2836996-95-1

2836996-95-1 structure
2836996-95-1 structure
  • Name: DPP IV/hCA II-IN-1
  • Chemical Name: DPP IV/hCA II-IN-1
  • CAS Number: 2836996-95-1
  • Molecular Formula: C17H20N2O5S
  • Molecular Weight: 364.42
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Carbonic Anhydrase
  • Create Date: 2022-11-05 16:16:20
  • Modify Date: 2024-01-21 14:59:05
  • 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].

Name DPP IV/hCA II-IN-1
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
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.

Molecular Formula C17H20N2O5S
Molecular Weight 364.42