(Rac)-5-Hydroxymethyl Tolterodine |
رقم الكتالوجGC63452 |
(Rac) -5-Hydroxymethyl Tolterodine ((Rac) -Desfesoterodine) ، مستقلب نشط من Tolterodine ، هو مضاد mAChR (قيم Ki تبلغ 2.3 نانومتر ، 2 نانومتر ، 2.5 نانومتر ، 2.8 نانومتر ، و 2.9 نانومتر لـ M1 ، M2 ، مستقبلات M3 و M4 و M5 على التوالي)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 200801-70-3
Sample solution is provided at 25 µL, 10mM.
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].
In vitro, (Rac)-5-Hydroxymethyl Tolterodine (PNU-200577) produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips (KB of 0.84 nM; pA2 of 9.14)[2].
(Rac)-5-Hydroxymethyl Tolterodine (5-HMT; 0.88 μmol/kg; i.v.) treatment shows the binding activity of (Rac)-5-Hydroxymethyl Tolterodine to muscarinic receptors is significantly observed in all tissues, except cerebral cortex, with a longer duration in bladder[3].
[1]. L Nilvebrant, et al. Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacol Toxicol. 1997 Oct;81(4):169-72.
[2]. B Malhotra, et al. The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine. Curr Med Chem. 2009;16(33):4481-9.
[3]. Shizuo Yamada, et al. Muscarinic receptor binding of fesoterodine, 5-hydroxymethyl tolterodine, and tolterodine in rat tissues after the oral, intravenous, or intravesical administration. J Pharmacol Sci. 2019 May;140(1):73-78.
Cas No. | 200801-70-3 | SDF | |
Formula | C22H31NO2 | M.Wt | 341.49 |
الذوبان | DMSO : 100 mg/mL (292.83 mM; Need ultrasonic) | Storage | 4°C, away from moisture |
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 | 0.5857 mL | 2.9283 mL | 5.8567 mL |
10 mM | 0.2928 mL | 1.4642 mL | 2.9283 mL |
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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.
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5
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