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(Rac)-5-Hydroxymethyl Tolterodine hydrochloride

(Rac)-5-Hydroxymethyl Tolterodine hydrochloride
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(Rac)-5-Hydroxymethyl Tolterodine hydrochloride

Catalog No. T40161Cas No. 250214-40-5
(Rac)-5-Hydroxymethyl Tolterodine hydrochloride, also known as (Rac)-Desfesoterodine hydrochloride, is an active metabolite of Tolterodine that functions as a mAChR antagonist. It exhibits significant affinity (K i values) for M1, M2, M3, M4, and M5 receptors, with values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM, respectively. This compound is commonly employed in research related to overactive bladder conditions.
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2 mg$1635 days
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Product Introduction

Bioactivity
Description
(Rac)-5-Hydroxymethyl Tolterodine hydrochloride, also known as (Rac)-Desfesoterodine hydrochloride, is an active metabolite of Tolterodine that functions as a mAChR antagonist. It exhibits significant affinity (K i values) for M1, M2, M3, M4, and M5 receptors, with values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM, respectively. This compound is commonly employed in research related to overactive bladder conditions.
In vitro
In vitro, (Rac)-5-Hydroxymethyl Tolterodine (PNU-200577) hydrochloride demonstrates competitive, concentration-dependent inhibition of carbachol-induced contraction in isolated guinea-pig urinary bladder strips, with a binding affinity (K B) of 0.84 nM and a potency of 9.14 (pA2)[2].
In vivo
Treatment with (Rac)-5-Hydroxymethyl Tolterodine (5-HMT; 0.88 μmol/kg; i.v.) hydrochloride demonstrates significant binding activity to muscarinic receptors across all tissues, barring the cerebral cortex, and exhibits prolonged activity in the bladder[3].
Alias(Rac)-5-Hydroxymethyl Tolterodine hydrochloride, (Rac)-PNU-200577hydrochloride, (Rac)-Desfesoterodine hydrochloride
Chemical Properties
Molecular Weight377.95
FormulaC22H32ClNO2
Cas No.250214-40-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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