DPP IV/hCA II-IN-1

Names

[ CAS No. ]:
2836996-95-1

[ Name ]:
DPP IV/hCA II-IN-1

Biological Activity

[Description]:

DPP IV/hCA II-IN-1 is a potent and selective dipeptidyl peptidase IV (DPP IV) and carbonic anhydrase (CA) inhibitor with an IC50 value of 0.049 μM for DPP IV and with Ki values of 0.0361, 0.0428, 0.0941, 0.1328, 0.2615, and 3.034 μM for CA II, CA VB, CA VA, CA IX, CA I, and CA IV, respectively[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Dipeptidyl Peptidase
Signaling Pathways >> Metabolic Enzyme/Protease >> Carbonic Anhydrase
Research Areas >> Metabolic Disease

[Target]

CA Ⅱ:36.1 nM (IC50)

CA I:0.2615 μM (Ki)

hCA II:0.0361 μM (Ki)

hCA IX:0.1328 (Ki)


[In Vitro]

DPP IV/hCA II-IN-1 (compound 12; 100 nM and 5 μM; 1 h; Caco-2 cells) inhibits cellular DPP IV activity by 60.65% and 71.86% at 100.0 nM and 5.0 μM, respectively[1]. DPP IV/hCA II-IN-1 (1.0 μM) can be uptaken by Caco-2 cells to 2874, 4562, and 6250 RFU after 15, 30, and 60 min, respectively[1].

[In Vivo]

DPP IV/hCA II-IN-1 (compound 12; 2 μM, 0.5 mg/mL; CD-1 mouse and Sprague-Dawley (SD) rat) exhibits modest stability in mouse and rat microsomes with 27.5 and 16.7% of remaining, respectively[1].

[References]

[1]. Artasensi A, et, al. Discovery of a Potent and Highly Selective Dipeptidyl Peptidase IV and Carbonic Anhydrase Inhibitor as "Antidiabesity" Agents Based on Repurposing and Morphing of WB-4101. J Med Chem. 2022 Oct 6.

Chemical & Physical Properties

[ Molecular Formula ]:
C17H20N2O5S

[ Molecular Weight ]:
364.42

Related Compounds