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:
Molecular Weight:
Phosphodiesterase (PDE)
PDE-9 inhibitor is useful for neurodegenerative diseases.
PDE 9 inhibitor; PDE9 inhibitor; PDE-9 inhibitor
Canonical SMILES:
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Phosphodiesterase (PDE) Products

CAS 171596-36-4 Nortadalafil

(CAS: 171596-36-4)

A N-desmethyl analogue of the human PDE5 inhibitor Tadalafil. A potential antiplasmodial drug.

CAS 2066488-39-7 (S)-C33

(CAS: 2066488-39-7)

(S)-C33 is a potent and selective PDE9 inhibitor (IC50 = 11 nM).

CAS 224789-15-5 Vardenafil dihydrochloride

Vardenafil dihydrochloride
(CAS: 224789-15-5)

Vardenafil, also called as Levitra and Nuviva, is a phosphodiesterase inhibitor that is selective for PDE5 and PDE1 (IC50 = 0.7 and 180 nM, respectively).

CAS 1904611-63-7 PDE1-IN-2

(CAS: 1904611-63-7)

PDE1-IN-2 is an inhibitor of PDE1 that has IC50 values of 6, 140 and 164 nM for PDE1C, PDE1B and PDE1A, respectvely.

CAS 1440898-82-7 Deltarasin hydrochloride

Deltarasin hydrochloride
(CAS: 1440898-82-7)

Small molecule inhibitor of the KRAS–PDEδ interaction that impairs oncogenic KRAS signalling by altering its localization to endomembranes (in cell Kd value 41 ...

CAS 152633-54-0 Win-62005

(CAS: 152633-54-0)

Win-62005 competitively and selectively inhibits cyclic GMP-inhibitable low Km cyclic AMP phosphodiesterase (PDE III) from rat heart and canine aorta (Kis= 25 a...

CAS 1160521-50-5 PDE1-IN-1

(CAS: 1160521-50-5)

PDE1-IN-1 is a potent PDE1 inhibitor and neuroprotective agent.

CAS 141184-34-1 Filaminast

(CAS: 141184-34-1)

Filaminast is a Type 4 cyclic nucleotide phosphodiesterase inhibitor. It is an analog of rolipram which served as a prototype molecule for several development e...

Chemical Structure

CAS 1082743-70-1 PDE-9 inhibitor

Quick Inquiry

Verification code

Featured Items