5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)CAS# 207679-81-0 |
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Quality Control & MSDS
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| Cas No. | 207679-81-0 | SDF | Download SDF |
| PubChem ID | 9819382 | Appearance | Powder |
| Formula | C22H31NO2 | M.Wt | 341.49 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Desfesoterodine; PNU-200577 | ||
| Solubility | DMSO : ≥ 100 mg/mL (292.83 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-[(1R)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenol | ||
| SMILES | CC(C)N(CCC(C1=CC=CC=C1)C2=C(C=CC(=C2)CO)O)C(C)C | ||
| Standard InChIKey | DUXZAXCGJSBGDW-HXUWFJFHSA-N | ||
| Standard InChI | 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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | (R)-5-Hydroxymethyl Tolterodine(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.
IC50 value: 0.84 nM (Kb)
Target: mAChR
(R)-5-Hydroxymethyl Tolterodine is a major pharmacologically active metabolite of tolterodine. In vitro, (R)-5-Hydroxymethyl Tolterodine prevented carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner. In vivo, (R)-5-Hydroxymethyl Tolterodine 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, (R)-5-Hydroxymethyl Tolterodine was not selective for any muscarinic receptor subtype. Thus, (R)-5-Hydroxymethyl Tolterodine 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. References: | |||||
5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM) Dilution Calculator
5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.9283 mL | 14.6417 mL | 29.2834 mL | 58.5669 mL | 73.2086 mL |
| 5 mM | 0.5857 mL | 2.9283 mL | 5.8567 mL | 11.7134 mL | 14.6417 mL |
| 10 mM | 0.2928 mL | 1.4642 mL | 2.9283 mL | 5.8567 mL | 7.3209 mL |
| 50 mM | 0.0586 mL | 0.2928 mL | 0.5857 mL | 1.1713 mL | 1.4642 mL |
| 100 mM | 0.0293 mL | 0.1464 mL | 0.2928 mL | 0.5857 mL | 0.7321 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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(R)-5-Hydroxymethyl Tolterodine is a potent and selective muscarinic receptor antagonist with a Kb and a pA2 of 0.84 nM and 9.14, respectively.
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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.
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