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RS-25344 hydrochloride

Names

[ CAS No. ]:
152815-28-6

[ Name ]:
RS-25344 hydrochloride

[Synonym ]:
1-(3-Nitrophenyl)-3-(4-pyridinylmethyl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione hydrochloride (1:1)
Pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione, 1-(3-nitrophenyl)-3-(4-pyridinylmethyl)-, hydrochloride (1:1)
1-(3-Nitrophenyl)-3-(pyridin-4-ylmethyl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione hydrochloride (1:1)

Biological Activity

[Description]:

RS-25344 hydrochloride is a selective cAMP-phosphodiesterase 4 (PDE 4; PDE IV) inhibitor with an IC50 of 0.28 nM in human lymphocytes. RS-25344 hydrochloride has only weak inhibitory effects on PDE I, II, III (IC50 of >100 μM, 160 μM, 330 μM, respectively). RS-25344 hydrochloride has anti-inflammatory, memory- and cognition enhancing, and antineoplastic effects[1][2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)
Research Areas >> Inflammation/Immunology
Research Areas >> Metabolic Disease
Research Areas >> Neurological Disease

[Target]

PDE Ⅳ:0.28 nM (IC50)

PDE Ⅰ:>100 μM (IC50)

PDE Ⅱ:160 μM (IC50)

PDE Ⅲ:330 μM (IC50)


[In Vitro]

RS-25344 hydrochloride (0-10 μM) is a potent inhibitor of sperm PDE activity, with an effective concentration of 0.3 nM and reaching maximum inhibition in the range of 100 nM[2].

[In Vivo]

RS-25344 hydrochloride (5 mg/kg; i.p.; twice daily for 72 h) results in significant increases in stomach weights in wild type C57BL/6 mice[3]. RS-25344 hydrochloride (1 mg/kg; i.p.; 30 min prior to food bolus) increases gastric retention in mice[3].

[References]

[1]. T Kaneko, et al. Elevated intracellular cyclic AMP inhibits chemotaxis in human eosinophils. Cell Signal. 1995 Jul;7(5):527-34.

[2]. J D Fisch, et al. Enhancement of motility and acrosome reaction in human spermatozoa: differential activation by type-specific phosphodiesterase inhibitors. Hum Reprod. 1998 May;13(5):1248-54.

[3]. Will McDonough, et al. PAN-selective inhibition of cAMP-phosphodiesterase 4 (PDE4) induces gastroparesis in mice. FASEB J. 2020 Sep;34(9):12533-12548.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H14ClN5O4

[ Molecular Weight ]:
411.799

[ Exact Mass ]:
411.073425

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds