PDE-9 inhibitor - CAS 1082743-70-1
Catalog number: 1082743-70-1
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C22H27N5O2
Molecular Weight:
393.48
COA:
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Targets:
Phosphodiesterase (PDE)
Description:
PDE-9 inhibitor is useful for neurodegenerative diseases.
Purity:
>98%
Synonyms:
PDE 9 inhibitor; PDE9 inhibitor; PDE-9 inhibitor
MSDS:
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InChIKey:
NINVWDFNTXENDC-DNVCBOLYSA-N
InChI:
InChI=1S/C22H27N5O2/c1-15-12-26(13-16-5-3-2-4-6-16)14-19(15)20-24-21-18(22(28)25-20)11-23-27(21)17-7-9-29-10-8-17/h2-6,11,15,17,19,23H,7-10,12-14H2,1H3/t15-,19-/m1/s1
Canonical SMILES:
CC1CN(CC1C2=NC(=O)C3=CNN(C3=N2)C4CCOCC4)CC5=CC=CC=C5
1.Discovery of a sulfamate-based steroid sulfatase inhibitor with intrinsic selective estrogen receptor modulator properties.
Ouellet C1, Maltais R1, Ouellet É1, Barbeau X2, Lagüe P3, Poirier D4. Eur J Med Chem. 2016 Apr 20;119:169-182. doi: 10.1016/j.ejmech.2016.04.044. [Epub ahead of print]
Steroid sulfatase (STS), the enzyme which converts inactive sulfated steroid precursors into active hormones, is a promising therapeutic target for the treatment of estrogen-sensitive breast cancer. We report herein the synthesis and in vitro study of dual-action STS inhibitors with selective estrogen-receptor modulator (SERM) effects. A library of tetrahydroisoquinoline-N-substituted derivatives (phenolic compounds) was synthesized by solid-phase chemistry and tested on estrogen-sensitive breast cancer T-47D cells. Three phenolic compounds devoid of estrogenic activity and toxicity emerged from this screening. Their sulfamate analogs were then synthesized, tested in STS-transfected HEK-293 cells, and found to be potent inhibitors of the enzyme (IC50 of 3.9, 8.9, and 16.6 nM). When tested in T-47D cells they showed no estrogenic activity and produced a moderate antiestrogenic activity. The compounds were further tested on osteoblast-like Saos-2 cells and found to significantly stimulate their proliferation as well as their alkaline phosphatase activity, thus suggesting a SERM activity.
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CAS 1082743-70-1 PDE-9 inhibitor

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