MBCQ

Names

[ Name ]:
MBCQ

[Synonym ]:
4-((3,4-Methylenedioxybenzyl)amino)-6-chloroquinazoline
UPCMLD-DP008
MBCQ

Biological Activity

[Description]:

MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ lacks inhibitory activity toward other PDE isozymes (all IC50s>100 μM). MBCQ dilates coronary arteries via specific inhibition of cGMP-PDE[1][2][3].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

[Target]

PDE V:19 nM (IC50)

PDE Ⅰ:>100 μM (IC50)

PDE Ⅱ:>100 μM (IC50)

PDE Ⅲ:>100 μM (IC50)

PDE Ⅳ:>100 μM (IC50)

[In Vitro]

MBCQ (compound 3d) induces relaxation of isolated porcine coronary arteries precontracted with prostaglandin F2α (PGF2α; EC50=190 nM)[1]. MBCQ (0.01-10 μM; 10 min) inhibits Carbachol (10 μM)-induced contractions in a concentration-dependent manner in rat ileal smooth muscle[3].

[References]

[1]. Y Takase, et al. Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity. J Med Chem. 1994 Jun 24;37(13):2106-11.

[2]. Jeffery D MacPherson, et al. Inhibition of phosphodiesterase 5 selectively reverses nitrate tolerance in the venous circulation J Pharmacol Exp Ther. 2006 Apr;317(1):188-95.

[3]. Takeharu Kaneda, et al. Lack of cyclic nucleotide regulation of MBCQ-induced relaxation of rat ileal smooth muscle. J Smooth Muscle Res. 2003 Jun;39(3):47-54.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₆H₁₂ClN₃O₂

[ Molecular Weight ]:
313.73800

[ Exact Mass ]:
313.06200

[ PSA ]:
56.27000

[ LogP ]:
3.69700

MSDS

Click to get detail MSDS

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

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