Fesoterodine fumarate

SKU: orb1225428

Description

Fesoterodine (PF-00695838) is a competitive muscarinic receptor antagonist with muscle relaxant and urinary antispasmodic properties; binds and inhibits muscarinic receptors on the bladder detrusor muscle, prevents bladder contractions or spasms caused by acetylcholine.Other Indication Approved(In Vitro):FFesoterodine Fumarate decreases micturition frequency, urgency severity and urgency incontinence episodes and increases the volume voided with each micturition.After oral administration, Fesoterodine Fumarate is rapidly and extensively hydrolysed in plasma by nonspecific esterases to Desfesoterodine (5-hydroxymethyl tolterodine; SPM 7605; HY-76569; an active metabolite of Fesoterodine).(In Vivo):Fesoterodine Fumarate (0.01-1 mg/kg; IV) reduces the micturition pressure and increases bladder capacity and ICIs (intercontraction intervas) at the lowest dose tested of 0.01 mg/kg.

Key Properties

• CAS Number: 286930-03-8
• MW: 527.658
• Purity: >98% (HPLC)
• Formula: C₃₀H₄₁NO₇
• SMILES: CC(C)C(=O)OC1=C(C=C(C=C1)CO)[C@H](CCN(C(C)C)C(C)C)C2=CC=CC=C2.C(=C/C(=O)O)\C(=O)O
• Target: mAChR
• Solubility: DMSO: 93 mg/mL (176.3 mM); Ethanol: 93 mg/mL (176.3 mM); Water: 92 mg/mL (174.4 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  Fesoterodine Fumarate (0.01-1 mg/kg; IV) reduces the micturition pressure and increases bladder capacity and ICIs (intercontraction intervas) at the lowest dose tested of 0.01 mg/kg. Animal model: Bladders from female Sprague-Dawley rats (225-275 g). Dosage: 0.01, 0.1 and 1 mg/kg. Administration: IV. Result: Reduced the micturition pressure and increased bladder capacity and ICIs at the lowest dose tested of 0.01 mg/kg.
• In Vitro:
  FFesoterodine Fumarate decreases micturition frequency, urgency severity and urgency incontinence episodes and increases the volume voided with each micturition. After oral administration, Fesoterodine Fumarate is rapidly and extensively hydrolysed in plasma by nonspecific esterases to Desfesoterodine (5-hydroxymethyl tolterodine; SPM 7605; HY-76569; an active metabolite of Fesoterodine).

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

PF-00695838 fumarate

Quick Database Links

Gene Symbol

mAChR