Desfesoterodine

SKU: orb1223194

Description

5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM.

Key Properties

• CAS Number: 207679-81-0
• MW: 341.49
• Purity: >98% (HPLC)
• Formula: C₂₂H₃₁NO₂
• SMILES: CC(C)N(CC[C@H](C1=CC=CC=C1)C1=C(O)C=CC(CO)=C1)C(C)C
• Target: Phosphatase
• Solubility: DMSO : ≥ 100 mg/mL; 292.83 mM

Bioactivity

• In Vivo:
  Desfesoterodine (PNU-200577; 5-Hydroxymethyl Tolterodine; 0.1 and 1 mg/kg; IV) significantly increases bladder compliance after moderate and high doses. In vivo, Desfesoterodine is 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). Animal model: Female Sprague Dawley rats at ages 9 to 11 weeks weighing 180 to 250 g. Dosage: 0.1 and 1 mg/kg. Administration: IV; single imidafenacin administration. Result: Significantly increased bladder compliance after moderate and high doses.
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• In Vitro:
  In vitro, Desfesoterodine preventes carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner. In radioligand binding studies carries out in homogenates of guinea-pig tissues and Chinese hamster ovary cell lines expressing human muscarinic m1-m5 receptors, Desfesoterodine is not selective for any muscarinic receptor subtype.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PNU-200577 | (R)-5-Hydroxymethyl Tolterodine

Quick Database Links

Gene Symbol

Phosphatase