2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. N-Desmethyl Sildenafil

N-Desmethyl Sildenafil  (Synonyms: Desmethylsildenafil; UK-103,320)

Cat. No.: HY-117605 Purity: 99.86%
COA Handling Instructions

N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor.

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

N-Desmethyl Sildenafil Chemical Structure

N-Desmethyl Sildenafil Chemical Structure

CAS No. : 139755-82-1

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Solution
10 mM * 1 mL in DMSO USD 132 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor[1][2].

In Vitro

N-Desmethyl Sildenafil increases the amplitude of electroretinogram (ERG) recorded from the dark-adapted isolated rat retina, most probably through the enhancement of the photoreceptor cell response[1].
The formation of N-Desmethyl Sildenafil is examined using CYP3A supersomes co-expressing human P450 oxidoreductase and cytochrome b5. N-Desmethyl Sildenafil is catalyzed by CYP3A4, CYP3A5, and to a lesser extent by CYP3A7[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

460.55

Appearance

Solid

Formula

C21H28N6O4S
CAS No.
SMILES

CCOC1=C(C=C(S(N2CCNCC2)(=O)=O)C=C1)C3=NC4=C(C(N3)=O)N(C)N=C4CCC
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 : 250 mg/mL (542.83 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1713 mL 10.8566 mL 21.7132 mL
5 mM 0.4343 mL 2.1713 mL 4.3426 mL
10 mM 0.2171 mL 1.0857 mL 2.1713 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: ≥ 2.08 mg/mL (4.52 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.52 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.52 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.86%

COA (250 KB) HNMR (249 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References
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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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

N-Desmethyl Sildenafil139755-82-1Desmethylsildenafil UK-103,320Phosphodiesterase (PDE)SildenafilmetabolitePDE5CYP3A4CYP3A5CYP3A7Inhibitorinhibitorinhibit

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