1H-1-Ethyl Candesartan Cilexetil Chemical Properties

Melting point:

90-93°C

Boiling point:

842.0±75.0 °C(Predicted)

Density 

1.32

storage temp. 

Refrigerator

solubility 

≤30mg/ml in DMSO;30mg/ml in dimethyl formamide

form 

crystalline solid

pka

3.95±0.10(Predicted)

1H-1-Ethyl Candesartan Cilexetil Usage And Synthesis

Chemical Properties

White Solid

Uses

Candesartan Cilexetil Impurity E (PHARMEUROPA).

Biological Activity

1h-1-ethyl candesartan cilexetil, which is a process-related impurity commonly found in the bulk synthesis of candesartan cilexetil, is a potent, long-acting, and selective angiotensin ii type 1 receptor (at1) antagonist.angiotensin ii is a peptide that is mainly generated by the angiotensin converting enzyme and chymase, which plays a vital role in regulating blood pressure and sodium homeostasis via specific receptors including at1[1]. at1, localized in the kidney, heart, brain, adrenal gland, adipocytes, vascular smooth muscle cells, platelets, and placenta, is a major component of the renin-angiotensin system. furthermore, at1 mediates the classical biological actions of angiotensin ii. also, at1 has seven helical transmembrane domains, which is the characteristic of the superfamily of g-protein-coupled receptors. carboxyl-terminal region structure of at1 plays important roles in receptor internalization, desensitization and phosphorylation [2].

References

[1]. otsuka, m. reduction of bleomycin induced lung fibrosis by candesartan cilexetil, an angiotensin ii type 1 receptor antagonist. thorax. 2004; 59(1): 31-38.
[2]. guo, d., sun, y., hamet, p., & inagami, t. the angiotensin ii type 1 receptor and receptor-associated proteins. cell research. 2001; 11(3): 165-180.

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