Desfesoterodine (Synonyms: PNU-200577; 5-Hydroxymethyl Tolterodine)

Name: Desfesoterodine
Brand: MedChemExpress
SKU: HY-76569
Rating: 4.5 (1 reviews)

Cat. No.: HY-76569 Purity: 99.82%: FAQs
Data Sheet SDS COA Handling Instructions

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Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a K_B and a pA₂ of 0.84 nM and 9.14, respectively. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053). Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats.

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Desfesoterodine Chemical Structure

CAS No. : 207679-81-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 198	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 198	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 700	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of Desfesoterodine:

(R)-Hydroxytolterodine-d₁₄ Get quote
Desfesoterodine (Standard) Get quote

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

Biological Activity
Purity & Documentation
References
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Description

Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a K_B and a pA₂ of 0.84 nM and 9.14, respectively^[1]. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053)^[2]^[3]. Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats^[4].

IC₅₀ & Target

Kb: 0.84 nM (mAChR)^[1].

In Vitro

In vitro, Desfesoterodine preventes carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner^[1].
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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Desfesoterodine (PNU-200577; 5-Hydroxymethyl Tolterodine; 0.1 and 1 mg/kg; IV) significantly increases bladder compliance after moderate and high doses^[4].
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) ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Sprague Dawley rats at ages 9 to 11 weeks weighing 180 to 250 g^[4]
Dosage:	0.1 and 1 mg/kg
Administration:	IV; single imidafenacin administration
Result:	Significantly increased bladder compliance after moderate and high doses.

Molecular Weight

341.50

Formula

C₂₂H₃₁NO₂

CAS No.

207679-81-0

Appearance

Solid

Color

White to yellow

SMILES

OC1=C(C=C(CO)C=C1)[C@@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (292.83 mM; Need ultrasonic)

DMSO : 50 mg/mL (146.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9283 mL	14.6415 mL	29.2830 mL
5 mM	0.5857 mL	2.9283 mL	5.8566 mL
10 mM	0.2928 mL	1.4642 mL	2.9283 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.82%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (250 KB) HNMR (179 KB) RP-HPLC (438 KB)

Handling Instructions (2659 KB)

References

[1]. Nilvebrant L, Gillberg PG, Sparf B. Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacol Toxicol. 1997 Oct;81(4):169-72. [Content Brief]

[2]. Fullhase, Claudius; Soler, Roberto; Gratzke, Christian et al. Spinal effects of the fesoterodine metabolite 5-hydroxymethyl tolterodine and/or doxazosin in rats with or without partial urethral obstruction. Journal of Urology (New York, NY, United States) (2010), 184(2), 783-789. [Content Brief]

[3]. 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. [Content Brief]

[4]. Naoki Aizawa, et al. Selective Inhibitory Effect of Imidafenacin and 5-hydroxymethyl Tolterodine on Capsaicin Sensitive C Fibers of the Primary Bladder Mechanosensitive Afferent Nerves in the Rat. J Urol. 2015 Apr;193(4):1423-32. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	2.9283 mL	14.6415 mL	29.2830 mL	73.2075 mL
	5 mM	0.5857 mL	2.9283 mL	5.8566 mL	14.6415 mL
	10 mM	0.2928 mL	1.4642 mL	2.9283 mL	7.3208 mL
	15 mM	0.1952 mL	0.9761 mL	1.9522 mL	4.8805 mL
	20 mM	0.1464 mL	0.7321 mL	1.4642 mL	3.6604 mL
	25 mM	0.1171 mL	0.5857 mL	1.1713 mL	2.9283 mL
	30 mM	0.0976 mL	0.4881 mL	0.9761 mL	2.4403 mL
	40 mM	0.0732 mL	0.3660 mL	0.7321 mL	1.8302 mL
	50 mM	0.0586 mL	0.2928 mL	0.5857 mL	1.4642 mL
	60 mM	0.0488 mL	0.2440 mL	0.4881 mL	1.2201 mL
	80 mM	0.0366 mL	0.1830 mL	0.3660 mL	0.9151 mL
	100 mM	0.0293 mL	0.1464 mL	0.2928 mL	0.7321 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Desfesoterodine Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Desfesoterodine207679-81-0PNU-200577 5-Hydroxymethyl TolterodinePNU200577PNU 200577mAChRMuscarinic acetylcholine receptormuscarinicreceptorKBpA2metaboliteTolterodinePNU-200583FesoterodineInhibitorinhibitorinhibit

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Desfesoterodine (Synonyms: PNU-200577; 5-Hydroxymethyl Tolterodine)

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Other Forms of Desfesoterodine:

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Complete Stock Solution Preparation Table

Desfesoterodine Related Classifications

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