MY-5445

Product NameMY-5445
CAS78351-75-4
MFC20H14ClN3
MW331.8
EINECS
MOL File78351-75-4.mol

Chemical Properties

Boiling point	539.7±50.0 °C(Predicted)
Density	1.310±0.06 g/cm3(Predicted)
storage temp.	Store at RT
solubility	DMF: 2 mg/ml; DMSO: 2 mg/ml; DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml
pka	4.91±0.30(Predicted)
form	Yellow solid.
color	White to Light yellow

Safety Information

Hazard Codes	Xi
Risk Statements	36/37/38
Safety Statements	26-36
HS Code	2933.99.8290

Usage And Synthesis

Description

MY-5445 is a selective inhibitor of the cyclic GMP (cGMP) phosphodiesterase, PDE5, with a K_i value of 1.3 μM. It inhibits calcium- and cAMP-selective PDEs with K_i values of >1,000 and 915 μM, respectively. MY-5445 has been shown to relax intact strips of rat aorta with an EC₅₀ value of 4 μM.

Uses

MY-5445 is a selective cGMP phosphodiesterase inhibitor. Potent PDE5 inhibitor.

Definition

ChEBI: N-(3-chlorophenyl)-4-phenyl-1-phthalazinamine is a ring assembly and a member of pyridazines.

Biological Activity

Specific inhibitor of cyclic GMP phosphodiesterase, selective for PDE5 (IC 50 = 0.5 μ M).

in vivo

MY-5445 (0.5-3 mg/kg; i.p.; twice a day; for 15 days) produces a significant relief of mechanical hypersensitivity^[3].

Animal Model:	C57BL/6J male mice^[3]
Dosage:	0.5 mg/kg, 3 mg/kg
Administration:	Intraperitoneal injection, twice a day, for 15 days
Result:	Alleviated the cuff-induced allodynia.

IC 50

PDE5: 1.3 μM (Ki); PDE5: 6.7 μM (IC₅₀); PDE4: 37 μM (IC₅₀)

References

[1] JOHN E. SOUNESS. Role of selective cyclic GMP phosphodiesterase inhibition in the myorelaxant actions of M&B 22,948, MY-5445, vinpocetine and 1-methyl-3-isobutyl-8-(methylamino)xanthine[J]. British Journal of Pharmacology, 1989, 98 3: 725-734. DOI: 10.1111/j.1476-5381.1989.tb14599.x
[2] T YAMAMOTO. Complex effects of inhibitors on cyclic GMP-stimulated cyclic nucleotide phosphodiesterase.[J]. The Journal of Biological Chemistry, 1983, 258 23: 14173-14177.

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