P-CAB agent 1

Names

[ CAS No. ]:
2374139-68-9

[ Name ]:
P-CAB agent 1

Biological Activity

[Description]:

P-CAB agent 1 (compound B19) is a highly potent potassium-competitive acid blocker agent with an IC50 value of 60.50 nM for H+/K+-ATPase. P-CAB agent 1 has acceptable oral absorption in rats. P-CAB agent 1 can be used for researching acid-related disorders (ARDs)[1].

[Related Catalog]:

Research Areas >> Others
Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[Target]

IC50: 60.50 nM (H+/K+-ATPase)[1]


[In Vivo]

P-CAB agent 1 has acceptable oral absorption in rats[1]. Pharmacokinetic Parameters of P-CAB agent 1 in female Sprague-Dawley rats[1]. IV (2 mg/kg) PO (8 mg/kg) AUC0-∞ (ug/L*hr) 519.57 341.49 t1/2 (ng/mL) 0.49 0.8 Cmax (ug/L) 149.93 17 F (%) 16.43

[References]

[1]. Wang X, et al. Design, synthesis and biological evaluation of novel 5-methyl-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole derivatives as potent potassium-competitive acid blockers. Bioorg Med Chem. 2022 Jun 15;64:116765.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H23FN4O

[ Molecular Weight ]:
426.49

Related Compounds