaesthetized cats, desfesoterodine significantly outperforms electrically produced salivation in terms of its ability to prevent acetylcholine-induced urinary bladder contraction (ID50=15 and 40 nmol/kg, respectively) [1].
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| Animal Protocol |
Animal/Disease Models: Female Sprague Dawley rats at ages 9 to 11 weeks weighing 180 to 250 g[4]
Doses: 0.1 and 1 mg /kg Route of Administration: IV; single imidafenacin administration Experimental Results: Dramatically increased bladder compliance after moderate and high doses. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
5-Hydroxymethyl tolterodine is a known human metabolite of tolterodine. |
| References |
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| Additional Infomation |
Desfesoterodine is a diarylmethane.
Desfesoterodine is a metabolite of [tolterodine]. |
| Molecular Formula |
C22H31NO2
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|---|---|---|
| Molecular Weight |
341.49
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| Exact Mass |
341.235
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| CAS # |
207679-81-0
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| Related CAS # |
380636-50-0 (fumarate);207679-81-0;
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| PubChem CID |
9819382
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| Appearance |
White to yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
490.7±45.0 °C at 760 mmHg
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| Melting Point |
68-72°C
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| Flash Point |
233.2±27.4 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.563
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| LogP |
4.12
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
25
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| Complexity |
357
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)N(CC[C@H](C1=CC=CC=C1)C2=C(C=CC(=C2)CO)O)C(C)C
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| InChi Key |
DUXZAXCGJSBGDW-HXUWFJFHSA-N
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| InChi Code |
InChI=1S/C22H31NO2/c1-16(2)23(17(3)4)13-12-20(19-8-6-5-7-9-19)21-14-18(15-24)10-11-22(21)25/h5-11,14,16-17,20,24-25H,12-13,15H2,1-4H3/t20-/m1/s1
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| Chemical Name |
(R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol
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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 |
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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 (7.32 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 (7.32 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 (7.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9283 mL | 14.6417 mL | 29.2834 mL | |
| 5 mM | 0.5857 mL | 2.9283 mL | 5.8567 mL | |
| 10 mM | 0.2928 mL | 1.4642 mL | 2.9283 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 |
| NCT01566760 | Completed | Drug: fesoterodine fumarate | Urinary Bladder, Overactive | Pfizer | May 2012 | Phase 1 |
| NCT04478357 | Completed | Drug: 4 mg Fesoterodine ER tablet from Zwickau Drug: 4 mg fesoterodine ER tablet from Freiburg Drug: 8 mg fesoterodine ER tablet from Zwickau Drug: 8 mg fesoterodine ER tablet from Freiburg |
Neurogenic Detrusor Overactivity | Pfizer | November 12, 2019 | Phase 1 |
| NCT02160158 | Completed | Drug: Fesoterodine ER (fasted) Drug: Fesoterodine SR3 (fasted) Drug: Fesoterodine SR3 (fed) |
Healthy | Pfizer | July 2014 | Phase 1 |
| NCT01042236 | Completed | Drug: tolterodine Drug: mirabegron |
Pharmacokinetics of Mirabegron and Tolterodine Healthy |
Pfizer | January 2009 | Phase 2 |
| NCT01042236 | Completed Has Results | Drug: Fesoterodine | Stress Urinary Incontinence | Pfizer | January 2009 | Phase 2 |
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