Desfesoterodine |
Catalog No.GC35842
One-Click Copy Product Info
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Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 207679-81-0
Sample solution is provided at 25 µL, 10mM.
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Desfesoterodine (PNU-200577; Desfesoterodine) is a potent and selective muscarinic receptor antagonist with a Kb and a pA2 of 0.84 nM and 9.14, respectively. Kb: 0.84 nM (mAChR)[1].
Desfesoterodine (PNU-200577; Desfesoterodine) is a major pharmacologically active metabolite of tolterodine. In vitro, Desfesoterodine (PNU-200577; Desfesoterodine) prevented carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner. In vivo, Desfesoterodine (PNU-200577; Desfesoterodine) was significantly more potent at suppressing acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50=15 and 40 nmol/kg, respectively). In radioligand binding studies carried out in homogenates of guinea-pig tissues and Chinese hamster ovary cell lines expressing human muscarinic m1-m5 receptors, Desfesoterodine (PNU-200577; Desfesoterodine) was not selective for any muscarinic receptor subtype. Thus, Desfesoterodine (PNU-200577; Desfesoterodine) is similar to tolterodine in terms of antimuscarinic potency, functional selectivity for the urinary bladder in vivo and absence of selectivity for muscarinic receptor subtypes in vitro. The results of this study clearly indicate that (R)-5-Hydroxymethyl Tolterodine contributes to the therapeutic action of tolterodine, in view of its high antimuscarinic potency, similar serum concentration and lower degree of protein binding.
[1]. Nilvebrant L, Gillberg PG, Sparf B. Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacol Toxicol. 1997 Oct;81(4):169-72. [2]. Fullhase, Claudius; Soler, Roberto; Gratzke, Christian et al. Spinal effects of the fesoterodine metabolite 5-hydroxymethyl tolterodine and/or doxazosin in rats with or without partial urethral obstruction. Journal of Urology (New York, NY, United States) (2010), 184(2), 783-789. [3]. Nilvebrant, Lisbeth Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacology & Toxicology (Oxford, United Kingdom) (2002), 90(5), 260-267. [4]. Yono, Makoto; Yoshida, Masaki; Wada, Yoshihiro et al. Pharmacological effects of tolterodine on human isolated urinary bladder. European Journal of Pharmacology (1999), 368(2/3), 223-230.
| Cas No. | 207679-81-0 | SDF | |
| Canonical SMILES | OC1=C(C=C(CO)C=C1)[C@@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C | ||
| Formula | C22H31NO2 | M.Wt | 341.49 |
| Solubility | DMSO: ≥ 100 mg/mL (292.83 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9283 mL | 14.6417 mL | 29.2834 mL |
| 5 mM | 585.7 μL | 2.9283 mL | 5.8567 mL |
| 10 mM | 292.8 μL | 1.4642 mL | 2.9283 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)