GS-5759|GS 5759;GS5759

Cas No.:	1346653-91-5
Chemical Name:	(R)-6-[(3-{[4-(5-{[2-Hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl]amino}pent-1-yn-1-yl)phenyl]carbamoyl}phenyl)sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methylquinoline-3-carboxamide
Synonyms:	GS 5759;GS5759
SMILES:	N1C2C(=CC(S(C3=CC=CC(C(=O)NC4=CC=C(C#CCCCNC[C@@H](O)C5=CC=C(O)C6=C5C=CC(=O)N6)C=C4)=C3)(=O)=O)=CC=2C)C(NC2=CC=CC(OC)=C2)=C(C(N)=O)C=1
Formula:	C₄₇H₄₂N₆O₈S
M.Wt:	850.95
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

A novel bifunctional PDE4 inhibitor (IC50=5 nM) and long acting β2-adrenoceptor agonist (EC50=8 nM); inhibits LPS-induced TNFα production in human PBMC (IC50=0.3 nM) and in human neutrophils fMLP-induced super oxide anion production (IC50=3 nM); also is a potent inhibitor of profibrotic and proinflammatory mediator release from human lung fibroblasts.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47387	PDE4-IN-3	PDE4-IN-3 is a novel and orally active PDE4 inhibitor with potent inhibitory affinity (IC50 = 4.2 nM).
DC47386	N-Desmethyl Sildenafil	N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor.
DC47223	Ro 20-1724	Ro 20-1724 (Ro 20-174) is a potent inhibitor of cAMP-specific phosphodiesterase (PDE4/PDE IV) with a Ki of 1930 nM. Neuroprotective effect.
DC47201	Irsenontrine	Irsenontrine (E2027) is an orally active and selective phosphodiesterase 9 (PDE 9) inhibitor. Irsenontrine can be used for the research of neurological diseases.
DC47087	Orismilast	Orismilast (LEO-32731) is a PDE4 inhibitor used for the research of inflammatory diseases.
DC46874	Carbazeran citrate	Carbazeran (citrate), a potent phosphodiesterase inhibitor, is aldehyde oxidase substrate. Carbazeran (citrate) can be used for the research of metabolic disease.
DC46873	Senazodan hydrochloride	Senazodan (MCI 154) (hydrochloride), as a Ca2+ sensitiser, shows inhibition effect on PDE III.
DC46435	PF-8380 hydrochloride	PF-8380 hydrochloride is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.
DC46402	Tovinontrine	Tovinontrine (IMR-687) is a highly potent and selective phosphodiesterase-9 (PDE9) inhibitor specifically for the treatment of sickle cell disease. IC50s are 8.19 nM and 9.99 nM for PDE9A1 and PDE9A2, respectively.
DC46253	LASSBio-1632	LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion.