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152815-28-6

152815-28-6 structure
152815-28-6 structure
  • Name: RS-25344 hydrochloride
  • Chemical Name: RS 25344 hydrochloride
  • CAS Number: 152815-28-6
  • Molecular Formula: C19H14ClN5O4
  • Molecular Weight: 411.799
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
  • Create Date: 2021-05-08 00:56:53
  • Modify Date: 2024-01-14 10:39:11
  • 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].

Name RS 25344 hydrochloride
Synonyms 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)
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
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.

Molecular Formula C19H14ClN5O4
Molecular Weight 411.799
Exact Mass 411.073425
Hazard Codes Xi