1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. Tolterodine tartrate

Tolterodine tartrate (Synonyms: Kabi-2234; PNU-200583E)

Cat. No.: HY-90010 Purity: 99.57%
Handling Instructions

Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.

For research use only. We do not sell to patients.

Tolterodine tartrate Chemical Structure

Tolterodine tartrate Chemical Structure

CAS No. : 124937-52-6

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10 mM * 1  mL in DMSO USD 55 In-stock
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250 mg USD 390 In-stock
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Description

Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.

In Vitro

Carbachol-induced contractions of isolated guinea pig bladder were effectively inhibited by tolterodine (IC50 14 nM) and 5-HM (IC50 5.7 nM). The IC50 values were in the microM range and the antimuscarinic potency of tolterodine was 27, 200 and 370-485 times higher, respectively, than its potency in blocking histamine receptors, alpha-adrenoceptors and calcium channels. The active metabolite, 5-HM, was >900 times less potent at these sites than at bladder muscarinic receptors[1].

In Vivo

Tolterodine was extensively metabolized in vivo[2]. In the passive-avoidance test, tolterodine at 1 or 3 mg/kg had no effect on memory; the latency to cross and percentage of animals crossing were comparable to controls. In contrast, scopolamine induced a memory deficit; the latency to cross was decreased, and the number of animals crossing was increased[3].

Clinical Trial
Molecular Weight

475.57

Formula

C₂₆H₃₇NO₇

CAS No.

124937-52-6

SMILES

OC1=CC=C(C=C1[[email protected]](CCN(C(C)C)C(C)C)C2=CC=CC=C2)C.O=C([[email protected]@H]([[email protected]](C(O)=O)O)O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (210.27 mM; Need ultrasonic)

H2O : 16.67 mg/mL (35.05 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1027 mL 10.5137 mL 21.0274 mL
5 mM 0.4205 mL 2.1027 mL 4.2055 mL
10 mM 0.2103 mL 1.0514 mL 2.1027 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

TolterodineKabi-2234 PNU-200583EKabi2234Kabi 2234mAChRMuscarinic acetylcholine receptormuscarinicreceptorurinarybladdersalivaryglandsInhibitorinhibitorinhibit

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Product Name:
Tolterodine tartrate
Cat. No.:
HY-90010
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