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PDE4 inhibitor Compound A

Chemical Structure : PDE4 inhibitor Compound A

CAS No.: 2222609-15-4

PDE4 inhibitor Compound A

Catalog No.: PC-20471Not For Human Use, Lab Use Only.

PDE4 inhibitor Compound A is a potent, highly selective PDE4 inhibitor with IC50 of 1.1 nM (PDE4B2), weakly inhibits PDE3 (IC50=150 nM) and does not inhibit other PDE subtypes.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PDE4 inhibitor Compound A is a potent, highly selective PDE4 inhibitor with IC50 of 1.1 nM (PDE4B2), weakly inhibits PDE3 (IC50=150 nM) and does not inhibit other PDE subtypes.
Compound A (1-10 mg/kg, QD, p.o.) showed dose-dependent and significant suppressive effects on glycosylated hemoglobin (GHb) and urinary albumin/creatinine ratio (UACR) in UNx-db/db mice.
Compound A suppressed pro-fibrotic and pro-inflammatory marker mRNAs and increased anti-reactive oxygen species marker mRNAs in the kidneys of UNx-db/db mice.

Physicochemical Properties

M.Wt 436.51
Formula C24H28N4O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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Solubility

10 mM in DMSO

Chemical Name/SMILES

N-((E)-amino(dimethylamino)methylene)-4-((3aS,9bR)-8-ethoxy-7-methoxy-1,3,3a,9b-tetrahydrofuro[3,4-c]isoquinolin-5-yl)benzamide

References

1. Mitsugi Ookawara, et al. Eur J Pharmacol. 2021 Mar 5;894:173852.

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