| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Tolterodine tartrate (PNU-200583E; PNU200583E; Detrol LA; Detrusitol) is a tartrate salt of tolterodine that is a potent and competitive muscarinic receptor antagonist. Tolterodines is an antimuscarinic drug that has been used for symptomatic treatment of urinary incontinence. Tolterodine acts on M2 and M3 subtypes of muscarinic receptors whereas older antimuscarinic treatments for overactive bladder act more specifically on M3 receptors. Tolterodine, although it acts on all types of receptors, has fewer side effects than oxybutynin (M3 and M1 selective, but more so in the parotid than in the bladder) as tolterodine targets the bladder more than other areas of the body.
| ln Vitro |
Both tolterodine (IC50 14 nM) and 5-HM (IC50 5.7 nM) were found to be effective in inhibiting the contractions of the isolated guinea pig bladder caused by carbachol. The antimuscarinic potency of tolterodine was 27, 200, and 370–485, times higher, respectively, than its potency in blocking calcium channels, alpha-adrenoceptors, and histamine receptors. The IC50 values were in the microM range. Compared to bladder muscarinic receptors, the active metabolite, 5-HM, was >900 times less potent at these locations[1].
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| ln Vivo |
In vivo tolterodine metabolism was extensive[2]. Tolterodine at 1 or 3 mg/kg did not affect memory in the passive-avoidance test; the percentage of animals crossing and the latency to cross were similar to controls. On the other hand, scopolamine caused a memory impairment, which resulted in a reduction in the latency to cross and an increase in the quantity of animals crossing[3].
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| References |
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| Additional Infomation |
Tolterodine Tartrate is the tartrate salt form of tolterodine, a benzhydryl compound and a muscarinic receptor antagonist possessing both antimuscarinic and antispasmodic properties. Both tolterodine and its active metabolite, 5-hydroxymethyltolterodine, competitively blocks muscarinic receptors, thereby inhibiting acetylcholine receptor binding. This antagonistic action results in an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure, indicating an antimuscarinic action on the lower urinary tract.. The 5-hydroxymethyl metabolite appears to contribute significantly to the therapeutic effects.
An ANTIMUSCARINIC AGENT selective for the MUSCARINIC RECEPTORS of the BLADDER that is used in the treatment of URINARY INCONTINENCE and URINARY URGE INCONTINENCE. See also: Tolterodine (has active moiety). |
| Molecular Formula |
C22H31NO.C4H6O6
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| Molecular Weight |
475.57
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| Exact Mass |
475.256
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| CAS # |
124937-52-6
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| Related CAS # |
Tolterodine;124937-51-5
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| PubChem CID |
443878
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| Appearance |
White to off-white solid powder
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| Density |
1.003 g/cm3
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| Boiling Point |
442.2ºC at 760 mmHg
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| Melting Point |
205-210ºC
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| Flash Point |
192.1ºC
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| Vapour Pressure |
1.97E-08mmHg at 25°C
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| LogP |
3.218
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
34
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| Complexity |
474
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC1=CC(=C(C=C1)O)[C@H](CCN(C(C)C)C(C)C)C2=CC=CC=C2.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
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| InChi Key |
TWHNMSJGYKMTRB-KXYUELECSA-N
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| InChi Code |
InChI=1S/C22H31NO.C4H6O6/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24;5-1(3(7)8)2(6)4(9)10/h6-12,15-17,20,24H,13-14H2,1-5H3;1-2,5-6H,(H,7,8)(H,9,10)/t20-;1-,2-/m11/s1
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| Chemical Name |
(R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-methylphenol (2R,3R)-2,3-dihydroxysuccinate
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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, 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 (5.26 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 (5.26 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 (5.26 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 | 2.1027 mL | 10.5137 mL | 21.0274 mL | |
| 5 mM | 0.4205 mL | 2.1027 mL | 4.2055 mL | |
| 10 mM | 0.2103 mL | 1.0514 mL | 2.1027 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 |
| NCT01488578 | Completed Has Results | Drug: Tolterodine tartrate | Overactive Bladder | Pfizer's Upjohn has merged with Mylan to form Viatris Inc. |
December 2006 | |
| NCT00768521 | Completed Has Results | Drug: tolterodine tartrate Drug: Comparator: Placebo to tolterodine tartrate |
Overactive Bladder | Merck Sharp & Dohme LLC | September 3, 2008 | Phase 1 |
| NCT02723279 | Completed | Behavioral: EPNS Drug: TT |
Urgency-frequency Syndrome | Shanghai Institute of Acupuncture, Moxibustion and Meridian | April 2016 | Not Applicable |
| NCT00939120 | Completed Has Results | Drug: Tolterodine ER 4mg Drug: Placebo Drug: Pre-randomization Dutasteride |
Benign Prostatic Hyperplasia (BPH) | Siami, Paul F., M.D. | July 2009 | Phase 4 |
| NCT05250245 | Completed | Drug: Tolterodine Tartrate 4 MG Other: Continuous positive airway pressure therapy (CPAP) |
Overactive Bladder Obstructive Sleep Apnea Overactive Bladder Syndrome |
Yuzuncu Yıl University | June 1, 2020 | Phase 4 |
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