N-Desmethyl Sildenafil


Catalog No. Size PriceQuantity
M33546-2 2 mg solid $130
M33546-10 10 mg solid $350
M33546-100 100 mg solid $2,255
M33546-C Contact sales@xcessbio.com for quotation $100

Description

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

Product information

CAS Number: 139755-82-1

Molecular Weight: 460.55

Formula: C21H28N6O4S

Chemical Name: 5-(2-ethoxy-5-piperazin-1-ylsulfonylphenyl)-1-methyl-3-propyl-6H-pyrazolo[4, 3-d]pyrimidin-7-one

Smiles: CN1N=C(CCC)C2N=C(NC(=O)C1=2)C1=CC(=CC=C1OCC)S(=O)(=O)N1CCNCC1

InChiKey: UZTKBZXHEOVDRL-UHFFFAOYSA-N

InChi: InChI=1S/C21H28N6O4S/c1-4-6-16-18-19(26(3)25-16)21(28)24-20(23-18)15-13-14(7-8-17(15)31-5-2)32(29,30)27-11-9-22-10-12-27/h7-8,13,22H,4-6,9-12H2,1-3H3,(H,23,24,28)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

References:

  1. Rikako Takahiro, et al. Contribution of CYP3A isoforms to dealkylation of PDE5 inhibitors: a comparison between sildenafil N-demethylation and tadalafil demethylenation. Biol Pharm Bull. 2015;38(1):58-65.
  2. Péter Barabás, et al. Sildenafil, N-desmethyl-sildenafil and Zaprinast enhance photoreceptor response in the isolated rat retina. Neurochem Int. 2003 Nov;43(6):591-5.

Products are for research use only. Not for human use.

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